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美沙拉嗪缓释胶囊 |Apriso ER (mesalamine capsules)

2011-03-28 17:14:25 作者：新特药房来源：中国新特药网天津分站浏览次数：830 文字大小：【大】【中】【小】

简介： 英文药名: Apriso ER (mesalamine capsules) 中文药名: 美沙拉嗪缓释胶囊药品说明药品名称：美沙拉嗪肠溶缓释微丸胶囊　适应症：溃疡性结肠炎的维持性治疗规格：0.375g/粒溃疡性结肠炎的 ...

关键字：美沙拉嗪缓释胶囊溃疡性结肠炎

英文药名: Apriso ER (mesalamine capsules)

中文药名: 美沙拉嗪缓释胶囊

药品说明

药品名称：美沙拉嗪肠溶缓释微丸胶囊　

适应症：溃疡性结肠炎的维持性治疗

规格：0.375g/粒

溃疡性结肠炎的治疗
溃疡性结肠炎（ulcerative colitis，UC）是一种发生于结肠粘膜的慢性、炎症性及溃疡性疾病，最典型的特征是血性腹泻。近年我国UC发病呈加快趋势，最近10年报道的病例数目是过去10年的3.8倍，而患者构成以慢性反复发作型为主。在缓解期如不进行干预，UC患者1年内的复发率则可能高达70％。由于UC病变范围广泛、病情反复发作、治疗效果欠佳，病情迁延不愈，癌变可能性大等特点，该病已被世界卫生组织确定为现代难治疾病。 UC的治疗方法包括药物治疗、营养治疗、心理治疗及手术治疗，其中药物治疗是治疗溃疡性结肠炎的主要方法。而美沙拉嗪（又名：5-氨基水杨酸，5-ASA）及其衍生物被证明是目前临床最常用的、有效的药物。
美沙拉嗪治疗溃疡性结肠炎的作用机制尚不甚明了，可能为局部作用而非系统作用。美沙拉嗪可在患者肠道内与大肠粘膜直接接触发挥作用，抑制肠粘膜中前列腺素E2、白三烯、及5-羟基十二碳四烯酸的合成和释放。
美沙拉嗪有局部用药和口服制剂，其中局部用药剂型有栓剂和灌肠液，对于轻-中型的远端结肠炎的患者，栓剂、灌肠剂的给药深度受限，无法治疗广泛性结肠炎。美沙拉嗪若直接口服可被胃和十二指肠迅速吸收，这样不能有足够量药物到达结肠而起抗炎作用，同时吸入体内的药物易产生肾毒性，因此口服制剂需要做成肠溶制剂，但无论是国产还是申请进口的美沙拉嗪肠溶制剂，维持期治疗都是一天3-4次，对于患者长期用药来说，存在诸多不便。因此做成肠溶+缓释制剂，显得很有意义！

美沙拉嗪肠溶缓释胶囊的特点与优势

1. 采用肠溶+缓释技术，使药物在炎症局部有较好的生物利用度，避免上消化道吸收，减少药物的全身性作用。美沙拉嗪肠溶缓释胶囊，在胃内胶囊溶解破裂，释放出微丸，但此时美沙拉嗪并不被释放和吸收，到达小肠后，在肠液pH≥6 时，微丸包衣溶解开始释放药物，微丸内为缓释骨架结构，药物缓慢释放，有利于在炎症局部维持较长时间。先前已上市的其他肠溶片在pH≥7时才开始释放药物，而已发布的研究数据证明，部分UC患者的小肠和大肠液pH值从未达到7。因此，该美沙拉嗪肠溶缓释胶囊为新型的、先进的药物给药系统，该给药系统可实现在小肠部位即开始释放药物，持续到整个结肠，治疗效果更佳。
2. 每天用药1次。药物微丸是缓释骨架结构，可在炎症局部缓慢释放药物，维持长时间的局部药物浓度，每天早晨1次服药即可。

2008年10月31日,美国FDA批准了Salix Pharmaceuticals, Ltd.公司的美沙拉嗪缓释胶囊（mesalamine extended-release capsules），商品名为Apriso ，该制剂为目前唯一的每日给药1次的24小时缓释制剂。
Falk公司缓释胶囊（规格375mg）上市较晚，未在中国申请。

APRISO

Manufacturer:

Salix Pharmaceuticals, Inc.

Pharmacological Class:

Aminosalicylate.

Active Ingredient(s):

Mesalamine 0.375g; ext-rel caps; contains phenylalanine 0.56mg/cap.

Indication(s):

Maintenance of remission of ulcerative colitis (UC) in adults.

Pharmacology:

Ulcerative colitis is a chronic inflammatory disease of the colon or large intestine. Symptoms of the disease include diarrhea (sometimes accompanied by blood) and abdominal pain. Patients with ulcerative colitis may experience periods of remission that can last for months or years. However, most patients’ symptoms eventually return. Maintenance therapy refers to treatment given to patients to enable them to stay in remission and to maintain their health in a disease-free state.

Although the exact mechanism of action of mesalamine is unknown, it appears to be local to the intestinal mucosa rather than systemic. In patients with ulcerative colitis, mucosal production of arachidonic acid metabolites both through the cyclooxygenase and lipooxygenase pathways is increased. It is possible that mesalamine diminishes inflammation by blocking production of arachidonic acid metabolites.

Apriso is a locally-acting aminosalicylate in an extended-release capsule formulation. Because dissolution of the coating of Apriso granules depends on pH, Apriso should not be co-administered with antacids.

Clinical Trials:

Two randomized, double-blind, placebo-controlled, multi-center studies were conducted in a total of 562 adult patients in remission from ulcerative colitis. Ulcerative colitis disease activity was assessed using a modified Sutherland Disease Activity Index (DAI), which is a sum of four subscores based on stool frequency, rectal bleeding, mucosal appearance on endoscopy, and physician’s rating of disease activity. Each subscore can range from 0–3, for a total possible DAI score of 12.

At baseline, approximately 80% of patients has a total DAI score of 0 or 1. Patients were randomized 2:1 to receive either Apriso 1.5g or placebo once daily in the morning for six months. Patients were assessed at baseline, 1 month, 3 months, and 6 months. Relapse was defined as a rectal bleeding subscale score of 1 or more and a mucosal appearance subscale score of 2 or more using the DAI. In both studies, the proportion of patients who remained relapse-free at six months was greater for Apriso than for placebo (Study 1: 68% for Apriso, 51% for placebo; Study 2: 71% for Apriso, 59% for placebo). The use of Apriso for treating ulcerative colitis beyond six months has not been evaluated in controlled clinical trials.

Legal Classification:

Adults:

≥18yrs: 1.5g once daily in the AM.

Children:

<18yrs: not recommended.

Warnings/Precautions:

Sulfasalazine allergy. Renal dysfunction or history of renal disease; assess renal function at the beginning and periodically during treatment. Hepatic impairment. Elderly (monitor CBCs). Pregnancy (Cat.B). Nursing mothers.

Interaction(s):

Do not co-administer with antacids.

Adverse Reaction(s):

Headache, GI upset, upper abdominal pain, nasopharyngitis, flu-like symptoms, sinusitis; renal impairment, mesalamine-induced acute intolerance syndrome (eg, cramping, abdominal pain, bloody diarrhea, fever, headache, rash); discontinue if occurs.