IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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OCTOBER 2014
1

METHOD DEVELOPMENT AND VALIDATION OF SIMULTANEOUS ESTIMATION OF AMLODIPINE AND CANDESARTAN BY REVERSE PHASE HPLC IN TABLET DOSAGE FORMS

M,Bindu, G.Kumaraswamy* ,N.Ravindra.

Department of pharmaceutical analysis, Chilkur Balaji College of Pharmacy, Aziz Nagar –Hyderabad. 500075, Telangana.

Abstract

A simple, accurate, rapid and precise isocratic reversed-phase high-performance liquid chromatographic method has been developed and validated for simultaneous determination of Amlodipine and Candesartan in tablets. The chromatographic separation was carried out on a Phenomenax Luna ODS analytical column (250×4.6 mm; 5 μm) with a mixture of acetonitrile: phosphate buffer pH 3 adjusted with orthophosphoric acid (80:20, v/v) as mobile phase; at a flow rate of 1.0 ml/min. UV detection was performed at 235 nm. The retention times were 2.526 and 5.526 min. for Amlodipine and Candesartan respectively. Calibration plots were linear (r2>0.998) over the concentration range 10-60 μg/ml for Amlodipine and 10-60 μg/ml Candesartan. The method was validated for accuracy, precision, specificity, linearity, and sensitivity. The proposed method was successfully used for quantitative analysis of tablets. No interference from any component of pharmaceutical dosage form was observed. Validation studies revealed that method is specific, rapid, reliable, and reproducible. The high recovery and low relative standard deviation confirm the suitability of the method for routine determination of Amlodipine and Candesartan in bulk drug and tablet dosage form.

2

DESIGN AND IN-VITRO EVALUATION OF COLON TARGETED ORAL MATRIX TABLETS OF MESALAMINE FOR THE TREATMENT OF INFLAMMATORY BOWEL DISEASES

M.Raju, Virajaji Kaya, Bonagiri Sreedevi, R.suthakaran, Mohammed Ehteshamuddin. 

Teegala Ram Reddy College of Pharmacy, Meerpet Hyderabad– 500097, Telangana (State). India.

 Abstract

Colon specific drug delivery has gained increased importance not just for the delivery of drugs for the treatment of local diseases associated with the colon but also as potential site for the systemic delivery of therapeutic peptide and proteins. Mesalamine is an anti-inflammatory agent mainly used in treatment of inflammatory bowel diseases. The colon targeted matrix tablets containing Guargum, Xanthumgum, Ethyl cellulose and Cellulose acetate pthalate as polymers were prepared by wet granulation method. Lactose was used as a diluents and mixture of Talc and Magnesium stearate (1:1) was used as a Glidant and Lubricant respectively. Accurate quantity of drug and all ingredients were weighed according to formula and mixed well except Magnesium stearate and Talc. Accurately weighed 550 mg granules were fed manually in to 16 stations Cadmach tablet compression machine and compressed with 14 mm flat faced punches. The dissolution study of CT2 Matrix tablet containing Guar gum and Xantham gum was concluded the best formulation among other formulations, which showing the most desired drug release which is considered as optimized formulation. This retardant capacity is more in CT2 as compared to CT1. Formulation CT2 showed the highest swelling index. This may be due to the increased viscosity of the Xanthumgum in presence of Guargum than the Guargum alone and Guargum in combination with Ethyl cellulose and cellulose acetate pthalate. Out of the eight formulations, it appears that CT2 has the maximum potential in providing colon targeted drug delivery.

3

ANTHELMINTIC ACTIVITY OFCLITORIA TERNATEA AGAINST PHERETIMA POSTHUMA

Kamarapu.Pallavi*,momula Swathi,thati swetha

SSJ College of pharmacy –Gandipet-Hyderabad.

Abstract

Shankhpushpi is a popular medicinal plant in the Ayurvedic system of medicine for treat mental disorders. It is used traditionally to treat nervous debility, insomnia, fatigue, low energy level and loss of memory. It has emerged as a good source of traditional medicine for Antifungal activity, Antibacterial activity and Antiviral activity. In present studies, Anthelmintic activity was also performed against Earth worm by using invitro method. The paralysis time and death time were determined. The various extracts of different concentrations are Methanol, Chloroform and Aqueous (i.e 10, 20,40,60,80 mg/ml) were prepared .In that methanol extract found to have a anthelmintic activity compared with other extracts against Earth worm by using the standard as Albendazole.

4

FORMULATION OF HERBAL HYDROGELS FOR WOUND HEALING ACTIVITY BY USING VITIS VINIFERA SEEDS EXTRACT

Raju .Manda, Virajaji kaya, Bonagiri sreedevi, Mohammed, R. Suthakaran, Ch. mounika.

Teegala Ram Reddy College of Pharmacy, Meerpet Hyderabad– 500097,Andhra Pradesh, India.

Abstract

The present study was carried out to explore the phytochemical and pharmacological studies on seeds of Vitis vinifera. Formulation was made by ethanolic extracts of Vitis vinifera and made into gel form. The extract was subjected to preliminary phytochemical screening which indicates the presence of carbohydrates, proteins, alkaloids, flavanoids, tannins. The wound healing activity of compound was pharmacologically evaluated by excision method on swiss albino rats. It was concluded that the ethanolic extract and herbal formulation shows significant wound healing activity compared to standard compounds.

5

FORMULATION DEVELOPMENT, EVALUATION AND ANTI-INFLAMMATORY EFFECTS OF ETORICOXIB CREAM

Muhammad Razi Ullah Khan1, 2, Musaddique Hussain1 , Shahid Masood Raza1, Saeed Ur Rashid Nazir2

1The University of Faisalabad, Faisalabad, Pakistan.

2University of Sargodha, Sargodha, Pakistan.

Abstract

Non-Steroidal Anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase (COX)-2 inhibitors, have come to play an important role in the pharmacologic management of musculoskeletal disorders. Clinical trials have established the efficacy of etoricoxib in Osteoarthritis, Rheumatoid Arthritis, Acute Gouty Arthritis, Ankylosing Spondylitis, Low back pain, acute postoperative pain, and primary dysmenorrheal. The present research has been undertaken with the aim to develop a novel topical cream formulation of etoricoxib, which would attenuate the gastrointestinal relater toxicities associated with oral administration. Etoricoxib is a highly selective cyclooxygenase‐2 (cox‐2) inhibitor. In the present study, a fixed concentration of Etoricoxib cream (1%) was prepared by using a different combination of Active ingredient and Excipients. To access the efficacy of formulated cream, in-vitro evaluation including stability studies, tube extrude ability, spread ability, pH, viscosity and rheological properties and drug diffusion studies were carried out. After in vitro evaluation of cream formulations, the formulation was evaluated for the anti‐inflammatory and skin irritation study. The results obtained were encouraging and formulation containing Etoricoxib (1%) exhibited the most satisfying results of all the parameters.

6

CHITINASE PRODUCTION FROM SEAFOOD WASTES BY FUSARIUM SOLANI SPS AND ITS APPLICATION IN BIOREMEDIATION STUDIES

Krishnaveni.B1 and Ragunathan.R2*
 
1Department of Biotechnology, Maharaja Co-education Arts and Science College, Perundurai, Erode, India-52.
2Senior Scientist (R&D), Synkromax Biotech Private Limited, Chennai, India-16.

