丙酸睾酮埋植剂体内释放模型的建立

发布时间：2018-06-24 07:38

本文选题：丙酸睾酮 + 埋植剂　；参考：《科学技术与工程》2017年09期

【摘要】：探讨丙酸睾酮(丙睾)埋植剂在大鼠体内的药物释放过程,建立释放模型。将丙睾埋植剂分别包装成2支和4支组,随后将70只雄性Wistar大白鼠按体重随机分为两组,在两组大鼠背部皮下分别植入2支和4支丙睾埋植剂。在丙睾埋植剂植入大白鼠体内前0 d及植入后的1 d、3 d、7 d、14 d、30 d、60 d、90 d、180 d,采用断尾方式采集2支组大鼠血样1 mL,用睾酮放射免疫试剂盒检测血清中睾酮含量。在埋植后的14 d、30 d、60 d、90 d、180 d将动物体内的丙睾埋植剂取出,通过重量的差值计算药物在体内的释放量。结果丙睾埋植剂在体内的累积释放量随着埋植时间的延长呈逐渐上升趋势。至180 d时,两组埋植剂内药物几乎全部释放出来。而体内血清中睾酮浓度变化趋势正好与体内释放量变化趋势相反,随着埋植天数的增加,睾酮浓度逐渐下降。经过释放模型验证,丙酸睾酮埋植剂体内释放遵循一级释放方程。埋植剂中的丙睾可以通过硅胶囊管壁渗透出来,被吸收入血后,可使血清中睾酮浓度维持几个月之久,可以认为本埋植剂是一种能长期缓慢释放丙睾药物的控释给药系统。
[Abstract]:To investigate the drug release process of testosterone propionate (testosterone propionate) implant in rats and establish a release model. 70 male Wistar rats were randomly divided into two groups according to their body weight. Two and four clondymal implants were implanted subcutaneously on the back of the two groups. The blood samples of the two groups were collected for 180 days at the first 0 days before implantation and 1 day 3 days after implantation. The serum testosterone levels were detected by testosterone radioimmunoassay kit. The rats were divided into two groups: 1 mL of blood samples were collected by tail-amputated method and 30 days, 30 days, 60 days, 90 days and 90 days, 180 days after implantation, and the serum testosterone levels were detected by testosterone radioimmunoassay kit. After 14 days, 30 days, 60 days, 90 days, 180 days after implantation, the implant agent was taken out, and the amount of drug released in vivo was calculated by the difference of weight. Results the accumulative release amount of the implants increased gradually with the prolongation of implantation time. At 180 days, almost all of the drugs in the two groups were released. However, the change trend of serum testosterone concentration was opposite to that of body release amount, and the testosterone concentration decreased gradually with the increase of embedding days. The release of testosterone propionate in vivo followed the first-order release equation. After being absorbed into blood, the concentration of testosterone in serum can be maintained for several months. It can be considered that this implant is a controlled release drug delivery system which can slowly release propididymal drugs for a long time.
【作者单位】：辽宁省计划生育科学研究院;国家卫生计生委生殖健康与遗传医学重点实验室;
【基金】：辽宁省自然科学基金(2013020170)资助
【分类号】：R965;R-332

【参考文献】