Borg N, Götharson E, Benfeldt E, Groth L, Ståhle L
Department of Clinical Pharmacology, Huddinge University Hospital, Sweden.
Acta Derm Venereol. 1999 Jul;79(4):274-7. doi: 10.1080/000155599750010643.
Penciclovir is a drug active against herpes simplex viruses located in the epidermis basal layer. The aim of this study was to compare the suction blister technique and microdialysis as methods to measure the penciclovir concentration in the skin after a single dose (250 mg) of its prodrug, famciclovir. Suction blister fluid, microdialysates and plasma were sampled from 11 healthy volunteers for 5 h after famciclovir administration. Both the suction blister technique and microdialysis showed that penciclovir reaches the skin in concentrations sufficient to inhibit herpes virus replication. The maximum concentration in both suction blister fluid and in microdialysate was observed later than in plasma. The microdialysis concentration was decreased by cooling of the skin surface and by adrenaline-mediated vasoconstriction. The microdialysis recovery of penciclovir was studied with respect to the flow-rate of perfusion medium through the microdialysis probe. Microdialysis and the suction blister technique can be used to study the time-concentration profile of penciclovir in the skin and microdialysis allows a continuous sampling of the drug for a prolonged time after administration.
喷昔洛韦是一种对位于表皮基底层的单纯疱疹病毒有活性的药物。本研究的目的是比较水疱抽吸技术和微透析技术,作为测量单次服用其前体药物泛昔洛韦(250毫克)后皮肤中喷昔洛韦浓度的方法。在泛昔洛韦给药后5小时,从11名健康志愿者身上采集水疱抽吸液、微透析液和血浆。水疱抽吸技术和微透析技术均显示,喷昔洛韦到达皮肤的浓度足以抑制疱疹病毒复制。水疱抽吸液和微透析液中的最大浓度出现时间均晚于血浆。皮肤表面冷却和肾上腺素介导的血管收缩会使微透析浓度降低。针对灌注介质通过微透析探头的流速,研究了喷昔洛韦的微透析回收率。微透析和水疱抽吸技术可用于研究喷昔洛韦在皮肤中的时间-浓度曲线,微透析允许在给药后长时间连续采集药物样本。