摘要
目的:对十一酸睾酮(TU)二元醇质体凝胶进行体内外透皮考察。方法:采用注入法制备TU二元醇质体,以卡波姆941为凝胶基质,制备TU二元醇质体凝胶剂;以小鼠皮肤为屏障,采用Franz扩散池法对其体外透皮特性进行考察;以大鼠为实验动物,背部给予TU二元醇质体凝胶剂后,于设定的时间点测定血浆中TU浓度,计算药动学参数,并与TU二元醇质体进行比较。结果:TU二元醇质体及其凝胶的体外累积透皮百分率Q与时间t均符合一级动力学模型,线性方程分别为:Q=8.68t+6.78(r=0.998 2)和Q=6.09 t+3.09(r=0.999 3),稳态透皮速率分别为8.68μg·cm^(-2)·h^(-1)和6.09μg·cm^(-2)·h^(-1),24 h后TU在皮肤中的滞留量分别为(208.80±55.26)μg·g^(-1)和(225.60±38.90)μg·g^(-1);大鼠体内TU二元醇质体及其凝胶的主要药动学参数分别为:Cmax(18.50±2.75)mg·L^(-1)和(20.80±2.42)mg·L^(-1);tmax(6.20±0.14)h和(9.54±0.52)h;AUC0-48h(336.74±2.05)h和(486.30±1.68)h。结论:TU二元醇质体及其凝胶均呈现较好的体内外透皮特性,且在缓释性上凝胶剂表现更优。
Objective： To study the in vitro and in vivo transdermal penetration of testosterone undecanoate （TU） binary ethosomes gel. Methods： TU binary ethosomes were prepared by an ethanol injection method, and using carbopol 941 as the gel base, TU binary ethosomes get was prepared. Using mouse skin as the barrier, Franz cells were applied to explore the in vitro transdermal penetration of TU binary ethosomes and the gel. Rats were used as the animals, and TU binary ethosomes and the gel was respectively administrated on the back skin. At the predetermined time points, plasma samples were withdrawn to detect the concentration of TU, and the main pharmacokinetics parameters were calculated. Results： The in vitro transdermal penetration of TU binary ethosomes and the gel was both fitted first-order equation ： Q = 8.68t ＋ 6.78 （ r = 0.998 2） and Q = 6.09t ＋ 3.09 （ r = 0.999 3 ）, and the stable penetration rate was 8.68 μg · cm-2 ·h-1 and 6.09μg cm-2· h-1 , respectively. After the 24-hour penetration, the residual amount in skin of TU binary ethosomes and the gel was （208.80 ±55.26） μg · g-1 and （225.60 ±38.90） μg ·g-1, respectively. The main pharmacokinet- ics parameters of TU binary ethosomes and the gel were Cm,x of（ 18. 50 ± 2. 75 ） mg · L - 1 and （ 20.80 ± 2.42 ） mg · L - l, tmax of（ 6. 20 ± 0. 14 ） h and （ 9.54 ±0.52 ） h, and A UC0-48h of（ 336.74 ± 2.05 ） h and （ 486.30± 1.68 ） h. Conclusion： TU binary ethosomes and the gel both exhibit promising in vitro transdermal penetration, and the gel shows better sustained release property.
出处
《中国药师》
CAS
2016年第10期1840-1842,共3页
China Pharmacist
关键词
十一酸睾酮
二元醇质体
凝胶剂
体外透皮
体内透皮
Testosterone undecanoate
Binary ethosomes
Gel
In vitro transdermal penetration
In vivo transdermal penetration
