张婷;王镜;申宝德;朱君君;王立强;袁海龙;
ZHANG Ting;WANG Jing;SHEN Bao-de;ZHU Jun-jun;WANG Li-qiang;YUAN Hai-long;School of Medicine, Huaqiao University;Department of Pharmacy,Air Force Medical Center;Department of Pharmac,Air Force Medical Center;

• 1:华侨大学医学院
• 2:空军特色医学中心药学部

摘要(Abstract)：

制备并优化共载细叶远志皂苷和β-细辛醚自微乳(TF/ASA-SMEDDS),并进行质量评价。通过溶解度试验、单因素试验及伪三元相图的绘制,筛选TF/ASA-SMEDDS的处方组成;采用Box-Behnken效应面法,以载药量和粒径为考察指标筛选最优处方,并进行乳化外观、粒径、形态以及体外释放的考察。最终确定TF/ASA-SMEDDS的最优处方为辛酸癸酸三甘油酯-聚氧乙烯蓖麻油-丙三醇(10.8∶39.2∶50),其中细叶远志皂苷载药量为(5.563±0.065)mg·g^(-1),β-细辛醚的载药量为(5.526±0.022)mg·g(-1),β-细辛醚的载药量为(5.526±0.022)mg·g^(-1),乳化后可形成均一透明泛蓝光的纳米乳,粒径为(28.84±0.44)nm;TEM显示TF/ASA-SMEDDS乳化后可形成粒径均一的圆球状结构;体外溶出试验结果显示细叶远志皂苷和β-细辛醚溶出速率及释放度均显著提高。TF/ASA-SMEDDS制备工艺简单,可有效提高细叶远志皂苷和β-细辛醚的释放度。
To prepare and optimize the self-microemulsion co-loaded with tenuifolin and β-asarone(TF/ASA-SMEDDS) and evaluate its quality. The prescription compositions of TF/ASA-SMEDDS were screened by solubility test, single factor test and pseudo-tern-ary phase diagram, and the prescriptions were further optimized by Box-Behnken response surface method, with the drug loading and particle size as the evaluation indexes. Then the optimized TF/ASA-SMEDDS was evaluated for emulsified appearance, particle size, morphology and drug release in vitro. The optimized prescription for TF/ASA-SMEDDS was as follows: caprylic citrate triglyceride polyoxyethylene castor oil-glycerol(10.8∶39.2∶50), drug loading of(5.563±0.065) mg·g(-1),乳化后可形成均一透明泛蓝光的纳米乳,粒径为(28.84±0.44)nm;TEM显示TF/ASA-SMEDDS乳化后可形成粒径均一的圆球状结构;体外溶出试验结果显示细叶远志皂苷和β-细辛醚溶出速率及释放度均显著提高。TF/ASA-SMEDDS制备工艺简单,可有效提高细叶远志皂苷和β-细辛醚的释放度。
To prepare and optimize the self-microemulsion co-loaded with tenuifolin and β-asarone(TF/ASA-SMEDDS) and evaluate its quality. The prescription compositions of TF/ASA-SMEDDS were screened by solubility test, single factor test and pseudo-tern-ary phase diagram, and the prescriptions were further optimized by Box-Behnken response surface method, with the drug loading and particle size as the evaluation indexes. Then the optimized TF/ASA-SMEDDS was evaluated for emulsified appearance, particle size, morphology and drug release in vitro. The optimized prescription for TF/ASA-SMEDDS was as follows: caprylic citrate triglyceride polyoxyethylene castor oil-glycerol(10.8∶39.2∶50), drug loading of(5.563±0.065) mg·g^(-1) for tenuifolin and(5.526±0.022) mg·g(-1) for tenuifolin and(5.526±0.022) mg·g^(-1) for β-asarone; uniform and transparent pan-blue nanoemulsion can be formed after emulsification, with particle size of(28.84±0.44) nm. TEM showed that TF/ASA-SMEDDS can form spherical droplets with a uniform particle size after emulsification; In vitro release test results showed that the drug release rate and cumulative release of tenuifolin and β-asarone were significantly improved. The preparation process of TF/ASA-SMEDDS was simple and can effectively improve in vitro release of tenuifolin and β-asarone.

关键词(KeyWords)： 细叶远志皂苷;β-细辛醚;自微乳;伪三元相图;Box-Behnken效应面法;体外质量评价
tenuifolin;β-asarone;self-microemulsion;pseudo-ternary phase diagram;Box-Behnken response surface methodology;in vitro quality evaluation

Abstract:

Keywords:

基金项目(Foundation): 军队后勤科研重点项目(BKJ15J005,BKJ16J011);; 全军医学科技青年培育计划拔尖项目(17QNP028);; 福建省高校产学合作重大项目(2019Y4007);; 福建省泉州市2020年专项(2020SY001)

作者(Authors): 张婷;王镜;申宝德;朱君君;王立强;袁海龙;
ZHANG Ting;WANG Jing;SHEN Bao-de;ZHU Jun-jun;WANG Li-qiang;YUAN Hai-long;School of Medicine, Huaqiao University;Department of Pharmacy,Air Force Medical Center;Department of Pharmac,Air Force Medical Center;

DOI: 10.19540/j.cnki.cjcmm.20200922.301

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