Mizuno N, Morita E, Nishikata M, Shinkuma D, Yamanaka Y
Arch Int Pharmacodyn Ther. 1986 Sep;283(1):30-8.
A two-compartment model could be used to describe the elimination of sulpiride from plasma after intravenous administration of 25 and 50 mg/kg doses to rat. The absolute bioavailability after oral administration was only about 15% which was also the level after intraduodenal administration. Higher bioavailabilities were found after mesenteric venous and intravenous administration (sham-operated rat) due to a decrease in the beta-value (elimination rate constant). The low bioavailability of sulpiride following oral administration was concluded to result, not from metabolism in the liver, but from reduced absorption by the gastrointestinal tract.
两室模型可用于描述大鼠静脉注射25和50mg/kg剂量舒必利后其从血浆中的消除情况。口服给药后的绝对生物利用度仅约为15%,十二指肠内给药后也是这个水平。由于β值(消除速率常数)降低,肠系膜静脉给药和静脉给药(假手术大鼠)后生物利用度更高。口服舒必利后生物利用度低的原因不是肝脏代谢,而是胃肠道吸收减少。