厚朴酚纳米晶体混悬剂的制备及质量评价

目的:制备厚朴酚纳米晶体混悬剂(MAG-NS),并对其进行质量评价。方法:采用星点设计-效应面法,以粒径和多分散系数的"归一值"(OD)为评价指标,有机相与水相的体积比、辅-药比、厚朴酚浓度为考察因素,优化MAG-NS制备工艺,并进行验证试验。对最优制备工艺所制MAG-NS进行质量评价。结果:优选的制备工艺为有机相与水相的体积比1:5,辅-药比4:1,厚朴酚浓度2 mg/mL。在3次验证试验中,平均OD为0.940 0(RSD=0.08%),与预测值0.977 7的相对误差为3.86%。最优制备工艺所制MAG-NS的厚朴酚纳米晶体为圆球状、大小均匀、表面光滑,粒径为(34.88±0.33)nm,多分散系数为0.032±0.001,载药量为(17.83±0.92)%。结论:建立的制备方法简单可行,所制MAG-NS质量符合要求,可为MAG-NS的进一步开发提供参考。

Preparation and Quality Evaluation of Magnolol Nano-crystal Suspension

OBJECTIVE:To prepare Magnolol nano-crystal suspension(MAG-NS),and to conduct quality evaluation.METHODS:The preparation technology of MAG-NS was optimized by central composite design-response surface methodology with OD value of particle size and polydispersity coefficient as evaluation indexes,using volume ratio of organic phase to water phase,ratio of excipient to drug,concentration of magnolol as factors and conduct validation tests.The quality of MAG-NS prepared optimal technology was evaluated.RESULTS:Optimized technology included that the volume ratio of organic phase to water phase was 1:5,mass ratio of excipient to drug was 4:1,concentration of magnolol was 2 mg/rmL.In 3 times of validation tests,average OD value was 0.940 0(RSD=0.08%),relative error of which to predicted value 0.977 7 was 3.86%.magnolol nano-crystals of MAG-NS prepared by the optimal technology were spherical,uniform in size,smooth in surface,with particle size of(34.88 ± 0.33)nm,polydispersity coefficient of 0.032 ± 0.001 and drug loading amount of(17.83 ± 0.92)%.CONCLUSIONS:Established preparation method is simple and feasible.Prepared MAG-NS is in line with quality requirements.It can provide reference for further development and utilization of MAG-NS.