十一酸睾酮自微乳制剂的大鼠体内药代动力学研究

目的制备十一酸睾酮自微乳化制剂,并对其大鼠体内药代动力学进行研究。方法采用血清睾酮放免法测定给药后大鼠体内血清睾酮水平的变化,并计算药代动力学参数。结果十一酸睾酮原料药混悬液基本没吸收,而自微乳制剂和市售Andriol药物的吸收大大提高。以Andriol为参比制剂,自微乳制剂的相对生物利用度为96.4%。结论自微乳化给药系统能提高脂溶性药物十一酸睾酮的吸收。

Study on Rat in Vivo Pharmacokinetics of Testosterone Undecanoate Self-Microemulsion Preparation

Objective To prepare testosterone undecanoate self-microemulsion preparation and to study its pharmacokinetic in rat in vivo. Methods The radioimmunoassay was used to detect the serum testosterone level in rats after oral administration,furthermore,the phar- macokinetic parameters were calculated. Results Testosterone undecanoate raw material suspension was basically not absorbed. But the absorption of self- microemulsion preparation and market Andriol drugs was greatly increased. With Andriol as the reference prepara- tion,the relative bioavailability of self- microemulsion preparation was 96.4%. Conclusion Self-microemulsifying drug delivery system can improve the absorption of liposoluble drug testosterone undecanoate.