Abstract

Mangrove environment contains very rich microbial diversity due to the high amount of dissolved organic matter. Chitinases are glycosyl hydrolases which catalyze the degradation of chitin. The aim of the study was to use the chitinolytic activity of fungus Fusarium solani CBNR BKRR isolated from the marine soils of Pichavaram, Tamil Nadu and consequently to use it for the biodegradation of four different marine wastes-Crab shells, Snail shell, Shrimp shell, Fish scales. The crude chitinase was characterized and maximum activity was obtained in reaction mixture of 50°C incubation temperature, 2 ml crude enzyme, 0.5 ml of 10% colloidal chitin, pH 6 and reaction time of 10 min. Maximum enzyme activity was obtained in the case of Snail shell wastes (5.5 U/min), followed by Crab shell (4.0 U/min), Shrimp shell (3.9 U/min) and fish scales (3.6 U/min). The amount of marine wastes degraded was as follows-Crab shell (0.02g), Snail shell (0.12g), Shrimp shell (0.52g) and Fish scales (1.44g). The results indicated that Fusarium solani is efficient fungus to produce highly active chitinase when grown in statistically optimized medium containing Snail shell, Crab shell, Fish scales and Shrimp shells as substrates.

7

VIRUSES AND HUMAN CANCER: FROM CAUSALITY TO CURE

Chaube Hitesh , Dhande Swati, Kadam Vilasrao

Department of Pharmacology, Bharati Vidyapeeth’s College of Pharmacy/Mumbai University, India.

Abstract

The role of viruses in cancer may be viewed as a double-edged sword. It is estimated that about 20% of all cancer case across the globe is due to persistent viral infections. Oncoviruses can be DNA or RNA viruses that induce mutation in the target host cell, although perseverance of viral infection alone is not adequate for formation of tumors but is one of the steps in the multi-step process of cancer development. The virus infected host cells after having undergone genetic changes enter cell cycle and produce next progeny of transformed cells which have characteristics of autonomous growth and survival completing their role as oncogenic virus. The traditional chemotherapy and radiotherapy have limited therapeutic index and plethora of treatment related side effects. This situation has provided a thrust for search of novel therapeutic strategies that can selectively destroy tumor cells, leaving the normal cells unharmed. Recent technical advances in the genetic modification of the virus to improve their tumor specificity have led to the transformation of virus as weapon against cancer called as Oncolytic virus. This review attempts to summarize the causative association of virus with cancer and the techniques by which the virus can be metamorphosed as cure that kills tumor cells along with developments made on Oncolytic virotherapy for cancer treatment.

8

THE EFFECT OF ALOE VERA JUICE ON DERMAL WOUND HEALING IN ALBINO MICE.

Mukesh Kumar, Neelmani,Ranjit Kumar,Nandjee Kumar

Mahavir Cancer Institute & Research Centre, Phulwarisharif, Patna.

Abstract

In spite of tremendous advances in the chemical drug industry, the availability of substances capable of stimulating the process of wound repair is still limited. The present work was aim to investigate wound healing efficiency of Aloe vera gel on excision wound model .This study was undertaken to evaluate the wound healing properties of Aloe vera,for this purpose different conc. of aloe vera juice(5%; 25%; 50% v/v topically) were applied with respect to NSS and chemotherapeutic agent like betadine on excision wound in albino mice. The effect of Aloe vera juice application on excision wound contraction (area in mm2) in mice was observed on 4th day, all means vary significantly (p<0.01) with each other. Higher wound contraction was achieved with 5% (137.427±3.454mm2) followed by 25% (85.068± 1.872mm2) and 50% (54.583 ±1.904mm2) of Aloe vera gel as compared to the Normal Saline Solution (NSS) ,(29.327±1.087mm2) and Betadine (50.265± 1.798mm2). It is clears that the higher wound contraction area (in mm2) was observed in Aloe vera treated wound having maximum with 5% (192.523± 2.903mm2) followed by 25% (179.118±4.511mm2) and 50% (152.452±15.577mm2) as compared to the NSS (114.665±6.066 mm2) and Betadine (143.842±11.446 mm2) treated group on 16th day of wound creation .The treated group varied significantly with p<0.01 on 16th day of wound creation. The difference of mean of healed area of two consecutive (0-4) days within treated groups was found to be maximum with 5% (137.427±3.454mm2) followed by 25% (85.068± 1.872mm2) and 50% (54.583 ±1.904mm2) as compared to the Normal Saline Solution (NSS),(29.327±1.087mm2) and Betadine (50.265±1.798mm2).On the basis of outcome of this present study,the application of Aloe vera gel(5% ) for the treatment of traumatic or cut wound is recommended.

9

IMPACT OF LEAF EXTRACT OF NEEM (AZADIRACHTA INDICA)ON GASTRO-INTESTINAL ULCER IN ALBINO MICE

Neelmani , Mukesh kumar, Ranjit Kumar, Nandjee kumar

Mahavir Cancer Institute & Research Centre, Phulwarisharif, Patna, India.

Abstract

The work embodied in this study is to evaluate the anti ulcer property of Neem leaf extract on aspirin induced gastric ulceration in albino mice. Ranitidine, the most widely used and common H2 blocker was taken. Ulcer induction was done by the administration of aspirin orally. This method was chosen because administrations of aspirin result in the production of gastric mucosal damage mainly in the glandular segment of the Albino mice stomach, which is analogous to the body of stomach in man. The freshly prepared aqueous solution of NLE administered in doses of 20, 40, 80, and 160 mg/kg body weight produced dose dependent reduction in ulcer index against aspirin induced ulcers in different groups of mice. The doses of NLE were selected according to Garg, who have studied NLE against stress ulcers in mice. The reduction in ulcer index with NLE was statistically significant at 40 and 80 mg/kg body weight and highly significant protection was observed with 160 mg/kg of NLE. NLE in a dose of 160mg/kg is more effective than ranitidine (25mg/kg) as regards its anti ulcer activity. This study had also established that a low dose of NLE produced equally beneficial effect in reducing gastric ulcer. Thus from the above study it may be inferred that NLE possess a significant and definite ulcer protective action. It is also postulated that the ulcer protective action of NLE is due to inhibition of H+ K+ ATPase activity in concentration dependent manner. This ultimately leads to the rational and logical conclusion of the antiulcer properties of NLE.

10

FORMULATION AND CHARACTERIZATION OF SR MATRIX OF ENDOTHELIN RECEPTOR ANTAGONIST OF BOSENTAN BY VARIOUS NATURAL POLYMERS

Y.Ganesh Kumar*1, J.Sreekanth2, D.Satyavati1

1Sree Dattha Institute of Pharmacy, Sheriguda, Ibrahimpatnam, R.R Dist, TS, India.

2R&D, MSN Laboratories Pvt. Ltd, Hyderabad, TS, India.

