Giachetti C, Mondino A, Silvestri S, Zanolo G, Bramanti G, Criscuoli M, Subissi A
Arzneimittelforschung. 1982;32(11):1433-6.
Absorption, distribution and excretion of 14C-D-glucitol hexanicotinate (sorbinicate, SN) were studied after oral dosing in the rat against 14C-nicotinic acid (NA). SN is absorbed in large quantities from the gastro-intestinal tract, even if to a lesser extent than NA. The serum 14C-radioactivity after SN presents a distinctly different trend from that after NA administration: peak at 8 h (against 15 min for NA), slow excretion, very low and constant levels (peak 1/10 of that induced by NA). The superior performance of SN is explained partly by the different absorption of the two drugs and partly by a strong tropism for the tissues, especially for the liver, of which SN gave proof in the distribution tests. The excretion of 14C after SN in the urine is about half of that after NA whereas excretion in the feces is several times greater. Some results obtained in the monkey substantially confirm the findings in the rat.
以14C-烟酸(NA)为对照,研究了大鼠口服给药后14C-D-葡萄糖醇己烟酸酯(山梨醇烟酸酯,SN)的吸收、分布和排泄情况。SN可从胃肠道大量吸收,尽管吸收程度低于NA。SN给药后血清中的14C放射性呈现出与NA给药后明显不同的趋势:在8小时达到峰值(NA为15分钟),排泄缓慢,水平非常低且恒定(峰值为NA诱导值的1/10)。SN的优越性能部分归因于两种药物吸收方式的不同,部分归因于其对组织,尤其是肝脏的强烈亲和性,这在分布试验中得到了证实。SN给药后,尿液中14C的排泄量约为NA给药后的一半,而粪便中的排泄量则是NA的数倍。在猴子身上获得的一些结果基本证实了在大鼠身上的发现。