Valsartan floating bioadhesive compression-coated mini-tablets: Formulation and pharmacokinetics

An attempt is made in the present study to develop the valsartan floating bioadhesive compression-coated mini-tablets. Among the various methods described, combination of floating and bioadhesive drug delivery systems is a promising way in gastro retention with few limitations, which has a great impact on the drug delivery to its intended site of administration. Mini-tablets have the advantages of both tablets as well as multiparticulates like pellets. The prepared mini-tablets were evaluated for weight variation, thickness, friability, hardness, drug content, in vitro buoyancy, in vitro release and in vivo studies. Prepared core mini-tablets were compression coated using polymers such as HPMC K4M and Carbopol 934P. From the results, formulations with HPMC K4M with Carbopol 934P in 1:1 ratio showed controlled release. Formulation F3 showed a satisfactory dissolution profile, detachment stress and floating characteristics, which can increase the gastric residence time as well as bioavailability. Pharmacokinetic studies of F3 formulation in albino male rabbits showed 2.25-fold higher bioavailability and 1.5-fold higher Cmax compared to immediate release core mini-tablets. Hence development of valsartan floating mini-tablets using combination of floating drug delivery and bioadhesive drug delivery systems is the best way to obtain gastro retention to gain therapeutic benefits.

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