首页|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

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

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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.
Preparation and quality evaluation of antihypertensive candidate drug 221s(2,9)lipid emulsion
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).

lipid emulsionantihypertensive candidate drug 221s(2,9)process optimizationquality evaluation

陈云梅、杨宽、余丽丽、王荣、唐一梅、秦蓓

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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

脂肪乳 抗高血压创制新药221s(2,9) 工艺优化 质量评价

陕西省教育厅科研项目陕西省重点研发计划西安医学院博士科研启动金资助项目陕西省教育厅青年创新团队项目陕西省大学生创新创业训练计划陕西省科技厅项目

23JK06512021ZDLSF03-052021DOC1723JP155S2022118400642024JC-YBQN-0956

2024

中国新药杂志
中国医药科技出版社 中国医药集团总公司 中国药学会

中国新药杂志

CSTPCD北大核心
影响因子：1.039
ISSN：1003-3734
年,卷(期)：2024.33(16)