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FANG Qilong; LIU Hongwei; LIU Jiangyun; HAO Lili; YANG Shilin

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更新时间：2023-03-01

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- China Pharmacy Vol. 27, Issue 3, (2016)
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FANG Qilong, LIU Hongwei, LIU Jiangyun, et al. [J]. China Pharmacy 27(3).(2016)
DOI：

FANG Qilong, LIU Hongwei, LIU Jiangyun, et al. [J]. China Pharmacy 27(3).(2016) DOI：

摘要

目的：测定败酱皂苷H1平衡溶解度和表观油水分配系数（lg P），为败酱皂苷后续的剂型设计和成药性研究提供参考。方法：采用高效液相色谱-蒸发光散射检测（HPLC-ELSD）法测定败酱皂苷H1在不同有机溶剂和不同pH缓冲液中的平衡溶解度；采用摇瓶法测定败酱皂苷H1的lg P。结果：25 ℃下败酱皂苷H1在水、甲醇和乙醇中的平衡溶解度依次为0.091 75、96.51、46.89 g/L，在磷酸盐缓冲液pH 7.6～10.0 范围内平衡溶解度随着pH 升高而明显增大；败酱皂苷H1在pH 6.0～8.0 缓冲液中其lg P 范围为 0.695～0.773。结论：败酱皂苷H1及该类齐墩果酸型皂苷属于低溶解度、低透过性的成分，因而不适宜作为常规口服制剂开发使用。

Abstract

OBJECTIVE：To determine the solubility and apparent oil and water partition coefficient（lg P）of saponin H1，and provide reference for dosage form design and druggability research of saponin. METHODS：HPLC-ELSD was conducted to determine the equilibrium solubility of saponin H1 in different organic solvents and pH buffer solutions；shaking flask was applied to determine lg P value of saponin H1. RESULTS：The equilibrium solubility of saponin H1 in water，methanol and ethanol at 25 ℃ was 0.09175 g/L，96.51 g/L and 46.89 g/L，respectively. The solubility increased apparently at high pH within pH range at 7.6-10.0； the lg P value was between 0.695-0.773 in buffers within pH range at 6.0-8.0. CONCLUSIONS：Saponin H1 and the oleanolic acid type saponins belong to low solubility

low transmission components

so it is not suitable for use as a conventional oral formulation is developed.

关键词

败酱皂苷H1高效液相色谱-蒸发光散射检测法平衡溶解度表观油水分配系数

Keywords

Saponin H1HPLC-ELSDEquilibrium solubilityApparent oil and water partition coefficient

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