酮洛芬聚氰基丙烯酸正丁酯毫微粒制备工艺研究

目的：制备酮洛芬聚氰基丙烯酸正丁酯毫微粒（ KP-PBCA-NP）。方法：采用乳化聚合法制备空白PBCA—NP，以粒径为指标，应用L9（3^4）正交试验优化处方工艺；吸附法制备KP—PBCA—NP，以包封率、载药量为指标，应用U10（10^8）均匀法设计实验，进行条件优化。结果：制备PBCA—NP的优化条件为反应液pH2～3，Pluronic F68的含量为1．0％～1．5％，优化条件下制备PBCA—NP平均粒径为50nm；在制备KP-PBCA—NP时，当反应液的pH值为1，PBCA含量为0．5％，KP含量为0．8mg／ml时，可获得较高的包封率（平均为95．64％）和载药量（15．32％）。结论：控制工艺条件，可制备不同粒径的PBCA—NP作为各种药物载体，并且可以从此为载体制备可用于注射给药的KP—PBCA—NP。

Preparation of ketoprofen - polybutylcyanoacrylate - nanoparticles

Objective: To prepare ketoprofen -polybutylcyanoacrylate -nanoparticles(KP -PBCA -NP). Methods: The PBCA -NP was firstly prepared with the emulsion polymerization method and L9(34) of orthogonal -design experiments was used for seeking the optimum formulation and technique. Then the KP -PBCA -NP was prepared by absorption and the factors that influenced the entrapment efficiency and quantity of drug -load were optimized with the U10(108) of Uniform design. Results: The pH 2 to 3, 1.0% PBCA and 1.0% to 1.5% dextrin 70 was the optimum conditions for the preparation of PBCA -NP, and the diameter of PBCA -NP was about 50 nm in this condition. The optimum condition for preparation of KP -PBCA -NP was pH 1, 0.5% PBCA and 0.8% mg/ml KP, and the entrapment efficiency and quantity of drug -load of KP -PBCA -NP were 95.64% and 15.32%, respectively. Conclusion: Under control conditions, PBCA -NP with different diameters can be prepared and used to load many kinds of drugs; meanwhile, injectable KP -PBCA -NP can be prepared.