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Past Articles Volume 4, Issue 6, 2013
Review Article

ECHINOCANDINS- A REVIEW

POOJAPRAJWAL*, SHARATHKUMAR K, MOHANDAS RAI, MANOHARVR, SPARSHADEEP EM

DOI:

616

ECHINOCANDINS- A REVIEW

POOJAPRAJWAL*, SHARATHKUMAR K, MOHANDAS RAI, MANOHARVR, SPARSHADEEP EM

Keywords: Echinocandins, caspofungin, micafungin, anidulafungin

Abstract:

Echinocandins are considered to be large molecules from the perspective of drugs used for medical purposes.Echinocandins are able to kill most types Candida species, a type of yeast, and at least prevent the progression of growth of one type of mould called Aspergillusspp. They have modest activity against dimorphic fungi and have little activity against other types of moulds. The semisynthetic pneumocandinanalogs of echinocandins were later found to have the same kind of antifungal activity, but low toxicity. The different echinocandins have been evaluated and are currently used for the different diseases in humans. Poor absorption after oral administration limits use to the intravenous route. Dosing is once daily and drug interactions are few. Adverse events are generally mild, including (for caspofungin) local phlebitis, fever, abnormal liver function tests, and mild haemolysis. Absence of antagonism in combination with other antifungal drugs suggests that combination antifungal therapy could become a general feature of the echinocandins, particularly for invasive aspergillosis.

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Original Research Article
617

QUANTITATIVE ANALYSIS OF CILNIDIPINE AND TELMISARTAN IN TABLETS BY HIGH PERFORMANCE THIN-LAYER CHROMATOGRAPHY WITH ULTRAVIOLET ABSORPTION DENSITOMETRIC DETECTION

M.HARIPRIYA*, Dr. P. JAYASEKHAR

Keywords: Cilnidipine, Telmisartan, HPTLC, Validation

Abstract:

A novel HPTLC method for the simultaneous estimation of Cilnidipine and Telmisartan in two component dosage forms has been developed and validated. Standard and sample solutions of cilnidipine and telmisartan were applied to precoated silica gel G 60 F254 HPTLC plates and the plates were developed with Toluene: Ethyl acetate: DMF in the ratio 6.5: 3.0: 0.5 (v/v), as mobile phase. UV detection was performed densitometrically at 260 nm. The Rf value for cilnidipine and telmisartan was found to be 0.47and 0.17 respectively. The correlation coefficients 0.9917 and 0.9852 for telmisartan respectively. The calibration curve was found to be linear between 100 to 1200 ng/spot for both cilnidipine and telmisartan. The limits of detection and quantitation were found to be 12.6 and 38.28 ng/spot, respectively for cilnidipine and 61.05 and 185.0 ng/spot, respectively for telmisartan. The results have been validated statistically as per ICH guidelines. The developed method can be successfully employed for the simultaneous determination of cilnidipine and telmisartan in marketed tablet formulation.

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Original Research Article
618

EFFECT OF TRIPHALA- AN AYURVEDIC HERBAL FORMULATION ON DOXORUBICIN INDUCED CARDIO TOXICITY IN RATS

MITRA M, SHIVALINGEGOWDA KP*

Keywords: Triphala, cardiotoxicity, catalase, lactate dehydragenase, electrocardiogram

Abstract:

The objective was to evaluate the cardioprotective activity of triphala in doxorubicin induced cardiotoxicity in albino wistar rats. Twenty- four rats were divided into four groups (n=6). Group I (normal) received normal saline (p.o.) for 10 days. The group II rats received doxorubicin HCl (15mg/kg, i.p.) on 7th day. The rats in group III and IV were pretreated with triphala (500mg/kg, p.o. and 1000 mg/kg, p.o.) followed by doxorubicin on 7thday. On 11th day, ECG studies, serum creatinine phosphokinase (CPK), CK-MB and lactate dehydrogenase (LDH) levels as well as anti-oxidant parameters like superoxide dismutase, catalase and lipid peroxidation along with histopathological changes were studied. The doxorubicin treated rats have shown abnormal ECG values along with elevated (*** P <0.001) serum creatinine phosphokinase (CPK), CK-MB, LDH as well as lipid peroxidation levels while significantly reduced values (*** P <0.001 ) of SOD and catalase were observed as compared to group I rats. The triphala and doxorubicin treated rats have shown significant alterations when compared to the doxorubicin alone treated rats suggesting the cardio protection. Histological observations of rat hearts further correlated the cardioprotective effect of triphala. The result of this study provides the experimental evidence for triphala’s cardioprotective effects.

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Original Research Article

ANTI ULCER ACTIVITY OF HYDROALCOHOLIC EXTRACT OF CISSUS QUADRANGULARIS STEM

SUDARSINI SARAVANABHAVAN*, FAHAD I. AL-SAIKHAN

DOI:

619

ANTI ULCER ACTIVITY OF HYDROALCOHOLIC EXTRACT OF CISSUS QUADRANGULARIS STEM

SUDARSINI SARAVANABHAVAN*, FAHAD I. AL-SAIKHAN

Keywords: Cissus quadrangularis, Anti-ulcer, Histopathology, Hydroalcohol

Abstract:

The hydroalcoholic extract of Cissus quadrangularis stem was investigated to evaluate its anti-ulcer activity by using aspirin induced gastric ulcer model, since non-steroidal anti-inflammatory drugs such as aspirin causes gastrointestinal damages as one of their side effects in human. The hydroalcoholic extract of Cissus quadrangularis stem was administered at the dose of 1000 mg/Kg.b.w to the groups of wistar rat orally for 7 consecutive days, after which gastric ulcer was induced by aspirin. Gross pathological examination reveals that Cissus quadrangularis promotes ulcer protection by decreasing the ulcer index which is evident in the Histopathological observation and qualitative analysis of C-reactive protein

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Original Research Article
620

SYNTHESIS AND EVALUATION OF NEW 2-CHLORO-N-[(Z)-(2-OXO-5 SULFAMOYL - INDOLIN-3-YLIDENE) AMINO] ACETAMIDE DERIVATIVES FOR THEIR ANTIMICROBIAL AND ANTI- INFLAMMATORY ACTIVITY

SRIKANTH LINGALA*, RAGHUNANDAN NERELLA, KIRAN POUDALA

Keywords: Isatins, Antimicrobial activity, Anti inflammatory activity, Amikacin, Amphoterecin

Abstract:

In view of various biological activities and enormous importance of indoles, isatins and their derivatives, it was our interest to synthesize and characterize some new 5 - Sulfamoyl Isatin derivatives and evaluate them for antimicrobial and anti-inflammatory activity. An appropriate quantity of isatin hydrazone was heated under reflux with chloroacetyl chloride to give 2-Chloro-N- [(Z)-(2-oxo-5-sulfamoyl-indolin-3-ylidine) amino]acetamide which was then heated under reflux with various secondary amines to give 2-chloro-n-[(z)-(2-oxo-5 sulfamoyl -indolin-3-ylidene) amino] acetamide derivatives. The intermediates and final compounds were purified and their chemical structures have been confirmed by IR, 1H NMR, and Mass spectral data. All the synthesized compounds were screened for antibacterial activity against B. subtilis, B.cereus, S. epidermidis, S. typhi, P. aeruginosa and K. pneumoniae, antifungal activity against A.flavus, F.oxysporium and P. notatum and anti-inflammatory activity using carrageenan induced rat paw edema model. Most of the compounds tested have shown promising activities when compared with the standard drugs.

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Original Research Article

A NOVEL VALIDATED RP-HPLC METHOD FOR THE DETERMINATION OF ESCITALOPRAM OXALATE IN BULK AND PHARMACEUTICAL TABLET DOSAGE FORMS

P.RAVISANKAR*, B. KRISHNA SWAPNA, K.V.S. SANTOSH KUMAR, CH.DEVADASU, P.SRINIVASA BABU, G.DEVALA RAO

DOI:

621

A NOVEL VALIDATED RP-HPLC METHOD FOR THE DETERMINATION OF ESCITALOPRAM OXALATE IN BULK AND PHARMACEUTICAL TABLET DOSAGE FORMS

P.RAVISANKAR*, B. KRISHNA SWAPNA, K.V.S. SANTOSH KUMAR, CH.DEVADASU, P.SRINIVASA BABU, G.DEVALA RAO

Keywords: Escitalopram oxalate, Isocratic RP-HPLC, UV-Vis detector, Method Validation.

