Endocrinological studies on TAP-144-SR, a sustained-release formulation of a potent GnRH agonist (D-Leu6-[des-Gly10-NH2]-GnRH ethylamide), in male rats.
Endocrinological studies on TAP-144-SR, a sustained-release formulation of a potent GnRH agonist (D-Leu6-[des-Gly10-NH2]-GnRH ethylamide), in male rats.
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TAP-144-SR 是一种强效 GnRH 激动剂（D-Leu6-[des-Gly10-NH2]-GnRH 乙酰胺）的缓释制剂，在雄性大鼠中进行的内分泌学研究。
DOI：
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发表时间：
1990
期刊：
影响因子：
--
通讯作者：
T. Fujita
中科院分区：
文献类型：
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作者：
K. Sudo;T. Masaki;K. Shiota;M. Kawase;T. Fujita
通过比较TAP-144-SR与TAP-144溶液的效力，在雄性大鼠中评价了TAP-144-SR（一种强效GnRH激动剂（TAP-144，醋酸亮丙瑞林）的生物可降解缓释制剂）的矛盾效应。通过将激动剂包封在共聚（DL-乳酸/乙醇酸）微胶囊中制备的TAP-144-SR（相当于0.1 mg/kg/天TAP-144）单次皮下注射可抑制雄激素的血清水平，并且该水平保持抑制4周。在治疗后4周，通过将TAP-144-SR与每日给药TAP-144溶液（持续4周）的效力进行比较，评价TAP-144-SR的矛盾效应效力。在4周试验中，每日注射TAP-144溶液和单次注射TAP-144-SR（相当于0.02、0.2或2 mg/kg/天TAP-144）均以剂量依赖性方式降低雄性大鼠睾丸、前列腺和精囊的重量。TAP-144-SR在减轻这些器官重量方面比TAP-144溶液更有效。TAP-144-SR给药大鼠的血清和垂体LH和FSH浓度以及血清睾酮水平也低于TAP-144溶液给药大鼠。这些结果表明，TAP-144-SR治疗后的矛盾效应更广泛，表明维持恒定的血清TAP-144水平导致垂体和睾丸更广泛的脱敏。这些结果还表明TAP-144-SR作为抗前列腺肿瘤剂在功效和方便性方面优于TAP-144溶液。
The paradoxical effects of TAP-144-SR, a biodegradable sustained-release formulation of a potent GnRH agonist (TAP-144, leuprolide acetate) were evaluated in male rats by comparing its potency with that of TAP-144 solution. A single sc injection of TAP-144-SR (equivalent to 0.1 mg/kg/day as TAP-144), prepared by encapsulating the agonist in microcapsules of copoly (DL-lactic/glycolic acid), suppressed serum levels of androgens, and the levels remained suppressed for 4 weeks. The potency of the paradoxical effects of TAP-144-SR was evaluated 4 weeks after treatment by comparing it with that of TAP-144 solution administered daily for 4 weeks. Both daily injections of TAP-144 solution and a single injection of TAP-144-SR (equivalent to 0.02, 0.2 or 2 mg/kg/day as TAP-144) decreased the weight of the testes, prostates and seminal vesicles in a dose-dependent manner in a 4-week assay in male rats. TAP-144-SR was more effective than TAP-144 solution in reducing these organ weights. Serum and pituitary concentrations of LH and FSH and serum testosterone levels were also lower in TAP-144-SR-treated than in TAP-144 solution-treated rats. These results indicate that the paradoxical effects were more extensive upon TAP-144-SR treatment, suggesting that maintaining constant serum TAP-144 levels results in more extensive desensitization of the pituitary and testes. These results also suggest advantages of TAP-144-SR over TAP-144 solution in both efficacy and convenience as an anti-prostatic tumor agent.
促性腺激素释放激素和促性腺激素释放激素类似物的临床应用。
影响因子：
6.7
作者：
Yen,SS
通讯作者：
Yen,SS