Novel NSAIDs ophthalmic formulation: Flurbiprofen axetil emulsion with low irritancy and improved anti-inflammation effect

doi:10.1016/j.ijpharm.2011.03.041

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药物制剂研究中心

	Novel NSAIDs ophthalmic formulation: Flurbiprofen axetil emulsion with low irritancy and improved anti-inflammation effect
	Shen, Jinqiu 1,2; Gan, Li 1; Zhu, Chunliu1 ; Zhang, Xinxin1 ; Dong, Yang 1; Jiang, Min 1,2; Zhu, Jiabi 2; Gan, Yong1
刊名	INTERNATIONAL JOURNAL OF PHARMACEUTICS
	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.
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关键词	OCULAR DELIVERY ; LIPID EMULSION ; PLGA NANOSPHERES ; DRUG ; STABILITY ; SYSTEM ; CHLORAMPHENICOL ; MICROEMULSIONS ; TOLERANCE ; UVEITIS
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000292802700015
内容类型	期刊论文
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.