蛇床子素发泡微乳剂制备研究  

Preparation of osthole foaming microemulsion

作　　者：江敏瑜 闫丹[1] 陈娇[1] 王云红[2] 张琳[1] 杨荣平[3] 张传辉[2] JIANG Min-yu;YAN Dan;CHEN Jiao;WANG Yun-hong;ZHANG Lin;YANG Rong-ping;ZHANG Chuan-hui(College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China;Chongqing Academy of Chinese Materia Medica, Chongqing 400065, China;College of Pharmacy, Southwest University, Chongqing 400715, China)

机构地区：[1]成都中医药大学药学院,四川成都611137 [2]重庆市中药研究院,重庆400065 [3]西南大学药学院,重庆400715

出　　处：《中草药》2018年第7期1562-1568,共7页Chinese Traditional and Herbal Drugs

基　　金：重庆市科委应用开发重大项目(cstc2014yykfC10006)

摘　　要：目的制备蛇床子素发泡微乳剂,并对其理化性质进行表征。方法在溶解度试验和伪三元相图的基础上,以微乳载药量、泡沫半衰期、泡沫形成力的总评归一值(OD)为评价指标,采用D-最优混料优化设计蛇床子素发泡微乳剂处方。结果蛇床子素发泡微乳剂的最优处方为油酸乙酯-聚氧乙烯蓖麻油40-二乙二醇单乙基醚-水(8.13∶14.81∶6.58∶71.44),平均粒径为(43.54±3.43)nm(n=3),平均多分散系数为(0.839±0.092)%(n=3),平均Zeta电位为(-2.32±0.78)mV(n=3),发泡量为(8.57±0.28)cm,半衰期为(6.79±0.32)min。37℃时,发泡微乳的最大载药量为13.62 mg/g,在水中的溶解度为0.42 mg/mL。结论该发泡微乳制剂稳定,可大幅提高蛇床子素的溶解度并显著增强其生物利用度。Objective To prepare osthole foaming microemulsion and study its foaming force. Methods In this paper, the overall desirability of drug loading rate, half foam life period, and foaming force was taken as index. Based on the result of solubility test and pseudo-ternary phase diagram, the formula for the osthole foaming microemulsion was optimized by D-optimal mixture optimization design test. Results The optimal ratio of the prescription was as follows： ethyl oleate-Cremophor EL-40-transcutol P-water（8.13∶14.81∶6.58∶71.44）; Average particle size was（43.54 ± 3.43） nm（n = 3）, average polydispersity factor was（0.839 ± 0.092） %（n = 3）, average potential was（-2.32 ± 0.78） mV（n = 3）, frothing volume was（8.57 ± 0.28） cm, half foam life period was（6.79 ± 0.32） min. At 37 ℃, the maximum drug loading of foaming microemulsion was 13.62 mg/g, and the solubility in water was 0.42 mg/mL. Conclusion Osthole foaming microemulsion was stable, which could greatly increase the solubility of osthole and remarkably enhance the bioavailability of osthole.

关 键 词：蛇床子素 发泡微乳 D-最优混料优化设计 伪三元相图 多分散系数 发泡量 半衰期 溶解度 

分 类 号：R283.6[医药卫生—中药学]