Transporter-targeted cholic acid-cytarabine conjugates for improved oral absorption

摘要：

　　This study intended to develop transporter-targeted cholic acid-cytarabine conjugates for enhanced drug oral bioavailability.Four conjugates of cytarabine with cholic acids were synthesized and characterized.The in vitro and in vivo metabolic stabilities of these conjugates were studied in rat plasma and liver homogenates.Among these conjugates, N4-ursodeoxycholic acid of cytarabine (compound 5) showed the optimal metabolic stabilities.The oral pharmacokinetic study indicated compound 5 exhibited a 2-fold enhanced oral bioavailability of cytarabine,demonstrating the feasibility of prodrug strategy based on the transporter targeting in enterocytes for improved oral drug delivery.

作者: Dong Zhang Dongpo Li Zhonggui He Jin Sun

作者单位: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China;State Key Lab of New-

会议类型: 国际会议

会议名称: The 4th Asian Symposium on Pharmaceutical Science and Technology & Enlarged Editorial Board Conference of the Asian Journal of Pharmaceutical Sciences (第四届亚洲药剂学论坛暨亚洲药物制剂科学杂志编委会扩大会议)

会议地点: 沈阳

会议语种:英文

页码: 271-272

在线出版日期: 2016-04-28（万方平台首次上网日期，不代表论文的发表时间）