Carvedilol-?-cyclodextrin Systems: Preparation, Characterization and in vitro Evaluation

Abstract

ABSTRACT:The purpose of this study was to improve the solubility and dissolution rate of carvedilol by forming a complex with β-cyclodextrin. Phase solubility diagrams revealed increase in solubility of the drug upon cyclodextrin addition, showing A N type curve. Complexation of carvedilol was carried out with β-cyclodextrin by physical mixing, kneading and co-precipitation method. The prepared complexes and physical mixture were characterized by Fourier transform infra red spectroscopy, differential scanning calorimetry, powder X-ray diffractometry and inclusion efficiency. It was also observed that the complexes exhibit higher dissolution rates than the pure drug and physical mixture. Among all carvedilol-cyclodextrin complexes, inclusion complex (1:5) prepared by co-precipitation method showed better release.

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“…The physical mixtures were formulated by triturating the calculated quantity of GMP and cyclodextrins (CDs) in a glass mortar. The physical mixtures thus obtained were screened through 120-mesh screen and then stored in a dessicator until utilized for further investigations 14,15 .…”

“…The damp mass thus obtained was passed through 60-mesh screen and the granules obtained were dried at 45 0 C under vacuum, until a constant weight was obtained. The granules after drying sufficiently were stored in a dessicator until used for further studies 14,15 .…”

“…The solvent was removed at 60 0 C under vacuum until binary complex was completely dried. The dried mass was crushed and screened through 120-mesh sieve and the powder obtained was stored in a dessicator until used in further studies 14,15 .…”

Carvedilol Solubility Enhancement by Inclusion Complexation and Solid Dispersion: Review

“…Solvent evaporation method is the most commonly used method when the experiment concerns complexation of two compounds. The method was evaluated by Tachibana and Nakamura [44] when they dissolved both drug and vacuum at temperature 40 -60˚C [42,43,45] , and ground to obtain the complex powder.…”

“…Several recent investigations showed that the inclusion complex is effective in the solubility and dissolution rate enhancement of Carvedilol. β-Cycldodextrin can reduce the interfacial tension between the solid particles of pure drug [42] because of its surfactant-like property. This improvement is guest/host ratio-dependent.…”