环孢素A纳米乳输液剂的制备及含量测定

Preparation and Content Determination of Cyclosporine A Nano-emulsion

目的：制备环孢素纳米乳输液剂并采用HPLC法测定该纳米乳制剂中环孢素A的含量。方法：以注射用大豆油为油相，磷脂为乳化剂，采用高压均制法制备环孢素纳米乳。HPLC法测定含量，采用Hypersil C18（ODS2）色谱柱（4．6mm×250mm，5岬）；流动相为甲醇：水（85：15，V：V）；流速为1mL／min；检测波长为225nm；柱温为50℃。结果：所制纳米乳平均粒径为35．9nm，表面电位为-33．1mV。可耐热压灭菌。在本实验分离条件下环孢素A与其他组分能较好地分离，环孢素A浓度在20—300mg／L范围内呈线形关系（r=0．9999），在高、中、低3个浓度的回收率（n=3）分别为100．28％（RSD=0．76％），100．91％（RSD=0．65％），101．11％（RSD=0．86％）。结论：制备的纳米乳稳定性较好，测定方法可以用于环孢素A纳米乳的含量测定。

Objective：To prepare Cyclosporine A（CsA） nano-emulsion injection and to determine the content of cyclosporine A（CsA） in the nano-emulsion by HPLC. Methods：An injectable soybean oil was used as the oil phase and lipoid S75 was used as the emulsifying agent. The CsA nano-emulsion injection was prepared by high pressure homogeniziton method. To determine the content, A Hypersil ODS2 （4.6 mm ×250 mm, 5 μm）with the column temperature of 50 ℃ was used. And the orther conditions under HPLC were as follows： mobile phase of methanol-water （85： 15）, the flow rate of 1mL/min and the UV detector wavelength of 225 nm. Results： The average diameter of the prepared nano-emulsion was 35.9 nm with the zeta potential of - 33.1 mV. The nano-emulsion could endure the high pressure steam sterilization. Under these test conditions of HPLC, CsA could be isolated from other components. The calibration curves were liner in the range of 20 - 300 μg/mL （ r = 0.999 9） for CsA. The recovery rates of three different concentrations were 100.28 % （ RSD = 0.79 % ）, 100.91% （ RSD = 0.65 % ）, 101.11% （ RSD = 0.86% ） respectively. Conclusion： The nano-emulsion was stable and the HPLC method could be used for determining the content of CsA in the nano-emulsion injection.