论文部分内容阅读
目的:研究白藜芦醇衍生物[(E)-3,5,4′-三甲氧基-1,2-二苯乙烯(BTM-0512)]在大鼠肠道的吸收特性。方法:采用大鼠在体肠循环实验,考察不同的药物浓度、肠段及胆汁对吸收参数的影响。BTM-0512在大鼠肠循环液中的药物浓度采用HPLC法测定;循环液中酚红浓度采用UV法测定。结果:在肠道正常PH值情况下,低、中、高3个浓度的BTM-0512的吸收速率常数(K_a)分别为0.6290、0.5329(扎胆管)、0.5330(未扎胆管)、0.6791h~(-1),表明不同浓度BTM-0512在肠道的吸收速率常数相近,且胆汁对BTM-05 12肠道吸收没有影响(P>0.05);在十二指肠、空肠、回肠、结肠的吸收速率常数分别为0.9492、0.5216、0.3835、0.1185 h~(-1),统计结果显示,不同肠段间吸收有明显差异(P<0.05)。结论:BTM-0512在肠道内是以被动扩散的方式被吸收,呈现一级动力学过程。因BTM-0512在整肠段均有吸收,剂型设计时可考虑肠溶制剂。
Objective: To study the absorption properties of resveratrol derivatives [(E)-3,5,4’-trimethoxy-stilbene (BTM-0512)] in the intestine of rats. METHODS: Intestinal circulation experiments were performed in rats to examine the effects of different drug concentrations, intestinal segments, and bile on absorption parameters. The drug concentration of BTM-0512 in rat intestinal circulatory fluid was determined by HPLC; the concentration of phenol red in the circulating fluid was determined by UV method. RESULTS: Under the condition of normal intestinal pH, the absorption rate constants (K_a) of BTM-0512 at low, medium, and high concentrations were 0.6290, 0.5329 (for gallbladder ducts), 0.5330 (for undilated ducts), 0.6791h~ (-1), indicating that the absorption rate constants of different concentrations of BTM-0512 in the intestine are similar, and bile has no effect on intestinal absorption of BTM-05 12 (P>0.05); in the duodenum, jejunum, ileum, colon Absorption rate constants were 0.9492, 0.5216, 0.3835, and 0.1185 h-1, respectively. Statistical results showed that there were significant differences in absorption between different intestinal segments (P<0.05). Conclusion: BTM-0512 is absorbed in the intestinal tract by passive diffusion and presents a first-order kinetic process. Since BTM-0512 is absorbed throughout the entire intestine, enteric preparations may be considered when designing the dosage form.