Limits...
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

In vitro release profile of different formulations of HPMC K100 M CR containing Hpβ-CD-darifenacin complex. Hb1–Hb5 formulations of HPMC K100 M CR containaing 1%–5% of the polymer, D-formulation containing pure drug.
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4595963&req=5

fig6: In vitro release profile of different formulations of HPMC K100 M CR containing Hpβ-CD-darifenacin complex. Hb1–Hb5 formulations of HPMC K100 M CR containaing 1%–5% of the polymer, D-formulation containing pure drug.

Mentions: In Vitro Drug Release Study. The release study was done in the Keshery-Chien diffusion cell using pH 6.8 buffer medium [21]. The cellophane membrane was carefully mounted in between the two compartments of a Keshery-Chien diffusion cell with internal diameter of 2.1 cm (3.46 cm2 area) with a receptor compartment volume of 12 mL of solution containing phosphate buffer pH (6.8) were placed in the receptor compartment. Temperature was maintained at 37 ± 2°C. Firstly the release study was done for the patches of different polymer concentrations of both HPMC K100CR and HPMC K15 and the result is shown in Figures 6 and 7. The patches Hb2 and Pb4 were selected for final formulation due to their release profile. Release study using egg membrane also conducted for the optimised formulations. The withdrawals were compensated using equal volumes of phosphate buffer pH 6.8 kept at the same temperature. The concentration of drug released in the medium was assayed spectrophotometrically at 285 nm after suitable dilution with the diffusion medium phosphate buffer pH 6.8 whenever necessary. The experiment was carried out continuous up to 10 h. All the experiments were conducted in 3 replicates.


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)

In vitro release profile of different formulations of HPMC K100 M CR containing Hpβ-CD-darifenacin complex. Hb1–Hb5 formulations of HPMC K100 M CR containaing 1%–5% of the polymer, D-formulation containing pure drug.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig6: In vitro release profile of different formulations of HPMC K100 M CR containing Hpβ-CD-darifenacin complex. Hb1–Hb5 formulations of HPMC K100 M CR containaing 1%–5% of the polymer, D-formulation containing pure drug.
Mentions: In Vitro Drug Release Study. The release study was done in the Keshery-Chien diffusion cell using pH 6.8 buffer medium [21]. The cellophane membrane was carefully mounted in between the two compartments of a Keshery-Chien diffusion cell with internal diameter of 2.1 cm (3.46 cm2 area) with a receptor compartment volume of 12 mL of solution containing phosphate buffer pH (6.8) were placed in the receptor compartment. Temperature was maintained at 37 ± 2°C. Firstly the release study was done for the patches of different polymer concentrations of both HPMC K100CR and HPMC K15 and the result is shown in Figures 6 and 7. The patches Hb2 and Pb4 were selected for final formulation due to their release profile. Release study using egg membrane also conducted for the optimised formulations. The withdrawals were compensated using equal volumes of phosphate buffer pH 6.8 kept at the same temperature. The concentration of drug released in the medium was assayed spectrophotometrically at 285 nm after suitable dilution with the diffusion medium phosphate buffer pH 6.8 whenever necessary. The experiment was carried out continuous up to 10 h. All the experiments were conducted in 3 replicates.

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