摘要
采用高压均质法制备酮康唑纳米晶,考察稳定剂种类及浓度、酮康唑浓度、高压均质机运行压力以及均质化循环次数对粒径和多分散指数的影响。结果表明,最优制备工艺为:10%(相对主药量)的泊洛沙姆407作为稳定剂,酮康唑浓度10 mg/m L,运行压力81.6 MPa,循环次数15次。优化条件下制得的酮康唑纳米晶平均粒径为120 nm,而且研磨前后药物的晶态及化学结构没有明显改变;与原料药相比,纳米晶的溶解度、溶出速率、溶出总量均有了显著地提高。
High pressure homogenization method was employed to prepare ketoconazole nanocrystals. The influence of drug concentrations,types and concentrations of stabilizer,the pressure and circle numbers on particle size and polydispersity index were investigated. Results showed that the optimized process parameters were as follows: the concentration of stabilizer is 10%,the concentration of drug is 10 mg / m L,the pressure is 81. 6 MPa,and the circle numbers is 15. Ketoconazole nanocrystals with an average size of120 nm can be obtained in the optimum condition. Furthermore,both drugs before and after milling maintained original crystalline state; compared to ketoconazole bulk,the dissolution rate and solubility of drug nanocrystals showed a significant increase.
出处
《应用化工》
CAS
CSCD
北大核心
2016年第9期1672-1676,共5页
Applied Chemical Industry
基金
河北省高等学校科学技术研究项目(ZD2014079)
河北省自然科学基金资助项目(H2014208151)
关键词
酮康唑
纳米晶
高压均质
溶解度
溶出速率
ketoconazole
nanocrystals
high pressure homogenization
solubility
dissolution rate