Journal of Pharmaceutical Sciences p. 1232 - 1236 (1993)
Update date:2022-08-03
Topics:
Hasegawa
Seki
Juni
Saneyoshi
Kawaguchi
Six ester prodrugs of 2',3'-didehydro-3'-deoxythymidine (D4T) were synthesized, and their physicochemical properties were evaluated. Marked differences were observed. All of the prodrugs were chemically stable within the pH range 2-7. Hydrolysis of these esters was observed in all cases for four rat enzyme systems (plasma, liver, duodenum, and kidney), with D4T being regenerated. D4T or the prodrug was administered orally to rats, and the plasma concentrations of D4T and a corresponding prodrug were measured. The half-life of D4T after intravenous administration was 35.9 min. The half- life calculated from the terminal phase and the maximum concentration in plasma following oral administration of D4T were 35.9 min and 48.4 μM, respectively. After oral prodrug administration (with water or olive oil as a solvent), though none of the prodrugs was detected in plasma except for 5'- hemisuccinyl D4T and 5'-hemiglutaryl D4T with olive oil as a solvent, retention time of plasma D4T concentration was extended and the elevated D4T concentration in plasma decreased.
View MoreShanghai Dynamic Industrial Co.,Ltd.
website:http://www.shdynamic.com
Contact:86-021 3392 6680
Address:Room 805 Information Tower, No.1403 Minsheng Road, Pudong New Area, Shanghai 200135, P. R. China
Beijing ZhongDaXinHe Chemical Product Co.,Ltd(expird)
Contact:010-52876516
Address:tongzhoubeiyuan
Daqing E-shine Chemical Co.,LTD
Contact:0086-024-31285112
Address:Hongweiyuan area, Ranghulu district
Yangzhou Zhongbao Pharmaceutical Co.,Ltd
Contact:+86-514-88290838
Address:Jiangsu Baoying county economic develpment zone in baoying avenue91
Wuhan Soleado Technology Co.,Ltd.
Contact:86-2783341481 18971291927
Address:RM2405 Unit 1 Builing 1, Taiyin Tower, Changqing Road,Wuhan China
Doi:10.1039/P29910000439
(1991)Doi:10.1002/mrc.1260290504
(1991)Doi:10.1021/ic50046a014
(1966)Doi:10.1016/j.tetasy.2012.01.010
(2012)Doi:10.1021/tx200337b
(2011)Doi:10.1021/ja210149g
(2011)