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４组（６人／组）健康志愿者分别单次口服２５０，５００，７５０，１０００ｍｇ国产美沙拉嗪后，除２５０和５００ｍｇ组少数人感轻度胃肠道不适外，其余受试者均耐受良好。１０名健康志愿者用随机交叉自身配对法分别口服美沙拉嗪和Ｓａｌｏｆａｌｋ片５００ｍｇ，每８ｈ一次，连续９次达稳态后，用ＨＰＬＣ法测定血浆或尿中５－氨水杨酸（５－ＡＳＡ）或乙酰－５－氨水杨酸（ＡＣ－５－ＡＳＡ）浓度。口服美沙拉嗪后，５－氨水杨酸的药代动力学主要参数：ＡＵＣ（０－２４）３２．６５±１５．８７ｍｇ·Ｌ（－１）·ｈ，Ｃ（ｍａｘ）４．２４±２．６４ｍｇ／Ｌ，Ｔ（ｍａｘ）３．９±３．４ｈ，ＭＲＴ８．１±１．７ｈ，相对生物利用度为７５．３±３８．０％。乙酰－５－氨水杨酸的ＡＵＣ（４０．２４±１３．９７ｍｇ·Ｌ（－１）·ｈ）为５－氨水杨酸的ＡＵＣ的１．２倍。末次给药２４ｈ尿累积排出量５－氨水杨酸为２４．０±１９．９ｍｇ（为末次药量的４．８１±３．９８％）。口服美沙拉嗪达稳态后血中较低浓度的５－ＡＳＡ和对单剂量的良好耐受性的结果表明，美沙拉嗪５００ｍｇ，一日三次的给药方案对于治疗溃疡性结肠炎是安全的。
After a single oral dose of 250, 500, 750 and 1000 mg of domestic mesalazine in healthy volunteers of 4 groups (6 persons / group), all the subjects except the 250 and 500 mg groups were mild gastrointestinal upset Good. Ten healthy volunteers were randomly assigned to receive either mesalazine and Salofalk 500 mg once daily for 8 consecutive hits. After reaching steady state for nine consecutive times, 5-aminosalicylic acid (5-ASA ) Or acetyl-5-aminosalicylic acid (AC-5-ASA) concentration. Pharmacokinetics of 5-aminosalicylic acid after oral administration of mesalazine The main parameters: AUC (0-24) 32.65 ± 15.87mg · L (-1) · h, C (max) 4.24 ± 2 .64mg / L, T (max) 3.9 ± 3.4h, MRT8.1 ± 1.7h, the relative bioavailability was 75.3 ± 38.0%. The AUC (40.24 ± 13.97 mg · L (-1) · h) of acetyl-5-aminosalicylic acid was 1.2 times that of 5-aminosalicylic acid. The final cumulative urinary excretion of 24h urinary 5-aminosalicylic acid was 24.0 ± 19.9 mg (4.81 ± 3.98% of the last dose). The results of oral administration of lower concentrations of 5-ASA in the blood following oral administration of mesalazine and good tolerance to a single dose showed that mesalazine 500 mg, once-daily dosing regimen was safe for the treatment of ulcerative colitis of.