Percutaneous absorption of iodochlorhydroxyquin in humans.

Percutaneous absorption of iodochlorhydroxyquin in humans.
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碘氯羟喹在人体中的经皮吸收。

DOI:
10.1111/1523-1747.ep12259839
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发表时间:
1984
期刊:
The Journal of investigative dermatology
影响因子:
--
通讯作者:
M. Makoid
M. Makoid
中科院分区:
--
文献类型:
--
作者:
S. Stohs;F. W. Ezzedeen;A. Anderson;J. N. Baldwin;M. Makoid

文献摘要

被引文献

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碘氯羟喹 (I) 用于治疗尿布疹和其他皮肤病,据推测经皮吸收很少或不吸收。对 5 名正常男性受试者单次使用 3% 乳膏 12 小时后对 (I) 的吸收进行了研究。首次使用后,追踪药物的血浆浓度 24 小时,同时测量尿液排泄 54 小时。 (I)从血浆和尿液中提取并通过高效液相色谱法进行测定。用药后2小时在血浆中检测到药物浓度为0.37-0.56微克/毫升,并在整个治疗期间持续存在。使用12小时后的平均排泄率为58.4微克/小时,处理后42小时的平均排泄率为8.8微克/小时。计算消除速率常数为0.15 h-1。大约 40% 的药物在 12 小时的施用期内被吸收。从以上结果可以看出,(I)发生显着的经皮吸收。
Iodochlorhydroxyquin (I) is used in the treatment of diaper rash and other skin disorders, and is presumed to undergo little or no percutaneous absorption. The absorption of (I) from a 3% cream was studied in 5 normal male subjects after a single application of the cream for 12 h. Plasma levels of the drug were followed for 24 h after initial application while urinary excretion was measured for 54 h. (I) was extracted from plasma and urine and assayed by high-performance liquid chromatography. The drug in the range of 0.37-0.56 micrograms/ml was detected in plasma 2 h after application and persisted throughout the treatment period. The mean excretion rate after 12 h of application was 58.4 micrograms/h and the excretion rate was 8.8 micrograms/h at 42 h posttreatment. The elimination rate constant was calculated to be 0.15 h-1. Approximately 40% of the drug was absorbed over the 12-h application period. From the above results it is apparent that significant percutaneous absorption of (I) occurs.