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

Jagdale SC, Bari NA, Kuchekar BS, Chabukswar AR - Biomed Res Int (2013)

Bottom Line: 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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, MAEER's Maharashtra Institute of Pharmacy, MIT Campus, Survey No. 124, Kothrud, Pune, Maharashtra 411 038, India.

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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(a) Response surface plot showing the influence on lag period and (b) contour plot.
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fig5: (a) Response surface plot showing the influence on lag period and (b) contour plot.

Mentions: The combined effect of concentration of Polyox WSR205 and Polyox WSR N12K on lag period is shown in Figure 5. From response surface plot and contour plot in Figure 5, it was observed that both polymers have significant effect on lag period. As concentration of Polyox WSR205 and Polyox WSR N12K increases (level +1, level +1) lag period is increased (>5 h) and uniformed. At maximum level of polymers lag period was increased but did inhibit drug release.


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

Jagdale SC, Bari NA, Kuchekar BS, Chabukswar AR - Biomed Res Int (2013)

(a) Response surface plot showing the influence on lag period and (b) contour plot.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3842062&req=5

fig5: (a) Response surface plot showing the influence on lag period and (b) contour plot.
Mentions: The combined effect of concentration of Polyox WSR205 and Polyox WSR N12K on lag period is shown in Figure 5. From response surface plot and contour plot in Figure 5, it was observed that both polymers have significant effect on lag period. As concentration of Polyox WSR205 and Polyox WSR N12K increases (level +1, level +1) lag period is increased (>5 h) and uniformed. At maximum level of polymers lag period was increased but did inhibit drug release.

Bottom Line: 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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, MAEER's Maharashtra Institute of Pharmacy, MIT Campus, Survey No. 124, Kothrud, Pune, Maharashtra 411 038, India.

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.

Show MeSH
Related in: MedlinePlus