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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 complexes. (a) Darifenacin, (b) physical mixture, (c) co-grounding complex, (d) coevaporation, (e) freeze dried, (f) spray dried, (g) melting method, (h) kneading method.
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fig4: FTIR spectra of darifenacin and complexes. (a) Darifenacin, (b) physical mixture, (c) co-grounding complex, (d) coevaporation, (e) freeze dried, (f) spray dried, (g) melting method, (h) kneading method.

Mentions: FT-IR spectra are presented in Figure 4. Darifenacin spectra showed the band at 3463 cm−1. From Figure 4 it was found that inclusion complexes of darifenacin showed spectra with broader bands at 1663 cm−1 and 3463 cm−1, suggesting the formation of hydrogen bonds between the carbonyl group and N–H group of darifenacin with the hydroxyl group of the host cavity.


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 complexes. (a) Darifenacin, (b) physical mixture, (c) co-grounding complex, (d) coevaporation, (e) freeze dried, (f) spray dried, (g) melting method, (h) kneading method.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig4: FTIR spectra of darifenacin and complexes. (a) Darifenacin, (b) physical mixture, (c) co-grounding complex, (d) coevaporation, (e) freeze dried, (f) spray dried, (g) melting method, (h) kneading method.
Mentions: FT-IR spectra are presented in Figure 4. Darifenacin spectra showed the band at 3463 cm−1. From Figure 4 it was found that inclusion complexes of darifenacin showed spectra with broader bands at 1663 cm−1 and 3463 cm−1, suggesting the formation of hydrogen bonds between the carbonyl group and N–H group of darifenacin with the hydroxyl group of the host cavity.

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