Abstract:

An accurate, novel, highly sensitive, precise, simple, efficient and reproducible, isocratic Reversed Phase-High Performance Liquid Chromatography (RP-HPLC) method was developed and validated for the quantitative determination of Escitalopram oxalate in pharmaceutical tablet dosage forms. RPHPLC method was developed by using Welchrom C18 Column (4.6 X 250mm, 5µm), Shimadzu LC20AT Prominence Liquid Chromatograph. The mobile phase composed of Phosphate buffer (pH-7.48, adjusted with triethylamine): acetonitrile (50:50 v/v). The flow rate was set to 1.0 mL/min with the responses measured at 240 nm using Shimadzu SPD-20A Prominence UV-Vis detector. The retention time of Escitalopram oxalate was found to be 5.43 min. Linearity was established for Escitalopram oxalate in the range of 2-10 µg/mL with correlation coefficient 0.999. The percentage recovery was found to be 99.14% to 101.3%. Validation parameters such as specificity, linearity, precision, accuracy, robustness, limit of detection (LOD) and limit of quantitation (LOQ) were evaluated for the method according to the International Conference on Harmonization (ICH) Q2 R1 guidelines. The developed method was successfully applied for the quantitative analysis of commercially available dosage form.

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Original Research Article
622

SYNTHESIS AND CHARACTERIZATION OF CHITIN ACETATE/PROPIONATE MIXED ESTERS

DEEPAK KUMAR JINDAL, S K SINGH*

Keywords: Chitin, Esterification, Chitin acetate/propionate, NMR, Mixed ester

Abstract:

Chitin, the natural biocompatible and biodegradable polymer has limited pharmaceutical and biomedical applications owing to its insolubility in common solvents. In the present investigation, a series of chitin acetate/propionate mixed esters with different content of acetyl and propionyl groups has been synthesized by the esterification of chitin with different ratios of acetic and propionic anhydride in the presence of perchloric acid as the catalyst under heterogenous conditions. Pure chitin dipropionate and chitin diacetate were also synthesized by using the same reaction and their structures were characterized by FTIR and 1H-NMR spectroscopy. The degree of substitution of propionyl and acetyl groups was 0.63-1.75 and 0.23-1.35, respectively as determined by 1H-NMR spectroscopy. The expected solubility in common solvents would result in the formation of various types of materials such as film, fiber etc. for pharmaceutical and biomedical applications.

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Original Research Article

DESIGN AND DEVELOPMENT OF MUCOADHESIVE BUCCAL TABLETS OF METOPROLOL SUCCINATE BY USING MORINGA OLEIFERA GUM

B. SUDHEER*, V. SAIKISHORE, M. SANDEEP, K. SRIKANTH, M. TEJA KRISHNA

DOI:

623

DESIGN AND DEVELOPMENT OF MUCOADHESIVE BUCCAL TABLETS OF METOPROLOL SUCCINATE BY USING MORINGA OLEIFERA GUM

B. SUDHEER*, V. SAIKISHORE, M. SANDEEP, K. SRIKANTH, M. TEJA KRISHNA

Keywords: Binder, gum, Moringa oleifera, release retardant, tablet

Abstract:

In the present work, the mucoadhesive tablets of Metoprolol succinate were prepared by using Moringa oleifera gum as a release retardant. The four tablet formulation were prepared by using drug and Moringa olifera gum ratios of 1:0.5, 1:0.75 1:1, 1:1.25 by direct compression technique. Tablets were subjected for evaluation of uniformity of weight, hardness, friability, drug content uniformity Swelling studies, Surface pH study, Ex-vivo mucoadhesion time, Ex-vivo Bioadhesive Strength and In vitro drug release study. Drug polymer interactions were evaluated by Fourier Transform Infrared Spectroscopy. All the formulations hardness, weight variation, friability and drug content values were found to be within pharmacopoeia limits. As the amount of polymer in the tablets increases, the drug release rate decreases, whereas swelling index and mucoadhesive strength increases. Based on the results F4 was found to be optimized formulation. The in-vitro drug release of all formulations exhibits complete release of Metoprolol succinate with zero order release kinetics and followed by Higuchi mechanism. From the study it can be conclude that the Moringa olifera gum used as a binding agent in mucoadhesive buccal tablet.

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Review Article

A COMPREHENSIVE REVIEW ON DENDRIMERS

AVINASH RANGARAJU*, UPPALA MOHAN KUMAR, KARIPE PRAGNA, ATELLI SANDEEP

DOI:

624

A COMPREHENSIVE REVIEW ON DENDRIMERS

AVINASH RANGARAJU*, UPPALA MOHAN KUMAR, KARIPE PRAGNA, ATELLI SANDEEP

Keywords: Dendrimers, Convergent synthesis, divergent synthesis, drug delivery, sensor technology

Abstract:

Dendrimers also known as arborols are nano-sized, radially symmetric molecules with well-defined, homogeneous and monodisperse structure consisting of tree-like arms or branches. These are synthetic 3-dimensional macromolecules prepared in a stepwise way from simple branched monomer units, whose nature and functionality can be easily controlled and varied. Their structure results in previously unknown or improved physical and chemical properties as compared to the common linear polymers. Dendrimers are now one of the most important nanometer-scale building blocks for the construction of nanoscale systems, molecular devices, advanced drug-delivery systems, etc. This review gives concise information about dendrimers‟ physico-chemical properties, synthetic strategies and their possible use in various areas of research, technology and treatment.

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Original Research Article
625

DEVELOPMENT AND VALIDATION OF A STABILITY INDICATING RP-HPLC METHOD FOR QUANTIFICATION OF FINGOLIMOD IN BULK AND PHARMACEUTICAL DOSAGE FORM

PAWANJEET.J.CHHABDA*, M. BALAJI, SRINIVASARAO.V

Keywords: Fingolimod, validation, HPLC, Stability indicating

Abstract:

A simple, precise, stability indicating RP-HPLC method was developed and validated for the assay determination of Fingolimod Hydrochloride in bulk drug and dosage form. LC separation was achieved gradient mode on a XBridge C18 (4.6x150) mm, 5 µm column using mobile phase containing solution A (0.1% perchloric acid) solution B( acetonitrile) at flow rate 0.8 ml/min. The detection wavelength was 220 nm and temperature was 40˚c. The retention time was 9.30 min and linearity was observed in the concentration range of 20-150 µg/ml with correlation coefficient of 0.9999. The percentage relative standard deviation in accuracy and precision studies was found to be less than 2%. The method was successfully validated as per ICH guidelines. Fingolimod undergoes degradation under acidic, basic, oxidation, dry heat and photolytic conditions, degradation impurities did not interfere with the retention time of fingolimod, and assay method is thus stability indicating.

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Original Research Article
626

MICROWAVE ENHANCED SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME NOVEL BENZOFURAN LINKED ISOXAZOLE DERIVATIVES

M. SRINIVAS*, D. SWAPNA, K. HARITHA , VPVS. KOTESWARA RAO

Keywords: Microwave mediated synthesis, Benzofuran, Isoxazoles, antimicrobial activity

Abstract:

The synthesis and biological evaluation of some novel benzofuran linked isoxazole derivatives 2a-j was aimed at creating a compact new structures with a hope to get much more potent compounds with less side effects. A simple, facile microwave mediated synthesis of ten new compounds were synthesized by reacting 1-(benzofuran-2-yl)-3-(substituted phenyl)-prop-2-en-1-ones with hydroxylamine hydrochloride to yield various isoxazoles 2a-j. All the compounds were characterized by physical and spectral data. The compounds were screened for anti-microbial activities. Compounds 2d & 2j were found to possess significant anti-bacterial activity against both gram positive and gram negative bacteria at the tested concentrations when compared with that of standard drug ampicillin. In anti-fungal study, compounds 2j, 2e and 2d have exhibited almost similar anti fungal activity when compared with standard drug fluconazole. These compounds can be further exploited to get the potent lead compound.

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Original Research Article
627

COMPARATIVE EVALUATION OF HYDROPHILIC AND HYDROPHOBIC POLYMERS ON THE IN VITRO RELEASE OF A MODEL WATER SOLUBLE DRUG FROM CONTROLLED RELEASE TABLETS

Y.DEEPA*, VINAY UMESH RAO, M.SUDHAKAR

Keywords: Hydrophilic polymers, hydrophobic waxes, melt granulation, Fluoxetine HCl (FLX-HCL)

Abstract:

The effect of two different viscosity grades of hydrophilic, hydroxy propyl methyl cellulose (HPMC K4M and K100M) and hydrophobic, Stearic Acid and Glyceryl Behenate on the in vitro dissolution of a model water soluble drug was evaluated. Fluoxetine HCl (FLX-HCL) was selected as the model drug due to its high aqueous solubility. Direct compression process was followed for the hydrophilic polymers and the melt granulation technique was followed for the wax matrix tablets. The dose of the drug (20 mg) and weight of the tablets (500mg) was maintained as constant.The wax matrix polymers are required to be used in significantly lower concentrations as compared to the hydrophilic HPMC polymers in order to control the drug release rate of a model water soluble drug like FLX-HCL.

