Casey B M, Bawdon R E
Department of Obstetrics and Gynecology, University of Texas Southwestern Medical Center, Dallas 75235-9032, USA.
Am J Obstet Gynecol. 1998 Sep;179(3 Pt 1):758-61. doi: 10.1016/s0002-9378(98)70078-x.
The object was to determine the placental transfer of ritonavir alone and in combination with zidovudine.
Twelve placental perfusion studies were performed at trough (1-2 microg/mL) and peak (approximately 20 microg/mL) combinations of ritonavir and zidovudine. Accumulation of ritonavir was determined.
Transfer of ritonavir at trough concentrations was undetectable (<0.025 microg/mL). The clearance index of ritonavir at peak concentration was 0.085 +/- 0.05 and was unaffected by zidovudine. The fetal concentration of ritonavir was 0.0758 +/- 0.22 microg/mL at a maternal concentration of approximately 20 microg/mL and 25.5 +/- 6.9 microg/mL at a concentration of 100 microg/mL. There was no tissue accumulation of ritonavir either alone or with zidovudine.
The clearance index of ritonavir at therapeutic levels was extremely low, with little accumulation in the fetal compartment and no accumulation in placental tissue. Zidovudine does not significantly affect the transfer or accumulation of ritonavir.
本研究旨在确定单独使用利托那韦以及利托那韦与齐多夫定联合使用时的胎盘转运情况。
在利托那韦与齐多夫定的谷浓度（1 - 2微克/毫升）和峰浓度（约20微克/毫升）组合下进行了12项胎盘灌注研究。测定了利托那韦的蓄积情况。
谷浓度下利托那韦的转运无法检测到（<0.025微克/毫升）。峰浓度下利托那韦的清除指数为0.085±0.05，且不受齐多夫定影响。母体浓度约为20微克/毫升时，胎儿体内利托那韦浓度为0.0758±0.22微克/毫升；母体浓度为100微克/毫升时，胎儿体内利托那韦浓度为25.5±6.9微克/毫升。单独使用或与齐多夫定联合使用时，利托那韦均无组织蓄积。
治疗水平下利托那韦的清除指数极低，在胎儿组织中蓄积极少，在胎盘组织中无蓄积。齐多夫定对利托那韦的转运或蓄积无显著影响。
