论文部分内容阅读
目的:制备阿托伐他汀钙纳米粒新剂型,对其性质进行研究,优选最佳工艺条件。方法:采用乳化-溶剂挥发法制备阿托伐他汀钙纳米粒溶液,通过对处方优化,以载体材料用量(X1)、有机溶剂用量(X2)、表面活性剂用量(X3)为自变量,利用Box Behnken设计响应面法以纳米粒粒径(Y)为响应值,优化了阿托伐他汀钙纳米粒的处方。用Malvern激光粒度分析仪测定了粒径分布和纳米粒的Zeta电位,扫描电镜分析了其形态,用高速冷冻离心法和紫外分光光度法测定了包封率和载药量。结果:采用乳化-溶剂挥发法制备阿托伐他汀钙纳米粒溶液是适合的。响应面优化最优值为阿托伐他汀钙20 mg、卵磷脂178mg、乙酸乙酯15 mL、聚山梨酯80 774 mg,所制备的阿托伐他汀钙纳米粒呈类球形,其平均粒径(71.99±13.62)nm,Zeta电位为(-31.48±2.46)mV,包封率为(91.27±1.7)%,载药量(9.58±0.22)%。结论:采用乳化-溶剂挥发法制备阿托伐他汀钙纳米粒处方及工艺适合,相关性质检测方法可行。
OBJECTIVE: To prepare a new dosage form of atorvastatin calcium nanoparticles and study its properties, and optimize the optimum technological conditions. Methods: Atorvastatin calcium nanoparticle solution was prepared by emulsification-solvent evaporation method. The optimum formulation was obtained by using the amount of carrier material (X1), the amount of organic solvent (X2) and the amount of surfactant (X3) Box Behnken Design Response Surface Method To optimize the formulation of atorvastatin calcium nanoparticles in response to nanoparticle size (Y). The particle size distribution and the Zeta potential of the nanoparticles were measured by Malvern laser particle size analyzer. The morphologies of the nanoparticles were analyzed by scanning electron microscopy. The entrapment efficiency and drug loading were determined by high speed freeze centrifugation and UV spectrophotometry. Results: It is suitable to prepare atorvastatin calcium nanoparticle solution by emulsion-solvent evaporation method. The optimum response surface was 20 mg of atorvastatin calcium, 178 mg of lecithin, 15 mL of ethyl acetate and 80 774 mg of polysorbate. The prepared atorvastatin calcium nanoparticles were spherical in shape and their average particle size (71.99 ± 13.62) nm, the Zeta potential was (-31.48 ± 2.46) mV, the entrapment efficiency was (91.27 ± 1.7)% and the drug loading was (9.58 ± 0.22)%. Conclusion: The formulation and technology of atorvastatin calcium nanoparticles prepared by emulsification - solvent evaporation method are suitable, and the detection methods of related properties are feasible.