当前位置： SCI文献检索 > CURRENT MEDICAL RESEARCH AND OPINION期刊下所有文献 > Stratum corneum pharmacokinetics of the anti-fungal drug, terbinafine, in a novel topical formulation, for single-dose application in dermatophytoses.

Stratum corneum pharmacokinetics of the anti-fungal drug, terbinafine, in a novel topical formulation, for single-dose application in dermatophytoses.

Abstract：

OBJECTIVE:The stratum corneum (SC) pharmacokinetics of terbinafine following single-dose administration of a novel cutaneous solution (film-forming solution, FFS) containing terbinafine hydrochloride and a film-forming agent, was investigated in three studies. Terbinafine 1% cream (Lamisil) was included as a benchmark in two of these studies. RESEARCH DESIGN AND METHODS:Drugs were applied to areas of the back, and skin strips were taken from defined areas at baseline and from 1 to 312 h after application. Samples were analysed using validated liquid chromatography/mass spectrometry. RESULTS:The residence time of the film on the skin was up to 72 h after application (up to 12 h for the 1% cream). After application of terbinafine FFS, 30% of the total amount of drug delivered into the SC occurred during the first 2 h, 31% from 2-12 h, and 39% thereafter. The C(max) was observed as early as 1.5 h (t(max)). SC levels were still detected after 13 days (24 ng/cm(2)) (t(1/2)) was 162 h). Terbinafine 1% cream showed a similar t(max) (2 h) with a lower C(max) than terbinafine 1% FFS, and mean SC levels after 7 days of treatment were 46 ng/cm(2) (day 13). The t(1/2) was 68 h. Washing at 30 min removed 86% of the film still present on the surface; the decrease of terbinafine concentration in the SC was 84%. A later washing at 12 h removed 73% of the film in comparison to non-washed skin and induced a decrease in the terbinafine content in the SC of 27%. CONCLUSIONS:The SC pharmacokinetic profile of terbinafine 1% FFS indicates that this novel formulation is efficient in delivering high amounts of terbinafine to the skin for a prolonged time and supports its use in the treatment of dermatophytoses with a single application.

journal_name

Curr Med Res Opin

journal_title

Current medical research and opinion

authors

Kienzler JL,Queille-Roussel C,Mugglestone C,Ortonne JP,Larnier C

doi

10.1185/030079907X199664

subject

Has Abstract

pub_date

2007-06-01 00:00:00

pages

1293-302

issue

eissn

0300-7995

issn

1473-4877

journal_volume

pub_type

杂志文章,meta分析

在线工具

Stratum corneum pharmacokinetics of the anti-fungal drug, terbinafine, in a novel topical formulation, for single-dose application in dermatophytoses.