茴拉西坦亚微乳处方及制备工艺考察

目的制备茴拉西坦亚微乳,并进行质量评价。方法采用组织捣碎-高压均质工艺制备茴拉西坦亚微乳,正交试验优化处方,单因素考察制备工艺,并测定所制乳剂zeta电位、粒径、pH值及药物含量。结果茴拉西坦亚微乳最佳处方和工艺为注射用中链油125 g.L-1、大豆磷脂和pluronicF68总量为30 g.L-1、大豆磷脂和pluronic F68的质量比为1∶4,56 MPa均质5次;所得乳剂zeta电位为-30.8 mV,粒径为(149±21)nm,pH值为6.0,茴拉西坦含量为1.5 g.L-1。结论所得乳剂理化性质良好,符合静脉注射要求。

Formulation and preparation procedure of aniracetam submicron emulsion

Objective To prepare aniracetam submicron emulsion and evaluate its quality. Methods The agitation of high-speed and high pressure homogenization method was employed to prepare the aniracetam submicron emulsion. The formulation and preparation procedure of emulsion were optimized through orthogonal design and single factor test, respectively. The emulsion was characterized by particle size, zeta potential, pH and aniracetam content. Results The optimal formulation was composed of medium-chain triglyceride 125 g·L^-1, emulsifiers 30 g·L^-1 with a ratio of lecithin and pluronic F68 in 1∶4, and the primary emulsion was homogenized five times at a pressure of 56 MPa. The zeta potential was -30.8 mV, the particle size was (149±21) nm, the pH was 6.0 and the content of aniracetam was 1.5 g·L^-1. Conclusions The aniracetam submicron emulsion with excellent physicochemical properties is successfully fabricated for intravenous administration.