Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test
文献类型：期刊论文
| 作者 | Wang, Yan-ping; Gan, Yong ; Zhang, Xin-xin
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2011-10 |
| 卷号 | 32期号:10页码:1294-1302 |
| 关键词 | immunosuppressants tacrolimus bioavailability self-microemulsifying lipid mixture gastroretentive sustained-release tablet |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2011.90 |
| 文献子类 | Article |
| 英文摘要 | Aim: To develop a novel gastroretentive drug delivery system based on a self-microemulsifying (SME) lipid mixture for improving the oral absorption of the immunosuppressant tacrolimus. Methods: Liquid SME mixture, composed of Cremophor RH40 and monocaprylin glycerate, was blended with polyethylene oxide, chitosan, polyvinylpyrrolidone and mannitol, and then transformed into tablets via granulation, with ethanol as the wetting agent. The tablets were characterized in respect of swelling, bioadhesive and SME properties. In vitro dissolution was conducted using an HCl buffer at pH 1.2. Oral bioavailability of the tablets was examined in fasted beagle dogs. Results: The tablet could expand to 13.5 mm in diameter and 15 mm in thickness during the initial 20 min of contact with the HCl buffer at pH 1.2. The bioadhesive strength was as high as 0.98 +/- 0.06 N/cm(2). The SME gastroretentive sustained-release tablets preserved the SME capability of the liquid SME formations under transmission electron microscope. The drug-release curve was fit to the zero-order release model, which was helpful in reducing fluctuations in blood concentration. Compared with the commercially available capsules of tacrolimus, the relative bioavailability of the SME gastroretentive sustained-release tablets was 553.4%+/- 353.8%. Conclusion: SME gastroretentive sustained-release tablets can enhance the oral bioavailability of tacrolimus with poor solubility and a narrow absorption window. |
| WOS关键词 | DRUG-DELIVERY SYSTEMS ; EMULSIFYING FORMULATION ; POLYETHYLENE OXIDE ; ORAL ABSORPTION ; LIPOPHILIC DRUGS ; DOSAGE FORMS ; DISSOLUTION ; SEDDS ; PHARMACOKINETICS ; OPTIMIZATION |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4335580 |
| WOS记录号 | WOS:000295921300015 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278383]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Zhang, Xin-xin |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Yan-ping,Gan, Yong,Zhang, Xin-xin. Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test[J]. ACTA PHARMACOLOGICA SINICA,2011,32(10):1294-1302. |
| APA | Wang, Yan-ping,Gan, Yong,&Zhang, Xin-xin.(2011).Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test.ACTA PHARMACOLOGICA SINICA,32(10),1294-1302. |
| MLA | Wang, Yan-ping,et al."Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test".ACTA PHARMACOLOGICA SINICA 32.10(2011):1294-1302. |
入库方式： OAI收割
来源：上海药物研究所
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