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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

Differential scanning calorimetry (DSC) of darifenacin and HpβCD complex. (a) Darifenacin, (b) physical mixture, (c) coevaporation complex.
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fig2: Differential scanning calorimetry (DSC) of darifenacin and HpβCD complex. (a) Darifenacin, (b) physical mixture, (c) coevaporation complex.

Mentions: DSC thermograms are shown in Figure 2. The DSC curve of darifenacin showed an endothermic event as a melting peak with the onset temperature of 235.02◦C, indicating a crystal polymorph form. The appearance of a peak, corresponding to darifenacin melting, was also evident in the thermogram of the physical mixture. The appearance of endothermic peak with decreased intensity in the thermogram of the co-grounding complex could be attributed to the inclusion of darifenacin in the Hpβ-CD cavity. On the other hand, the absence of DSC signal indicates amorphous character of the co-evaporation complex.


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)

Differential scanning calorimetry (DSC) of darifenacin and HpβCD complex. (a) Darifenacin, (b) physical mixture, (c) coevaporation complex.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig2: Differential scanning calorimetry (DSC) of darifenacin and HpβCD complex. (a) Darifenacin, (b) physical mixture, (c) coevaporation complex.
Mentions: DSC thermograms are shown in Figure 2. The DSC curve of darifenacin showed an endothermic event as a melting peak with the onset temperature of 235.02◦C, indicating a crystal polymorph form. The appearance of a peak, corresponding to darifenacin melting, was also evident in the thermogram of the physical mixture. The appearance of endothermic peak with decreased intensity in the thermogram of the co-grounding complex could be attributed to the inclusion of darifenacin in the Hpβ-CD cavity. On the other hand, the absence of DSC signal indicates amorphous character of the co-evaporation complex.

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