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Original Research Article
628

DEVELOPMENT AND VALIDATION OF UV SPECTROPHOTOMETRIC METHOD FOR THE ESTIMATION OF DEFLAZACORT

DEEPTI.K?, ATUL RAI

Keywords: Deflazacort, UV spectrophotometry, methanol

Abstract:

UV spectrophotometric method have been developed for the estimation of Deflazacort in pure and its pharmaceutical formulations. In UV method Deflazacort showed absorption maximum at 242.8nm in methanol medium and it obeyes Beers law in the concentration range of 5-25µg/ml.

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Original Research Article

FORMULATION AND EVALUATION OF PROPRANOLOL HCl EXTENDED RELEASE PELLETS

RAMYASRI ALAPATI*, BHANU PRASAD M, Dr.V.UMAMAHESHWAR RAO, R.SHIREESH KIRAN

DOI:

629

FORMULATION AND EVALUATION OF PROPRANOLOL HCl EXTENDED RELEASE PELLETS

RAMYASRI ALAPATI*, BHANU PRASAD M, Dr.V.UMAMAHESHWAR RAO, R.SHIREESH KIRAN

Keywords: Propranolol HCl, Extended release pellets, antihypertensive, fluid bed coating

Abstract:

The present study performed by Formulation and Evaluation of Extended Release Pellets of Propranolol HCl which is an anti-hypertensive drug. Pellets were formulated with various materials like ethyl cellulose 7cps, HPMC E-5, HPMC phthalate 55 as rate controlling polymers, Diethyl phthalate as plasticizer, povidone K-30 as binder and Acetone, Isopropyl alcohol as solvents. The pellets were prepared by both Pan coating and fluid bed coating technology. The variant proportion of the polymers ethyl cellulose 7cps, HPMC E-5 and HPMC pthalate 55 showed significant difference in the release rates. The drug release rate decreased as the concentration of ethyl cellulose is increased.

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Original Research Article

FORMULATION AND EVALUATION OF BILAYER TABLETS OF SITAGLIPTIN PHOSPHATE AND METFORMIN HYDROCHLORIDE

SAI SUPRAJA.B*, AJAY KUMAR.B, Dr.V.UMAMAHESHWAR RAO, SWARUPA ARVAPALLY

DOI:

630

FORMULATION AND EVALUATION OF BILAYER TABLETS OF SITAGLIPTIN PHOSPHATE AND METFORMIN HYDROCHLORIDE

SAI SUPRAJA.B*, AJAY KUMAR.B, Dr.V.UMAMAHESHWAR RAO, SWARUPA ARVAPALLY

Keywords: Metformin Hydrochloride, Sitagliptin Phosphate, UV Visisble spectrophotometer.

Abstract:

The purpose of this research work is to establish Metformin Hydrochloride (500mg) as sustained release layer and Sitagliptin Phosphate (50mg) as immediate release layer in the form of bilayer tablets. Sustained release layer is prepared by direct compression method using combination of different polymers like Sodium alginate, HPMC K4M, Carbomer, and Xanthum gum. Immediate release layer is prepared by Wet granulation method by using combination of Superdisintegrants like Crosspovidone, Crosscarmellose intragranularly and extragranularly. Finally both the layers were compressed by direct compression. Tablets were evaluated for different parameters like friability, weight variation, hardness, drug content, dissolution studies, stability studies, ft-ir studies for compatability purpose. The release of one drug remain unaffected in presence of other drug. The optimized formulation gave an Immediate release effect followed by Sustained release effect. The release pattern of Metformin Hydrochloride was fitted to different models based on coefficient of correlation. The present study concluded that bilayer tablets can effectively be formulated to deliver more than one drug so as to have improved patience compliance and better disease management.

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Original Research Article
631

A FACTORIAL STUDY ON ENHANCEMENT OF DISSOLUTION RATE OF PIROXICAM BY SOLID DISPERSION TECHNIQUE EMPLOYING STARCH CITRATE, PVP K-30 AND PEG 4000

VEERAIAH ENTURI*, BOYAPATI MRUDULA, K.P.R. CHOWDARY, DEBASISH SWAIN

Keywords: Solid dispersions, Piroxicam, Starch Citrate, PVP K-30, PEG 4000, Factorial Study

Abstract:

Solid dispersion is a widely accepted technique for enhancing the dissolution rate of poorly soluble BCS class II drugs. In the present study starch citrate- a new modified starch, PVP and PEG 4000 were evaluated as a carriers in solid dispersions for enhancing the dissolution rate and efficiency of piroxicam, a BCS class II drug. Their individual and combined (interaction) effects in enhancing the dissolution rate and dissolution efficiency of piroxicam were evaluated in a 23- factorial study. Among the individual effects starch citrate gave highest enhancement in the dissolution rate of piroxicam (11.71 fold), followed by PVP (6.03 fold). Addition of PVP and PEG 4000 to the solid dispersions in starch citrate has further enhanced the dissolution rate upto 66.40 fold and dissolution efficiency upto 13.38 fold.

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Original Research Article
632

EVALUATION OF IN-VITRO ANTI-UROLITHIATIC ACTIVITY OF PORTULACA OLERACEA L

KUMKUM AGARWAL*, RANJANA VARMA

Keywords: Urolithiasis, calcium oxalate (CaOx), calcium oxalate monohydrate (COM), Portulaca oleracea L. (PO), in-vitro

Abstract:

The inhibition of in-vitro calcium-oxalate crystal formation by Portulaca oleracea L. extract was investigated by different methods i.e nucleation assay and synthetic urine assay. In nucleation assay, the aim was to evaluate the effectiveness of the extract on calcium oxalate crystallization in vitro while in synthetic urine method the percentage inhibition and growth of the COM crystals of oxalate from synthetic urine at different concentrations of extract was investigated. In nucleation assay % inhibition for CaOx crystal formation was found directly proportional to the increase in concentration of the plant extract with maximum inhibition of 71.07%, while in synthetic urine assay maximum inhibition was 79.31 %. Thus Portulaca oleracea L. was found to be a potent anti-urolithiatic agent.

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Review Article

BREATHING TROUBLE- ASTHMA

G.K.SUDHAKAR*, VENKATESH KAMATH B, ARAVIND PAI

DOI:

633

BREATHING TROUBLE- ASTHMA

G.K.SUDHAKAR*, VENKATESH KAMATH B, ARAVIND PAI

Keywords: Asthma, Pathophysiology, Inhaled steroid, Selective agonist, Methyl Xanthine

Abstract:

Asthma is an immune inflammatory disease that needs prolonged treatment. Each patient is supposed to know the course of the disease and the method of its management. Several factors such aerosols, allergens, drugs, chemicals, exercise, cold dry air, infections and emotions can aggravate the symptoms and precipitate attacks. The incidence of asthma is increasing especially in children especially in developing countries like India. The basic therapeutic principle for this disease dictates that treatment should be based on working diagnosis followed by therapy required so as to reduce the severity of asthma.

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Original Research Article
634

A NEW VALIDATED RP-HPLC METHOD FOR THE ESTIMATION OF CITALOPRAM IN TABLET DOSAGE FORMS

K. SUJATHA*, J.V.L.N. SESHAGIRI RAO

Keywords: : Citalopram, Estimation, Tablets, HPLC

Abstract:

An accurate high performance liquid chromatographic method was developed for quantification of citalopram in its tablet dosage forms. Ideal separation of the drug was achieved on an Agilent Eclipse XDB C18 column (150 x 4.6 mm; 5) by eluting with a mobile phase consisting of a mixture of acetate buffer (pH 4.5) and acetonitrile (65:35 v/v) at a flow rate of 1.0 mL/min. The drug in the eluates was monitored by U V detection at 240 nm. Under optimized conditions, the retention time obtained for the drug was 3.72 min. The relevant calibration plot was linear in the concentration range of 25-150 µg/mL of the drug. The validation of the method was done by following the ICH guidelines. The proposed method could be applied for determination of citalopram in its tablet dosage forms without any interference from normal excipients. The method thus, is suitable for routine quality control analysis of citalopram.

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Original Research Article
635

HEPATOPROTECTIVE ACTIVITY OF ZIZYPHUS NUMMULARIA (BURM.F.)WIGHT & ARN. AGAINST CCL4 INDUCED HEPATOTOXICITY IN RATS

RAJASEKARAN S*, R ANANDAN, NISHAD.K.M, VANNAMALAR.S

Keywords: Zizyphus nummularia, carbontetra chloride, hepatotoxins, transaminases, Histopathological studies.

