在日本健康志愿者中，研究了 Asacol 片剂单剂量和多剂量的药代动力学和安全性。

Pharmacokinetics and safety of single and multiple doses of Asacol tablets in Japanese healthy volunteers.

机构信息

Digestive Disease Center of Excellence, Kitano Hospital, The Tazuke Kofukai Medical Research Institute, Kita-ku, Osaka, Japan.

出版信息

Adv Ther. 2009 Aug;26(8):749-61. doi: 10.1007/s12325-009-0059-9.

DOI:10.1007/s12325-009-0059-9

PMID:19730804

Abstract

INTRODUCTION

The pharmacokinetics and safety of Asacol (Tillotts Pharma AG, Ziefen, Switzerland), which has been used worldwide to treat ulcerative colitis and Crohn's disease, were studied in Japanese healthy male volunteers.

METHODS

Drug plasma concentrations and urinary and fecal excretions after a single dose (400-4800 mg) and multiple doses (3600 mg/day for 7 days) were investigated.

RESULTS

All adverse events were "not serious." The peak plasma concentration (C max) was reached at 12.3-18.0 hours after a single dose, and the C max and area under the plasma concentration-time curve (AUC) of mesalazine and its N-acetyl metabolite were proportional to the doses. The C max and AUC in non-Japanese subjects reported in the literature were closely correlated to findings in Japanese subjects, and external excretions were also similar in the Japanese and non-Japanese subjects.

CONCLUSIONS

Asacol was safe and well tolerated in this Japanese population, and the non-Japanese clinical data could be extrapolated to the Japanese population.

摘要

简介

已在全球范围内用于治疗溃疡性结肠炎和克罗恩病的艾莎克（特罗特药厂，瑞士），其药代动力学和安全性已在日本健康男性志愿者中进行了研究。

方法

单次剂量（400-4800mg）和多次剂量（3600mg/天，共 7 天）后，检测药物血浆浓度以及尿和粪便排泄。

结果

所有不良事件均为“不严重”。单次给药后 12.3-18.0 小时达到血药峰浓度（C max），且美沙拉嗪及其 N-乙酰代谢物的 C max 和血药浓度-时间曲线下面积（AUC）与剂量成正比。文献中报道的非日本受试者的 C max 和 AUC 与日本受试者的结果密切相关，且日本和非日本受试者的外排也相似。