| 熊果酸共晶固体分散体的体外特性研究 |
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| 引用本文： | 祁 雯,施 斌,黄雄伟,奚之骏,姜嫣嫣,裴元英.熊果酸共晶固体分散体的体外特性研究[J].中草药,2013,44(20):2845-2851. |
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| 作者姓名： | 祁 雯 施 斌 黄雄伟 奚之骏 姜嫣嫣 裴元英 |
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| 作者单位： | 1.复旦大学药学院 药剂教研室，上海 201203 2.上海中医药大学附属龙华医院 药剂科，上海 200032 3.上海睿智化学研究有限公司，上海 201318 4.上海同济大学附属杨浦中心医院 药剂科，上海 200090 |
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| 基金项目： | 上海市科委中药现代化专项（10DZ1972600） |
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| 摘 要： | 目的 采用共晶与固体分散体技术相结合策略，筛选合适的载体材料制备熊果酸共晶的固体分散体，更进一步提高熊果酸的溶解度、溶出度，以更好地改善其生物利用度。方法 选择泊洛沙姆188（F68）、聚维酮S630（PVP-S630）、硬脂酸聚烃氧（40）（S40）和羟丙甲纤维素（HPMC）4种载体材料，采用溶剂法，分别将原药、熊果酸-哌嗪共晶（UA-PP）与不同载体制成固体分散体。测定溶解度，进行体外溶出实验，比较并评价熊果酸制成共晶和固体分散体后改善生物利用度的潜力。结果 熊果酸共晶和熊果酸固体分散体均能增加熊果酸的溶解度和溶出度。共晶制成固体分散体后能进一步提高熊果酸的溶解度，加快其体外溶出。结论 将熊果酸共晶制成固体分散体后其溶解度和溶出度显著优于熊果酸共晶和熊果酸固体分散体。
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| 关 键 词： | 熊果酸 共晶 固体分散体 溶解度 溶出度 生物利用度 |
In vitro characteristic evaluation of ursolic acid co-crystal solid dispersions |
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| QI Wen,SHI Bin,HUANG Xiong-wei,XI Zhi-jun,JIANG Yan-yan,PEI Yuan-ying.In vitro characteristic evaluation of ursolic acid co-crystal solid dispersions[J].Chinese Traditional and Herbal Drugs,2013,44(20):2845-2851. |
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| Authors: | QI Wen SHI Bin HUANG Xiong-wei XI Zhi-jun JIANG Yan-yan PEI Yuan-ying |
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| Institution: | 1.Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 201203, China 2.Department of Pharmacy, Longhua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 200032, China 3.Simcere Pharmaceutical Group, Shanghai 201318, China 4.Department of Pharmacy, Yangpu District Central Hospital of Tongji University, Shanghai 200090, China |
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| Abstract: | Objective To use co-crystal and solid dispersion technology, screen a suitable carrier material to prepare ursolic acid (UA) co-crystal solid dispersion in order to improve the solubility and dissolution of UA. Methods UA and UA piperazine co-crystal (UA-PP) solid dispersions were prepared with solvent method by using four carriers, respectively. The solubility and in vitro dissolution of free drug, co-crystal, and solid dispersions were determined. Results The solubility of UA and UA-PP solid dispersions was significantly higher than free drug and its physical mixtures. Solid dispersion technology could further increase the solubility of UA-PP and accelerate its in vitro dissolution rate. The result layed the foundation for the development of a novel oral formulation of ursolic acid. Conclusion The co-crystal and solid dispersion technology could improve the solubility and dissolution of UA. The UA-PP solid dispersions show the best improvement in the solubility and dissolution of UA. |
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| Keywords: | ursolic acid co-crystal solid dispersion solubility dissolution bioavailability |
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