摘要
目的研究熊果酸纳米乳的制备和质量评价。方法考察熊果酸在不同油相、表面活性剂和助表面活性剂中的平衡溶解度,并通过水滴定法绘制伪三元相图,确定最优的Km值和纳米乳处方,研制出适合经口给药的纳米乳制剂。分别采用离心法考察熊果酸纳米乳的外观和形态,通过电导率判断其类型以及使用激光粒度测定仪测定粒径大小,使用电子透射显微镜观察纳米乳形态。用HPLC测定含药纳米乳中熊果酸的含量,同时考察其稳定性、载药量、包封率等。结果优选处方为Cremophor RH40-聚乙二醇400-油酸乙酯(52.5∶17.5∶30,m/m/m)。所制熊果酸纳米乳为澄清或略带乳光的淡蓝色液体,离心后稳定不分层,电导率为33.7 ms·m^-1,平均粒径(53.09±10.47)nm,呈Gauss分布,纳米乳液滴,外观圆整,大小均一,状态良好。HPLC检测其稳定性良好,包封率为86.5%,载药量为0.425mg·mL^-1。结论熊果酸在纳米乳中的溶解度明显增加,所制得的含药纳米乳易于制备且质量稳定,可以通过制作熊果酸纳米乳的方法来提高熊果酸的生物利用度。
Objective To prepare and evaluate the quality of ursolic acid nanoemulsion. Methods The equilibrium solubility of ursolic acid in different oil phases, surfactants and cosurfactants was investigated. The pseudo-ternaryphase diagram was drawn by water titration;the optimal Km value and the formulation of nanoemulsion were determined;and the preparation of nanoemulsion suitable for oral administration was developed. The appearance and morphology of ursolic acid nanoemulsion were investigated by centrifugation, the type was determined by electrical conductivity, and the particle size was determined by laser particle size analyzer. The morphology of ursolic acid nanoemulsion was observed by electron transmission microscope. The content of ursolic acid was determined by HPLC. Results The optimal prescription was Cremophor RH40- polyethylene glycol400-ethyl oleate (52.5 ∶ 17.5 ∶ 30, m/m/m). The ursolic acid nanoemulsion was a clear or light blue liquid with slight emulsion. After centrifuged, it was stable and unstratified, with a conductivity of 33.7 ms·m^-1 and an average particle size of (53.09±10.47) nm, with Gauss distribution. The nanoemulsion was round in appearance and uniform in size and in good condition. HPLC tested its stability, with the encapsulation rate at 86.5%, and drug loading at 0.425 mg·mL^-1 . Conclusion The solubility of ursolic acid in nanoemulsion is significantly increased, and the prepared nanoemulsion is easy to prepare with stable quality. Therefore, the bioavailability of ursolic acid may be improved by preparing ursolic acid nanoemulsion.
作者
邹荣
要辉
胡隽
尹超
王伦
陈曦文
潘阳阳
许汉林
ZOU Rong;YAO Hui;HU Jun;YIN Chao;WANG Lun;CHEN Xi-wen;PAN Yang-yang;XU Han-lin(Hubei University of Chinese Medicine,Wuhan 430065)
出处
《中南药学》
CAS
2019年第6期830-835,共6页
Central South Pharmacy
