Cruciani M, Gatti G, Mengoli C, Cazzadori A, Lazzarini L, Miletich F, Graziani M S, Malena M, Bassetti D
Divisione Clinicizzata di Malattie Infettive, Ospedale Civile Maggiore, Verona, Italy.
Antimicrob Agents Chemother. 1997 May;41(5):1077-81. doi: 10.1128/AAC.41.5.1077.
We studied the penetration of dapsone into the epithelial lining fluid (ELF) of sixteen human immunodeficiency virus type 1-infected patients who had received the drug at a dose of 100 mg twice weekly as primary prophylaxis for Pneumocystis carinii pneumonia. Bronchoscopy, bronchoalveolar lavage (BAL), and venipuncture were performed for each patient at a specific time after administration of the last dose of dapsone. Dapsone concentrations in plasma and BAL were determined by high-performance liquid chromatography. The apparent volume of ELF recovered by BAL was determined by using urea as an endogenous marker. The mean concentrations of dapsone in ELF at 2 h (five patients), 4 h (three patients), 12 h (two patients), 24 h (three patients), and 48 h (three patients) were 0.95, 0.70, 1.55, 0.23, and 0.45 mg/liter, respectively, while concentrations in plasma were 1.23, 0.79, 1.31, 0.83, and 0.18 mg/liter, respectively. Dapsone concentrations in ELF were 76, 79, 115, 65, and 291% of those observed in plasma at the same times, respectively. These data show that dapsone is well distributed into ELF and that a twice-weekly 100-mg prophylactic regimen results in sustained concentrations in this compartment.
我们研究了氨苯砜在16例1型人类免疫缺陷病毒感染患者上皮衬液（ELF）中的渗透情况，这些患者接受了每周两次、每次100毫克的氨苯砜治疗，作为卡氏肺孢子虫肺炎的一级预防。在给予最后一剂氨苯砜后的特定时间，对每位患者进行支气管镜检查、支气管肺泡灌洗（BAL）和静脉穿刺。通过高效液相色谱法测定血浆和BAL中的氨苯砜浓度。使用尿素作为内源性标记物来测定通过BAL回收的ELF的表观体积。在2小时（5例患者）、4小时（3例患者）、12小时（2例患者）、24小时（3例患者）和48小时（3例患者）时，ELF中氨苯砜的平均浓度分别为0.95、0.70、1.55、0.23和0.45毫克/升，而血浆中的浓度分别为1.23、0.79、1.31、0.83和0.18毫克/升。ELF中氨苯砜的浓度分别是同一时间血浆中浓度的76%、79%、115%、65%和291%。这些数据表明氨苯砜能很好地分布到ELF中，并且每周两次100毫克的预防方案能使该腔室中的浓度持续保持。
