中文摘要：

目的：研究斯皮诺素在大鼠胃、肠及各肠段的吸收动力学,为其剂型设计提供生物药剂学依据。方法：采用大鼠在体胃肠吸收模型,用高效液相色谱法测定胃肠灌注液中药物的浓度。结果：不同质量浓度（10,20,40 mg·L-1）的斯皮诺素在大鼠胃部2 h的吸收百分率分别为20.35%,21.88%,20.23%;药物在十二指肠、空肠、回肠、结肠的吸收速率常数为（0.026 4±0.001 4）,（0.023 4±0.000 9）,（0.022 6±0.000 9）,（0.026 5±0.000 6）h-1;药物质量浓度为10,20,40 mg·L-1时,肠的吸收速率常数分别为（0.023 1±0.001 5）,（0.024 1±0.001 6）,（0.023 3±0.002 9）h-1;当pH为6.5,7.2,7.8时,肠的吸收速率常数分别为（0.023 5±0.001 5）,（0.024 1±0.001 6）,（0.022 1±0.002 6）h-1。结论：斯皮诺素在大鼠胃肠道各部分均有吸收,且吸收呈一级动力学过程,吸收机制为被动扩散;药物在大鼠肠内吸收不受药物浓度和pH的影响;药物的吸收按十二指肠、结肠、空肠、回肠的顺序依次下降,药物在胃中的吸收较好。

英文摘要：

Objective： To investigate the absorption kinetics of spinosin in the gastrointestinal of rat, to provide the biological pharmaceutical basis for dosage design. Method： The absorption kinetics was investigated in rats using situ perfusion method. RP-HPLC was used to determine the concentrations of spinosin. Result： The absorption percentages at concentration of （10, 20, 40 m· L^-1） in stomach were 20.35%, 21.88%, 20.23% , respectively. The absorption rate constant （Ka）in duodenum, jejunum, ileum and colon were （0. 026 4 ± 0.001 4）, （0. 023 4 ±0. 000 9）, （0. 0226 ±0. 000 9）, （0. 026 5 ±0. 000 6） h^-1, respectively. Intestinal Ka of spinosin at different concentrations （ 10, 20, 40 mg. L^-1 ） were （0. 023 1 ± 0. 001 5 ）, （0. 024 1 ± 0. 001 6）, （0. 023 3 ±0.002 9） h^-1, respectively. Ka at pH of 6.5, 7.2 and 7.8 for the whole intestine were （0. 023 5 ± 0.001 5）, （0.024 1 ±0.001 6）, （0.022 1 ±0.002 6） h^-1. Conclusion： Spinosin was absorbed in all segments in the pattern of first-order kinetics with the passive diffusion absorption mechanism; concentration and pH of the drug solution have no effect on the absorption kinetics; the absorption at duodenum, colon, jejunumand ileum align in a decreasing order. Spinosin was well absorbed at stomach.