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羟丙基-β-环糊精对卡维地洛溶解度的影响

Effect of hydroxylpropyl-beta-cyclodextrin on Solubility of Carvedilol.

作者信息

Shewale B D, Sapkal N P, Raut N A, Gaikwad N J, Fursule R A

机构信息

H. R. Patel Women's Collage of Pharmacy, Karwand Naka (Shirpur)- 425 405, India.

出版信息

Indian J Pharm Sci. 2008 Mar-Apr;70(2):255-7. doi: 10.4103/0250-474X.41470.

Abstract

The present study was undertaken to examine the effect of pH and concentration of hydroxypropyl-beta-cyclodextrin on the solubility of carvedilol as it shows pH-dependent solubility. The equilibrium solubility of carvedilol in a series of solutions of varying pH (from 1.2 to 11) was determined and compared with the equilibrium solubility of carvedilol in the presence of 20% hydroxypropyl-beta-cyclodextrin at same pH values. It was observed that solubility of protonated form is more than neutral molecule. Hydroxypropyl-beta-cyclodextrin resulted in increased solubility at all the pH. But inclusion in the cavity of hydroxypropyl-beta-cyclodextrin might depend upon charge state of the molecule. So it can be concluded that solubility of carvedilol, can be increased either by the addition of hydroxypropyl-beta-cyclodextrin or by adding pH lowering agents. But both these methods if are to be used together, pH should be selected carefully.

摘要

由于卡维地洛表现出pH依赖性溶解度,本研究旨在考察pH值和羟丙基-β-环糊精浓度对其溶解度的影响。测定了卡维地洛在一系列不同pH值(1.2至11)溶液中的平衡溶解度,并与相同pH值下20%羟丙基-β-环糊精存在时卡维地洛的平衡溶解度进行比较。观察到质子化形式的溶解度大于中性分子。羟丙基-β-环糊精在所有pH值下均导致溶解度增加。但分子进入羟丙基-β-环糊精的空腔可能取决于分子的电荷状态。因此可以得出结论,卡维地洛的溶解度可以通过添加羟丙基-β-环糊精或添加pH降低剂来提高。但如果要同时使用这两种方法,则应谨慎选择pH值。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/114a/2792477/dd05055eaf20/IJPhS-70-255-g001.jpg

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