摘要
目的制备硝酸毛果芸香碱纳米液晶制剂,以包封率(EE)和粒径为考察指标对处方进行单因素考察,然后以正交设计对处方进行筛选。方法处方前研究硝酸毛果芸香碱的平衡溶解度、油水分配系数,为剂型设计提供理论依据;选择高压均质法制备硝酸毛果芸香碱液晶纳米粒;以EE和粒径为考察指标对处方进行单因素考察,然后以正交设计对处方进行筛选。结果药物在水中易溶,溶解度约为146.87mg/mL,油水分配系数LogP约为-0.278。本研究通过单因素考察了单油酸甘油酯(GMO)/水的比例、搅拌速度、滴加速度、均质压力和均质次数。综合考虑最大EE和粒径,选用的最佳处方工艺为:GMO∶泊洛沙姆407∶水=2∶0.22∶20,搅拌速度为1000r/min,均质压力为350bar,均质次数为3次。结论硝酸毛果芸香碱液晶纳米粒制备工艺简单,稳定性好,具有临床应用价值。
Objective To prepare liquid crystal nanoparticles loaded with pilocarpine nitrate （PN-LCNPs） for effective ocular drug delivery. Indexes of the optimal formulation of entrapment efficiency and particle size were obtained by single factor evaluation. Methods Based on the investigation on solubility and partition coefficients of pilocarpine,PN-LCNPs was prepared by the method of high-pressure homogenization. The optimal formulation of entrapment efficiency and particle size was obtained by single factor evaluation. Results PN was soluble in water, about 146.87 mg/mL, the partition coefficient of PN in octanol/water system was about -0. 278. Optimal formulation of PN-LCNPs was as follows： the mixture of GMO, F127 was heated to 37 ~C and dissolved in water under stirring at 1 000 rpm （GMO ： F127 ： water=2 ： 0.22 ： 20）. The resulting dispersion was extruded through high-pressure homogenizerby three cycles at 350 bars to form an opalescent dispersion. Conelusion The preparation of PN-LCNPs is simple,however,had a good stability, so it has good prospects for clinical application.
出处
《成都医学院学报》
CAS
2013年第3期257-261,共5页
Journal of Chengdu Medical College
基金
中国高校医学期刊临床专项资金项目(NO:11321062)
关键词
硝酸毛果芸香碱
纳米液晶
单油酸甘油酯
高压均质法
单因素考察
Pilocarpine nitrate
Liquid crystal nanoparticle
Glycerol monooleate
High-pressure homogenization
Single factor evaluation
