枸橼酸莫沙必利分散片对豚鼠胃排空的影响

Effect of Mosapride Citrate Dispersible Tablet on Gastric Emptying in Guinea Pigs

背景:枸橼酸莫沙必利为强效、选择性5-羟色胺4(5-HT4)受体激动剂,其分散片是一种能在水中迅速崩解的口服片剂,溶解吸收快,便于临床应用。目的:观察枸橼酸莫沙必利分散片对豚鼠胃排空的影响,并与普通枸橼酸莫沙必利片进行比较。方法:将豚鼠随机分为枸橼酸莫沙必利分散片组(商品名:新络纳)、三组普通枸橼酸莫沙必利片组(商品名:贝络纳、加斯清和鲁南枸橼酸莫沙必利片)和对照组,分别于相应药物灌胃后5、10、20、30min和1h、2h采用称重法测定胃排空率。结果:灌胃10min后,枸橼酸莫沙必利分散片组的胃排空率较三组普通枸橼酸莫沙必利片组和对照组显著增加(P<0.01)。灌胃20min后,枸橼酸莫沙必利分散片组的胃排空率仅与一组普通枸橼酸莫沙必利片组和对照组有显著差异(P<0.05)。灌胃30min、1h和2h后,枸橼酸莫沙必利分散片组的胃排空率较三组普通枸橼酸莫沙必利片组和对照组有增加的趋势,但差异无统计学意义。结论:枸橼酸莫沙必利分散片对豚鼠胃排空的影响较普通枸橼酸莫沙必利片起效更快,可能更适用于功能性消化不良胃排空延迟的治疗。

Background: Mosapride citrate is a potent and selective 5-hydroxytryptamine4 (5-HT4) receptor agonist, its dispersible tablet is a water-soluble, rapidly disintegrated and easily absorbed oral pill, which is conveniently used clinically. Aims: To observe the effect of mosapride citrate dispersible tablet on gastric emptying in guinea pigs by comparing with various ordinary mosapride citrate tablets. Methods: Guinea pigs used in this study were randomly divided into mosapride citrate dispersible tablet group (brand name: New Boronia), three ordinary mosapride citrate tablets groups (brands name: Boronia, Gasmotin and Lu-Nan mosapride citrate tablet) and saline controls. The emptying rate of stomach was evaluated by using weighing method 5, 10, 20, 30 minutes, 1 hour and 2 hours, respectively after single intragastric administration of the corresponding agent. Results: Ten minutes after intragastric administration, the guinea pigs in mosapride citrate dispersible tablet group showed a significantly higher gastric emptying rate than that in the three ordinary mosapride citrate tablets groups and the controls, respectively (P<0.01). Twenty minutes after administration, the guinea pigs in mosapride citrate dispersible tablet group exhibited a further increased emptying rate of stomach as compared with that in one of the ordinary mosapride citrate tablets groups and the controls, respectively (P<0.05). Thirty minutes later, an elevated tendency (but not of statistical significance) of gastric emptying rate in mosapride citrate dispersible tablet group was observed when compared with that in the three ordinary mosapride citrate tablets groups and the controls, respectively; the same results were observed 1 hour and 2 hours after administration in the four above experimental groups and the controls. Conclusions: Mosapride citrate dispersible tablet shows a faster effect on gastric emptying in guinea pigs as compared with ordinary mosapride citrate tablets, indicating that it might be a drug of choice in the treatment of delayed gastric emptying in patients with functional dyspepsia.