Bork K, Kaiser T, Benes P
Department of Dermatology, University of Mainz, Germany.
Arzneimittelforschung. 2000 Jul;50(7):656-8. doi: 10.1055/s-0031-1300267.
Aciclovir (CAS 59277-89-3) is frequently used in herpes simplex virus diseases, but administration to lactating women occurs only rarely. Therefore, information about the pharmacokinetics of aciclovir in human breast milk is limited. The concentration in breast milk is 2 to 3 fold increased compared to plasma. The reason for this increase is unknown until now. An active transport mechanism has been assumed. The aim of this study was to prove whether the higher concentration of aciclovir in human breast milk is due to only a passive transfer. Two chambers separated by a semipermeable membrane were used. The first chamber contained plasma with aciclovir, the second chamber breast milk without aciclovir. The increase in aciclovir concentration in the second chamber was determined. The concentration of aciclovir in breast milk exceeded that of plasma after 2 h and reached a higher concentration. Thus, the higher aciclovir concentration in human breast milk is due to passive diffusion. No active transport mechanism is needed.
阿昔洛韦(CAS 59277-89-3)常用于治疗单纯疱疹病毒疾病,但很少用于哺乳期妇女。因此,关于阿昔洛韦在人母乳中的药代动力学信息有限。母乳中的浓度比血浆中高2至3倍。到目前为止,这种增加的原因尚不清楚。人们推测存在一种主动转运机制。本研究的目的是证明人母乳中阿昔洛韦浓度较高是否仅由于被动转运。使用了由半透膜隔开的两个腔室。第一个腔室含有含阿昔洛韦的血浆,第二个腔室含有不含阿昔洛韦的母乳。测定了第二个腔室中阿昔洛韦浓度的增加。2小时后,母乳中阿昔洛韦的浓度超过了血浆中的浓度,并达到了更高的浓度。因此,人母乳中较高的阿昔洛韦浓度是由于被动扩散。不需要主动转运机制。