Abstract:

Effect of ethanol and aqueous extracts of leaves of Zizyphus nummularia (ZPN) was investigated against carbon tetra chloride-induced hepatic damage. carbon tetra chloride at the rate of 1 ml/kg produced liver damage in rats as manifested by the significant (P<0.001) rise in serum levels of Serum oxaloacetate transaminase(SGOT), Serum glutamate pyruvate transaminase(SGPT), alkaline phosphatase (ALP), Totalprotein Totalbilirubin and Directbilirubin compared to respective control values. Histopathological observation also revealed that pretreatment with ZPN protected the animals from carbon tetra chloride induced liver damage. The results indicate that the leaves of Zizyphus nummularia possess the Hepatoprotective activity. This property may be attributed to the flavonoids present in the leaves of Zizyphus nummularia.

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Original Research Article

SPECTROPHOTOMETRIC METHOD DEVELOPMENT AND VALIDATION FOR NAPROXEN AND RIZATRIPTAN IN BULK AND TABLET DOSAGE FORM USING ABSORPTION RATIO METHOD

DINAKARAN SATHIS KUMAR*, ANUSHA POTHULA, DURGANAGA PRASHANTHI BOTLA, HAREESH KUMAR PASINIBILLI, AVASARALA HARANI, RAVISHANKAR K

DOI:

636

SPECTROPHOTOMETRIC METHOD DEVELOPMENT AND VALIDATION FOR NAPROXEN AND RIZATRIPTAN IN BULK AND TABLET DOSAGE FORM USING ABSORPTION RATIO METHOD

DINAKARAN SATHIS KUMAR*, ANUSHA POTHULA, DURGANAGA PRASHANTHI BOTLA, HAREESH KUMAR PASINIBILLI, AVASARALA HARANI, RAVISHANKAR K

Keywords: Absorption ratio, Naproxen, Phosphate Buffer pH 7.4, Rizatriptan

Abstract:

A simple, economic and accurate absorption ratio method was developed for the simultaneous estimation of Naproxen (NAP) and Rizatriptan (RIZ) in bulk and tablet dosage form.Phosphate Buffer pH 7.4 was used as a diluent. The absorptions were observed at 216.34nm and 230.19nm which were selected based on overlap spectra of NAP and RIZ. The Linearity range was found to be 2-4.5 g/ml (r2 =0.9905) at 216.34nm and (r2 = 0.9998) at 230.19nm. The proposed method was validated. The reports was expressed that the proposed method was found to be simple, precise, accurate and rapid for the simultaneous estimation of NAP and RIZ in bulk and tablet dosage form using absorption ratio method.

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Original Research Article

FORMULATION AND EVALUATION OF FLOATING BIOADHESIVE TABLETS OF CIPROFLOXACIN HCL USING NATURAL POLYMERS

SWARUPA ARVAPALLY*, AJAY KUMAR.B, Dr.V.UMAMAHESHWAR RAO, R.SHIREESH KIRAN, SAI SUPRAJA

DOI:

637

FORMULATION AND EVALUATION OF FLOATING BIOADHESIVE TABLETS OF CIPROFLOXACIN HCL USING NATURAL POLYMERS

SWARUPA ARVAPALLY*, AJAY KUMAR.B, Dr.V.UMAMAHESHWAR RAO, R.SHIREESH KIRAN, SAI SUPRAJA

Keywords: Ciprofloxacin HCL, floating bioadhesive tablets, flouroquinolone antibiotic

Abstract:

The present study performed by Formulation and Evaluation of Floating Bioadhesive Tablets of Ciprofloxacin HCl as a model drug for prolongation of gastric residence time. Floating Bioadhesive tablets were formulated with various materials like Xanthangum and Guargum,Chitosan at varying concentrations were used for release controlling properties, sodium bicarbonate act as a effervescent agent and Lactose is used as Diluent. The tablets were prepared by direct compression technique and the prepared tablets remained buoyant for more than 12 hours in the released medium and showed good Bioadhesion Strength. The variant proportion of the polymers Xanthangum and Guargum, Chitosan showed significant difference in the release rate, buoyancy, bioadhesive strength and lag of the tablet.

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Original Research Article

SOLUBILITY ENHANCEMENT OF LAMOTRIGINE USING SOLID SELF EMULSIFIED DRUG DELIVERY SYSTEMS

G.SUSHMA*, K.UJJAINI, KALYAN RAJ, RAJYA LAXMI, VINAY UMESH RAO, M.SUDHAKAR

DOI:

638

SOLUBILITY ENHANCEMENT OF LAMOTRIGINE USING SOLID SELF EMULSIFIED DRUG DELIVERY SYSTEMS

G.SUSHMA*, K.UJJAINI, KALYAN RAJ, RAJYA LAXMI, VINAY UMESH RAO, M.SUDHAKAR

Keywords: Lamotrigine, BCS class II, oil phase, s-mix, HLB

Abstract:

Lamotrigine is a novel anti epileptic drug which belongs to BCS Class II. Its poor aqueous solubility limits its oral bioavailability. The aim of the current work was to utilize the self emulsifying drug delivery platform to enhance the dissolution of Lamotrigine and thereby improve its oral bioavailability. The composition of the oil phase and the surfactant and co surfactant mixture (S-mix) was optimized by varying the HLB value of the S mix from low of 6 to a high of 14. The stability of the emulsion was determined by physical observation. The drug loaded s-mix was adsorbed on to a solid carrier and the resultant powder was subjected to in vitro dissolution testing in water and in the compendia media. The results were compared to those of plain drug from equivalent mixture.

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Original Research Article
639

FORMULATION AND EVALUATION OF ACYCLOVIR MULTIUNIT FLOATING FORMULATIONS TO INCREASE GASTRIC RETENTION BY EMPLOYING LIPOIDAL CARRIERS

SWAPNA VELIVELA*, Dr. K. ABBULU, Dr. D.VARUN

Keywords: Acyclovir, Gelucire 43/01, Gelucire 50/02, Compritol ATO 888, Geleol Pellets

Abstract:

The purpose of this investigation was to formulate hydrodynamically balanced gastric retentive drug delivery system of Acyclovir. Acyclovir is a synthetic purine nucleoside analogue with in vitro and in vivo inhibitory activity against herpes simplex virus types 1 (HSV-1), 2 (HSV-2), and varicella-zoster virus (VZV). It has an elimination half life of about 2.5-3.3 hours. Non-effervescent formulations of Acyclovir were prepared with novel lipoid carriers like Gelucire 43/01, Gelucire 50/02, Compritol ATO 888, Geleol pellets by using different granulation techniques in the ratios of 1:1, 1:1.25 and 1:1.5 were compared to effervescent formulations comprising HPMC K4M, HPMC K15M, HPMC K100M. All the formulations were evaluated for Micromeritic properties, buoyancy parameters and in vitro drug release studies were carried out for 12 hours. The in vitro release data obtained was fitted to various linear and regression kinetic models to assess the release profile of the drug. Based on results obtained from the preliminary formulations, optimized formulations are selected for further studies. Short-term stability studies were done for optimized formulations. The data obtained in this study suggests that the multiunit floating formulations of Acyclovir can be successfully designed to give controlled drug delivery and improved oral bioavailability.

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Original Research Article
640

FORMULATION AND EVALUATION OF EFAVIRENZ TABLETS DEVELOPED BY MOISTURE ACTIVATED DRY GRANULATION

P.NITHIN*

Keywords: Efavirenz, NNRTI, Formulation, Evaluation, MADG.

Abstract:

The aim of present work is to formulate and evaluate efavirenz tablets. Efavirenz tablets were prepared by using Moisture Activated Dry Granulation. Efavirenz is a nonnucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS. As with other anti-retroviral drugs, HIV rapidly develops resistance if efavirenz is used alone. So recommended therapy consists of combinations of three or more anti-retroviral. Objective is to monitor the manufacturing process of efavirenz tablets to facilitate the formulation, evaluation, optimization and confirmation of the critical product / process parameter identified during the developmental stage of the formulation so that the final product at pilot scale / test batch will produce consistent results.

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Original Research Article
641

SYNTHESIS AND ANTIBACTERIAL EVALUATION OF SOME N-(P-SUBSTITUTED BENZYLIDENE)-5-PROPYL-1, 3, 4-THIADIAZOLE-2-AMINES

SUNIL KUMAR*, S. K. SHARMA, SANDEEP JAIN, NEELAM JAIN

Keywords: 1, 3, 4-Thiadiazole, Schiff’s base, antibacterial, minimum inhibitory concentration (MIC).

