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目的:研究法罗培南在大鼠各肠段的吸收率,以确定最佳吸收部位,为制定合理的药物制剂提供科学依据。方法:采用大鼠在体肠循环法,各肠段区间如下:十二指肠段自幽门1cm处开始;空肠段离幽门15cm处开始;回肠段离盲肠上行20cm处开始;结肠段从盲肠后段开始。各肠段取10cm左右,将所取肠段两端开口、插管并结扎,插管与恒流泵连接,形成各自的回路。用HPLC法梯度洗脱测定法罗培南的浓度,依据药物在肠段中回流2小时后的减少量来确定各肠段法罗培南的吸收量。结果:法罗培南在大鼠各肠段吸收率平均值为十二指肠6.91±3.08%;空肠5.66±2.29%;回肠9.62±4.08%;结肠4.65±1.29%。稳定性实验、精密度实验、回收率实验的RSD分别为0.48%、0.234%和2.01%。结论:法罗培南在各肠段均有吸收,吸收率按回肠、十二指肠、空肠、结肠顺序依次降低。
OBJECTIVE: To study the absorption rate of faropenem in various intestine of rats to determine the best absorption site and provide a scientific basis for the formulation of rational drug preparations. Methods: The rats in the intestine circulation method, the intestine range as follows: duodenal segment from the pylorus 1cm Department; jejunum segment from the pylorus 15cm Department; ileum segment cecum upward 20cm Department began; colon segment from the cecum Segment begins. The intestine to take about 10cm, both ends of the intestine taken open, intubation and ligation, intubation and constant flow pump connected to form their own circuit. The concentration of faropenem was determined by HPLC gradient elution, and the dose of faropenem in each bowel segment was determined based on the decrease after 2 hours of reflux of the drug in the bowel segment. Results: The average absorption rate of faropenem in various intestinal segments of rats was 6.91 ± 3.08% in duodenum, 5.66 ± 2.29% in jejunum, 9.62 ± 4.08% in ileum and 4.65 ± 1.29% in colon. RSD of stability, precision and recovery experiments were 0.48%, 0.234% and 2.01% respectively. Conclusion: Faropenem is absorbed in all intestine segments, and the absorption rate decreases in the order of ileum, duodenum, jejunum and colon.