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Dissolution Rate Enhancement, Design and Development of Buccal Drug Delivery of Darifenacin Hydroxypropyl β-Cyclodextrin Inclusion Complexes.

Jagdale SC, Mohanty P, Chabukswar AR, Kuchekar BS - J Pharm (Cairo) (2012)

Bottom Line: The solid inclusion complexes were found to be amorphous in the characterization.Formulations Hb2 (2%) and Pb4 (4%) were found to be optimized.These two formulations can be used for buccal delivery of darifenacin which avoids first pass effect and leads to increased bioavailability of darifenacin.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, MAEER's Maharashtra Institute of Pharmacy, S. Number 124, MIT Campus, Kothrud, Maharashtra, Pune 411 038, India.

ABSTRACT
Darifenacin is a urinary antispasmodic. The oral absorption of darifenacin is poor due to its low solubility and poor bioavailability (15-19%). Darifenacin was complexed with hydroxylropyl beta-cyclodextrin (Hpβ-CD). The best results were obtained with the coevaporation that interacts in a 1 : 1 drug : cyclodextrin molar ratio. The solid inclusion complexes were found to be amorphous in the characterization. The dissolution rate of darifenacin from the Hpβ-CD solid inclusion complex was increased compared to the powdered drug. The controlled release buccoadhesive patches for the delivery of darifenacin were prepared using HPMC K100M CR and HPMC K15. The coevaporation complex of the drug was used in the formulation due to its increased saturation solubility and increased ease of dissolution. The patches were evaluated for their surface pH, folding endurance, swelling, mucoadhesive properties, in vitro residence time, vapour transmission test, and in vitro and ex vivo release studies. Formulations Hb2 (2%) and Pb4 (4%) were found to be optimized. These two formulations can be used for buccal delivery of darifenacin which avoids first pass effect and leads to increased bioavailability of darifenacin.

No MeSH data available.


Related in: MedlinePlus

FTIR spectra of darifenacin and formulations. (a) Darifenacin, (b) drug-Hpβ-CD complex with HPMC K15, (c) drug-Hpβ-CD complex with HPMC K100 M CR.
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fig9: FTIR spectra of darifenacin and formulations. (a) Darifenacin, (b) drug-Hpβ-CD complex with HPMC K15, (c) drug-Hpβ-CD complex with HPMC K100 M CR.

Mentions: The data analysis during and after stability studies up to 3 months indicates that the drug molecules remain unchanged in the patches and shows no interaction with the polymers (Figure 9) and no degradation. Percentage drug content in 1st, 2nd, and 3rd month analysis was within 94–97%. Diffusion study of the optimised formulations in the subsequent 3 months was same as the initial in vitro and ex vivo release studies.


Dissolution Rate Enhancement, Design and Development of Buccal Drug Delivery of Darifenacin Hydroxypropyl β-Cyclodextrin Inclusion Complexes.

Jagdale SC, Mohanty P, Chabukswar AR, Kuchekar BS - J Pharm (Cairo) (2012)

FTIR spectra of darifenacin and formulations. (a) Darifenacin, (b) drug-Hpβ-CD complex with HPMC K15, (c) drug-Hpβ-CD complex with HPMC K100 M CR.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4595963&req=5

fig9: FTIR spectra of darifenacin and formulations. (a) Darifenacin, (b) drug-Hpβ-CD complex with HPMC K15, (c) drug-Hpβ-CD complex with HPMC K100 M CR.
Mentions: The data analysis during and after stability studies up to 3 months indicates that the drug molecules remain unchanged in the patches and shows no interaction with the polymers (Figure 9) and no degradation. Percentage drug content in 1st, 2nd, and 3rd month analysis was within 94–97%. Diffusion study of the optimised formulations in the subsequent 3 months was same as the initial in vitro and ex vivo release studies.

Bottom Line: The solid inclusion complexes were found to be amorphous in the characterization.Formulations Hb2 (2%) and Pb4 (4%) were found to be optimized.These two formulations can be used for buccal delivery of darifenacin which avoids first pass effect and leads to increased bioavailability of darifenacin.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, MAEER's Maharashtra Institute of Pharmacy, S. Number 124, MIT Campus, Kothrud, Maharashtra, Pune 411 038, India.

ABSTRACT
Darifenacin is a urinary antispasmodic. The oral absorption of darifenacin is poor due to its low solubility and poor bioavailability (15-19%). Darifenacin was complexed with hydroxylropyl beta-cyclodextrin (Hpβ-CD). The best results were obtained with the coevaporation that interacts in a 1 : 1 drug : cyclodextrin molar ratio. The solid inclusion complexes were found to be amorphous in the characterization. The dissolution rate of darifenacin from the Hpβ-CD solid inclusion complex was increased compared to the powdered drug. The controlled release buccoadhesive patches for the delivery of darifenacin were prepared using HPMC K100M CR and HPMC K15. The coevaporation complex of the drug was used in the formulation due to its increased saturation solubility and increased ease of dissolution. The patches were evaluated for their surface pH, folding endurance, swelling, mucoadhesive properties, in vitro residence time, vapour transmission test, and in vitro and ex vivo release studies. Formulations Hb2 (2%) and Pb4 (4%) were found to be optimized. These two formulations can be used for buccal delivery of darifenacin which avoids first pass effect and leads to increased bioavailability of darifenacin.

No MeSH data available.


Related in: MedlinePlus