Novel NSAIDs ophthalmic formulation: Flurbiprofen axetil emulsion with low irritancy and improved anti-inflammation effect
文献类型：期刊论文
| 作者 | Shen, Jinqiu1,2; Gan, Li1; Zhu, Chunliu1 ; Zhang, Xinxin1; Dong, Yang1; Jiang, Min1,2; Zhu, Jiabi2; Gan, Yong1
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| 刊名 | INTERNATIONAL JOURNAL OF PHARMACEUTICS
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| 出版日期 | 2011-06-30 |
| 卷号 | 412期号:1-2页码:115-122 |
| 关键词 | Flurbiprofen axetil Emulsion Aqueous humor pharmacokinetics Ocular irritation Anti-inflammation Uveitis |
| ISSN号 | 0378-5173 |
| DOI | 10.1016/j.ijpharm.2011.03.041 |
| 文献子类 | Article |
| 英文摘要 | The aim of this study was to design and formulate a novel low-irritant NSAIDs ophthalmic emulsion of flurbiprofen axetil (FBA), the prodrug of flurbiprofen (FB). FBA ophthalmic emulsion (FBA-EM) was prepared by high-pressure homogenization with caster oil as oil phase and tween 80 as emulsifying agent. Results from the stability evaluation suggested the protect effect of oil droplets on the stability of FBA. Compared with FBA-oil solution, the AUC(0 -> 10h) of FB in aqueous humor administered in FBA-EMs exhibited 6.7-fold (F2), 4.5-fold (F3) and 4.6-fold (F4) increase. With the increment of oil content, the MRT also prolonged, which of FBA-EM F2-F4 were 5.14 +/- 2.23, 5.73 +/- 3.35 and 8.71 +/- 0.94 h, respectively. No significant difference was found between the ocular bioavailability of FBA-EM F2 and 0.03% FB-Na eye drops. Ocular irritation evaluation revealed that FBA-EM F2 had better ocular biocompatibility than 0.03% FB-Na eye drops, even though the FBA concentration was up to 0.1%. Intraocular anti-inflammation effect evaluation showed that FBA-EM F2 had a quite good anti-inflammation effect. In conclusion, FBA-EM F2 with elevated FBA concentration to be 0.1% might represent a promising NSAIDs ophthalmic emulsion with low irritancy and improved anti-inflammation effect. (C) 2011 Elsevier B.V. All rights reserved. |
| WOS关键词 | OCULAR DELIVERY ; LIPID EMULSION ; PLGA NANOSPHERES ; DRUG ; STABILITY ; SYSTEM ; CHLORAMPHENICOL ; MICROEMULSIONS ; TOLERANCE ; UVEITIS |
| 资助项目 | National Basic Research Program of China[2009CB930300] ; National Science and Technology Major Project "Key New Drug Creation and Manufacturing Program"[2009ZX09301-001] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000292802700015 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278493]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Zhu, Jiabi |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.China Pharmaceut Univ, Sch Pharm, Nanjing 210009, Peoples R China |
| 推荐引用方式 GB/T 7714 | Shen, Jinqiu,Gan, Li,Zhu, Chunliu,et al. Novel NSAIDs ophthalmic formulation: Flurbiprofen axetil emulsion with low irritancy and improved anti-inflammation effect[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2011,412(1-2):115-122. |
| APA | Shen, Jinqiu.,Gan, Li.,Zhu, Chunliu.,Zhang, Xinxin.,Dong, Yang.,...&Gan, Yong.(2011).Novel NSAIDs ophthalmic formulation: Flurbiprofen axetil emulsion with low irritancy and improved anti-inflammation effect.INTERNATIONAL JOURNAL OF PHARMACEUTICS,412(1-2),115-122. |
| MLA | Shen, Jinqiu,et al."Novel NSAIDs ophthalmic formulation: Flurbiprofen axetil emulsion with low irritancy and improved anti-inflammation effect".INTERNATIONAL JOURNAL OF PHARMACEUTICS 412.1-2(2011):115-122. |
入库方式： OAI收割
来源：上海药物研究所
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