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. 2013:2013:801769.
doi: 10.1155/2013/801769. Epub 2013 Nov 10.

Optimization studies on compression coated floating-pulsatile drug delivery of bisoprolol

Swati C Jagdale  1 , Nilesh A Bari  1 , Bhanudas S Kuchekar  1 , Aniruddha R Chabukswar  1
Affiliations

Optimization studies on compression coated floating-pulsatile drug delivery of bisoprolol

Swati C Jagdale et al. Biomed Res Int. 2013.

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.

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Figures

Figure 1
Figure 1
In vitro drug release profile of core tablet.
Figure 2
Figure 2
In vitro release profiles of batch P1–P6.
Figure 3
Figure 3
In vitro floating behavior of a representative tablet of Polyox WSR.
Figure 4
Figure 4
In vitro drug release profiles of FPRT of batches F10–F18.
Figure 5
Figure 5
(a) Response surface plot showing the influence on lag period and (b) contour plot.
Figure 6
Figure 6
(a) Response surface plot showing the influence on drug release and (b) contour plot.
Figure 7
Figure 7
(a) Response surface plot showing the influence on swelling index and (b) contour plot.
Figure 8
Figure 8
IR spectroscopic study of polymers, drug, and formulations.
Figure 9
Figure 9
DSC curves of bisoprolol fumarate polymers and formulation F13.
Figure 10
Figure 10
X-ray of formulation F13 at different time intervals.
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