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Basavaraj ¹, B. Someswara Rao ¹, S. V. Kulkarni ¹, Pramod Patil ¹, Chetan Surpur ¹

Affiliations
1 Sree Siddaganga College of Pharmacy, B H Road, Tumkur- 572102, IN

Abstract

Sustained release formulation of Aceclofenac based on monolithic matrix technology was developed and evaluated. It is practically insoluble in water so it is suitable to develop sustained release matrix tablet using hydrophilic polymer. Aceclofenac is non-steroidal anti-inflammatory drug (NSAID) used extensively in the treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. It is newer derivative of diclofenac and having less GIT complication, with short biological half-life 4 hrs, so developed formulation provides the advantages of sustained release formulations. The tamarind seed polysaccharide (TSP) was extracted from tamarind kernel powder and this polysaccharide was utilized in the formulation of matrix tablets containing Aceclofenac by wet granulation technique and evaluated for its drug release characteristics. TSP is a hydrophilic and rate controlling polymer. Granules were prepared and evaluated for loose bulk density, tapped bulk density, compressibility index and angle of repose, shows satisfactory results. Formulation was optimized on the basis of acceptable tablet properties (hardness, friability, drug content and weight variations), in vitro drug release and stability studies. All the formulations showed compliance with pharmacopieal standards. The in vitro release study of matrix tablets were carried out in phosphate buffer pH 7.4 for 12 hr. Among all the formulations, F 5 shows 98.062% better controlled release at the end of 12 hr. The results indicated that a decrease in release kinetics of the drug was observed by increasing the polymer concentration. The release data was fitted to various mathematical models such as, Higuchi, Korsmeyer-Peppas, First-order, and Zero order to evaluate the kinetics and mechanism of the drug release. The drug release of optimized formulations F-5 follows zero order kinetics and the mechanism was found to be diffusion coupled with erosion (non-Fickian diffusion/anomalous). The stability studies were carried out according to ICH guideline which indicates that the selected formulations were stable.

Keywords

Aceclofenac, Extracted Tamarind Seed Polysaccharide, Matrix Tablet, Sustained Release, Wet Granulation.

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Pramod Patil ¹, B. Someshwara Rao ¹, Suresh V. Kulkarni ¹, Basavaraj ¹, Chetan Surpur ¹, Anand Ammanage ¹

Affiliations
1 Department of Pharmaceutics, Sree Siddaganga College of Pharmacy, B.H.Road, Tumkur-572102, Karnataka, IN

Abstract

The present study concerns the development of floating tablets of ofloxacin which were designed to prolong the gastric residence time after oral administration. Ofloxacin is a fluoroquinolone antibacterial agent which is highly effective against gram positive and gram negative bacteria. Ofloxacin floating tablets were prepared by wet granulation method incorporating natural polymer like guar gum, locust bean gum, either alone or in combination with HPMC K100M as swelling polymers, with sodium bicarbonate as gas generating agent and were evaluated for parameters such as Weight variation, Hardness, Friability, Drug content, Swelling index, in vitro buoyancy study, in vitro drug release study. All the formulation showed compliance with pharmacopieal standards. Based on the evaluation results, F3 and F6 formulations were selected as the best formulations and were checked for stability as per ICH guidelines. These results indicated that the selected formulations were stable. The drug release profile of the best formulations was well controlled and uniform throughout the dissolution studies. The drug release of optimized formulation follows the Higuchi kinetic model, and the mechanism is found to be non-Fickian/anomalous according to Korsmeyer-Peppas equation.

Keywords

Floating Tablets, Ofloxacin, Guar Gum, Locust Bean Gum.

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Nikunj Patel ¹, P. Ashok Kumar ², Basavaraj ¹, Tom Damien ¹, B. Someshwara Rao ¹, Suresh V. Kulkarni ¹

Affiliations
1 Department of Pharmaceutics, Sree Siddaganga College of Pharmacy, B.H. Road, Tumkur-572102, Karnataka, IN
2 Department of Pharmaceutics, Sree Siddaganga College of Pharmacy, B. H. Road, Tumkur-572102, Karnataka, IN

Abstract

In the present investigation an attempt was made to formulate the oral controlled release metformin hydrochloride matrix tablets by using Guar gum as rate controlling polymer and to evaluate drug release parameters as per various release kinetic models. The tablets were prepared by wet granulation method. Granules were prepared and evaluated for loose bulk density, tapped density, compressibility index and angle of repose, shows satisfactory results. All the granules were lubricated and compressed using 12.8 mm flat faced punches. Compressed tablets were evaluated for uniformity of weight, content of active ingredient, friability, hardness, in vitro release studies and swelling index. All the formulations showed compliance with Pharmacopoeial standards. The in vitro dissolution study was carried out for 12 hours using paddle (USP type II) method in phosphate buffer (pH 6.8) as dissolution media. The prepared matrix tablets were shown 99.92%, 97.41%, 94.95%, 89.29%, 86.41% and 84.72% release over a period of 12 hours. Formulations F-1 and F-2 failed to sustain release beyond 9 hours and 11 hours, respectively. Among all the formulations, F-5 showed the controlled release of drug for 12 hours with 86.41% release and the release profile was close to the marketed sample of metformin hydrochloride (M-SR). Selected formulation (F-5) was subjected to stability studies for 3 months, which showed stability with respect to release pattern. The drug release follows first order kinetics and the mechanism was found to be diffusion coupled with erosion.

Keywords

Metformin Hydrochloride, Guar Gum, Matrix Tablets, Wet Granulation, Controlled Release.

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