Design and Evaluation of Floating-Bioadhesive Drug Delivery System for Risedronate Sodium to Improve the Oral Bioavailability

Author(s): Gollapudi Rajesh and Ajmeera Ramarao*

Abstract: The objective of the present research work was to formulate and evaluate risedronate sodium floating-bioadhesive tablets (RSFBT) to increase the gastric residence time, and further compare their pharmacokinetics with conventional immediate release tablets. The RSFBT were prepared with combination of Gelucire 43/01 and Sodium CMC/ Gelucire 54/02 and CP 971P by direct compression method. The prepared RSFBT were evaluated for hardness, thickness, weight variation, friability, drug content, in vitro buoyancy and drug release. One of the optimized formulations (RSF10) floated with a lag time of 52.6±4.8 sec, duration of floating 12 h and released about 99.25±1.85 % of drug in 12 h, and then followed the non-Fickian diffusion release mechanism with n value of 0.635. The RSF10 of RSFBT loaded with BaSO4 remained in stomach for 5.00 ± 0.86 h (n=3) in radiological studies. The formulation, RSF10 exhibited maximum bioadhesive strength (1.139±0.073 N) than other formulations. The bioavailability studies were carried out for RSF10 and compared with that of reference IR tablets, Actonel in eight healthy human volunteers. Based on in vivo pharmacokinetic study, significant difference was observed between Cmax, tmax, t1/2, AUC0–∞, and MRT of RSF10 and Actonel IR tablets. The increase in relative bioavailability of RSF10 was 1.59 fold when compared to reference IR tablets. The increased relative oral bioavailability may be due to the floating-bioadhesive mechanism of dosage form, which is desirable for drugs absorbed from the upper part of gastrointestinal tract.

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