Schmidt A, von Engelhardt W
Arzneimittelforschung. 1982;32(2):106-10.
Segments of the intestine of anaesthetized guinea-pigs and the colon of conscious sheep were perfused with saline containing 0.1--25 mg/l 1,4:3,6-dianhydrosorbitol-2,5-dinitrate (isosorbide dinitrate, ISDN). The increase in ISDN uptake was linearly related to its concentration. Absorption was rapid. In the jejunum and the ileum of guinea-pig, 7% of perfused ISDN was absorbed per 10 cm of intestine in the proximal and 15% in the distal colon, respectively. In the total colon of sheep, 83% disappeared during the perfusion. Per unit of length, surface or dry weight of mucosa the net flux of ISDN in the small intestine was only half that in the colon. Absorption from the colon per unit of wet weight of the gut was only slightly higher compared to the small intestine. 1 h after the infusion of 14C-labelled ISDN into the large intestine of sheep filled with normal contents 14C-activity was detected in the plasma, a maximum was reached after 4 h. Renal excretion of ISDN or its 14C-labelled metabolites was parallel to the ISDN concentration in blood. Microbial degradation of ISDN to CO2 in colon contents was insignificant.
用含有0.1 - 25毫克/升1,4:3,6 - 二脱水山梨醇 - 2,5 - 二硝酸酯(硝酸异山梨酯,ISDN)的生理盐水灌注麻醉豚鼠的肠段和清醒绵羊的结肠。ISDN摄取量的增加与其浓度呈线性相关。吸收迅速。在豚鼠的空肠和回肠中,每10厘米肠段灌注的ISDN分别有7%在近端和15%在远端结肠被吸收。在绵羊的整个结肠中,83%在灌注过程中消失。每单位长度、黏膜表面积或干重,ISDN在小肠中的净通量仅为结肠中的一半。每单位肠道湿重,结肠的吸收仅比小肠略高。将14C标记的ISDN注入充满正常内容物的绵羊大肠1小时后,在血浆中检测到14C活性,4小时后达到最大值。ISDN或其14C标记代谢物的肾脏排泄与血液中ISDN浓度平行。结肠内容物中ISDN微生物降解为二氧化碳的量微不足道。