一种抗高血压创制新药221s(2,9)脂肪乳的工艺研究及质量评价
Preparation and quality evaluation of antihypertensive candidate drug 221s(2,9)lipid emulsion
陈云梅 1杨宽 1余丽丽 1王荣 1唐一梅 1秦蓓1
作者信息
- 1. 西安医学院药学院,西安 710021;西安市多靶协同抗高血压创新药物研制重点实验室,西安 710021;西安医学院药物研究所,西安 710021
- 折叠
摘要
目的:本研究以抗高血压创制新药221s(2,9)为研究对象制备脂肪乳,对其进行处方工艺优化并进行质量评价.方法:采用两步乳化法制备221s(2,9)脂肪乳(221-LE),以粒径、粒径分布等为评价指标对处方进行筛选及工艺优化,同时对制备的 221-LE进行质量评价.结果:最佳处方及制备工艺为油相(长链三酰甘油∶中链三酰甘油=1∶4):10%、蛋黄卵磷脂:2%、油酸:0.05%和F68:0.1%;初乳剪切转速和时间分别为15 000 r·min-1和5 min;高压均质压力和次数分别为80 MPa和10 次.该工艺所制脂肪乳平均粒径为(131.50±1.53)nm,多分散系数(polydispersity index,PDI)为(0.12±0.01),电位为-(27.87±0.73)mV,包封率>85%;无溶血现象,稳定性良好.结论:制备的221-LE稳定性好,安全性符合要求,为221s(2,9)临床前研究提供新思路.
Abstract
Objective:To study the optimum preparation conditions of 221s(2,9)lipid emulsion(221-LE)and evaluate its quality.Methods:221-LE was prepared by two-step emulsification method.The particle size and polydispersity index(PDI)were taken as evaluation indexes to determine the formulation and preparation process.Results:The optimal prescription and preparation were as follows:by mass percentage,the compositions of long-chain triglyceride:medium-chain triglyceride(1∶4),egg yolk lecithin,F68 and oleic acid were 10%,2%,0.1%and 0.05%,respectively.The high shear rate of colostrum was 15 000 r·min-1 and high shear time was 5 min.The homogeneous pressure was 80 MPa,homogeneous cycle time was 10 times.221-LE,with the particle size of(131.50±1.53)nm,PDI of(0.12±0.01),Zeta potential of-(27.87±0.73)mV and entrapment efficiency of over 85%,had no hemolysis effect.Conclusion:The prescription process of 221-LE is stable and the quality is controllable,which provides a new perspective for the preclinical study of 221s(2,9).
关键词
脂肪乳/抗高血压创制新药221s(2,9)/工艺优化/质量评价Key words
lipid emulsion/antihypertensive candidate drug 221s(2,9)/process optimization/quality evaluation引用本文复制引用
基金项目
陕西省教育厅科研项目(23JK0651)
陕西省重点研发计划(2021ZDLSF03-05)
西安医学院博士科研启动金资助项目(2021DOC17)
陕西省教育厅青年创新团队项目(23JP155)
陕西省大学生创新创业训练计划(S202211840064)
陕西省科技厅项目(2024JC-YBQN-0956)
出版年
2024
NETL
NSTL
万方数据