溶解介质的性质对积雪草苷溶解度的影响  

Effects of the property of solution medium on the solubility of asiaticoside

作　　者：彭倩 陈有权 曹梓珍 闫帅[1] 熊金玲[1] 张莉[1] 王晓辉[1] 

机构地区：[1]武警后勤学院救援医学系生药与药剂学教研室 [2]解放军75222部队

出　　处：《中国新药杂志》2017年第17期2082-2086,共5页Chinese Journal of New Drugs

基　　金：武警后勤学院基础研究项目(WHJ201501;WHJ2015012)

摘　　要：目的:研究积雪草苷在表面活性剂、助表面活性剂及油相中的平衡溶解度,并考察溶解介质的性质对积雪草苷溶解度的影响。方法:采用摇瓶-HPLC法测定积雪草苷在各油水中的分配比,并测定其在油相中的平衡溶解度。采用HPLC法测定积雪草苷在不同表面活性剂、助表面活性剂中的平衡溶解度。结果:37℃时,积雪草苷在单亚油酸甘油酯和蓖麻油中平衡溶解度较高,分别为1 742.98和108.08μg·mL^(-1),在油酸、辛癸酸甘油酯、棕榈酸异丙酯、辛酸/癸酸三甘酯、肉豆蔻酸异丙酯中几乎不溶;在表面活性剂聚氧乙烯氢化蓖麻油中平衡溶解度较高,为60 796.50μg·mL^(-1),在辛酸癸酸聚乙二醇甘油酯中略溶,在聚山梨酯-20和聚山梨酯-80中微溶;在助表面活性剂乙氧基二乙二醇、二乙二醇单乙基醚及聚乙二醇-400中溶解度较高,分别为79 477.24,67 492.32,41 091.48μg·mL^(-1),在1,2-丙二醇中略溶,在正丙醇、异丙醇、聚甘油-6-双异油酸酯、丙三醇及聚甘油-6-异硬脂酸酯中微溶。结论:研究积雪草苷在不同介质中的平衡溶解度,为进一步研究积雪草苷微乳等制剂提供理论依据。Objective： To study the effects of the property of solution medium on the solubility of asiaticoside,the equilibrium solubility of asiaticoside in different surfactants,cosurfactants and oils were investigated. Methods：The equilibrium solubility of asiaticoside in different surfactants,cosurfactants and oils were determined with HPLC,and the oil-water partition ratio of asiaticoside was determined by shake-flask method. Results： At 37 ℃,the equilibrium solubility of asiaticoside in glyceryl monolinoleate and caster oil were higher,which were 1 742. 98 and 108. 08 μg·mL^-1,respectively. And the equilibrium solubility was poorly soluble in oleic acid,caprylic/capric triglyceride,isopropyl palmitate,Labrafac Lipophile WL 1349 and isopropyl myristate. In the surfactants,the equilibrium solubility was the most dissolvability in Cremophor RH 40,which was 60 796. 50 μg·mL^-1. The equilibrium solubility was slightly soluble in Tween-20 and Tween-80. In the cosurfactants,Transcutol CG,Transcutol P and PEG-400 had more better solubility property and they were 79 477. 24,67 492. 32 and 41 091. 48 μg·mL^-1,respectively. The equilibrium solubility was sparingly soluble in 1,2-propanediol,slightly soluble in propanol,isopropanol,plurol oleique,glycerol and plurol isostearique. Conclusion： The study of equilibriumsolubility of asiaticoside in different solution medium provides theoretical basis for further study of asiaticoside microemulsion and other formulations.

关 键 词：积雪草苷 表面活性剂 油相 单亚油酸甘油酯 聚氧乙烯氢化蓖麻油 辛酸癸酸聚乙二醇甘油酯 乙氧基二乙二醇 

分 类 号：R943[医药卫生—药剂学]