Comparison of in vivo and in vitro Permeation Behaviors of the Ethosome Gels of Testosterone and Its Es-ters
10.6039/j.issn.1001-0408.2015.22.15
- VernacularTitle:睾酮及其酯类醇质体凝胶剂的体内外渗透行为比较
- Author:
Shu MENG
;
Yang LI
;
Cong ZHANG
;
Jing QU
;
Wei ZHANG
;
Ying JIN
;
Jing GUO
;
Miao LI
- Publication Type:Journal Article
- Keywords:
Testosterone;
Testosterone propionate;
Testosterone undecanoate;
Ethosome gel;
Pharmacokenetics;
in vitro perme-ation
- From:
China Pharmacy
2015;(22):3072-3074
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE:To compare in vivo and in vitro permeation behaviors of the ethosome gels of testosterone,testoster-one propionate and testosterone undecanoate. METHODS:The ethosome gels of testosterone,testosterone propionate and testoster-one undecanoate were prepared. With cumulative permeating amount and permeation rate as the indexes,Franz diffusion cell and HPLC were employed to compare in vitro permeation behaviors of 3 kinds of ethosome gels in mouse skin. With testosterone patch as the positive control drug, electrochemistry method was adopted to detect the concentration of testosterone in plasma 0,3,6, 9,12,24,36 and 48 h after applying such 3 kinds of ethosome gels on the back of rats,and then pharmacokinetic parameters were calculated with DAS 2.0 software. RESULTS:24 h cumulative permeating amounts of the ethosome gels of testosterone,tes-tosterone propionate and testosterone undecanoate were(234.31±13.8),(175.63±41.1)and(72.60±15.3)μg/cm2,and the per-meation rates were(10.25±1.9),(7.64±1.4)and(2.96±0.8)μg/(cm2·h),respectively. The pharmacokinetic parameters of the above-mentioned three kinds of ethosome gels and the positive control drug were respectively as follows as cmax of(20.19±2.57), (17.50±2.91),(0.23±0.04),(14.97±2.12)ng/ml,t1/2Ka of(2.80±0.45),(3.36±0.59),(4.02±0.62),(4.20±0.71)h,AUC0-48 h of(13.85±1.96),(13.93±2.13),(0.35±0.07),(11.76±2.31)ng·h/ml. CONCLUSIONS:in vivo and in vitro permeation behav-iors of the ethosome gels of testosterone and testosterone propionate are fairly good.
