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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 investigate the transdermal in vitro and in vivo effects of dihydrogenated testosterone undecanoate (TU) gel. Methods: The TU dihydric alcohol was prepared by injection method and carbopol 941 was used as gel matrix to prepare TU dihydric alcohol gel. The mouse skin was used as the barrier and the Franz diffusion cell method After the TU dihydric alcohol gel was administered to the back of the rats, the concentration of TU in the plasma was measured at the set time points, and the pharmacokinetic parameters were calculated and compared with the TU diols Body to compare. Results: The cumulative transdermal percentage Q and time t of TU diol and its gel were in accordance with the first-order kinetic model. The linear equations were: Q = 8.68t + 6.78 (r = 0.998 2) and Q = 6.09 t + 3.09 (r = 0.999 3). The steady-state transdermal rates were 8.68 μg · cm -2 · h -1 and 6.09 μg · cm -2 · h -1 ), The retention of TU in skin after 24 h were (208.80 ± 55.26) μg · g -1 and (225.60 ± 38.90) μg · g -1, respectively. TU diol The main pharmacokinetic parameters of body and gel were as follows: Cmax (18.50 ± 2.75) mg · L -1 and (20.80 ± 2.42) mg · L -1; tmax (6.20 ± 0.14) h And (9.54 ± 0.52) h respectively; AUC0-48h (336.74 ± 2.05) h and (486.30 ± 1.68) h. CONCLUSION: Both TU dihydric alcohol and its gel show good in vivo and in vitro transdermal properties and exhibit better performance in sustained release.