Abstract

The Present investigation an attempt has been made to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance, by developing SR Matrix tablets of Bosentan is an Endothelin Receptor Antagonist (ERA) indicated for the treatment of Pulmonary Arterial Hypertension (PAH). Bosentan Sustained Release Matrix Tablets were prepared by using different natural polymers like Xanthan gum, Guar gum, Pectin at different ratios of Drug: Polymer. The Matrix tablets were prepared by Wet granulation method. The prepared tablets were selected for DSC and FTIR studies. The tablets were selected for DSC and FTIR studies did not show any chemical interaction between drug and polymer. The prepared tablets were evaluated for various Physico chemical parameters. Invitro drug release study was carried out in simulated gastric fluid (0.1N Hcl) for the first 2 hours and in Phosphate buffer (PH 6.8) for the next 10 hours following USP Paddle method. The release kinetics was analyzed using the Zero-order, first order model equation, Higuchi’s- square root equation, and Korsmeyer-Peppas model. Among the all formulations, F7 formulation containing Drug to Pectin in ratio 1:0.5 is optimized based on its ability to sustain drug release till 12 hrs of dissolution study. The Optimized formulation F7 showed zero order release with fairly linear as indicated by their high regression values (R2 = 0.9928). Results revealed that F7 formulation follows the zero order transport mechanism.

11

EFFECT OF SELENIUM FORTIFICATION ON BIOCHEMICAL ACTIVITIES OF TOMATO (SOLANUM LYCOPERSICUM) PLANTS

Nancy D & P. Indra Arulselvi*

Plant and Microbial Biotechnology Lab, Department of Biotechnology, Periyar University, Salem, Tamil Nadu, India.

Abstract

Nutritional research is being the most required ground, due to the existing human health and micronutrients deficiencies. Hence, urged the need to supplement the micronutrients through the diet. Fortification is known to be an effective way to improve the organic content in plants. Fortification of micronutrients will lead to biochemical modifications, during its assimilation into the plants. This in turn affects the plant growth parameters and consequently the nutritional profile of the fruits. Thus, the present work is carried out to study the effect of selenium (Se) fortification on the biochemical characteristics. However, results can differ significantly among the different modes of fortification, concentrations of inorganic source supplemented and the cultivars. Hence, this work includes fortification by three methods; like seed soaking, soil application and foliar spray using sodium selenate as inorganic source. Compared with the control, the selenium fortification had improved the growth parameters and the fruit quality. The reduction of photosynthetic pigment contents indicates the site of selenium accumulation in the chloroplasts, which reduced the pigment production. It was supported by increase in nitrate and total protein contents by 28.5 and 25% respectively in the fruits. Similarly increase in total phenolic content and antioxidant activity by 46.54 and 54% respectively, in T4 concentration of foliar spray method proves the nutritional enhancement on selenium fortification. The results suggested that foliar application of sodium selenate at 8 and 10mg.L-1concentrations could accelerate high selenium accumulation in tomato plants. The highest amount of total selenium was recorded as 52.24 μg.g-1DW in T4 fruits by foliar application. The form of selenocompounds accumulated in the fortified fruits was investigated as MeSeCys and SeMet. The biochemical characterization proved the nutritional quality enhancement of selenium fortified tomatoes by its increase in total phenolic and total protein contents. It indirectly indicates the increase in antioxidant enzyme production in the selenium fortified tomatoes. It is indispensable to emphasize selenium fortification in different genotypes, to develop the selenium fortification. Thus, selenium fortified tomatoes can serve as a nutraceutical food to improve the human health.

12

REVIEW ON MARINE ALGINATES AND ITS APPLICATIONS

Neelaveni Nalamothu*, Anusha Potluri, Madhu B Muppalla

*Department of Pharmaceutics, Birla Institute of Technology & Science (BITS), Hyderabad.

Abstract

Marine organisms are good candidates for biomedical field due to their characteristic properties like biocompatibility and biodegradability which is almost uncountable and continuously increasing with the research in deeper waters. Sulfated polysaccharides found in different algae species in the marine environment, resemble the chemical and biological properties of mammalian glycosaminoglycans because of which they are receiving growing interest for application in health-related fields. Alginates belongs to a family of un-branched binary copolymers, consisting of (1→4) linked β-D Mannuronic acid (M) and α-L-glucuronic acid (G) residues of varying composition and sequence. The potential commercial uses of alginates is due to simplification of alginates chemical structure which consisting of two monomer units like M-block and G-block. Commercial alginates are polyuronic saccharides that are isolated from the cell walls of a number of brown seaweeds or brown algae species around the world and also produced as an extracellular matrix by certain bacteria. The improvement in the performance of marine-derived polysaccharides will directly impact on their competitiveness against synthetic biodegradable polymers. Even though, to obtain medical grade biopolymers from marine raw materials in a reproducible way strong efforts are still required. The future growth in the market of alginates is expected to be most likely qualitative rather than quantitative as manufacturers moving away from alginate commodity to refined products. In this review special emphasis was given on the occurrence along with the extraction of alginates, their different properties (specifically ion binding, gel formation and biological properties)and finally reviewing the application of the alginates in specific sectors like biomedical and pharmaceutical, in particular their participation on the development of controlled drug delivery systems , tissue engineering and food industry.

13

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF POORLY SOLUBLE DRUG LORATIDINE USING SOLID DISPERSION AND NATURAL SUPERDISINTEGRANTS

R.S.Pentewar1, S.Somwanshi1, S.S.Thonte1, S.Talde1, Anoop Singh2
 
1Channabasweshwar Pharmacu College, Latur.
2Department of Pharmaceutical science, NIMS University, Jaipur.

Abstract

Fast disintegrating tablets are the solid dosage forms consist of drugs that disintegrate in the oral cavity within less than one minute leaving an easy to swallow residue. The demand for FDT’s has been growing during the last decade especially for elderly &children who have swallowing difficulties. In this research work we have developed Loratidine fast dissolving tablet using natural superdisintegrants. Loratidine is usually used alone or in combination with pseudoephedrine sulphate for the symptomatic relief of seasonal allergic rhinitis, pruritis, erythemia & urticaria associated with chronic idiopathic urticaria. The oral bioavailability of Loratidine is around 40% with biological half life of 8.4 hrs. In the present work FDT of Loratidine were prepared primarily using solid dispersion to enhance solubility & then FDT’s were prepared using natural superdisintegrants viz Isapgol & Fenugreek. The prepared tablets were evaluated for Pre & post compressional parameter. The FDT’s using solid dispersion & natural superdisintegrants passes weight variation in the range of 100 ± 0.65 SD to 106 ± 0.86 SD & hardness was 2.1 to 2.6. % Friability 0.819 to 0.983 disintegration times was 40-58 seconds & in-vitro drug release 71.24 to 86.00% at the end of 30mins from F1 to F4 & which was fitted to pharmacokinetic model & it shows zero order drug release. From FTIR study reveals that there is no interaction between drug & the excipients used for FDT. The results concluded that FDT of Loratidine showing increased dissolution rate may lead to increased bioavailability by using solid dispersion.

14

ANTIDIABETIC ACTIVITY OF ETHANOLIC EXTRACT OF HUGONIA MYSTAX LEAVES LINN IN STREPTOZOTOCIN-NICOTINAMIDE INDUCED DIABETIC RATS

M.Mohankumar*, K.Srinivasan, V.Lalitha, S.Hajasherief, T.Sivakumar

Natural Product Research Laboratory, Nandha College of Pharmacy, Erode-52.

