Fang S M, Lin C S, Lyon V
J Pharm Sci. 1977 Dec;66(12):1744-8. doi: 10.1002/jps.2600661223.
Tritium-labeled progesterone was administered to mature female rats in the proestrous stage by three different routes, gastric intubation, subcutaneous injection, and uterine intraluminal instillation, to study the kinetics involved in the uptake and retention of radioactivity by the uterus and various other tissues. Progesterone was retained at a much higher level and for a more prolonged period in the rat uterus after uterine intraluminal instillation. Progesterone bioavailability to the uterus was 45 times higher by uterine intraluminal instillation than by either gastric intubation or subcutaneous injection. Progesterone absorption by the rat endometrium was extremely fast. The observed biphasic decrease of radioactivity from the uterine tissue was explained adequately by a pharmacokinetic model in which progesterone is assumed to be present in two compartments within the uterine tissue. The pharmacokinetic parameters showed that the progesterone biological half-life in the uterine tissue during the alpha-phase was about 6.5 min while that in the beta-phase was about 230 min.
给处于动情前期的成熟雌性大鼠通过三种不同途径给予氚标记的孕酮，即胃内插管、皮下注射和子宫腔内灌注，以研究子宫和其他各种组织摄取和保留放射性所涉及的动力学。子宫腔内灌注后，孕酮在大鼠子宫内的保留水平要高得多，且持续时间更长。子宫腔内灌注时孕酮对子宫的生物利用度比胃内插管或皮下注射高45倍。大鼠子宫内膜对孕酮的吸收极快。通过一个药代动力学模型可以充分解释观察到的子宫组织放射性的双相下降，该模型假定子宫组织内的孕酮存在于两个隔室中。药代动力学参数表明，在α相期间，子宫组织中孕酮的生物半衰期约为6.5分钟，而在β相期间约为230分钟。
