摘要：The purpose of this study was to improve the solubility and dissolution rate of carvedilol by forming a ternary complex with b-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 the buccal cavity.This would help to overcome its first-pass metabolism and thereby improve bioavailability.Phase solubility studies revealed the ability of b-cyclodextrin and citric acid to complex with carvedilol and significantly increase its solubility.Ternary complexation of carvedilol was carried out with b-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.