Abstract

Objective: To evaluate the antidiabetic potential of ethanolic extract of Hugonia mystax leaves in Streptozotocin-nicotinamide induced diabetic rats. Methods: Group I = Control (Animal received Normal saline- 1ml/kg), Group II = Diabetic Control (Animal received Streptozotocin-nicotinamide 150mg/kg), Group III = Animal received ethanolic extract of Hugonia mystax leaves (200mg/kg), Group IV =Animal received ethanolic extract of Hugonia mystax leaves (400mg/kg) and Group V=Animal received Glibenclamide (5mg/kg) respectively. Results: The results of the study indicates that Hugonia mystax leaves extract significantly (P<0.01) reduced the blood sugar level. The leaf extract also significantly reduced the levels of serum cholesterol, triglycerides, and low density lipoprotein and increase HDL levels in diabetic rats. The leaf extract significantly (P<0.01) decrease in the elevated alkaline phospatase, SGOT and SGPT in Streptozotocin-nicotinamide treated rats and the level significantly (P<0.01) restored to normal level after treatment. Conclusions: Ethanolic extract of Hugonia mystax leaves has protective effects on the protection of vital tissues (pancreas, kidney, liver, heart and spleen), thereby reducing the causation of diabetes in experimental animals.

15

RP-HPLC METHOD FOR DETERMINATION OF PIPERINE, GUGGULUSTERONE AND EMBELIN IN AYURVEDIC FORMULATION KAISHORAGUGGULU

D.Vishakante Gowda 2,Ganesh Muguli1,*, Atul N. Jadhav1, Nagraja P1, Sarathchandraprakash1, Babu UV1, Rangesh Paramesh1, Rohan D. Deshpande2

1Research & Development Center, The Himalaya Drug Company, Makali, Bangalore, India.

2Department of Pharmaceutics, JSS College of Pharmacy, JSS University, Mysore, India.

Abstract

Traditional system of medicine has got an overwhelming response during recent years. Across the world these medicaments have been used by people to support chronic ailments like arthritis, diabetes mellitus, respiratory disease and some chronic skin infections. Kaisoraguggulu is one of the traditional recipe mentioned in authoritative ayurvedic texts have found to support chronic skin infections, to control inflammation in gout, cleanses blood etc, due to global demand for herbal preparations a robust manufacturing methods and standardization of marker compounds specially for polyherbal formulations which can assess batch to batch consistency in quality and quantity is the need of the hour. This can be accomplished by modern scientific tools which can ensure the quality, efficacy and safety of the product. To address this, novel and simple analytical method for Piperine, Guggulusterone and Embelin using RP-HPLC method was developed.The elution was carried out using Chromolith® RP-18 (100 x 4.6 mm) 3μm pore size column, mobile phase consisted of 80% methanol and 0.05m phosphate buffer, with gradient elution, compounds were eluted at 6.0, 8.38,10.87 and 16 minutes for piperine, guggulusterone E & Z and embelin respectively. The detection of analytes was at 254nm for Piperine, 291nm for Guggulusterone and 340nm for Embelin. The established and validated method can be applied for quantification of above said compounds during bulk manufacturing.

16

SIMULTANEOUS DETERMINATION OF METFORMIN HYDROCHLORIDE AND LINAGLIPTIN BY RP-HPLC IN BULK AND PHARMACEUTICAL FORMULATIONS

Mrs Sheena Moncy*, Miss G. Rohini Reddy, Mr. P. Sunil Kumar Chaitanya, Miss G.Priyanka, Miss E. Hima Bindu

St. Pauls College of Pharmacy, Turkayamjal, R.R.Dist, Andhra Pradesh.

Abstract

A simple, rapid and precise reverse phase high performance liquid chromatographic (RP- HPLC) method has been developed and validated for simultaneous determination of Metformin hydrochloride and Linagliptin in pure and pharmaceutical dosage forms. The drugs were separated on an analytical column, Phenomex Luna RP-18; reverse phase C 18 column (150×4.6 mm I.D, particle size 5 μm). The mobile phase employed was Phosphate buffer: Methanol: Acetonitrile (65:10:25) in isocratic mode at a flow rate of 1.0 ml/min. 10μl was fixed as injection volume and UV detection was performed at 231 nm. The retention times of Metformin hydrochloride and Linagliptin were 2.2 and 7.8 min respectively. Calibration plots were linear over the concentration ranges 125-750 μg/ml and 0.625-3.75 μg/ml for Metformin hydrochloride and Linagliptin respectively. The method was validated for specificity, accuracy, precision, linearity and robustness. The LOD and LOQ values were calculated mathematically and value for Metformin hydrochloride was 3.08μg/ml and 9.3μg/ml and that of Linagliptin was 2.64μg/ml and 6.9μg/ml respectively. The proposed method was successfully applied for simultaneous analysis of these drugs both in pure and dosage forms.

17

NEW VALIDATED RP - HPLC METHOD FOR THE ESTIMATION OF DIAZEPAM IN DOSAGE FORMS

K. Uma Maheswar, P.V.Lakshmana Rao, K.Balamurali Krishna and C.Rambabu

Department of Chemistry, Acharya Nagarjuna University, Nagarjuanagar, A.P., India -522510.

Abstract

A simple reverse phase – HPLC method was developed and validated for the estimation of diazepam in bulk and tablet dosage forms. Isocratic elution at a flow rate of 1.0 mL/min was employed on BDS Hypersil C18 (250 X 4.6) at ambient temperature. A mixture of 0.05M formic acid, methanol and acetonitrile in a ratio of 45:20:35 (v/v) was used as the mobile phase. The UV detection wavelength was 239nm and the sample size was 20μL. The retention time for diazepam in this method was 5.272min. Linearity was obtained in the range of 40-100 μg/mL for diazepam. The mean recovery of diazepam was found to be 99.93%. The method was validated as per the ICH guidelines. The validated method was found to be precise and accurate for the estimation of diazepam in tablet dosage forms.

18

SIMPLIFIED METHOD FOR PURIFICATION OF C-FRAGMENT FROM TETANUS TOXIN AND TOXOID BY ENZYMATIC FRAGMENTATION AND CHROMATOGRAPHY

Kripa Murzello1,3, John Oswald Kaundinya2, Sucheta Dandekar3

1Bharat Serums and Vaccines Limited, DIL Complex, Ghodbunder Road, Thane 400610.

2BSV Biosciences, Inc., 380 Woodview Avenue, Morgan Hill, CA 95037, USA.

3Department of Biochemistry, Seth G.S.Medical College & KEM Hospital, Parel, Mumbai-400012, Maharashtra, India.

Abstract

Tetanus toxin has a molecular weight of 150,000 and is composed of three domains A, B and C. Two complementary non-toxic fragments, the light chain A (52,000) and the heavy chains B-C (98,000) were isolated from extracellular nicked toxin. Dissociation by mild enzyme treatment with Papain created another set of fragments, namely A-B and C. Of these fragments, fragment C is the most important in epitope studies. Fragment C is capable of eliciting antibodies which block neurotoxicity, though it is itself atoxic. It has been concluded that the binding site for gangliosides is located on the heavy chain portion of tetanus toxin, in the region comprised of Fragment C. The paper discuses how crude Tetanus Toxin and Toxoids, can be enzymatically digested using Papain to obtain a major polypeptide (C-Fragment), having a molecular weight of approximately 47,000 (±5%) and how the fragment can be isolated and purified using Sephadex G-100. The pure C Fragment was later collected after passing the same through a Tosoh TSK gel G3000SW Column. Comparative analysis with commercially available C fragment, indicated its purity by HPLC and Western Blot analysis. The purified C fragment was used to study the reactivity of Antibodies against Tetanus. Commercially available C fragment is very expensive and the method describes a simplified and cost effective method of isolating the same.

