中国现代中药2016，Vol.18Issue(2)：213-218,6.DOI:10.13313/j.issn.1673-4890.2016.2.020
3种非离子型表面活性剂对清开灵注射液中难溶性成分的增溶效果比较
Comparison of Solubilization Effect of three Nonionic Surfactants on Insoluble Components in Qingkailing Injection
摘要
Abstract
Objective:Qingkailing Injection Intermediate which contains three insoluble ingredients(baicalin,cholic acid and hyodeoxycholic acid),were used as research carriers.Polysorbate 80 (Tween-80),Poloxamer 1 88 (P1 88 )and polyethylene glycol 400(PEG400),a total of three non-ionic surfactants were taken as solubilizer,and this paper is aimed to compare the solubilization efficiency.Method:According to the solubility of BCL in three classes of solvent(water、buffer and QKL)and the dissolution of CA and HA in QKL,the Absolute Solubilization Quantity(ΔS)and Relative Solubilization Rate (RS)as the evaluation index to study the solubilization effect,the contents of insoluble ingredients after solubilization by three non-ionic surfactants were determined by HPLC.Result:Three solubilizers showed the effect of solubilization on the BCL and the solubility increase mainly in linear way with the growth of the concentration of the solubilizer.When the concentration of Tween-80,P1 88 and PEG400 were 1 %,the RS were 1 .22,0.38 and 0.7 respectively;the order of solubilization efficiency of among the three kinds of non-ionic surfactants was following:Tween-80 >PEG400 >P1 88;the solubility of BCL increased remarkably with buffer of a certain pH value,The ΔS of BCL was greatly increased by Tween-80 in water,while the RS was greatly reduced(RS <0.2 );In Qingkailing Injection Intermediate,The effect of the concentration of the solvent on the solubility of the solvent is weaker than that of the pH.The effect of Tween-80 was higher than that of CA and HA to BCL.Conclusion:In different solvents,three solubilizers had an effect of solubilization on the insoluble ingredients,and solubilization efficiency was positively correlated with the concentration of the solubilizer.The optimization should be carried out when selecting solubilizer.The pH of solvents had a greater impact on the solubility of the insoluble ingredients and suggested that attention should be paid to pH adjustment in the solubilization of insoluble ingredients.Solubilization efficiency is correlation relationship with the logP of insoluble ingredients.关键词
增溶/非离子型表面活性剂/清开灵注射液/黄芩苷/胆酸/猪去氧胆酸Key words
Solubilization/Nonionic Surfactant/Qingkailing Injection/baicalin/cholic acid/hyodeoxycholic acid引用本文复制引用
金云峰,刘瑞新,李宇辉,史新元,乔延江..3种非离子型表面活性剂对清开灵注射液中难溶性成分的增溶效果比较[J].中国现代中药,2016,18(2):213-218,6.基金项目
［基金项目］国家自然科学基金（81001646）；国家中医药管理局中医药行业科研专项 （）
