Stohs S J, Ezzedeen F W, Anderson A K, Baldwin J N, Makoid M C
J Invest Dermatol. 1984 Feb;82(2):195-8. doi: 10.1111/1523-1747.ep12259839.
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.
碘氯羟喹(I)用于治疗尿布疹和其他皮肤疾病,据推测其经皮吸收很少或几乎不发生。在5名正常男性受试者单次涂抹3%乳膏12小时后,研究了(I)从该乳膏中的吸收情况。在初次涂抹后对药物血浆水平进行24小时监测,同时对尿液排泄情况进行54小时测量。从血浆和尿液中提取(I),并通过高效液相色谱法进行测定。涂抹后2小时在血浆中检测到药物浓度在0.37 - 0.56微克/毫升范围内,且在整个治疗期间一直存在。涂抹12小时后的平均排泄率为58.4微克/小时,治疗后42小时的排泄率为8.8微克/小时。计算得出消除速率常数为0.15小时⁻¹。在12小时的涂抹期间,约40%的药物被吸收。从上述结果明显可见,(I)发生了显著的经皮吸收。