| 引用本文: | 肖寒露,何超芹,陈军,李俊,杨涛,方芸.星点设计-效应面法优化普萘洛尔传递体的处方工艺[J].中国现代应用药学,2012,29(12):1107-1112. |
| XIAO Hanlu,HE Chaoqin,CHEN Jun,LI Jun,YANG Tao,FANG Yun.Study on the Optimal Formulation and Preparation Conditions of Propranolol-loaded Transfersomes by Central Composite Design and Response Surface Method[J].Chin J Mod Appl Pharm(中国现代应用药学),2012,29(12):1107-1112. |
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| 摘要: |
| 目的 应用星点设计-效应面法优化普萘洛尔传递体的处方工艺。方法 采用硫酸铵梯度法制备普萘洛尔传递体。将药物/磷脂摩尔比、Span-80/磷脂摩尔比、探头超声时间作为考察因素，以包封率、载药量、平均粒径及变形性指数为效应指标，求算总评“归一值”并采用Design-Expert 8.0软件进行效应面法优化，确定最佳处方工艺并进行验证。结果 确定最优制备工艺为：药物/磷脂摩尔比19.83%、Span-80/磷脂摩尔比21.08%、探头超声时间10.29 min，以该处方工艺制备所得传递体的包封率、载药量、平均粒径及变形性指数分别为76.63%，4.80%，52.82 nm，20.83，且实测值与预测值的偏差均较小。结论 星点设计-效应面法适用于普萘洛尔传递体的处方工艺优化，优化所得处方工艺稳定、可行。
关键词：普萘洛尔；传递体；Span-80；星点设计；效应面 |
| 关键词: 普萘洛尔 传递体 Span-80 星点设计 效应面 |
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| 基金项目:南京医科大学科技发展基金重点项目(2010NJMUZ10) |
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| Study on the Optimal Formulation and Preparation Conditions of Propranolol-loaded Transfersomes by Central Composite Design and Response Surface Method |
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XIAO Hanlu1, HE Chaoqin1, CHEN Jun1, LI Jun2, YANG Tao2, FANG Yun3
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1.Department of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China;2.Nanjing Maternity and Child Health Care Hospital of Nanjing Medical University, Nanjing 210004, China;3.The Affiliated Drum Tower Hospital of Nanjing University Medical School, Nanjing 210008, China
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| Abstract: |
| OBJECTIVE To optimize the formulation and preparation of propranolol-loaded transfersomes by central composite design and response surface method. METHODS Transfersomes were prepared using the ammonium sulfate gradient method. The effects of drug/lipoid molar ratio, Span-80 molar ratio and time of probe ultrasonication on entrapment efficiency, drug-loading, vesicle size and deformability index were investigated. After each overall desirability was calculated, the optimal conditions for preparing propranolol transfersomes were achieved by Design-Expert 8.0 software, and were validated experimentally. RESULTS The optimal preparation conditions were determined as drug molar ratio 19.83%, Span-80/lipoid molar ratio 21.08%, time of probe ultrasonication 10.29 min. Under these conditions, the evaluated entrapment efficiency, drug-loading, vesicle size and deformability index of propranolol transfersomes were 76.63%, 4.80%, 152.82 nm, 20.83 respectively, and all approximated to the forecasted ones. CONCLUSION The central composite design and response surface method is applicable for the formulation and preparation conditions of optimization of propranolol transfersomes, and the resulting optimal preparation technique is stable and feasible. |
| Key words: propranolol transfersomes Span-80 central composite design response surface |