Abstract:

A series of Schiff’s bases i.e., N-(p-substituted benzylidene)-5-propyl-1, 3, 4-thiadiazole-2-amines were synthesized from 2-amino-5-propyl-1, 3, 4-thiadiazole 1 and evaluated for their in vitro antibacterial activity. Reaction of thiosemicarbazide with butanoic acid in presence of concentrated sulfuric acid furnished the compound 1 which on further reaction with different p-substituted benzaldehydes yielded the Schiff’s bases 2. These compounds were characterized by spectral analysis. All the synthesized compounds were screened for their in vitro for their antibacterial activity against two Gram positive bacterial strains (Bacillus subtilis and Staphylococcus aureus) and two Gram negative bacterial strains (Escherichia coli and Pseudomonas aeruginosa) and their minimum inhibitory concentration (MIC) were determined.

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Original Research Article
642

A STUDY ON THE EFFECT OF GREEN TEA EXTRACT ON THE LIPID PROFILE OF POST MYOCARDIAL INFARCTION PATIENTS ON HYPOLIPIDAEMIC AND ANTIPLATELET THERAPY

JOSEPH STALIN D*

Keywords: Green Tea Extract, Cholesterol, Atorvastatin, LDL, Lipid profile

Abstract:

This open randomized controlled trial was conducted on post MI patients receiving hypolipidaemic and antiplatelet therapy to assess the effect of Green Tea Extract on their lipid profiles. The 102 patients who were enrolled for the study were divided in to two groups at random and categorized as Group 1 and Group 2. Their baseline serum lipid profiles were measured and documented on the patient data sheet. Then Group 1 was given atorvastatin 40 mg/day and clopidogrel 75 mg/day as they were already taking that along with drugs for diabetes and/or hypertension. Group 2 patients additionally received Green Tea Extract 75 mg/day orally. Both the groups of patients were monitored for compliance, and for ADRs and side effects. At the end of 6 months the lipid profiles of Group 1 were measured and compared with those of Group 2. The results showed that the reduction in serum total cholesterol, and LDL, were much higher in Group 2, compared to Group 1. There were no significant changes in triglyceride, HDL, and VLDL levels in both the groups. The study gives a strong evidence for the lipid lowering action of Green Tea Extract.

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Original Research Article

ANALGESIC ACTIVITY OF LEAVES, FLOWERS AND FRUIT PEEL OF LUFFA CYLINDRICA (L.) ROEM

KANWAL WASEEM KHAN, SYED WASEEMUDDIN AHMED, SALMAN AHMED*

DOI:

643

ANALGESIC ACTIVITY OF LEAVES, FLOWERS AND FRUIT PEEL OF LUFFA CYLINDRICA (L.) ROEM

KANWAL WASEEM KHAN, SYED WASEEMUDDIN AHMED, SALMAN AHMED*

Keywords: Luffa cylindrica, analgesic activity, analgesy meter test, mechanically induced pain

Abstract:

Ethanol extracts of leaves, male flowers and fruit peel of Luffa cylindrica (L.) Roem., were evaluated for analgesic effect using analgesy meter test, a mechanically induced pain model. Extracts at the dose of 500 mg/kg, p.o., were tested and compared with diclofenac sodium 50mg/kg as standard analgesic drug. Mechanical force was applied on the rat paw and continuously increased. The point at which rat can’t bear further pressure and starts struggle to free paw was taken as nociceptive response. Readings were taken before and after 1, 2 and 3hr following drug administration. Analgesic response was continuously increasing till 3hrs. Tested extracts produced significant and comparable analgesic effect as with diclofenac sodium.

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Original Research Article
644

GENOME ANALYSIS AND ANNOTATION OF PKC GENE IN BIPOLAR DISORDER

S. SHANTHIPRIYA*, VA DOSS

Keywords: PKC gene, Bipolar disorder, Genome Analysis.

Abstract:

Bipolar disorder (BPD) is a complex genetic disorder in which the core feature is pathological disturbance in mood ranging from extreme elation, or mania, to severe depression usually accompanied by disturbances in thinking and behavior. Recent evidence indicates that an alteration in PKC activity plays a significant role in pathophysiology of BPD. Protein kinase C (PKC) is a group of calcium and phospholipid – dependent enzymes, enriched in brain, where it plays a major role in regulating both pre-and postsynaptic aspects of neurotransmission. Inhibition of PKC plays an important role in neuroprotection against BPD. In this paper we have carried out the Gene location in chromosome, Analysis and Annotation. Coding and non-coding region was also identified to predict the Exon in the gene sequence. By using various Bioinformatics tools, the downstream genes were also identified. This analysis may help in further comparative analysis of genes in various organisms and to design a definite drug which inhibits the activity of the gene in Bipolar disorder

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Original Research Article

BIOPROSPECTING OF MICROBES PRODUCING COMMERCIALLY USEFUL PRODUCTS

SMRITHI S, K. NARAYANAN, J.VENKATA RAO, VENKATESH KAMATH B

DOI:

645

BIOPROSPECTING OF MICROBES PRODUCING COMMERCIALLY USEFUL PRODUCTS

SMRITHI S, K. NARAYANAN, J.VENKATA RAO, VENKATESH KAMATH B

Keywords: Screening, Bioprospecting, Amylase, Antibiotic.

Abstract:

Microbial bioprospecting is screening, isolating and identifying microbes from their natural sources which could be helpful in producing industrially useful products. It is estimated that more than 50 % of the molecules discovered in the world are from natural sources. Among these, microbes form an integral part in production of novel molecules. Although soil screening is an age old method in isolating commercially useful microbes, still it remains largely unexplored. In the present study, bioprospecting of soil samples around Udupi was carried out. Soil samples collected around various locations near Udupi were screened for microbes with antibiotic and amylolytic activities. Among the various isolates screened, KWF-2 showed significant antibiotic and amylolytic activity. Due to the promising result, further studies on characterization and optimization for increasing the yield of antibiotic and amylase are being carried out.

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Original Research Article

COMPUTER AIDED DRUG DESIGN AND DOCKING ANALYSIS OF SOME NOVEL ACAT INHIBITORS

SHAINDA LAEEQ*, ANUP K. SIRBAIYA, HEFAZAT H. SIDDIQUI

DOI:

646

COMPUTER AIDED DRUG DESIGN AND DOCKING ANALYSIS OF SOME NOVEL ACAT INHIBITORS

SHAINDA LAEEQ*, ANUP K. SIRBAIYA, HEFAZAT H. SIDDIQUI

Keywords: Docking, Hyperlipidaemia, Scaffold, Hydrophobic group, Statins.

Abstract:

In the present paper we carried out computational drug designing and docking studies of benzoxazole derivatives on ACAT domain (1WL5) with very low energies.

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Original Research Article
647

DESIGN OF CULTURAL CONDITIONS FOR ENHANCEMENT OF ALKALINE PROTEASE PRODUCTION

SMRITHI, K NARAYANAN, VENKATESH KAMATH B*

Keywords: Screening, Protease, Optimization.

Abstract:

Among the various industrial enzymes studied, proteases are the most widely explored enzyme. They occupy the top position in terms of the amount of enzyme produced commercially. In the present study, soil samples collected from various locations around Manipal, Udupi District, Karnataka were screened for proteolytic activity. Casein agar medium was used as basal medium. The isolate showing highest activity during primary screening was further studied for proteolytic activity. Among the isolates screened, KWF-2 obtained from drains of kitchen waste, showed significant proteolytic activity. Therefore, it was further studied by shake flask culture method. Protease yield was improved through cultural condition optimization. These conditions were optimized by one-factor-at-a-time method. The protease was found to be an alkaline protease. Due to the promising result, further studies on characterization of the enzyme are being carried out.

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Original Research Article
648

PRELIMINARY PHYTOCHEMICAL INVESTIGATION ON RHIZOMES OF COSTUS SPECIOSUS FOUND IN ASSAM, INDIA

BIMAN BHUYAN*, DIPAK CHETIA, PRAKASH RAJAK

Keywords: Costus speciosus, Phytochemical, Ethno medicine, Microscopy, TLC, Pharmacopoeial standards.

Abstract:

Northeast part of India is very rich in natural resources. It is also the home to many ethnic communities who are engaged in practicing traditional medicine since time immemorial. The treatment regimen usually involves the incorporation of natural ingredients thereby developing formulations for treating various ailments. The present study tends to undertake the study of Costus speciosus in the traditional medicines that are practiced in Assam. In this study the initial phytochemical investigation on the plant was carried out that include microscopical analysis of fresh as well as powdered drug, phytochemical analysis of successively extracted crude drugs, TLC characterization and Pharmacopoeial standard determination such as ash value, loss on drying, extractive value etc. The initial study gave preliminary information regarding phytochemical makeup and microscopical characteristic of the plant.