19

SIMULTANEOUS ESTIMATION OF GALLIC ACID AND STIGMASTEROL IN MAYDIS STIGMA (CORN SILK) BY HIGH PERFORMANCE THIN LAYER CHROMATOGRAPHY.

Tejashree S. Masurekar, Vilasrao Kadam, Varsha Jadhav*

Department of Quality Assurance, Mumbai University, Bhartividyapeeth’s College of Pharmacy, sector 8 C.B.D. Belapur, Navi Mumbai-400614, Maharashtra, India.

Abstract 

This study presents the report of TLC densitometric method, which has been developedand validated forSimultaneous estimation and quantification of Gallic acid and Stigmasterol from chloroforn extract of Maydis stigma (Corn Silk). The separation was performed on TLC aluminum plates precoated with silica gel 60 F254. Good separation was achieved in mobile phase usingToluene: ethylAcetate: Methanol (6:3:1.5). Determination and quantitation were performed by densitometric scanning at 244nm in reflection/ absorbance mode. This method gave compact spots at Rf0.2±0.05 and 0.7±0.05 for Gallic acid andStigmasterol respectively. The validation of method is done as per ICH guidelines for precision, repeatability and accuracy. Linearity range for Gallic acid and Stigmasterol was 200–1000 ng/spot with correlation coefficient R2 ±SD = 0.9949 ±5.05% and R2 ±SD = 0.9942 ±5.05% in the concentration range 100-1000ng/spot respectively. The LOD and LOQ were found to be 0.6066ng and 1.8362ng for Gallic acid and 0.9674ng and 2.9235ng for Stigmasterol. The contents in crude extract obtained from corn silk were found to be 0.2332± 0.005% w/w and 0.18944± 0.002% w/w respectively. HPTLC method was found to be simple, precise, accurate and convenient method for rapid screening of active constituents present in chloroform extracts of Maydis stigma (MS) and can be used for analysis and routine quality control of herbal material and formulations containing Maydis stigma. In conclusion, the statistical analysis of data showed that the method is reproducible and selective for estimation of both the components. The proposed HPTLC method can be applied for identification and quantitative determination of Gallic acid and Stigmasterol in the extract and in the marketed formulation.

20

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETSOF TENOXICAM

Ramesh KVRNS*1, Shahnaz Usman1, Omar Sarheed1, Fasiha Shah1, Tahera Parveen2, B.VenkataKameswara Rao 2, M.Vinay Kumar3

1RAK College of Pharmaceutical Sciences, RAK Medical & Health Sciences University, Ras Al Khaimah, UAE.

2Julphar Gulf Pharmaceutical Industries, Ras Al Khaimah, UAE 3Aditya Institute of Pharmaceutical Sciences & Research, India.

Abstract

Tenoxicam is a nonsteroidal anti-inflammatory drug belonging to the oxicam group.The drug is slightly soluble in water. In the present investigation, solvent deposited systems of the dispersions of tenoxicam in Gelucire – 50/13 (G) and Hydroxypropyl cellulose(HPC) on Microcrystalline cellulose (MCC) were prepared to enhance the dissolution of tenoxicam. Dispersions were prepared employing different proportions of the carriers. The prepared dispersions were characterized by infra-red spectroscopy, x – ray diffraction and differential scanning calorimetry. The dispersions exhibited higher dissolution compared to the pure drug and there were no interactions with the carriers. Dispersion in gelucire showed much higher dissolution than the dispersion in hydroxypropyl cellulose. There was an 8 and 4.8 fold increase in dissolution rate and dissolution efficiency respectively with the T-G-MCC (1:2:7) solvent deposited system when compared with the pure drug tenoxicam. When the dispersions were deposited on microcrystalline cellulose – it resulted in products with not only much higher dissolution but also having better flow properties enabling easy compression into tablets. Fast dissolving tablets of tenoxicam wereformulated by employing the solvent deposited systems of the dispersions of the drug in gelucire and hydroxypropyl cellulose. All the tablets showed good pharmaceutical characteristics and exhibited rapid dissolution. From the results of the investigation in may be concluded that employing solvent deposited systems of the solid dispersions of tenoxicam is a useful approach to prepare the fast dissolving tablets of tenoxicam.

21

PSYCHIATRIC MORBIDITY, STRESSFUL LIFE EVENTS (SLE), COPING STYLES OF ELDERLY ADULTS LIVING IN AN URBAN COMMUNITY- A CROSSSECTIONAL AND COMPARITIVE STUDY.

Sireesha Srinivasa Rao1, Srinivas K Rao2, Siva Kumar Chennam Setty3

1.Associate Professor Psychiatry,Institute of mental health(IMH) ,Hyderabad, Telangana,India.

2.Civil Surgeon Specialist- Orthopaedics, Employee State Insurance (ESI)Hospital,Sanathnagar,Hyderabd,Telangana,India. 

3.Assistant Professor, Psychiatry, Institute of mental health(IMH) ,Hyderabad, Telangana,India.

Abstract

While research has documented the adverse effects of life events on depressive symptoms and cognitive function less research has explicitly examined such links among older adults. This study was planned to study the number, type of life events ,quantify the stress produced by the life event ,coping stress adopted by the elderly adult with psychiatric morbidity and compare it with those without psychiatric morbidity. This is a crosssectional study carried out on 50 elderly adults between 23rd February to 23rd April, living in urban community , Moula-ali Hyderabad .The study sample was selected by simple random sampling and those who met inclusion criteria were assessed onGHQ, MMSE, MINI-plus, PSLES,CCL .Prevalence of psychiatric morbidity among elderly adults living in urban community was found to be 26%.Stressful life events (SLE) were statistically significantly more in those with psychiatric morbidity (100%) than those without psychiatric morbidity(67.5%) (p =0.02).Mean stress scores were high in elderly with psychiatric morbidity (p value=0.04).The mean number of SLE were more in those with psychiatric morbidity(3.56) than those without(2.25).Elderly with psychiatric morbidity reported health related SLE (61.53%) and in those without psychiatric morbidity , non health related SLE (52%) were reported as the most stressful. Elderly with psychiatric morbidity who reported health related stressor, adopted emotion focused coping and the association was statistically significant (p=0.02). Sociodemographic factors were matched across two groups .Elderly adults presenting with psychiatric problem must be screened for stressful life events and counseled accordingly.

22

STANDARDIZATION, PREPARATION AND EVALUATION OF AN AYURVEDIC POLYHERBAL FORMULATION IN CAPSULE DOSAGE FORM SUITABLE FOR USE IN CLINICAL TRIALS

Harshika Awasthi1, Dayanandan Mani2*, Rajendra Nath1, Anuradha Nischal1, Kauser Usman3, Sanjay Khattri1

1Department of Pharmacology and Therapeutics, King George’s Medical University, Lucknow, (U.P) India.

2CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow, (U.P) India.

3Department of Medicine, King George’s Medical University, Lucknow, (U.P) India.

Abstract

Application of modern scientific tools and techniques is important for the quality evaluation and standardization of polyherbal formulations. Herbal formulations that are being prepared on traditional methods lack quality and batch-to-batch consistency. The present study aimed to develop an ayurvedic polyherbal extract into a capsule dosage form, evaluating its physio-chemical, phytochemical, formulation parameters and setting up its quality control standards. Hard gelatin capsules for oral administration were prepared by lyophilizing the traditional liquid dosage form of the standardized extract. The formulation was then characterized as per pharmacopoeial standards. The variation of weight among the capsules was least, which showed a good ratio of excipients in the formulation with dissolution of 92%.The current work revealed that encapsulation of the lyophilized extract resulted in the concealing of bitter taste. It can be concluded that these parameters can be conveniently used to check the quality control of various herbal formulations thereby paving a way for their pharmacological activities.

