Abstract
The aim of this investigation was to develop and optimize bisoprolol fumarate matrix tablets for sustained release application by response surface methodology based on 23 factorial design. The effects of the amounts of calcium alginate, HPMC K4M, and Carbopol 943 in bisoprolol fumarate matrix tablets on the properties of bisoprolol fumarate sustained release matrix tablets like drug release and hardness were analyzed and optimized. The observed responses were coincided well with the predicted values by the experimental design. The optimized bisoprolol fumarate matrix tablets showed prolonged sustained release of bisoprolol fumarate over 6 hours. These matrix tablets followed the first-order model with anomalous (non-Fickian) diffusion mechanism.
Highlights
Matrix tablets offer a great potential as oral drug delivery system due to their simplicity, cost effectiveness, reduced risk of systemic toxicity, and minimal chance of dose dumping [1, 2]
A computer-aided optimization technique using 23 factorial design was employed to investigate the effect of the amounts of various hydrophilic polymers, namely, calcium alginate, HPMC K4M, and Carbopol 943 in polymer-blend used as three independent process variables, on the properties of bisoprolol fumarate sustained release matrix tablets like drug release and hardness
A total of 8 trial formulations of bisoprolol fumarate matrix tablets were proposed by the 23 factorial design for three independent variables: amounts of calcium alginate (A, mg), HPMC K4M (B, mg), and Carbopol 943 (C, mg), which were varied at two different levels
Summary
Matrix tablets offer a great potential as oral drug delivery system due to their simplicity, cost effectiveness, reduced risk of systemic toxicity, and minimal chance of dose dumping [1, 2]. They exclude complex production procedures such as coating and pelleatization during manufacturing, and drug release rate from the dosage form is controlled mainly by the type and proportion of polymer used in the preparations [3]. Bisoprolol fumarate, chemically 1-[4-(2-isopropoxyethoxymethyl)phenoxy]-N-isopropyl-3-aminopropan-2-ol fumarate, is a cardioselective β-blocker (Scheme 1) without membrane stabilizing activity or intrinsic sympathomimetic activity [10, 11] It is used for the treatment of hypertension and angina pectoris [11]. In the development of any pharmaceutical formulation like matrix tablet for sustained release ability, an important issue is to design a formulation with optimized quality in ISRN Pharmaceutics
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