Optimization Studies on Compression Coated Floating-Pulsatile Drug Delivery of Bisoprolol

Swati C Jagdale,Aniruddha R Chabukswar,Bhanudas S Kuchekar,Nilesh A Bari

doi:10.1155/2013/801769

Abstract

The purpose of the present work was to design and optimize compression coated floating pulsatile drug delivery systems of bisoprolol. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. The prepared system consisted of two parts: a core tablet containing the active ingredient and an erodible outer shell with gas generating agent. The rapid release core tablet (RRCT) was prepared by using superdisintegrants with active ingredient. Press coating of optimized RRCT was done by polymer. A 32 full factorial design was used for optimization. The amount of Polyox WSR205 and Polyox WSR N12K was selected as independent variables. Lag period, drug release, and swelling index were selected as dependent variables. Floating pulsatile release formulation (FPRT) F13 at level 0 (55 mg) for Polyox WSR205 and level +1 (65 mg) for Polyox WSR N12K showed lag time of 4 h with >90% drug release. The data were statistically analyzed using ANOVA, and P < 0.05 was statistically significant. Release kinetics of the optimized formulation best fitted the zero order model. In vivo study confirms burst effect at 4 h in indicating the optimization of the dosage form.

Highlights

Due to poor drug efficacy, the incidence of side effects, and frequency of administration to conventional drug preparations, many traditional drug dosage forms are undergoing replacement by second-generation, modified drug release dosage forms
Lag period at 4 h, drug released, and swelling index were selected as dependent variables
The hardness was observed in range of (2.4–2.7 ± 0.18 Kg/cm2), whereas friability was less than 1% which indicated that tablet had good mechanical resistance

Summary

Introduction

Due to poor drug efficacy, the incidence of side effects, and frequency of administration to conventional drug preparations, many traditional drug dosage forms are undergoing replacement by second-generation, modified drug release dosage forms. During the early 1990s, second-generation modified release drug preparations achieved continuous and constant rate drug delivery, in which constant or sustained drug output minimize drug concentration “peak and valley” levels in the blood, promoting drug efficacy and reducing adverse effects [1, 2]. The symptoms of many diseases, such as bronchial asthma, myocardial infarction, angina pectoris, hypertension, and rheumatic disease have followed the body’s biological rhythm [4,5,6]. Day night variation in asthmatic dyspnea and variations in the incidence of myocardial infarction occur throughout the early morning hours

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Conclusion