Bioavailability Improvement of Diltiazem Hydrochloride Gastroretentive Sustained Release Tablets
Journal Title: IOSR Journal of Pharmacy and Biological Sciences (IOSR-JPBS) - Year 2016, Vol 11, Issue 6
Abstract
Floating drug delivery system (FDDS) is the greatest interesting endeavors facing the pharmaceutical scientist. FDDS are associated with advantages of improved bioavailability and minimizing the dosing frequency. Diltiazem hydrochloride (DTZ HCl) is a calcium channel blockers, anti-anginal drug and anti-hypertensive which undergo extensive first-pass metabolism and display poor bioavailability about 30- 40%. In this research, formulation of DTZ HCl sustained release floating tablets to be taken once was attempted. These tablets were formulated using different release-retarding polymers as; sodium alginate (S ALG), hydroxypropyl methylcellulose K15 (HPMC), and Carpobol 934 (CP). The prepared tablets were characterized for the assessment of floating, swelling and dissolution behavior. The bioavailability of DTZ HCl from the optimized formulation was evaluated. The obtained results showed that, the prepared formulations show better and significant results for all the evaluated parameters. The floating, swelling and in-vitro release characteristics were found to be a function of the type and ratios of polymer used. Moreover, a combination of HPMC-CP in a ratio of 1.5:1 (F6) exhibited desirable floating, swelling and extended drug release, thereby bioavailability which indicated by higher AUC and relative bioavailability values.
Authors and Affiliations
Thanaa M. Borg, Marwa S. El-Dahan, Hayder A. Hammoodi
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