Acyclovir concentrations in the skin of humans after a single oral dose assessed by in vivo cutaneous microdialysis

Abstract

In selected cases skin concentrations should be determined rather than those in blood plasma when studying the distribution of orally administered drugs. Evaluation of acyclovir concentrations in the skin cannot be replaced by the calculation of the theoretical peripheral compartment.

Physiologically Based Pharmacokinetic Models to Predict Maternal Pharmacokinetics and Fetal Exposure to Emtricitabine and Acyclovir

“…PK simulations in the nonpregnant population were evaluated by comparison with in vivo data obtained from 5 different studies that investigated the PK of emtricitabine in nonpregnant subjects after single and multiple oral administration of 200 mg. [20][21][22] In pregnant women the PK was predicted in different populations, namely in 3 different gestational age groups of nonlaboring pregnant women (23)(24)(25)(26)(27)(28)(29)(30)(31)(32)(33)(34)(35), and 36-42 gestational weeks) and in women in labor between 34 and 39 weeks of gestation. Drug concentrations in the umbilical vein were predicted in the latter group.…”

“…A, The dashed line represents the reported half-maximal inhibitory concentration (IC 50 ), 30 the solid line the predicted median trough level (C min ), and the shaded area the predicted 5th to 95th percentile range. B, The dashed line represents the reported average exposure (AUC) in nonpregnant subjects, 15,[32][33][34][35][36][37] the solid line the predicted AUC, and the shaded area the predicted 5th to 95th percentile range. C, The upper and lower dashed lines represent the reported IC 50 and 90% of maximal inhibitory concentration (IC 90 ), 31 respectively, the solid line the predicted C min , and the shaded area the predicted 5th to 95th percentile range.…”

Evaluation of skin penetration of topically applied drugs in humans by cutaneous microdialysis: acyclovir vs. salicylic acid

“…The samples were prepared as follows: to 100 μ L of microdialysate 50 μ L of aqueous solution of internal standard (metronidazole) and 50 μ L of 0·33 M perchloric acid were added and vortexed. An aliquot of 50 μ L was injected onto the column (17).…”

In vivo Quantification of Acyclovir Exposure in the Dermis Following Iontophoresis of Semisolid Formulations

“…Experiments were conducted in vivo in a rabbit model using microdialysis as the sampling technique. Intradermal microdialysis of ACV has been successfully performed in rabbit9 and human skin,12 and appeared to be the ideal tool to perform such a study since the dermis is as close to the site of Herpes infection as practically possible. A neutral cream formulation and the soluble fraction of the same cream were tested under anodal and cathodal‐current, and two formulations of pH 11 gels (one without and one with stabilizers and preservatives) were tested under cathodal‐current (Tab.…”