中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Ion-sensitive nanoemulsion-in situ gel system for ophthalmic delivery of flurbiprofen axetil

文献类型:期刊论文

作者SHEN Jin-qiu1; GAN Yong2; GAN Li2; ZHU Chun-liu2; ZHU Jia-bi1
刊名Acta Pharmaceutica Sinica
出版日期2010
卷号45期号:1页码:120-125
关键词flurbiprofen axetil nanoemulsion ion-sensitive in situ gel cornea retention aqueous humor pharmacokinetics
ISSN号0513-4870
其他题名氟比洛芬酯眼用纳米乳-离子敏感型原位凝胶的研究
文献子类Article
英文摘要The aim of the study is to prepare flurbiprofen axetil nanoemulsion-in situ gel system(FBA/NE-ISG) and observe its ocular pharmacokinetics,rheological behavior,TEM images,irritation and cornea retention Production of nanoemulsion was based on high-speed shear and homogenization process,and then mixed with gellan gum to prepare FBA/NE-ISG.Rheological study showed that FBA/NE-ISG possesses strong gelation capacity and its viscosity and elastic modulus increases by 2 Pa·s and 5 Pa respectively when mixed with artificial tear at the ratio of 40:7.TEM images suggested no significant changes in particle morphology of the pre and post gelation. Good ocular compatibility of FBA,NE-ISG was testified by the irritation test based on histological examination. In vivo fuorescence imaging system was applied to investigate the characteristics of cornea retention,and the results indicated that the nanoemulsion-in situ gel(NE-ISG)prolonged the cornea retention time significantly since K_(NE-ISG)(0.008 5 min~(-1))was much lower compared with flurbiprofen sodium eye drops(FB-Na,0.03%w/v)of which the K_(Eye drops) was 0.1 05 2 min~(-1),indicated that the cornea retention time of NE-ISG was prolonged significantly.Pharmacokinetics of FBA/NE-ISG in rabbit aqueous humor was studied by cornea puncture,the MRT(12.3 h)and AUC_(0h12 h)(126.8 mug·min·mL~(-1))of FBA/NE-ISG was 2.7 and 2.9 times higher than that of the flrubiprofen sodium eye drops respectively,which meant that the ocular bioavailability was improved greatly by the novel preparation.Therefore,FBA/NE-ISG can enhance the ocular bioavailability by prolonging drug corneal retention significantly.What's more,encapsulated by emulsion droplets prodrug flurbiprofen(FBA)instead of flurbiprofen(FB)can reduce the ocular irritation.
WOS研究方向Pharmacology & Pharmacy (provided by Clarivate Analytics)
语种中文
CSCD记录号CSCD:3805489
源URL[http://119.78.100.183/handle/2S10ELR8/267962]  
专题药物制剂研究中心
作者单位1.China Pharmaceutical University, Nanjing, Jiangsu 210009, China.;
2.Shanghai Institute of Materia Medica,Chinese Academy o fSciences, Shanghai 201203, China.
推荐引用方式
GB/T 7714
SHEN Jin-qiu,GAN Yong,GAN Li,et al. Ion-sensitive nanoemulsion-in situ gel system for ophthalmic delivery of flurbiprofen axetil[J]. Acta Pharmaceutica Sinica,2010,45(1):120-125.
APA SHEN Jin-qiu,GAN Yong,GAN Li,ZHU Chun-liu,&ZHU Jia-bi.(2010).Ion-sensitive nanoemulsion-in situ gel system for ophthalmic delivery of flurbiprofen axetil.Acta Pharmaceutica Sinica,45(1),120-125.
MLA SHEN Jin-qiu,et al."Ion-sensitive nanoemulsion-in situ gel system for ophthalmic delivery of flurbiprofen axetil".Acta Pharmaceutica Sinica 45.1(2010):120-125.

入库方式: OAI收割

来源:上海药物研究所

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