摘要
目的制备稳定的莪术醇纳米混悬剂以改善药物在水中的溶解度,提高生物利用度。方法以莪术醇为主药,采用沉淀法和高压均质法联合制备纳米混悬剂。考察处方中表面活性剂的种类、反应温度、高速剪切时间、均质反应的压力、表面活性剂与药物质量比、均质反应的次数、冻干保护剂等因素,通过单因素考察以药物粒径为考察指标,筛选出莪术醇纳米混悬剂的最佳处方,制备成稳定的莪术醇纳米混悬剂冻干粉。结果最佳制备工艺为,低温(0~3℃)下搅拌分散、2×10~4r·min^(-1)下高速剪切4 min、m(莪术醇)∶m(聚乙烯吡咯烷酮)∶m(卵磷脂)=2∶1∶1、均质压力为13.6×10~7Pa、均质次数为15次、冻干保护剂为质量分数为10%的葡萄糖溶液。莪术醇纳米混悬液平均粒径为110.4 nm,多分散系数为0.239,冻干粉复溶后粒径略微增大,平均粒径为134.7 nm,多分散系数为0.247。结论以聚乙烯吡咯烷酮为稳定剂,可将难溶性药物莪术醇制备成纳米混悬剂,改善其溶解性,提高生物利用度。莪术醇纳米混悬剂冻干粉稳定性良好。
Objective To prepare a nanosuspension containing curcumol and improve the solubility and bioaviability of curcumol. Methods Curcumol nanosuspension was prepared by precipitation method combined with high pressure homogenization method. Single factor experiment was used to screening out the best prescription of curcumol nanosuspension. The screening of freeze-dried protective additives were also studied to prepare a stable nanosuspension and lyophilized powder. Results The optimized technology was as follows ：the stiring temperature was 0 -3 ~C ,high speed shearing time was 4 min（2 x 104 r.min-~ ） ,and the ratio of amount of curcumenol ,polyvinylpyrrolidone（PVP） and lecithin was 2：1：1 ;homogenization pressure was 1.36 x 10s Pa and homogenization time was 15 times. 10% （w） glucose was used as freeze-dried protective agent. Mean particle size of prepared nanosuspension was 110.4 nm and the polydispersity index was 0.239, while the lyophilized powder dispersed again in the aqueous, the particle size was a little changed which was reached to 134.7 nm,polydispersity index was 0. 247. Conclusions Nanosuspension of insoluble drug curcumenol can be prepared using polyvinylpyrrolidone （ PVP ） as stabilizer. The solubility was increased, and the curcumol nanosuspension lyophilized powder was stable.
出处
《沈阳药科大学学报》
CSCD
北大核心
2017年第8期623-628,共6页
Journal of Shenyang Pharmaceutical University
基金
国家自然科学基金青年基金项目(81503024)
关键词
纳米混悬剂
冻干粉
联用法
单因素考察
莪术醇
nanosuspension
lyophilized powder
method combination
single factory study
curcumenol