23

POLY HERBAL METHANOLIC EXTRACTION FOR SCREENING OF ANTI DEPRESSANT ACTIVITY

J.Anantha Lakshmi*1, Dr. D. Satyavati2

1Sri Venkateshwara College of Pharmacy, Madhapur. Hyderabad.

2Sri Datta College of Pharmacy, sheriguda, Ibrahimapatnam. Hyderabad.

Abstract

The present study investigate the Antidepressant activityof poly herbal methanolic extraction (Rhodiola Rodantha Rhizomes, Blepharis Maderaspatensis seed, Celastrus Paniculatus whole Plant , Brassica Caulorapa Bud) by using Forced swim test and tail suspension test. Many of its individual constituents have been used for central nervous system (CNS) activities but no systematic work was carried on this combination. In this study its effect on depression was explored in rats. Acute and Subacute toxicity study revealed the dose upto 2000mg/kg the extract had not toxic symptoms and no mortality. The therapeutic dose was found to be 200mg/kg, 300mg/kg and there was no toxic damage to liver and kidney observed in subacute toxicity study. The methanolic extract of the polyherbal combination exhibited significant (P<0.001) antidepressant activity as indicated by its ability to decrease swim stress and tail suspension induced immobility time in rats as compared with that standard Fluoxetine. The result indicates this polyherbal combination can be a potential candidate for .managing depression. However further studies are required to confirm the exact therapeutic efficacy.

24

TETHERING: A NOVEL TOOL IN DRUG DISCOVERY

Yadav Rupali, Jagdale Deepali, Kadam Vilasrao

Department of Pharmaceutical Chemistry, Bharati Vidyapeeth’s College of Pharmacy/Mumbai University, India.

Abstract

The concept of tethering has become enormously popular in the past few years which facilitated binding of protein targets with smaller molecules or fragments in order to achieve successful leads and their optimization. The concept behind tethering is additive binding to yield a high affinity lead molecule which involves binding to protein, chemical modification and then its optimization to get a lead structure. Three types of tethering studies are Co-operative tethering, Extended tethering and Breakaway tethering which are studied with reference to various enzymes like Caspase3, Interlukin-2, Protein Tyrosine Phosphatase 1B etc. The need for rapid target identification and evaluation is resulting in an increase in pressure on an already strained pharmaceutical industry. As a first step toward target validation, tool compounds are invaluable in assessing the potential of drug targets. This review attempts to summarize how Tethering can rapidly identify tool compounds for a difficult target and provide effective hits. Although Tethering was initially developed to provide high-quality starting points for well-validated, highly characterized targets, the use of IL-2 as a model system proves its potential in early target assessment.

25

MICROWAVE ASSISTED IMPROVED METHOD FOR THE SYNTHESIS, CHARACTERISATION AND ANTIMICROBIAL STUDIES OF NEWLY SYNHTESIZED BENZOTHIAZOLYL AND BENZIMIDAZOLYL SUBSTITUTED DERIVATIVES

Ankush W. Wakode*, Archana S. Burghate and Shrikant A. Wadhal
Department of Chemistry, Shri Shivaji Science College, Amravati-444603, MS, India.

Abstract

The present research has systematic approach to synthesized a series of benzothiazolyl and benzimidazolyl substituted derivatives and to study their antimicrobial activity. The compounds were synthesized by green chemistry technique. i.e. (1-Benzothiazol-2-yl-[1,2]diazetidin-3-ylidene)-(4-phenyl-thiazol-2-yl)-amine, (1-Benzothiazol-2-yl-[1,2]diazetidin-3-ylidene)-substituted phenyl-amine (1c-1i) were prepared from 1-Benzothiazol-2-yl-[1,2]diazetidin-3-one and (1,2-Dihydro-benzo[4,5]imidazo[2,1-c][1,2,4]triazin-3-ylidene)-(4-phenyl-thiazole-2-yl)-amine from 1,2-Dihydro-benzo[4,5]imidazo[2,1-c][1,2,4]triazin-3-one. Antimicrobial study of these series of compounds was implemented with respect to Klebsiella pneumoniae, Escherichia coli and Staphylococcus aureus. Structures of all the newly synthesized compounds were confirmed by their IR, 1H-NMR and CHN analysis. The selected compounds may be used to design more potent biologically active compounds.

26

STUDIES ON EXTRACTION, ISOLATION AND APPLICATIONS OF LYCOPENE

Sanjay Metkar., Supriya Saptarshi., Aditi Kadam.

Department of Biotechnology, MGM’s Inst. of Biosciences and Technology, Aurangabad (MS), India.

Abstract

Lycopene is a pigment principally responsible for the characteristic deep-red color of ripe tomato fruits.It has a natural source of antioxidants, has attracted attentions due to its biological and physicochemical properties. In this study tomato paste prepared From fresh, processed, EMS mutagenesis plants fresh fruits and riped fruits was dehydrated with methanol, then lycopene was extracted with methanol-carbon tetrachloride mixture.Pure lycopene was obtained by twice crystallization of crude product from benzene through addition of boiling methanol.Further purification was achieved by using column chromatography with silica as the adsorbent.Its antioxidant capacity was performed by H2O2 radical scavenging assay.The lycopene showed great inihibition agains free radicals generated from H2O2.H2O2 also cause damage to the RNA ,In this study lycopene employed to protect standard RNA sample from oxidative insult, and it showed good results.Due to its antioxidant property and deep red color it was used in as a food color and its color efficiency was observed against the standard food color. From this study we can conclude that lycopene from tomato would be beneficial in the treatment of cancer as well as Alzheimer’s disease.

27

DEVELOPMENT AND VALIDATION OF RP-HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF THIOCOLCHICOSIDE AND FLUPIRTINE MALEATE IN PHARMACEUTICAL DOSAGE FORM

T.Sarath Chand*1, M.Sarbudeen1, Ch.Balashekar Reddy1, T.Mohan Rao1, Chandra K Sekhar2 

*1Department of Pharmaceutical Analysis and Qaulity Assurance, Vagdevi College of Pharmacy, Acharya Nagarjuna University, Gurazala, Andhra Pradesh, India. 

2Quality Control, Richer Pharmaceuticals, Prasanthinagar, Kukatpally, Hyderabad, India.

Abstract

A new simple accurate and economical reverse phase high performance liquid chromatographic method was developed for the determination of Thiocolchicoside and Flupirtine Maleate in bulk and tablet dosage form. The separation was eluted on a C18 column (250 mm x 4.6 mm; 5μ) using a mobile phase mixture of mixed phosphate buffer 6.5 and acetonitrile in a ratio of 50:50 v/v at a flow rate of 1.0ml/min. The detection was made at 255 nm. The retention times were 1.96min for Malic acid, 2.52min for Thiocolchicoside and 4.97min for Flupirtine. Calibration curve was linear over the concentration range of 4-24 μg/ml for Thiocolchicoside and 50 to 300 μg/ml for Flupirtine. The propose method was validated as per the ICH guidelines parameters like Linearity, specificity, precision, accuracy, robustness and ruggedness. The method was accurate, precise, specific and rapid found to be suitable for the quantitative analysis of the drug and dosage form.

