Drotaverine hydrochloride gastroretentive floating mini-tablets: Formulation, in-vitro and in-vivo evaluation

摘要

Drotaverine hydrochloride (DRH) is an antispasmodic drug which has a short residence in the intestine during diarrhea that prompts poor bioavailability and frequent dosing. The aim of the present study was to increase the gastric residence time and sustain the release of DRH so increasing patient compliance. Nine floating mini-tablets of DRH were prepared employing different amounts of sodium alginate and sodium bicarbonate by wet granulation technique adopting 32factorial design. The prepared formulae were evaluated for various physical parameters, floating behaviors and in vitro release studies. Formula FF9 (sodium alginate 200?mg and sodium bicarbonate 120?mg) showed optimum floating behavior (floating lag time 49.1?±?5.3?s and total floating time ??24?h) and optimum sustained release for DRH (7.60?±?1.25% after 0.5?h and 78.14?±?3.10% after 12?h). The candidate formula with the highest desirability value (0.942) was evaluated for its bioavailability compared to the marketed product. Statistical analysis revealed significant increase in AUC(0-∞)3311.31?±?182.18?ng?h/ml with delayed Tmaxcompared to 1589.54?±?127.97?ng?h/ml for the marketed product. The results revealed that FF9 could be a promising candidate for gastroretentive drug delivery system for DRH.