目的:观察国产那法瑞林(nafarelin )长效制剂的长效作用及对大鼠垂体功能影响,并探讨其作用部位。方法:采用大鼠间质细胞睾酮 (RICT)法检测血清LH(luteinizing hormone)生物活性水平。结果:那法瑞林长效制剂在体内的持续释药时间为((40.0±6.8)d。单次理植3周后大鼠血LH的周期性分泌高峰及激发高峰均消失。预先理植长效制剂组大鼠血LH在切除双侧卵巢后变化不明显。结论:那法瑞林长效制剂确有长效作用,其通过作用于垂体而抑制大鼠垂体功能。
Abstract
OBJECTIVE: To observe the duration and mechanism of action and effect of nafarelin(Naf ) depot formulation on pituitary function in the rat. METHODS: A modified RICT(the rat interstitial cell testosterone) assay was used to determine serum bioactive LH levels of rats. RESULTS: The duration of action of Naf depot formulation in vivo was (40.0±6.8) d. The peak concentrations of serum LH levels in the estrous cycle and in the responses to an acute LHRH agonist challenge were suppressed significantly in the Naf depot formulation-treated rats. No changes in serum LH levels before and after ovariectomy were observed in the rat previously treated with Naf depot formulation 2 weeks before ovariectomy. CONCLUSION: The long action of domestic Naf depot formulation is certain. The pituitary function of rats was suppressed directly and significantly 3 weeks after treatment with a single administration of Naf depot formulation.
关键词
那法瑞林 /
长效制剂 /
RICT法
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Key words
nafarelin /
depot formulation /
RICT assay
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参考文献
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脚注
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基金
高等学校博士科点专项科研基金资助项目第211102号
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