28

DEVELOPMENT AND VALIDATION OF STABILITY INDICATING METHOD FOR THE SIMULTANEOUS DETERMINATION OF TAMSULOSIN AND DUTASTERIDE IN BULK DRUGS AND PHARMACEUTICAL DOSAGE FORMS USING RP-HPLC METHOD

Khaled Bin Sayeed*, S.H. Rizwan, Hanifa Begum

Department of Pharmaceutical Analysis, Deccan School of Pharmacy, Hyderabad-500001, A.P. India.

Abstract

A new simple, accurate, RP-HPLC method and stability indicating test was developed and validated for determination of TAMSULOSIN HYDROCHLORIDE and DUTASTERIDE tablet dosage forms. Chromatographic separation was achieved on a Kromosil C18 column (250×4.6mm×5μ) using mobile phase consisting of a mixture ofAmmonium acetate Buffer:ACN:MeOH (40:30:30v/v) PH 3.5, with detection of 228 nm. Linearity was observed in the range 19.2-44.8 μg /ml for TAMSULOSIN HYDROCHLORIDE (r2 =0.9961) and 24-56μg /ml for DUTASTERIDE (r2 =0.9981).LOD was found to be 0.74 μg/ml (TAM) and 1.29 μg/ml (DUTA) & LOQ was 2.24 μg/ml / ml (TAM) and 3.91 μg/ml (DUTA) respectively. Recovery studies was found to be 100.23 % (TAM) - 99.47% (DUTA) within the range. The method developed was precise, accurate Robust, Rugged showing %RSD NMT 2.00.Then FD studies were conducted for both drugs in RP-HPLC, the results showed that drugs are stable in all stress conditions. Hence all statistical data proves validity of the proposed method and can be used for routine analysis of bulk drug and pharmaceutical dosage form.

29

STABILITY INDICATING ANALYTICAL METHOD DEVELOPMENT AND VALIDATION FOR ESTIMATION OF EZETIMIBE AND GLIMEPIRIDE USING RP- HPLC METHOD IN BULK DRUGS AND MARKETED FROMULATION

Hanifa Begum *, S.H. Rizwan, Khaled Bin Sayeed

Department of Pharmaceutical Analysis, Deccan School of Pharmacy, Hyderabad-500001, A.P. India.

Abstract

A simple, specific, accurate, and precise reverse phase high performance liquid chromatographic (RP-HPLC) method and Stability indicating tests was developed and validated for the estimation of Ezetimibe and Glimepiride in Bulk drugs and pharmaceutical dosage forms. The Reverse phase chromatographic separation of Ezetimibe and Glimepiride was achieved on Inertsil C18 (250 x 4.6 mm; 5 μm) column using UV detection at 228 nm, the optimized mobile phase consisted of ACN: Phosphate Buffer (70:30) the flow rate was 1.4 ml / min. The retention time was found to be 3.921 ± 0.02min for EZET and 5.102 ± 0.02 min for GLIM. The method was validated as per ICH guidelines with respect to various parameters. The calibration curve showed linearity with correlation coefficient 0.997 for EZET & GLIM concentration range 60 -140 mcg & 6 -14 mcg and %RSD NMT 2 and LOD was found to be 3.09 μg / ml (EZET) and 0.23 μg / ml (GLIM) & LOQ was 9.37 μg / ml (EZET) and 0.69 μg / ml(GLIM) respectively. Recovery studies for EZET and GLIM was found to be in the range of 98.79% - 98.82%. The method developed was precise, accurate robust, rugged showing %RSD NMT 2.00. Then FD studies were conducted for both drugs in RP-HPLC the results showed that drugs are stable in all stress conditions. Hence all statistical data proves validity of the proposed methods and can be used for routine analysis of bulk drug and pharmaceutical dosage form.

30

COCRYSTALS : A NOVEL APPROACH TO IMPROVE THE PHYSICOCHEMICAL AND MECHANICAL PROPERTIES

Pooja Vaghela*, Dr. H. M. Tank1 , Paun Jalpa2

*School of Pharmacy, RK University, Rajkot.

*Shantilal Shah Pharmacy College, M. K. Bhavnagar University, Bhavnagar.

1Mts. V. B. Manvar College of Pharmacy, Dumiyani, Upleta, Dist. Rajkot.

2B. K. Mody Govt. Pharmacy College, Rajkot.

Abstract 

Cocrystals consists of an API and stoichiometric amount of a pharmaceutically acceptable cocrystal former which may be an another API. Cocrystals can be made by different types of interaction like hydrogen bonding, π-π stacking, and van der waals forces. Cocrystals are nonionic supramolecular complexes and can be used to optimize physicochemical properties like solubility, dissolution rate, stability, and mechanical properties like flowability, compressibility, compactibility as well as pharmacokinetic properties like bioavailability of the API without changing its chemical composition and pharmacological action. Cocrystallization approach alters the molecular composition of active pharmaceutical ingredients and is considered better alternatives to improve physicochemical, mechanical, pharmacotechnical and pharmacokinetic drug properties. Factors affecting cocrystal stability and phase transformations are reported is only likely to form if it is thermodynamically more stable than the crystals of its individual components. Objective of pharmaceutical cocrystal formulation is to improve physicochemical and mechanical properties of BCS Class II drugs having poor flowability, and hence via cocrystallization approach directly compressible tablet dosage form can be prepared with greater improvement in pharmacokinetic and manufacturing parameters.

31

IN SILICO MODELLING AND STRUCTURAL CHARACTERIZATION OF Γ-AMINOBUTYRATE AMINOTRANSFERASE (GABA-AT)

Pankaj Kalita1,2, Rituparna Sarma3, Pratap Parida4, Chadipiralla Kiranmai5, Manash Barthakur1, & P. Vijaya Bhaskar Reddy2*

1Institutional Level Biotech Hub, Pub Kamrup College, Baihata Chariali-781381, Kamrup, Assam, India.

2Department of Life Science & Bioinformatics, Assam University: Diphu Campus, Diphu-782462, Karbi Anglong, Assam, India.

3Department of Zoology, Gauhati University, Guwahati-781014, Assam, India.

4Centre for Studies in Biotechnology, Dibrugarh University, Dibrugarh-786004, Assam, India.

5Department of Biotechnology, Vikrama Simhapuri University, Nellore-524003, Andhra Pradesh, India.

Abstract

Gama aminobutyrate aminotransferase (GABA-AT) (500aa) is a pyridoxal phosphate dependent GABA degrading homodimeric enzyme of 50-kD subunits, a potential drug target to control epilepsy. There are no records of the structural characterization of GABA-AT. So, in this experiment attempt has been made to predict homology model of the human GABA-AT on the template of the pig liver GABA-AT sequence. Structural characterization of GABA-AT would greatly advance the development of novel lead compounds targeting this molecule. Homology modeling was carried out using MODELLER 9.12, SWISS model and Phyre2 Servers. Analysis suggested that the SWISS model had better scores in ERRAT and RAMPAGE compared to MODELLER and Phyre2 models. Though, MODELLER scored highest in PROCHECK analysis. After refinement, MODELLER and SWISS models scored better than Phyre2 models. Analysis of active sites suggested that SWISS model had largest numbers of cavities and pockets compared to MODELLER and SWISS models. 3D structure of SWISS model had 119 numbers of cavities while Phyre2 had 65 cavities and MODELLER model had 62 cavities. It could be assumed from the evaluation results that the refined model of SWISS model had an edge over the other two structures. From this study we could suggest that the homology models of GABA-AT generated by MODELLER and SWISS model both were reliable could be used for further studies.

