Acta Pharmaceutica, Vol. 59 No. 2, 2009.
Original scientific paper
https://doi.org/10.2478/v10007-009-0012-0
Ternary complexation of carvedilol, β-cyclodextrin and citric acid for mouth-dissolving tablet formulation
VARSHA POKHARKAR
; Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune-411038, Maharashtra, India
ABHISHEK KHANNA
; Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune-411038, Maharashtra, India
VINOD VENKATPURWAR
; Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune-411038, Maharashtra, India
SHEETAL DHAR
; Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune-411038, Maharashtra, India
LEENATA MANDPE
; Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune-411038, Maharashtra, India
Abstract
The purpose of this study was to improve the solubility and dissolution rate of carvedilol by forming a ternary complex with β-cyclodextrin and citric acid and to formulate its mouth-dissolving tablets. The rationale for preparing mouth-dissolving tablet of carvedilol was to make the drug available in a soluble form in the mouth, which would facilitate its absorption from ther buccal cavity. Phase solubility studies revealed the ability of β-cyclodextrin and citric acid to complex with carvedilol and significantly increase its solubility. Ternary complexation of carvedilol was carried out with β-cyclodextrin and citric acid by physical mixing, kneading and spray drying methods and the prepared complexes were characterized by Fourier transform infra red spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, scanning electron microscopy and complexation efficiency. The complex obtained by the spray drying method resulted in highest complexation efficiency and a 110-fold increase in the solubility of carvedilol. The mouth-dissolving tablets formulated using the spray dried complex with suitable excipients showed 100 % dissolution within five minutes. Accelerated stability studies of mouth dissolving tablets carried out as per ICH guidelines revealed that the tablets were stable.
Keywords
carvedilol; cyclodextrin; citric acid; ternary complex; solubility; spray drying; mouth-dissolving tablet
Hrčak ID:
33501
URI
Publication date:
1.6.2009.
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