Gerlóczy A, Fónagy A, Keresztes P, Perlaky L, Szejtli J
Arzneimittelforschung. 1985;35(7):1042-7.
The absorption, distribution, excretion and metabolism of orally administered universally labelled 14C-beta-cyclodextrin and 14C-glucose were compared in rat. The maximum radioactivity of the blood derived from 14C-beta-cyclodextrin was observed between 4th and 11th h and the value of the maximum in different experiments ranged between 5 and 17 0/00 of the total administered radioactivity. Following 14C-glucose treatment radioactivity reached the maximum within half-an-hour, with values of 15 to 82 0/00. In the 8th h after a high dose (313.5 mg/kg) of beta-cyclodextrin no more than 3-50 ppm beta-cyclodextrin was detectable in the blood by HPLC. After 14C-beta-cyclodextrin treatment 4.2-4.8% of the administered total radioactivity was excreted by the urine and about the same quantity (2-3.6%) in case of 14C-glucose. No specific accumulation was observed after 14C-beta-cyclodextrin treatment in the different organs. The large intestine contained 10-15% of the cyclodextrin radioactivity while this value was only 2% in case of 14C-glucose. Following p.o. administration of different doses of 14C-beta-cyclodextrin the radioactivity peak was detected in the exhaled air between the 4-6th and 6-8th h, respectively, depending on the administered doses, while in case of 14C-glucose treatment it was observed within 2 h. The total radioactivity exhaled by 14C-beta-cyclodextrin treated animals in 24 h was 55 to 64% of the administered radioactivity and 58% in case of 14C-glucose. It is assumed that beta-cyclodextrin is metabolized in rats slower but similarly to glucose, therefore p.o. administered beta-cyclodextrin cannot induce toxic symptoms.
在大鼠体内比较了口服通用标记的14C-β-环糊精和14C-葡萄糖的吸收、分布、排泄及代谢情况。源自14C-β-环糊精的血液中放射性在第4至11小时达到最大值，不同实验中最大值在总给药放射性的5至17‰之间。给予14C-葡萄糖后，放射性在半小时内达到最大值，数值为15至82‰。在高剂量（313.5mg/kg）β-环糊精给药后第8小时，通过高效液相色谱法在血液中检测到的β-环糊精不超过3 - 50ppm。给予14C-β-环糊精后，4.2 - 4.8%的总给药放射性通过尿液排出，14C-葡萄糖的情况约为相同数量（2 - 3.6%）。给予14C-β-环糊精后，在不同器官中未观察到特异性蓄积。大肠中含有10 - 15%的环糊精放射性，而14C-葡萄糖的该值仅为2%。口服不同剂量的14C-β-环糊精后，呼出空气中的放射性峰值分别在第4 - 6小时和第6 - 8小时检测到，具体取决于给药剂量，而给予14C-葡萄糖后在2小时内观察到。14C-β-环糊精处理的动物在24小时内呼出的总放射性为给药放射性的55%至64%，14C-葡萄糖为58%。据推测，β-环糊精在大鼠体内的代谢比葡萄糖慢但类似，因此口服β-环糊精不会引发毒性症状。
