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用放射免疫法研究了左旋１８－甲基炔诺酮（ＬＮＧ）微球和ＬＮＧ微晶在大鼠的药代动力学。大鼠单次ｉｍＬＮＧ微晶３５ｍｇ·ｋｇ－１后４．８８ｈ．血药峰值达６７．６６ｎｍｏｌ·Ｌ－１，ＭＲＴ为１０．１６ｄ，Ｔ＜０．３２ｎｍｏｌ·Ｌ－１为４１．５０ｄ；而单次ｉｍＬＮＧ微球２０．４，４１．１和８３．３ｍｇ·ｋｇ－１后，血药分别于６，４．６７和４．３３ｈ达峰浓度１５．１９，３３．６１和３８．５５ｎｍｏｌ·Ｌ－１，ＭＲＴ分别为６９．２３，６５．１２和６３．２５ｄ，Ｔ＜０．３ｎｍｏｌ·Ｌ－１分别为１６７．８１，１６９．７３和１６７．２３ｄ。可见ＬＮＧ微球在大鼠的ＭＲＴ和Ｔ＜０．３２ｎｍｏｌ·Ｌ－１分别约为ＬＮＧ微晶的６．６和４．２倍，提示该微球具有明显的缓释长效作用，且初始血药峰值明显低于肌注ＬＮＧ微晶。
The pharmacokinetics of L-18-norgestrel (LNG) microspheres and LNG microcrystals in rats were studied by radioimmunoassay. After a single rat imLNG crystallite 35mg · kg-1 4.88h. Peak blood levels of 67.66nmol·L-1, MRT of 10.16d, T <0.32nmol·L-1 was 41.50d; and single imLNG microspheres 20.4,41.1 and 83.3mg · kg-1, the peak plasma concentrations reached 15.19, 33.61 and 38.55 nmol·L-1 at 6, 4.67 and 4.33 h, respectively, with MRTs of 69.23, 65.12 and 63, respectively. 25d, T <0.3nmol·L-1 were 167.81,169.73 and 167.23d respectively. It can be seen that the MRT and T <0.32nmol·L-1 of LNG microspheres are about 6.6 and 4.2 times that of LNG microcrystals, respectively, suggesting that the microspheres have obvious sustained release and long-acting effects, and the initial Peak blood pressure was significantly lower than intramuscular LNG microcrystalline.