败酱皂苷H1平衡溶解度和表观油水分配系数的测定
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篇名: 败酱皂苷H1平衡溶解度和表观油水分配系数的测定
TITLE:
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.

期刊: 2016年第27卷第3期
作者: 房启龙,刘宏尉,刘江云,郝丽莉,杨世林
AUTHORS: FANG Qilong,LIU Hongwei,LIU Jiangyun,HAO Lili,YANG Shilin
关键字: 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 H1;HPLC-ELSD;Equilibrium solubility;Apparent oil and water partition coefficient
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