Institute of Drug Research, Academy of Sciences of the GDR, Alfred-Kowalke-Strasse 4, DDR-1136, Berlin, GDR.
Pharm Res. 1985 Sep;2(5):198-202. doi: 10.1023/A:1016352509025.
Prolonged release of the peptide gonadotropin-releasing hormone (GnRH) from its aqueous solution was achieved by addition of the polymer dextran (Mw ∼ 500,000). This effect observed in an in vitro system was caused by a decrease of the diffusion coefficient of the peptide. When GnRH was intramuscularly injected into male rats, the addition of dextran to the injected peptide solution led to a prolongation of the GnRH plasma level at the expense of its peak value. This change can be explained by a decrease of the absorption rate of GnRH into blood, which parallels the in vitro observation. As a result, the gonadotropin response to GnRH was stronly increased.
通过添加聚合物葡聚糖(Mw∼500000),可实现从水性溶液中延长肽促性腺激素释放激素(GnRH)的释放。在体外系统中观察到的这种效果是由于肽的扩散系数降低引起的。当 GnRH 被肌肉内注射到雄性大鼠中时,向注射的肽溶液中添加葡聚糖会导致 GnRH 血浆水平延长,而牺牲其峰值。这种变化可以通过 GnRH 进入血液的吸收速率降低来解释,这与体外观察结果一致。结果,促性腺激素对 GnRH 的反应大大增强。