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基于“药辅合一”制备归桂自微乳载药系统
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| 篇名： | 基于“药辅合一”制备归桂自微乳载药系统 |
| TITLE： | Preparation of Angelica•Cinnamomum self•microemulsion drug delivery system based on the concept of “unifica- tion of drugs and excipients ” |
| 摘要： | 目的 制备归桂（即当归-桂枝）自微乳载药系统（AC•SMEDDS），优化其处方并表征所得制剂。方法以当归和桂枝的混合挥发油（以下简称“归桂混合挥发油”）为油相和模型药物，在乳化剂、助乳化剂筛选及两者质量比范围优化的基础上，以油相（归桂混合挥发油）占比、乳化剂与助乳化剂质量比为因素，挥发油含量、粒径、乳化时间的综合评分为指标，采用中心复合设计•效应面法优化处方；对优化后AC•SMEDDS的形态、粒径、载药量和包封率、稳定性等参数进行表征。结果AC•SMEDDS的最优处方为油相占比30%、乳化剂（EL•40）与助乳化剂（乙醇）质量比9∶1。验证实验表明，3批AC•SMEDDS的平均粒径为（148.33±1.53）nm，乳化时间为（18.44±0.11）s；综合评分为0.68，与预测值（0.70）的相对误差为2.86%。按最优处方所制AC-SMEDDS为淡黄色，均匀、澄清液体，透射电镜下可见边缘半透明的球形微粒；以藁本内酯、桂皮醛计，载药量分别为（7.58±0.03）、（4.17±0.01）mg/g，包封率分别为（93.25±0.01）%、（88.89±0.02）%；10000r/min离心5min或4、25℃下放置7d均无分层或沉淀产生，藁本内酯、桂皮醛含量稳定；以水稀释50、100、200倍对粒径均无明显影响。结论成功制备了AC-SMEDDS并优化了其处方，所得制剂的稳定性良好。 |
| ABSTRACT： | OBJECTIVE To prepare Angelica•Cinnamomum（Angelica sinensis-Cinnamomum cassia ）self•microemulsion drug delivery system （AC•SMEDDS），and to optimize its formulation and characterize its preparation . METHODS Using Angelica• Cinnamomum mixed volatile oil as oil phase and model drug ，on the basis of selecting emulsifier and co -emulsifier and the optimization of their mass ratio range ，the formulation was optimized with central composite design •response surface methodology using the ratio of oil phase （Angelica•Cinnamomum mixed volatile oil ），mass ratio of emulsifier and co -emulsifier as factors ，the comprehensive score of volatile oil content ，particle size and emulsifying time as index . Morphology，particle size ，drug loading ， entrapped efficiency and stability of optimized AC•SMEDDS were characterized . RESULTS The optimum formulation of AC•SMEDDS contained the ratio of oil phase was 30%，and the mass ratio of emulsifier （EL•40）and co -emulsifier（ethanol）was 9∶1. Results of validation tests showed that the average particle size of AC•SMEDDS was （148.33±1.53）nm，and emulsifying time was （18.44±0.11）s. The comprehensive score was 0.68，relative deviation of which from the predicted value （0.70）was 2.86%. AC•SMEDDS prepared by optimal formulation was faint yellow ，uniform and transparent liquid ，and spherical particals with translucent edge were observed under transmission electron microscope . Calculated by ligustilide and cinnamaldehyde ，the drug loading was （7.58±0.03） and （4.17±0.01） mg/g，and entrapped efficiency was （93.25±0.01）% and （88.89±0.02）% ， respectively. No stratification or precipitation occurred after centrifugation at the speed of 10 000 r/min or placing within 7 （No.2019-0520） days at 4 and 25 ℃ . The contents of ligustilide and cinnamaldehyde were stable . Its particle size had no significant change after 50，100 and 200 times dilution by purified water . CONCLUTIONS AC•SMEDDS is prepared successfully and its formulation is optimized . The stability of the preparation is good . |
| 期刊： | 2022年第33卷第18期 |
| 作者： | 李燕，王滨，王慧凯，高新富，宫凯凯，高俊玲，丁长玲 |
| AUTHORS： | LI Yan，WANG Bin，WANG Huikai ，GAO Xinfu，GONG Kaikai ，GAO Junling ，DING Changling |
| 关键字： | 药辅合一；归桂自微乳载药系统；处方优化；中心复合设计•效应面法 |
| KEYWORDS： | nification of drugs and excipients ；Angelica•Cinnamomum self•microemulsion drug delivery system ；formulation |
| 阅读数： | 119 次 |
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