FORMULATION AND EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF AMOXICILLIN TRIHYDRATE
Namitha P. V.* and Dr. Suja C.
ABSTRACT
The aim of the present study was to formulate and evaluate gastroretentive floating tablets of Amoxicillin trihydrate, to provide local action in the treatment of Helicobacter pylori by prolonging the gastric residence time. The sustained release of Amoxicillin trihydrate is desired because of its short biological half-life (1-1.5hr) and bioavailability (60%). The gastro retentive floating tablets of Amoxicillin trihydrate will provide site-specific drug delivery and thereby extend its duration of action. The dosage form was designed by using HPMC and Carbopol as release retarding polymers, Sodium bicarbonate and Citric acid as gas - generating agents and other excipients by direct compression process. Optimization studies have been done by Design Expert Stat Ease software using Central composite design. 13 formulations were prepared as suggested by the software. The pharmaceutical properties of formulations, their buoyancy lag time and total floating time and in vitro drug release were evaluated. The in vitro drug release studies indicated that the optimized formulation containing equal concentration of HPMC and Carbopol (F3) showed highest drug release of 99.87% and floating lag time of 68 seconds. The in vitro drug release data was treated with mathematical equations, and it was concluded that Amoxicillin trihydrate released from the tablet followed First order kinetics with non-fickian super case-II transport. In this study the effect of two release retarding polymers ie, carbopol and HPMC were also studied so as to improve the drug release, total floating time and hence improve its site specific action. From this study it was concluded that gastro retentive floating tablets of Amoxicillin trihydrate is a promising approach as it can decrease in the frequency of administration and ultimately provide better patient compliance by gastric retention.
Keywords: Gastroretentive floating tablets, Amoxicillin trihydrate, Helicobacter pylori, Carbopol, HPMC, optimization.
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