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Review Article

CHELATION THERAPY

G.K.SUDHAKAR*, VENKATESH KAMATH B, ARAVIND PAI,VASUDEV PAI

DOI:

649

CHELATION THERAPY

G.K.SUDHAKAR*, VENKATESH KAMATH B, ARAVIND PAI, VASUDEV PAI

Keywords: Chelating agents, Lead poisoning, Wilson?s disease, Iron poisoning, Thalassemia.

Abstract:

Chelating agents are drugs that complex with and thereby „hold‟ metal ions in inactive form that are suitable for mobilization and subsequent excretion. The principal therapeutic use of chelating agent is to treat heavy metal poisoning. This article describes a list of six chelating agents commonly employed in clinical practice.

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Original Research Article

IDENTIFICATION OF MICROBIOLOGICAL PROFILE OF LEUCORRHOEA IN REPRODUCTIVE AGE GROUP

Dr.NISHAT AFROZE*, Dr.MOHAMMAD IBRAHIM.SHAIK, Dr.SHAIK JAFFAR

DOI:

650

IDENTIFICATION OF MICROBIOLOGICAL PROFILE OF LEUCORRHOEA IN REPRODUCTIVE AGE GROUP

Dr.NISHAT AFROZE*, Dr.MOHAMMAD IBRAHIM.SHAIK, Dr.SHAIK JAFFAR

Keywords: Leucorrhoea, Gynaecology, Candida, Gardenella vaginalis.

Abstract:

Leucorrhoea or vaginal discharge is one of the very common problems or complaints among females of reproductive age group (15 yrs. - 45yrs.) attending to Gynaecology and Veneriology outpatient department .Leucorrhoea or vaginal discharge constitute a considerable problem for many women causing discomfort, anxiety affecting women’s quality of life and consuming considerable resources. The aim of the present study to isolation, identification and to assess the frequency of occurrence of various microbial agents in patients with leucorrhoea attending to Gynaecology,obstetrics and Veneriology, outpatient departments in Owisi Hospital, Hyderabad. This study helps to assess the role of microorganisms in causation of leucorrhoeas. It helps the clinician to give proper treatment and better patient care in this era of antibiotic resistance and immuno deficiency.

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Original Research Article
651

QUANTITATIVE ANALYSIS OF SILODOSIN IN CAPSULES USING UV SPECTROPHOTOMETRY AND RP-HPLC METHODS: APPLICATION TO DISSOLUTION TESTING

CH. DEVADASU*, P. RAVISANKAR, P. SRINIVASA BABU, S.GANANADHAMU, S. SOWJANYA

Keywords: Silodosin, Reversed Phase HPLC, Validation, Dissolution testing

Abstract:

Assay of Silodosin in capsule formulation was done by two ultraviolet spectrophotometric and one isocratic RP-HPLC method. The wavelength of maximum absorption for Silodosin in water was found at 268nm (method-I).The area under the absorption curve was recorded between 263nm and 273nm for each solution (method-II). A reversed phase column C18 (250 x 4.6 mm, 5µm particle size), mobile phase consisting of phosphate buffer pH 3.2: Acetonitrile (60:40v/v) with a flow rate 1.0 mL/min. was used. The effluents of the column were monitored through a variable wavelength UV detector at 230nm (method-III). The proposed methods obeys linearity in the range of 10-60 µg/mL and 4-20 µg/mL for method-I, II and method-III respectively with correlation coefficient values above 0.999. The % RSD was found to be less than 2.0.The mean recoveries were found in the range of 97.50- 99.75%. Validation of the developed methods was performed in terms of accuracy, precision, linearity, etc. The proposed HPLC method has been applied to dissolution testing of the formulation.

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Original Research Article
652

FORMULATION AND EVALUATION OF PULSATILE COLON SPECIFIC HYDROGEL BEADS OF TERBUTALINE SULFATE FOR NOCTURNAL ASTHMA

PADALA SHRUTI*, BOTLA SIRISHA, Dr.V.UMAMAHESHWAR RAO, P.RAJ KUMAR

Keywords: Pulsatile, colon specific, nocturnal asthma, Terbutaline Sulfate.

Abstract:

The purpose of this research was to design and evaluate an oral, pulsutile, colon specific multiparticulate device (hydrogel beads) to achieve time and/or site specific release of Terbutaline Sulfate based on chronopharmaceutical approach. Terbutaline Sulfate is short acting beta-adrenergic agonists which are used only for symptomatic relief of asthma. Nocturnal asthma needs chronotherapeutic approach and Terbutaline Sulfate has short half life with a bioavailability of 30-50% orally. In order to provide a oral colon specific action after predetermined lag time this was chosen as the model drug. Hydrogel beads containing Terbutaline sulfate were prepared by ionotropic gelation technique. Various polymers like sodium alginate, celkol, PVA, metalose SR and chitosan were used in different concentrations and combination in the preparation of hydrogel beads. All the formulations were evaluated for surface morphology, particle size analysis, drug content, entrapment efficiency, swelling index , in vitro drug release was carried out in 1.2 pH buffer, 6.8 pH buffer and 7.4 pH buffer for 2 hours,3 hours and 3 hours respectively to mimic the conditions in GIT. It is concluded that hydrogel beads are the potential system for oral pulsatile colon specific delivery of Terbutaline Sulfate for chronotherapy of nocturnal asthma.

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Original Research Article
653

FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF CARVEDILOL PHOSPHATE

CH. SWATHI KUMARI*, G. SAILAJA, D. PAVITHRA

Keywords: Carvedilol phosphate, Sustained release, Sodium Carboxy Methyl Cellulose, COREG.

Abstract:

The objective of the present research work was to develop sustained release matrix tablets of Carvedilol phosphate (40 mg) using Sodium Carboxy Methyl Cellulose polymer in different ratios, to reduce the dosing frequency. The drug polymer interaction was investigated by FTIR and their results directed further course of formulation. The tablets were prepared by employing direct compression method and were evaluated for various pre compression parameters and post compression studies like weight variation, hardness, friability, thickness, disintegration, drug content and in vitro dissolution studies. In vitro dissolution studies were performed using USP apparatus II (paddle) over a period of 24 hours in 0.1N HCl. The release kinetics was analyzed as per Zero-order, First-order, Higuchi and Peppas equations. The invitro dissolution studies of optimized formulation (F3) showed percentage drug release of about 92.45 % up to 24hrs and showed First-order release kinetics with Fickian diffusion model. The optimized formulation F3 showed similar drug release when compared with innovator (COREG). The result of stability studies (40±2oC/75±5% RH), showed no change in physical properties and in vitro dissolution profile of F3. As per release profile, a decrease in release rate was observed with increase in the viscosity of polymer.

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Original Research Article
654

FORMULATION AND EVALUATION OF TRIHEXYPHENIDYL HYDROCHLORIDE IMMEDIATE RELEASE TABLETS

SURAJ PRAKASH. H*, P. VISHNU, V.UMAMAHESWARA RAO

Keywords: Trihexyphenidyl, Immediate release, Super disintegrants, Wet granulation, Parkinson’disease.

Abstract:

The main objective of this research work was to formulate and evaluate the immediate release tablets of Trihexyphenidyl HCL 5mg, an M1 muscarinic acetylcholine receptor antagonist. It blocks cholinergic activity in CNS, which is responsible for the symptoms of Parkinson's disease. The tablets are prepared by direct compression method and wet granulation method. The formulations was optimized by incorporating varying composition of sodium starch glycollate and pregelatinised starch as super disintegrant, lactose and microcrystalline cellulose as diluent, povidone K-30 as binder and magnesium stearate agent as lubricant. All the excipients are tested for compatibility with drug, which revealed that there was no physical and chemical interaction occurred. The Preformulation parameters such as bulk density, tapped density, compressibility index and Hausner ratio were analyzed. The thickness, hardness, friability, weight variation, disintegration time and drug content uniformity was evaluated for core tablets. The effect of these variables on drug release also studied. The In-vitro drug release studied was performed in the USP dissolution apparatus-II (paddle) using pH 4.5 acetate buffer as dissolution media at 100rpm. The cumulative amount of drug release at different intervals is estimated using HPLC method. Based on the evaluation result the formulations F-8 containing MCC and SSG (6%) showed 98.5% release in 30 mins and so it was optimized as best formulation.

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Original Research Article

FORMULATION AND IN-VITRO EVALUATION OF BOSENTAN MONOHYDRATE MICROSPHERES

M.DIVYA*, Mrs.CH.S.VIJAYA VANI, Dr.V.UMAMAHESHWAR RAO

DOI:

655

FORMULATION AND IN-VITRO EVALUATION OF BOSENTAN MONOHYDRATE MICROSPHERES

M.DIVYA*, Mrs.CH.S.VIJAYA VANI, Dr.V.UMAMAHESHWAR RAO

Keywords: Bosentan monohydrate, microspheres, antihypertensive, solvent evaporation method.

