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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

IR spectroscopic study of polymers, drug, and formulations.
© Copyright Policy - open-access
Related In: Results  -  Collection


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fig8: IR spectroscopic study of polymers, drug, and formulations.

Mentions: There were no interaction between the drug and polymers as showed in Figure 8. IR spectrum of Bisoprolol fumarate is characterized by the absorption of C=O group at 1652 cm−1. Polyox WSR-205 has shown major peak at 2959, 1942, and 1482. Polyox WSR N12 K has shown major peak at 3649, 2854, and 1304. Major peaks of polymer are retained in F13 spectra showing no chemical interaction between drug and polymer. In formulation due to cross linking of polymers few bands disappeared and merged. Whereas formulation F13 spectra shown 1652 peak indicating of pure drug and no change in structure of drug.


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

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

IR spectroscopic study of polymers, drug, and formulations.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig8: IR spectroscopic study of polymers, drug, and formulations.
Mentions: There were no interaction between the drug and polymers as showed in Figure 8. IR spectrum of Bisoprolol fumarate is characterized by the absorption of C=O group at 1652 cm−1. Polyox WSR-205 has shown major peak at 2959, 1942, and 1482. Polyox WSR N12 K has shown major peak at 3649, 2854, and 1304. Major peaks of polymer are retained in F13 spectra showing no chemical interaction between drug and polymer. In formulation due to cross linking of polymers few bands disappeared and merged. Whereas formulation F13 spectra shown 1652 peak indicating of pure drug and no change in structure of drug.

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