光散射法测定难溶性药物粒度

Determination of Particle Size Distribution of Poorly Water-soluble Drugs by Laser Light Diffraction Technique

目的研究光散射法中湿法测定难溶性药物粒度的方法及要求。方法通过仪器参数设定、样品的制备、分析方法验证确定原料药粒度测定的方法,根据生产工艺、体外溶出及体内吸收制定原料药粒度标准,对利伐沙班原料药进行粒度测定。结果与结论粒度对药物的有效性、安全性、稳定性都有重要影响,湿法测定原料药的粒度方法稳定、结果准确、重现性好,在药物开发过程中应对药物粒度的测定方法进行详细研究并制定符合要求的粒度标准。

OBJECTIVE To stu poorly water-soluble drugs dispersed preparation and analysis method process, dissolution in vitro and dy the methods and requirements about the determination of particle size when in suitable liquids. METHODS By instrumental parameter setting, sample validation, the method for particle size determination was confirmed. By production absorption in vivo of the formulation, the specification was established. The particle size distribution of rivaroxaban was determinated by liquid dispersion. RESULTS and CONCLUSION Particle size has an important effect on the efficacy, safety and stability of drugs, the determination of particle size using liquid dispersion in laser light diffraction technique was stable,accurate and reproducible. Particle size should be studied in detail to obtain specification for product requirements in drug development process.