<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml"><p>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 the buccal cavity. This would help to overcome its first-pass metabolism and thereby improve bioavailability. 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.</p></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 the buccal cavity. This would help to overcome its first-pass metabolism and thereby improve bioavailability. 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.

Ternary complexation of carvedilol, β-cyclodextrin and citric acid for mouth-dissolving tablet formulation

Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune-411038 Maharashtra, India

Acta Pharmaceutica

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...

Ternary complexation of carvedilol, β-cyclodextrin and citric acid for mouth-dissolving tablet formulation

Publié en ligne: 20 mars 2009

Pages: 121 - 132

DOI: https://doi.org/10.2478/v10007-009-0001-3

Mots clés
karvedilol, ciklodekstrin, liminska kiselina, kompleksacija, topljivost, sušenje raspršivanjem, tablete topljive u ustima

This content is open access.

Ternary complexation of carvedilol, β-cyclodextrin and citric acid for mouth-dissolving tablet formulation

Publié en ligne: 20 mars 2009

Pages: 121 - 132

DOI: https://doi.org/10.2478/v10007-009-0001-3

Mots cléskarvedilol, ciklodekstrin, liminska kiselina, kompleksacija, topljivost, sušenje raspršivanjem, tablete topljive u ustima

This content is open access.

Mots clés
karvedilol, ciklodekstrin, liminska kiselina, kompleksacija, topljivost, sušenje raspršivanjem, tablete topljive u ustima