Abstract:

The present study performed by Formulation and Evaluation of microspheres of Bosentan monohydrate which is an anti-hypertensive drug. Microspheres were formulated with various materials like HPMC K4M, HPMC K15M, HPMC K100M, Carbopol 934P as rate controlling polymers. The microspheres were prepared by Solvent evaporation method. The variant proportion of the polymers HPMC K100M, Carbopol showed significant difference in the release rates. The drug release rate decreased as the concentration of carbopol is increased.

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Original Research Article
656

RP-HPLC METHOD DEVELOPMENT AND VALIDATION FOR THE ASSAY OF ZILEUTON IN BULK DRUG AND PHARMACEUTICAL FORMULATIONS

M.MOUSAMI*, A.KRISHNAMANJARI PAWAR, D.V.V. RAMA RAJU

Keywords: Zileuton, RP-HPLC, isocratic mode.

Abstract:

Zileuton is an antiasthmatic durg. It acts by inhibiting 5-lipoxygenase enzyme thereby preventing formation of leukotrienes that cause bronchoconstriction. The new, simple, accurate, sensitive robust, reproducible, isocratic RP-HPLC method was developed using Xterra C 18 column (5µm, 250 × 4.6mm), at 1ml/min flow rate with 10min run time using 20µl injection volume and 25°C temperature conditions. The detection wavelength used is 299.5nm. Retention time is obtained at 3.155min. Linearity was established in the range of 2 to 10µg/ml with 0.999 correlation coefficient and % recovery of 99.6 – 99.9%. The method is validated according to the specifications in ICH guidelines.

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Original Research Article
657

STUDIES ON OPTIMIZATION OF ANTIBIOTIC PRODUCTION BY ISOLATE C9

*S. JOSHNA RANI

Keywords: Actinomycete, Antibiotics, nutrient effects, cultural conditions.

Abstract:

A new actinomycete species (Pseudonocardia species) which was designated as C9 with broad antibacterial activities was isolated from soil samples of Tirumala Hills and characterized by our Lab. Nutritional and cultural conditions for the production of antibiotic by this organism under shakeflask conditions have been optimized. The results shown the inhibition rate is the highest under the optimum medium composition containing soyabean meal 2.5%, Glucose 2.6%, NaNO3 0.5%, K2HPO4 0.4%, Nacl 0.25%, ZnSO4 0.004%, CaCO3 0.04%. Maximum antibiotic activity is obtained at the inoculation volume 10%, medium to flask ratio was maintained at 0.2 levels, incubated at 280C on a rotary shaker (140 rpm) fermentation was terminated at 144hr. The results indicated that against this test organism (pseudomonas fluorescens) the zone of inhibition observed in the initial production was 28mm, which increased to 33mm in production medium PM, after optimization of the constituents and cultural conditions of production medium PM the zone of inhibition increased to 36mm. this indicates that a significant increase in antibiotic production was achieved after optimization.

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Review Article

ABC OF SLEEPING DISORDER

G.K.SUDHAKAR*, ARAVINDA PAI, VENKATESH KAMATH B

DOI:

658

ABC OF SLEEPING DISORDER

G.K.SUDHAKAR*, ARAVINDA PAI, VENKATESH KAMATH B

Keywords: Sleep disorder, rapid eye movement, insomnia

Abstract:

Sleep is said to be the overall barometer of our health. Alterations in the quality, quantity and pattern of sleep can result in sleep disorders. Persistent and repeated interruption of sleep affects the health of an individual. The lack of quality sleep can have a negative impact on an individual’s energy and emotional balance.

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Review Article
659

METALLIC NANOPARTICLES – VERSATILE PLATFORMS FOR TARGETED DRUG DELIVERY

V. SWATHI*, P. RAVISANKAR

Keywords: : Metallic nanoparticles, cancer, drug delivery, specificity, gold nanoparticles

Abstract:

In the past few decades there has been tremendous enhancement in usage of nanotechnology for formulation of novel drug delivery systems that are intended for diagnosis and treatment of diseases in general and cancer in particular. Cancer is the most wide spread disease throughout the world with millions of new cases every year. Nanotechnology based cancer therapy with minimal side effects and maximum target specificity is on wave, with the main challenge to develop a molecular therapy that circulates in blood undetected by the immune system and recognize the specific target site or organ at which it elicits its therapeutic action. Metallic nanoparticles target cancer cells and cause death of tumor by thermal ablation, hyperthermia etc. The nano size of these metallic nanoparticles also helps in increasing their accessibility towards various compartments of the cells including their nucleus and also cross the blood brain barrier. This potential of nanoparticles to cross the blood brain barrier opens a new way for drug delivery to the brain. The interaction of nanoparticles with various cells, tissues and their toxicity depends upon their composition and chemical nature. Nanoparticles, especially metallic nanoparticles act as versatile agents with a number of bio-medical applications. Hence formulation of metallic nanoparticles brought about a ―big revolution‖ in both medical and pharmaceutical fields.

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Review Article

A REVIEW ON POLYMERS OF GASTRORETENTIVE DRUG DELIVERY: FLOATING MICROSPHERE

BOGA.SHALINI KRISHNA*, Dr.V.UMA MAHESWARA RAO, K.MAHALASKHMI, K.SHRUTHI

DOI:

660

A REVIEW ON POLYMERS OF GASTRORETENTIVE DRUG DELIVERY: FLOATING MICROSPHERE

BOGA.SHALINI KRISHNA*, Dr.V.UMA MAHESWARA RAO, K.MAHALASKHMI, K.SHRUTHI

Keywords: Floating microspheres, Gastroretentive drug delivery, Floating Drug Delivery Systems, Polymers

Abstract:

Delivery of the drug at controlled release rate to the specific body site is of paramount importance in the health care system. Gastroretentive drug delivery system helps in increasing the retention of the drugs at the intestinal region which have narrow absorption window, low bioavailability etc. Therefore, different novel strategies have been undertaken for the designing of several Gastroretentive drug delivery systems including floating microspheres. Floating microspheres are one of the novel approaches which are specially gaining attention due to their wide applicability in the targeting of drugs to stomach. These floating microspheres have the advantage that they remain buoyant and distributed uniformly over the gastric fluid to avoid the vagaries of gastric emptying and release the drug for prolonged period of time. The polymers used in the Floating Drug Delivery Systems are mainly involved in controlled release of drug from the delivery system which shows better results on selection of proper polymers and in their optimization. This article mainly emphasis on development techniques, effect of polymers on floating microspheres, characterization and applications.

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Original Research Article

FORMULATION AND EVALUATION OF BILAYERED TABLETS OF CANDESARTAN CILEXITIL

M.PRAVEENKUMARREDDY*, CH.S.VIJAYA VANI, P. VISHNU, K B.V YASASWI

DOI:

661

FORMULATION AND EVALUATION OF BILAYERED TABLETS OF CANDESARTAN CILEXITIL

M.PRAVEENKUMARREDDY*, CH.S.VIJAYA VANI, P. VISHNU, K B.V YASASWI

Keywords: Candesartan cilexitil, bilayered tablets, direct compression technique Cross povidone, carbopol

Abstract:

Candesartan cilexitil is an angiotensin II receptor antagonist used mainly for treatment of hypertension. Results from the CHARM (Candesartan in Heart failure - Assessment of moRtality and Morbidity) study in the early 2000s demonstrated the morbidity and mortality reduction benefits of Candesartan therapy in congestive heart failure. Candesartan cilexetil is sold under the brand name “Atacand” in the United States by ASTRAZENECA. So, the aim of the present study is to develop and evaluate Candesartan cilexetil bilayered tablets.Candesartan cilexitil immediate release formulation were prepared by direct compression technique using Cross povidone as super disintegrant in order to enhance its solubility and bioavailability and S.R formulation were prepared by direct compression technique using carbopol as polymer In total 21(9 I.R and12S.R )formulations have been prepared. Precompression and post compression parameters have been evaluated. The dissolution studies were carried out using USP Type 2 apparatus. Among the formulations F-12 showing a maximum drug release of 99.9% in 16 hrs was selected as the best one.

