pH和羟丙基-b-环糊精对格列齐特溶解度和稳定性的影响

International journal of health research and innovation Pub Date : 2009-11-17 DOI:10.4314/IJHR.V1I2.47921

B. D. Shewale, R. Fursule, Nidhi Sapkal

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引用次数: 7

摘要

目的:羟基丙基β环糊精(HP-β-CD)已被用于改善多种药理化合物的水溶性。通过HP-β-CD的络合，可以提高水溶性，从而提高口服给药后的药物生物利用度。本研究考察了pH和HP-β-CD浓度对格列齐特溶解度的影响，因为它具有pH依赖性的溶解度和稳定性。方法:测定格列齐特在不同pH值(1.2 ~ 11)溶液中的平衡溶解度，并与相同pH值下20% HP- β-CD存在下的平衡溶解度进行比较。结果:当pH值从9.2增加到11时，其溶解度相对稳定(3.5 μg/ml±0.5)。20% HP-- cd在pH 1.2和pH 4下的溶解度提高了约9倍;pH 6.8时15倍;pH 7.4时40次;pH 9.2时58倍，pH 11时67倍。观察到质子化形式的溶解度高于中性分子。HP-β-CD在所有pH值下都增加了溶解度。但在HP-β-CD的空腔中是否包含药物可能取决于分子的带电状态。结论:加入HP-β-CD或加入降pH剂均可提高格列齐特的溶解度。关键词:pH，羟丙基-β-环糊精(HP-β-CD)，格列齐特

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Effect of pH and Hydroxylpropyl-b-Cyclodextrin on Solubility and Stability of Gliclazide

Purpose: Hydroxy propylated β cyclodextrin (HP-β-CD) has been used to improve the aqueous solubility of a variety of pharmacological compounds. Through the complexation of HP-β-CD, it is possible to enhance the water solubility and hence the drug bioavailability after oral administration. The present study was undertaken to examine the effect of pH and concentration of HP-β-CD on the solubility of gliclazide as it shows pH dependent solubility and stability. Method: The equilibrium solubility of gliclazide in a series of solutions of varying pH (from 1.2 to 11) was determined and compared with the equilibrium solubility of gliclazide in the presence of 20% HP- β-CD at same pH values. Result: As the pH increases from 9.2 to 11 its solubility relatively constant (3.5 μg/ml ± 0.5). Addition of 20% HP--CD increased the solubility to about 9 times at pH 1.2 and 4; 15 times at pH 6.8; 40 times at pH 7.4; 58 times at pH 9.2 and 67 times at pH 11. It was observed that solubility of protonated form is more than neutral molecule. HP-β-CD resulted in increased solubility at all pH values. But inclusion of drug in the cavity of HP-β-CD might depend upon charged state of the molecule. Conclusion: The solubility of gliclazide can be increased either by the addition of HP-β-CD or by adding pH lowering agents. Keywords: pH, hydroxypropylated-β-cyclodextrin (HP-β-CD), gliclazide.

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International journal of health research and innovation

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