Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture： in vitro evaluation and in vivo bioavailability test

• Published in: Acta pharmacologica Sinica Vol. 32; no. 10; pp. 1294 - 1302
• Main Authors: Wang, Yan-ping, Gan, Yong, Zhang, Xin-xin
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 01.10.2011; Nature Publishing Group
• Subjects: Animals; Beagle犬; Biological Availability; Biomedical and Life Sciences; Biomedicine; Caprylates - chemistry; Delayed-Action Preparations - chemistry; Dogs; Emulsions - chemistry; Female; Gastrointestinal Tract - metabolism; Glycerides - chemistry; Immunology; Immunosuppressive Agents - administration & dosage; Immunosuppressive Agents - pharmacokinetics; Internal Medicine; Male; Medical Microbiology; Original; original-article; Pharmacology/Toxicology; Polyethylene Glycols - chemistry; Rabbits; Tablets; Tacrolimus - administration & dosage; Tacrolimus - pharmacokinetics; Vaccine; 中小企业; 体外溶出度; 微乳化; 混合物; 生物利用度; 缓释片; 聚乙烯吡咯烷酮; gastroretentive sustained-release tablet; bioavailability; self-microemulsifying lipid mixture; immunosuppressants; tacrolimus

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 o...