32

PREPARATION OF NOVEL CO-PROCESSED EXCIPIENT- STUDY OF FLOW PROPERTIES AND COMPATIBILITY

Peravadhanulu Uppuluri*, T Chakraborty, V Kusum Devi, Vinay Raichur
*Dept. of Pharmaceutics, Al-Ameen College of Pharmacy, Bangalore, India.

Abstract

This study emanates from the current industrial requirements keeping in view of the advancements in tablet manufacturing and was aimed towards the development of novel co-processed excipient comprising of corn starch and sodium lauryl sulphate for use in direct compression technique of tableting which we were able to do successfully. The co-processed excipient to be prepared could be able to overcome the flowability drawbacks of individual excipients and also could improve their characteristic properties. Corn starch and Sodium lauryl sulphate were selected for co-processing. The co-processed excipients were prepared by two methods; solvent evaporation method and co-grinding method. Initially, the co-processed excipients were prepared by solvent evaporation method using three solvents out of which water was selected as best solvent based on the flow properties. Large scale preparation of the co-processed excipient was carried out with water as solvent and by solvent evaporation method. Three best ratios were screened out (3:7, 4:6, 5:5 of Corn starch: SLS) based on their performance in flow properties and were chosen for further studies. However, co-processed excipients prepared by co-grinding method are ignored since they have shown poor performance in flow properties. The flowability of the prepared co-processed excipient (CoP CS-SLS) is compared with that of the individual excipients. The comparative study exhibited improvement in flowability. The FTIR study was carried out to check the compatibility between the excipients and it was proved that there are no unwanted interactions and thus proven the co-processing is a novel approach. It can be concluded that the CoP CS-SLS was successfully blended with proven improved flowability and good compatibility.

33

A MILD AND EFFICIENT METHOD FOR THE SYNTHESIS OF ACYL AZIDES FROM CARBOXYLIC ACIDS UTILIZING PHOSPHONITRILIC CHLORIDE

Jitendra S. Pulle*1, Ashok D. Sagar2, Saneev M. Reddy3 and Manjusha V. Yadav2
1Department of Chemistry, S.G.B. College, Purna (Jn.), Dist. Parbhani (M.S.), India.
2School of Chemical Sciences, S.R.T.M. University, Nanded 431 606, India.
3Department of Chemistry, G.M.V. Kotgyal, Dist. Nanded (M.S.) India.

Abstract

An efficient method has been described for the one pot synthesis of acyl azides from corresponding carboxylic acids and sodium azide utilizing phosphonitrilic chloride trimer (Cl6N3P3) in combination with NMM under extremely mild conditions. A variety of carboxylic acids has been converted to azides in good to excellent yields. Aromatic carboxylic acids as well as aliphatic and unsaturated carboxylic acids have been smoothly converted into corresponding acyl azides without Curtius rearrangement to an isocyanate.

34

ANTIBIOTIC ACTIVITY AND SUSCEPTIBILITY OF NOVEL PONTIBACTER SPS., ISOLATED FROM LABEO ROHITA

C.Sumathi1,2*, D.Mohanapriya2, G.Sekaran2
1 Asan Memorial Dental College & Hospitals, Chengalpattu.
2*CSIR-Central Leather Research Institute, Adyar, Chennai.

Abstract

Aim: The present investigation was to explore the unexploited application of novel fish gut bacteria Pontibacter sps as an antibacterial and antifungal drug. Methods and Results: The isolate is a gram negative, non motile, red pigmented, rod shaped bacterium, designated as strain PROLR15T. The strain PROLR15 T produces a distinct red color pigmentation which makes it different from the other Pontibacters. The 16S rRNA sequence analysis showed 92% similarity with an existing existing Pontibacter korlensis strain. The major cellular fatty acids were Iso-c15:0 and Iso c17:0 3OH. Predominant menaquinone of the strain is MK-7. It produces extracellular polymeric substances under anaerobic condition which portraits its facultative anaerobic nature. Phylogenetic studies and the phenotypic characterizations strongly support the idea that the isolated bacterium belongs to the genus Pontibacter. (HQ005734). Pontibacter sps possess antimicrobial activity. Conclusion: Among the pathogenic species Salmonella typhii, Klebsiella pneumonia and Staphylococcus aureus were most susceptible at minimum concentration. Most of the pathogenic fungi were susceptible to the isolated bacteria Pontibacter sps., with the MIC90 below 5000 μg/mL. Significance: Antimicrobial activity against most serious disease causing pathogens and susceptibility to most of the antibiotics paves way to utilize them for treatment of diseases and as a probiotic supplement.

35

SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL EVALUATION OF NOVEL TRI-ARM STAR SHAPED CHALCONES FROM 2,4,6-TRIS(4-ACETYLPHENOXY)-1,3,5-TRIAZINE

Firdous G. Khan, Manjusha V. Yadav and Ashok D. Sagar*

School of Chemical Sciences, Swami Ramanand Teerth Marathwada University, Dnyanteerth Vishnupuri, Nanded- 431606 Maharahstra, India.

Abstract

A series of ten new tri-arm star shaped chalcones were synthesized using 2,4,6-tris(4-acetylphenoxy)-1,3,5-triazine as a template. The intermediate 2,4,6-tris(4-acetylphenoxy)-1,3,5-triazine was synthesized by the reaction of cyanuric chloride with sodium salt of 4-hydroxy acetophenone using phase-transfer catalyst. Thus, the prepared 2,4,6-tris(4-acetylphenoxy)-1,3,5-triazine has been subsequently treated with various aldehydes to afford title compound in excellent yields. The structures of intermediate and newly synthesized tri-arm star shaped chalcones were confirmed by physical and spectral analysis. All the tri-arm star shaped chalcones were evaluated for antibacterial and antifungal activities. Selected tri-arm star shaped chalcones showed good to excellent antibacterial and antifungal activities with reference to the well-established standards.

36

SPECTROFLUORIMETRIC METHOD FOR THE DETERMINATION OF SILODOSIN IN BULK AND PHARMACEUTICAL DOSAGE FORM

PrachiBhamre, Sadhana J. Rajput*

Pharmaceutical Quality Assurance Laboratory, Centre of Relevance and Excellence in Novel Drug Delivery System, Shri G H Patel Pharmacy Building, Pharmacy Department, The Maharaja Sayajirao University of Baroda, Fatehgunj, Vadodara-390 002, Gujarat, INDIA.

Abstract

A simple, accurate, sensitive and reproducible spectrofluorimetric method has been developed for the analysis of Silodosin in pure and pharmaceutical dosage form. Silodosin shows strong native fluorescence in methanol having excitation wavelength at 272 nm and emission wavelength at 450 nm. The calibration graph was linear in the range from 0.01 to 1μg/ml. The proposed method was statistically validated and successfully applied for analysis of capsule dosage form. The limit of detection and limit of quantification were found to be 0.003μg/ml and 0.0091μg/ml respectively. The percentage recovery was found to be in the range of 98.53% ± 0.53 to 99.27% ± 0.49.