利福平Si02纳米微球制备及影响因素的研究

目的,研究纳米SiO2微球组分及制备影响因素、微球表征以及利福平纳米微球的释放效果。方法：1)正交试验选出制备纳米SiO2微球各因素的最佳水平组合；2)乳化剂挥发法制备利福平纳米SiO2微球,并考察和表征其粒径大小、载药量和包封率等指标。3)利福平纳米二氧化硅微球释放评价试验。结果显示：最佳水平组合为A1B3C3D3,即纳米Si02粒径10nm、PLA 80mg/ml、明胶40mg/ml和二氯甲烷:丙酮=2:2。制备的利福平纳米SiO2微球外观圆整,大小均匀,粒径可控。影响载药量因素最主要为聚乳酸含量,其次为两种溶剂(疏水与亲水)的比例,然后是孔径和稳定剂的含量。结论：该方法制备的利福平纳米SiO2微球其载药量、包封率均在60%以上,且体外释放稳定,符合药物缓释的要求。

Study on the preparation and influencing factors of Rifampicinof nano Si02 microspheres

Objective: to study the constituent and preparation of nano Si02 microspheres, microsphere characterization and the release effect of Rifampicin nanoparticles. Methods: 1) the orthogonal test design was used to select the optimum combination of the various factors of nano- Si02 microspheres. 2) the emulsifier volatilizayion method was used to prepare Rifampicin nano- Si02 microspheres, and under the condition, the size of its particle, load and encapsulation rate and other indicator were investigated and characterized. 3) the evaluation test of the Rifampicin nano Si02 microspheres was carried out for releasing effectiveness. The results showed that the optimal combination was A1B3C3D3, namely nano Si02 microspheres size is 10 nm, PLA(polylactic acid) is 80mg/mL, gelatin is 40mg/mL and dichloromethane: aceone=2:2. There are a smooth appearance, uniform size and controllable particle size in the Rifampicin nano-Si02 microspheres this time. The main factors affecting the loading of the drug are PAL content, followed by the ratio of two solvents (hydrpphobic and hydrophilic), and then the content of pore diameter and stabilizer. Conclusion: the dosage and encapsulation rate of Rifampicin nano Si02 microspheres prepared by this method are more than 60%, and the release stability in vitro is consistent with the requirements of drug release.