硫酸氢氯吡格雷亚微乳注射液的制备及其性质考察

目的:制备硫酸氢氯吡格雷亚微乳注射液,并对其性质进行考察。方法:以注射用大豆油和注射用中链脂肪酸三酰甘油为混合油相,以蛋黄卵磷脂、泊洛沙姆188和聚山梨酯-80为复合乳化剂,采用高压均质法制备硫酸氢氯吡格雷亚微乳注射液,通过粒度和粒度分布、Zeta电位、pH值、渗透压和含量测定以及稳定性考察等对其性质进行研究。结果:制备的乳剂外观为乳白色,略带蓝色乳光。3批样品的粒径分别为(158±22)、(160±22)和(161±33)nm,平均Zeta电位为(-37.70±0.79)mV,平均pH值为(7.51±0.03),平均渗透压为(279.33±0.58)mmol.kg-1,平均含量为(99.19±1.68)%,在(6±2)和(25±2)℃条件下放置6个月稳定。结论:制备工艺可行,制剂理化性质稳定,符合静脉注射要求。

Preparation and characterization of clopidogrel bisulfate submicron emulsion for injection

Objective: To characterize the newly developed clopidogrel bisulfate submicron emulsion for injection.Methods: The clopidogrel bisulfate submicron emulsion for injection was prepared by high pressure homogenization.Injectable soybean oil and medium chain triglycerides were used as mixed oil phase,and the egg yolk lecithin,Poloxamer 188 and Tween-80 as compounded emulsifiers.The clopidogrel bisulfate submicron emulsion for injection was studied for its stability,and the determination of the particle size,Zeta potential,pH,osmotic pressure and assay.Results: The submicron emulsion was milkiness and blue opalescence.The particle sizes of the prepared clopidogrel bisulfate submicron emulsion in three batches were(158±22),(160±22) and(161±33) nm,respectively.Average zeta potential was(-37.70±0.79) mV,average pH was(7.51±0.03),average osmotic pressure was(279.33±0.58) mmol·kg-1,and average assay was(99.19±1.68)%.The submicron emulsion was stable for six months at(6±2) and(25±20) ℃.Conclusion: The preparation process for the clopidogrel bisulfate submicron emulsion for injection is feasible.The preparation possesses stable physicochemical properties and meets the standards of injection preparation.