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Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione: Effects of lipid composition and formulation

文献类型：期刊论文

作者Han, Si-fei2; Yao, Ting-ting1; Zhang, Xin-xin2; Gan, Li2; Zhu, Chunliu2; Yua, Hong-zhen2; Gan, Yong2
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
出版日期2009-09-08
卷号379期号:1页码:18-24
关键词Anethol trithione Lipid formulation Lipid digestion Intestinal absorption
ISSN号0378-5173
DOI10.1016/j.ijpharm.2009.06.001
文献子类Article
英文摘要This study has explored the use of lipid-based formulations to enhance the oral bioavailability of the poorly water-soluble drug anethol trithione (ATT), and compared the performance of different formulations. Two groups of lipid-based formulations, sub-microemulsion (SME) and oil solution, were prepared using short (SCT), medium (MCT) and long (LCT) chain triglycerides respectively; aqueous suspension was used as the reference formulation. In vitro and in vivo studies were conducted to investigate the impact of lipid composition and formulation on drug absorption. In vitro digestion was used to analyze lipid digestion rates and drug distribution/solubilization. After in vitro digestion, the performance rank order for drug solubilization was SCT < MCT < LCL SME formulations were digested more rapidly in vitro than oil solutions. The bioavailability of the drug from different formulations was investigated in rats. All six lipid-based formulations enhanced drug absorption compared to the aqueous suspension. For the SMEs, which were rapidly digested, in vivo bioavailability increased in accordance with the increase of solubilization data obtained by in vitro digestion, with the rank order SCT-SME < MCT-SME < LCT-SME. For the oil solutions, which were digested more slowly, there was no significant difference in drug bioavailability for the different formulations. in conclusion, lipid-based formulations can enhance the oral bioavailability of ATT, and for this BCS class II drug, both the lipid composition and type of lipid formulation are likely to govern in vivo performance. (C) 2009 Elsevier B.V. All rights reserved.
WOS关键词IN-VITRO DIGESTION ; LONG-CHAIN TRIGLYCERIDES ; DELIVERY-SYSTEMS ; SOLUBILIZATION BEHAVIOR ; HPLC DETERMINATION ; LIPOPHILIC DRUGS ; LIPOLYSIS MODEL ; ABSORPTION ; DANAZOL ; IMPACT
资助项目National Natural Sciences Foundation of China[30701054] ; New Drug Basic Research[00000000] ; Chinese Academy of Sciences[07G603H071] ; National Basic Research Program of China[2009CB930300]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000269809600003
出版者ELSEVIER SCIENCE BV
源URL[http://119.78.100.183/handle/2S10ELR8/279133]  
专题药物制剂研究中心
通讯作者Gan, Yong
作者单位1.Shenyang Pharmaceut Univ, Sch Pharm, Shenyang 110016, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Han, Si-fei,Yao, Ting-ting,Zhang, Xin-xin,et al. Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione: Effects of lipid composition and formulation[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2009,379(1):18-24.
APA Han, Si-fei.,Yao, Ting-ting.,Zhang, Xin-xin.,Gan, Li.,Zhu, Chunliu.,...&Gan, Yong.(2009).Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione: Effects of lipid composition and formulation.INTERNATIONAL JOURNAL OF PHARMACEUTICS,379(1),18-24.
MLA Han, Si-fei,et al."Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione: Effects of lipid composition and formulation".INTERNATIONAL JOURNAL OF PHARMACEUTICS 379.1(2009):18-24.

入库方式： OAI收割

来源：上海药物研究所

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