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醋酸甲地孕酮(MA)能与人、动物(兔、犬、大鼠、豚鼠)血浆蛋白结合。与人血浆蛋白结合率为86.39±2.28％,其外观结合常数为6.38±0.52×10~4L/mol,与动物(除与豚鼠结合率较低外)的血浆蛋白结合率与人的相比无显著差异。MA、睾丸酮、可的松对~3H-MA与血浆蛋白的结合均无显著影响;MA并不显著改变~3H-孕酮与妊娠豚鼠血浆蛋白的结合率及~3H-睾丸酮与性激素结合球蛋白(SHBG)的结合率;~3H-MA不与孕妇血清SHBG结合,提示MA在血浆中无专一结合,MA是与血浆蛋白中的白蛋白结合。
Megestrol acetate (MA) can bind to human, animal (rabbit, dog, rat, guinea pig) plasma proteins. The binding rate to human plasma protein was 86.39 ± 2.28%, and its apparent binding constant was 6.38 ± 0.52 × 10 ~ 4 L / mol. The binding rate of plasma protein to that of animals (except for the lower binding rate to guinea pigs) Significant differences. MA, testosterone, cortisone had no significant effect on the binding of ~ 3H-MA to plasma proteins; MA did not significantly change the binding rate of ~ 3H-progesterone to plasma protein of pregnant guinea pigs and the binding of ~ 3H-testosterone to sex hormone binding globulin (SHBG); ~ 3H-MA does not bind to serum SHBG in pregnant women, suggesting that there is no specific binding of MA in plasma. MA is bound to albumin in plasma proteins.