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Original Research Article
662

ANTIDIABETIC ACTIVITY OF BAMBUSA ARUNDINACEAE ROOT EXTRACTS ON ALLOXAN INDUCED DIABETIC RATS

SRIDHAR RAO.GONA*, NAGA APARNA.T

Keywords: Bambusa arundinaceae root, Antidiabetic activity, Alloxan, Glibenclamide

Abstract:

Aqueous ethanolic solvent extracts of Bambusa Arundinaceae root (Bambsaceae) were tested for antidiabetic activity using alloxan induced diabetic rats and compared with standard. The results expressed that aqueous ethanolic extracts had shown significant protection and maximum reduction in blood glucose was observed in alloxan induced diabetic rats. The results of this comprehensive study reveal that Bambusa arundinaceae seed shown statistically significant Anti-Diabetic activity in comparison to the standard glibenclamide.

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Original Research Article

FORMULATION AND EVALUATION OF EXTENDED RELEASE TABLETS OF DARIFENACIN HYDROBROMIDE

R.RAVI TEJA*, G.CHIRANEEVI, Dr.V.UMAMAHESHWARA RAO, P.VISHNU

DOI:

663

FORMULATION AND EVALUATION OF EXTENDED RELEASE TABLETS OF DARIFENACIN HYDROBROMIDE

R.RAVI TEJA*, G.CHIRANEEVI, Dr.V.UMAMAHESHWARA RAO, P.VISHNU

Keywords: Darifenacin Hydrobromide, Direct Compression, Hydroxy propyl methyl cellulose, Metalose 60SH 50, Extended Release

Abstract:

The objective of this research work was to develop extended release tablets of Darifenacin Hydrobromide using different hydrophilic polymers like HPMC K15M, HPMC K100M, Metalose60SH 50, Xanthan gum by direct compression method. Various amounts of polymers was used in the twenty one proposed formulations (F1to F21) for the study of release rate retardant effect at 15%, 20%, and 30% of total weight of tablet matrix respectively. Then the tablets were evaluated in terms of their physical parameters (weight variation, hardness, friability and thickness), drug content and in-vitro release studies. All the formulations showed compliance with pharmacopoeial standards, their in-vitro dissolution study were conducted using USP dissolution apparatus type-II (paddle method) in 900 ml 0.1 N HCl for first 2 hrs and remaining period performed in 7.4 pH phosphate buffer at 100rpm for a total period of 24hrs. The release mechanisms were explored and explained by Zero order, Higuchi, First order and Krosmeyer-Peppas equations. Based on the dissolution data comparison with innovator product, formulation F17 was found as the best formulation. The drug release profile of this formulation was well controlled and uniform throughout the dissolution studies. The drug release of formulation F17 followed First Order kinetic model and the mechanism was found to be non-Fickian/anomalous according to Korsmeyer-Peppas equation.

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Review Article
664

REGULATION OF COSMETICS AND ITS ADVERTISEMENTS IN INDIA WITH AN OVERVIEW OF US REGULATIONS

DEEPTHI V, SUDHEER MOORKOTH*

Keywords: Cosmetics, Labelling, Regulations, India, US, Licensing, Safety.

Abstract:

Cosmetic products are the subjects for regulatory controls in all the markets in order to ensure safety of these products and to avoid adverse impacts on the health of the users. Media advertising is an important means for a cosmetic seller to awaken interest in his products. There are different regulatory bodies worldwide having their own regulations to ensure safety of the cosmetic products and to control advertisements. European Union (EU) andthe United States of America (US) constitute the major cosmetics market. The Cosmetics market in India is growing at 15-20% annually, twice as fast as that of the United States and the European market. A regulation that can ensure safety of the consumers is the need of the day in this scenario. The regulations which impact directly on the manufacture and sale of cosmetic products include definitionof cosmetic, licensing, labeling, safety substantiation, stability studies and legal authority. This studyanalyses the current cosmetics regulations put forward by the Drugs and Cosmetics rules and various advertisements regulation concerning cosmetics in India. An overview of United States (US) regulations concerning cosmetics also is provided to analyse the differences in regulations and to propose the need for harmonisation of regulations concerning cosmetics globally.

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Review Article
665

CURRENT SCENARIO AND REGULATORY FRAMEWORK OF PAEDIATRIC DRUGS IN THE UNITED STATES (US) AND EUROPE WITH A BRIEF PERSPECTIVE TO INDIA

SARASWATHI DEEPTHI, SUDEEP M, SUDHEER MOORKOTH*

Keywords: Paediatric drugs, Regulatory framework, United States, Europe, India

Abstract:

Since from decades, healthcare professionals were unable to provide suitable information for prescribing medicines for the treatment ofpaediatric population. Many depended on off-labeled drugs by manipulating the adult dosage form, simply by crushing the tablets or diluting the syrups. Even though there iseminent differences between children and adults, most of the drugs that have been developed for adults are simply used for children without necessary studies. This kind of practice is therapeutically successful for the drugs which have a wide therapeutic window and thus are relatively safe.There exist some barriers in developing paediatric drugs. Major regulated nations have identified these barriers and have developed specific regulations that will enhance the paediatric drug development. This includes the Best Pharmaceuticals for Children‟s Act (BPCA), Paediatric Research Equity Act (PREA) of the United States and the Paediatric Investigation Plan (PIP) of Europe. This article highlights the global situation of paediatric medicines and their regulations in Europe and United States (US) with a brief perspective to India.

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Original Research Article

FORMULATION AND EVALUATION OF FLOATING TABLETS OF FAMOTIDINE

S. RAVINDER REDDY*, P. VISHNU, V.UMAMAHESWARA RAO, SURAJ PRAKASH.H, K.B.V.YASASWI

DOI:

666

FORMULATION AND EVALUATION OF FLOATING TABLETS OF FAMOTIDINE

S. RAVINDER REDDY*, P. VISHNU, V.UMAMAHESWARA RAO, SURAJ PRAKASH.H, K.B.V.YASASWI

Keywords: Famotidine, Floating tablets, HPMC, Carbopol 934p, Sodium bicarbonate, direct compression, sustained release

Abstract:

The objective of the present investigation is to formulate floating tablets of Famotidine. A histamine H2 receptor antagonist widely prescribed in ulcers like duodenal and gastric Ulcer. The short biological half-life (2.5 - 4 hours) and maximum absorption in initial part of small intestine, colonic metabolism of Famotidine favors’ development of gastro retentive floating dosage form. In the present study Famotidine floating tablets were prepared by effervescence method using sodium bicarbonate as a gas generating agent. The tablets were formulated using direct compression technology by employing polymers like HPMC K4M, HPMC K15M, HPCM K 100M and carbopol 934p. The drug-excipient compatible studies were performed by FTIR, The FTIR study revealed that there is no drug-excipient interaction. The prepared floating tablets were evaluated for various physicochemical parameters such as flow properties, hardness, weight variation, friability, in vitro buoyancy (floating lag time, total floating time), swelling studies, drug content and in-vitro drug release. The in vitro drug release pattern of Famotidine floating tablets was fitted to different kinetic models which showed highest regression for zero order kinetics with higuchi mechanism. Out of all formulations the one prepared with carbopol 934p and HPMC K100Mcombination was optimized based on desired sustained release time (12hrs) followed by acceptable swelling and floating properties.

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Original Research Article

FORMULATION AND EVALUATION OF EXTENDED RELEASE TABLETS OF PALIPERIDONE

THIRUMAL KOLA*, Dr.V.UMAMAHESHWARA RAO, CH.S.VIJAYA VANI

DOI:

667

FORMULATION AND EVALUATION OF EXTENDED RELEASE TABLETS OF PALIPERIDONE

THIRUMAL KOLA*, Dr.V.UMAMAHESHWARA RAO, CH.S.VIJAYA VANI

Keywords: Paliperidone, HPMC, PVP, Poly ethylene oxide, Evaluation parameters, In-vitro dissolution studies, release kinetics

Abstract:

The present research work was an attempt to formulate and Evaluate paliperidone extended release tablets. A combination of Hydroxy propyl methyl cellulose (HPMC K100M) and PVP, poly ethylene oxide were used as polymers. The tablets were prepared by direct compression method 12 formulations were prepared by changing the ratios of the drug and polymer to study the effect of variable concentrations of polymers and characteristics of the tablets. The prepared tablets were evaluated by different parameters such as Thickness, Weight variation, Hardness, Content Uniformity. The tablets were also evaluated for in vitro drug release in 0.1N HCl for 12 h in USP Type II dissolution apparatus. Among all the formulations (F-I to F-XII) prepared, batch F-12 gave relatively slow release of Paliperidone over 24 h when compared to other formulations. The invitro data is fitted in to different kinetic models and the best-fit was achieved with the Korsmeyer-Peppas model. Hence, formulation F12 was found to be equivalent to marketed product with good bioavailability properties. It also showed no significant change in physical appearance, Drug content. The drug carrier interactions were investigated in the solid state by Fourier transform infrared spectroscopic study(FTIR), which was further confirmed by DSC.

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