al Jaser M, el-Yazigi A, Kojan M, Croft S L
Department of Biological and Medical Research, King Faisal Specialist Hospital and Research Centre, Riyadh, Saudi Arabia.
Antimicrob Agents Chemother. 1995 Feb;39(2):516-9. doi: 10.1128/AAC.39.2.516.
We examined in this study the pharmacokinetics of Sb in the affected skin and normal skin of patients treated with sodium stibogluconate for cutaneous leishmaniasis and compared the results with those for the blood. The procedure was fully explained, and a written consent was obtained from each of nine patients. After a dose of sodium stibogluconate equivalent to 600 mg of Sb was administered intramuscularly, small skin biopsies were collected under local anesthesia at different time intervals from the circumferences of the lesions and simultaneously from normal skin. Antimony was measured in these biopsies after suitable ashing and processing by flameless atomic absorption spectrophotometry. The means (with standard errors of the means in parentheses) of the peak concentration, time to peak concentration, area under the curve, half-life, and mean residence time in lesions were 5.02 (1.43) micrograms/g, 2.1 (0.4) h, 32.8 (6.1) micrograms.h/g, 6.88 (0.54) h, and 10.4 (1.2) h, respectively, and those in normal skin were 6.56 (2.01) micrograms/g, 2.6 (0.8) h, 44.0 (15.8) micrograms.h/g, 5.44 (0.83) h, and 8.08 (1.34) h, respectively. There was no significant difference in any of these parameters between lesions and normal skin, whereas the differences in peak concentration, half-life, and mean residence time between lesions and whole blood were significant (P < or = 0.05). The penetration of Sb into skin, either affected or normal, as measured by the skin/blood area under the curve ratio appears to be complete, but the disposition is slow compared with that from the blood.
在本研究中,我们检测了接受葡糖酸锑钠治疗皮肤利什曼病患者的患部皮肤和正常皮肤中锑的药代动力学,并将结果与血液中的结果进行比较。该程序已得到充分解释,并获得了9名患者每人的书面同意书。肌肉注射相当于600mg锑的葡糖酸锑钠剂量后,在局部麻醉下于不同时间间隔从病灶周边以及同时从正常皮肤采集小块皮肤活检样本。在对这些活检样本进行适当的灰化和处理后,通过无火焰原子吸收分光光度法测定锑含量。病灶中锑的峰值浓度、达峰时间、曲线下面积、半衰期和平均驻留时间的均值(括号内为均值的标准误)分别为5.02(1.43)μg/g、2.1(0.4)h、32.8(6.1)μg·h/g、6.88(0.54)h和10.4(1.2)h,正常皮肤中的相应均值分别为6.56(2.01)μg/g、2.6(0.8)h、44.0(15.8)μg·h/g、5.44(0.83)h和8.08(1.34)h。病灶与正常皮肤之间这些参数均无显著差异,而病灶与全血之间在峰值浓度、半衰期和平均驻留时间方面的差异具有显著性(P≤0.05)。通过皮肤/血液曲线下面积比值测量,锑在患部皮肤和正常皮肤中的渗透似乎是完全的,但与血液中的情况相比,其处置过程较为缓慢。