Abstract

DEVELOPMENT, OPTIMIZATION AND COMPARATIVE IN-VIVO EVALUATION OF SALBUTAMOL FLOATING CAPSULE FORMULATION

Abubakr O. Nur*, Balgees M. Abd Elbasit, Basheir I. Osman and Zuheir A. Osman

ABSTRACT

In this study different contents of low viscosity grade hydroxypropyl methylcellulose (HPMC, 50cps) and Tragacanth were conceived to develop and optimize salbutamol gastric floating capsules capable to sustain the release of loaded drug over a prolonged time duration through consecutive application of full factorial and composite index based mathematical designs. Tragacanth content was established to have a more influence on floating duration of developed capsule formulations whilst content of both HPMC and Tragacanth were found to affect the rate and kinetics of the drug release. Significant increase (p< 0.05) in floating duration and drug release rate was monitored with increasing content of HPMC in capsule formulations composed of polymer combination. Formulation composed of 16% w/w HPMC and 36% w/w Tragacanth (F8) was considered as best ranked formulation that fulfill preset constraints for floating duration, % drug release in the first hour and % drug release within 4 hours. Upon optimization of F8 with regard to drug release kinetics, a formulation comprised of 8% and 36% w/w HPMC and Tragacanth, respectively, was achieved and measured floating duration of 6.8 hr, 30% drug release at the first hour, 72% of loaded drug release after 4 hours with a diffusion exponent of 0.7888. Compared to an immediate release non floating capsule formulation, in vivo investigation in 8 dogs has shown that there was significant increase (p≤0.05) in Tmax, AUC0-∞, elimination t½ and mean resident time of salbutamol associated with the optimized salbutamol floating capsule formulation, indicating the improved bioavailability and duration tendency of duration tendency of duration tendency of duration tendency of duration tendency of duration tendency of duration tendency of duration tendency of duration tendency of duration tendency of salbutamol salbutamol salbutamol salbutamol salbutamol from the optimized gastric floating capsule formulation.

Keywords: Salbutamol, Floating capsules, In vitro investigation, In vivo evaluation.