那法瑞林长效制剂对大鼠垂体功能影响

曹倩;周美华;王方敏;陆锦芳;

中国药学杂志 ›› 1997, Vol. 32 ›› Issue (06) : 340-342.

中国药学杂志 ›› 1997, Vol. 32 ›› Issue (06) : 340-342.
药理

那法瑞林长效制剂对大鼠垂体功能影响

  • 曹倩;周美华;王方敏;陆锦芳;
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Effect of depot formulation of nafarelin on pituitary function in rats

  • Cao Qian
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摘要

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

Key words

nafarelin / depot formulation / RICT assay

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导出引用
曹倩;周美华;王方敏;陆锦芳;. 那法瑞林长效制剂对大鼠垂体功能影响[J]. 中国药学杂志, 1997, 32(06): 340-342
Co Qin . Effect of depot formulation of nafarelin on pituitary function in rats[J]. Chinese Pharmaceutical Journal, 1997, 32(06): 340-342

参考文献

1 Chrisp P, Goa KL. Nafarelin: a revive of its pharm-acodynamic and pharmacokinetic properties, and clinical potential in sex hormonerelated conditions. Drugs, 1990.39(4):523. 2 Sanders LM, Kell BA, Mcrae GI, et al .Prolonged contr-olled-release of nafarelin, a luteinizing hormone-releasing hormone analogue, from biodegradable polymeric implants: influence of composition and molecular weight of polymer. J Pharm Sci,1986,75(4):356. 3 Moyle WR, Ramachandran J. Effect of LH on steroidogene-sis and cyclic AMP accumulation in rat leydig cell preparations and mouse tumor leydig cell. Endocrinology,1973,93(1):127. 4 Dufau ML, Pock R, Neubauer A, et al. In vitro bioassay of LH in human serum: the rat interstitial cell testosterone (RICT) assay. J Clin Endocrinol Metab, 1976,42(5):958. 5 Furr BLA, Hutchinson FG. A biodegradable delivery system for peptides: preclinical experience with the gonadotropin-releasing hormone agonist Zoladex. J Controlled Release,1992, 211:117.6 Matikainen T, Ding Y, Vergara M, et al .Differing responses of plasma bioactive and immunoreactive follicle-stimulation hormone and luteinizing hormone to gonadotropin-releasing hormone antagonist and agonisttreatments in postmenopausal women. J Clin Endocrinol Metab, 1992, 75(3):820. 7 Broekmans F1, Bernardus RE, Broeders A, et al. Pituitary responsiveness after administration of a GnRH agonist depot formulation: Decapeptyl CR. Clin Endocrinol,1993,38(6):579.

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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