多基质系统(MMX)美沙拉嗪治疗溃疡性结肠炎的研究进展

A. Hawthorne
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摘要

MMXTM美沙拉嗪是一种新型延迟释放美沙拉嗪制剂,高强度1.2 g片剂,用于治疗活动性轻中度结肠炎并维持缓解。体外和体内研究表明,药物在回肠末端和盲肠开始释放,随着片剂通过结肠逐渐释放5-ASA。药代动力学数据与其他5-ASA配方相当,系统吸收低,在粪便和左结肠粘膜活检中含量高。临床试验显示活动性轻至中度结肠炎的临床和内镜下缓解率高,服用2.4 g每日一次,超过8周。4.8 g剂量似乎没有更高的缓解率。对于最初8周治疗失败的患者,再延长治疗8周,每日两次,剂量为2.4 g,可诱导缓解。一项纳入在急性研究中获得缓解的患者的维持研究显示,使用积极治疗试验中使用的严格的缓解定义(包括粘膜愈合),每天1.2 g两次(68.5%)和每天2.4 g一次(64.4%),一年的缓解率维持在高水平。这种药对结肠炎安全有效。高片剂强度和每日一次的剂量使该制剂成为结肠炎患者的一个受欢迎的治疗选择。
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A Review of Multimatrix System (MMX) Mesalazine in the Management of Ulcerative Colitis
MMXTM mesalazine is a novel delayed release mesalazine formulation with a high-strength 1.2 g tablet for the treatment of active mild to moderate colitis and maintenance of remission. In vitro and in vivo studies show initiation of drug release in the terminal ileum and caecum with gradual release of 5-ASA as the tablet passes through the colon. Pharmacokinetic data are comparable to other 5-ASA formulations with low systemic absorption and high levels in feces and in mucosal biopsies in the left colon. Clinical trials have shown high rates of clinical and endoscopic remission in active mild to moderate colitis over 8 weeks with a 2.4 g once daily dose. There do not appear to be higher remission rates with the 4.8 g dose. Prolongation of treatment with a further 8 weeks of 2.4 g twice daily can induce remission in those failing the initial 8 weeks of therapy. A maintenance study enrolling patients who achieved remission in the acute studies showed high rates of remission maintained at one year with 1.2 g twice daily (68.5%) and 2.4 g once daily (64.4%) using the strict definition of remission (including mucosal healing) that was used in the active treatment trials. The drug is safe and effective in colitis. The high tablet strength, and once-daily dosage make this formulation a welcome addition to therapy options for patients with colitis.
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