4-氨基水杨酸口服结肠定位包衣片的体内药效学研究(英文)

目的：评价自制的4-氨基水杨酸口服结肠定位包衣片在大鼠体内的药效学。方法：以2,4,6-三硝基苯磺酸(TNBS)的乙醇溶液灌肠,制作溃疡性结肠炎大鼠模型。将大鼠随机分为7组：健康对照组,TNBS对照组,TNBS+低剂量(包衣片)组,TNBS+中剂量(包衣片)组,TNBS+高剂量(包衣片)组,TNBS+柳氮磺吡啶(SASP)组,TNBS+中剂量非包衣片组。大鼠连续给药5 d后,对结肠部位的大体形态学改变、组织学损伤以及组织髓过氧化物酶(MPO)活性进行评分或测定,评价4-氨基水杨酸(4-ASA)结肠定位包衣片在大鼠体内的药效学。结果：以TNBS灌肠可一次性制作大鼠溃疡性结肠炎模型。与4-ASA非包衣片组相比,包衣片组或SASP组显示,给药后动物结肠的大体形态改变评分、组织损伤评分及MPO活性均有所降低；高剂量组对各指标的影响与SASP无显著差异(P>0．05)。结论：与非包衣片比较,自制的4-氨基水杨酸口服结肠定位包衣片在治疗大鼠溃疡性结肠炎方面有更好的疗效。

An in vivo study on pharmacodynamics of 4-aminosalicylic acid oral colon-specific delivery coated tablets

AIM: To examine the pharmacodynamics of a self-developed oral colon-specific delivery coated tablets of 4-aminosalicylic acid (4-ASA) on rats. METHODS: Ulcerative colitis rat model was developed by intrarectal administration of 2, 4, 6-trinitrobenzenesulfonic acid (TNBS) in alcohol. Rats were divided randomly into healthy control group, TNBS control group, TNBS + lower dose (coated tablets) group, TNBS +medium dose (coated tablets) group, TNBS + higher dose (coated tablets) group, TNBS + sulfasalazine (SASP) group, TNBS + medium dose non-coated tablet group. Several indices including macroscopic change,histological damage, and tissue myeloperoxidase (MPO) activity were examined after 5 consecutive oral drug administration to assess pharmacodynamics of the coated tablets. RESULTS: An experimental ulcerative colitis in rats was induced by TNBS. Compared with 4-ASA non-coated tablet group, decreased macroscopic and histological damage score and lower MPO activity were observed after the oral administration of 4-ASA coated tablets or SASP. There was no significant difference between the effects on the indices of higher dose of coated tablets and SASP (P ＞ 0.05) CONCLUSION: The self-made 4-ASA oral colon-specific delivery coated tablet showes higher effect than non-coated tablets to treat ulcerative colitis in rats.