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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

X-ray diffractometry of (a) darifenacin, (b) coevaporation complex and (c) physical mixture complex.
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fig3: X-ray diffractometry of (a) darifenacin, (b) coevaporation complex and (c) physical mixture complex.

Mentions: The X-ray diffractometry studies (Figure 3) revealed the crystalline nature of darifenacin. Darifenacin shows major peaks at 2θ values 11.3, 11.4, 11.5, 17.00, 18.2, 20.1, 20.2, 20.3, 25.2, 26.8, 27.3, 27.6, 30.3, and 30.8. The peaks observed were less intense than those of the drug in physical mixture and co-evaporation complex. The diffractogram of the co-evaporation complex showed no darifenacin crystal signals, demonstrating the amorphous nature of the product. The study of these spectra indicated that degree of crystallinity was decreased by complexation with Hpβ-CD.


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)

X-ray diffractometry of (a) darifenacin, (b) coevaporation complex and (c) physical mixture complex.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig3: X-ray diffractometry of (a) darifenacin, (b) coevaporation complex and (c) physical mixture complex.
Mentions: The X-ray diffractometry studies (Figure 3) revealed the crystalline nature of darifenacin. Darifenacin shows major peaks at 2θ values 11.3, 11.4, 11.5, 17.00, 18.2, 20.1, 20.2, 20.3, 25.2, 26.8, 27.3, 27.6, 30.3, and 30.8. The peaks observed were less intense than those of the drug in physical mixture and co-evaporation complex. The diffractogram of the co-evaporation complex showed no darifenacin crystal signals, demonstrating the amorphous nature of the product. The study of these spectra indicated that degree of crystallinity was decreased by complexation with Hpβ-CD.

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