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[关于从含有水杨酸甲酯和水杨酸的浴液中水杨酸经皮吸收的药代动力学研究]

[Pharmacokinetic study of percutaneous absorption of salicylic acid from baths with salicylate methyl ester and salicylic acid].

作者信息

Pratzel H G, Schubert E, Muhanna N

机构信息

Institut für Medizinische Balneologie und Klimatologie, Ludwig-Maximilians-Universität München.

出版信息

Z Rheumatol. 1990 Jul-Aug;49(4):185-91.

PMID:2238859
Abstract

Percutaneous uptake of methyl salicylate was investigated by use of Leukona-Rheumabad (Dr. Atzinger) in 10 volunteers. Percutaneous uptake of salicylic acid was investigated by use of Contrheuma-Bad (Spitzner) in 15 volunteers. By use of bathing concentration of 0.03 g/l of methyl salicylate, plasma levels of 220-820 ng/ml were found 1 h after beginning, and 46-193 ng/ml after 6 h. 2.3-8.7 mg of salicyluric acid was eliminated on the first day, and 0.47 to 1.48 mg on the second day. By use of bathing concentration of 0.33 g/l of salicylic acid constant plasma levels of 10 +/- 1.27 ng/ml were found in a period of 24 h. The renal elimination of 0.92 +/- 0.14 at first day, 0.72 +/- 0.11 at second day, and 0.50 +/- 0.08 mg salicyluric acid at third day was found. Salicylic acid was eliminated 0.086 +/- 0.009 resp. 0.079 +/- 0.007 resp. 0.043 +/- 0.011 mg by those days. The half-time of elimination in urine after methyl salicylate bathing is (as with injected salicylic acid) between 2.4 to 4 h. Conversely half-time of elimination in urine by salicylic acid bathing is between 30 to 50 h, and is greater with salicylic acid bathing than with other application forms. This is in agreement with earlier examinations and results which point out the deposition of salicylic acid in skin. Any definitive deposition of salicylic acid in skin by methyl salicylate bathing was not found.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在10名志愿者中使用乐可纳-风湿浴剂(阿青格博士)研究了水杨酸甲酯的经皮吸收。在15名志愿者中使用抗风湿浴剂(施皮茨纳)研究了水杨酸的经皮吸收。使用0.03 g/l的水杨酸甲酯沐浴浓度时,开始后1小时血浆水平为220 - 820 ng/ml,6小时后为46 - 193 ng/ml。第一天排出2.3 - 8.7 mg水杨尿酸,第二天排出0.47至1.48 mg。使用0.33 g/l的水杨酸沐浴浓度时,在24小时内血浆水平恒定为10±1.27 ng/ml。第一天肾脏排出水杨尿酸0.92±0.14 mg,第二天排出0.72±0.11 mg,第三天排出0.50±0.08 mg。这几天分别排出水杨酸0.086±0.009 mg、0.079±0.007 mg、0.043±0.011 mg。水杨酸甲酯沐浴后尿液中消除半衰期(与注射水杨酸时一样)在2.4至4小时之间。相反,水杨酸沐浴后尿液中消除半衰期在30至50小时之间,且水杨酸沐浴时的半衰期比其他给药形式更长。这与早期指出水杨酸在皮肤中沉积的检查和结果一致。未发现水杨酸甲酯沐浴后水杨酸在皮肤中有任何明确的沉积。(摘要截选至250字)

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