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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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Related in: MedlinePlus

In vitro release profiles of batch P1–P6.
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Related In: Results  -  Collection


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fig2: In vitro release profiles of batch P1–P6.

Mentions: From Figure 2 it was observed that compression-coated Polyox WSR205 (P2) and Polyox WSR N12K (P5) when used alone as polymer with croscarmellose sodium (C4) has shown optimal lag period with burst at 3.40 ± 0.2 h and 4.0 ± 0.1 h and drug release 98.97% and 99.16%, respectively. During the dissolution kinetics, the coating layer gradually starts to erode up to a limiting thickness of the coat. After this stage, a rupture of the shell was observed under the pressure which has applied by the swelling of the core tablet due to presence of superdisintegrant. This pressure was high due to high swelling property of croscarmellose sodium, resulted in burst effect after 4 h along with complete and rapid drug release. Formulation P2 and P5 were considered as final batch to study effect of polymers on optimization.


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

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

In vitro release profiles of batch P1–P6.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig2: In vitro release profiles of batch P1–P6.
Mentions: From Figure 2 it was observed that compression-coated Polyox WSR205 (P2) and Polyox WSR N12K (P5) when used alone as polymer with croscarmellose sodium (C4) has shown optimal lag period with burst at 3.40 ± 0.2 h and 4.0 ± 0.1 h and drug release 98.97% and 99.16%, respectively. During the dissolution kinetics, the coating layer gradually starts to erode up to a limiting thickness of the coat. After this stage, a rupture of the shell was observed under the pressure which has applied by the swelling of the core tablet due to presence of superdisintegrant. This pressure was high due to high swelling property of croscarmellose sodium, resulted in burst effect after 4 h along with complete and rapid drug release. Formulation P2 and P5 were considered as final batch to study effect of polymers on optimization.

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