黄芩苷-盐酸小檗碱复合物的溶解度与油水分配系数测定

孙磊; 冯军; 雷艳丽; 隋宏; 王文苹

doi:10.13422/j.cnki.syfjx.2017210035

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黄芩苷-盐酸小檗碱复合物的溶解度与油水分配系数测定

药剂与炮制 | 更新时间：2024-01-04

- 黄芩苷-盐酸小檗碱复合物的溶解度与油水分配系数测定
- Determination of Equilibrium Solubility and Oil-water Partition Coefficient of Baicalin-berberine Hydrochloride Complex
- 中国实验方剂学杂志 2017年23卷第21期页码：35-38
- 作者机构：
- 作者简介：
- 基金信息：
  
  宁夏自然科学基金项目（NZ14090）
- DOI：10.13422/j.cnki.syfjx.2017210035
  中图分类号： R284.1
- 纸质出版日期：2017
- 稿件说明：
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孙磊, 冯军, 雷艳丽, 等. 黄芩苷-盐酸小檗碱复合物的溶解度与油水分配系数测定[J]. 中国实验方剂学杂志, 2017,23(21):35-38.

SUN Lei, FENG Jun, LEI Yan-li, et al. Determination of Equilibrium Solubility and Oil-water Partition Coefficient of Baicalin-berberine Hydrochloride Complex[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(21): 35-38.
孙磊, 冯军, 雷艳丽, 等. 黄芩苷-盐酸小檗碱复合物的溶解度与油水分配系数测定[J]. 中国实验方剂学杂志, 2017,23(21):35-38. DOI： 10.13422/j.cnki.syfjx.2017210035.

SUN Lei, FENG Jun, LEI Yan-li, et al. Determination of Equilibrium Solubility and Oil-water Partition Coefficient of Baicalin-berberine Hydrochloride Complex[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(21): 35-38. DOI： 10.13422/j.cnki.syfjx.2017210035.

摘要

目的：测定黄芩苷-盐酸小檗碱复合物的平衡溶解度与油水分配系数，为相关制剂研究奠定基础。方法：建立HPLC分别测定盐酸小檗碱和黄芩苷含量，PntulipsTM BP-C18色谱柱（4.6 mm×250 mm，5 μm），流动相乙腈-0.2%磷酸水溶液（30：70），检测波长230 nm，流速1 mL·min-1，柱温30 ℃。采用摇瓶法测定黄芩苷-盐酸小檗碱复合物在水、不同pH介质中的平衡溶解度；测定该复合物在正辛醇-水中的浓度并计算油水分配系数。结果：在pH 6.8~8.0的介质中，复合物中黄芩苷和盐酸小檗碱的溶解度与原药相比分别降低了50，2倍左右；复合物中黄芩苷和盐酸小檗碱的油水分配系数分别为0.109和0.399，分别较原药提高了2.37，4.69倍。结论：黄芩苷-盐酸小檗碱复合物的溶解度和油水分配系数与原药存在差异，可能会影响药物的体内行为和口服给药后的胃肠道吸收情况。

Abstract

Objective: To determine the equilibrium solubility and the oil-water partition coefficient of baicalin-berberine hydrochloride complex for further study on the related preparations. Method: HPLC was validated for analysis of berberine hydrochloride and baicalin.The equilibrium solubilities of baicalin-berberine hydrochloride complex in water and media with different pH were measured by shaking flask method.The concentration of this complex in n-octanol and water was determined to calculate the oil-water partition coefficient. Result: The solubilities of berberine hydrochloride and baicalin in the complex were 2-fold and 50-fold lower than that of crude drugs in medium with pH of 6.8-8.0.The oil-water partition coefficients of baicalin and berberine hydrochloride in the complex were 2.37 times and 4.69 times higher than that of the pure drugs

respectively. Conclusion: Differences of solubility and partition coefficient are revealed between baicalin-berberine hydrochloride complex and pure drugs

which may affect the in vivo performance and gastrointestinal absorption of the complex.

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