Rege A B, Walker-Cador J Y, Clark R A, Lertora J J, Hyslop N E, George W J
Department of Pharmacology, Tulane University School of Medicine, New Orleans, Louisiana 70112.
Antimicrob Agents Chemother. 1992 Mar;36(3):647-50. doi: 10.1128/AAC.36.3.647.
Fluconazole, an orally active antifungal agent, has been shown to be clinically beneficial for maintenance therapy of cryptococcal meningitis. A sensitive gas-liquid chromatographic assay with electron capture detection, which required only a single extraction step and precluded any pretreatment of the chromatographic column, was developed for fluconazole. The assay was linear from 0.1 to 20 micrograms/ml, with a correlation coefficient of 0.999. The intraassay and interassay coefficients of variation were less than 9%. The measured values on average were within 8% of the target values. The extraction recoveries ranged from 87 to 106%. Steady-state plasma fluconazole levels (mean +/- standard deviation) in three AIDS patients with cryptococcal meningitis receiving 200 mg of fluconazole per day ranged from 8.95 +/- 1.32 to 11.41 +/- 0.63 micrograms/ml and were within the expected range for this dosing rate, on the basis of previous studies. The ratio of fluconazole concentration in cerebrospinal fluid to fluconazole concentration in plasma in one patient receiving 400 mg/day was 0.73 at steady state and was consistent with published reports.
氟康唑是一种口服有效的抗真菌药物，已被证明对隐球菌性脑膜炎的维持治疗具有临床益处。我们开发了一种灵敏的气相色谱法，采用电子捕获检测，该方法仅需一步萃取，且无需对色谱柱进行任何预处理，用于测定氟康唑。该测定方法在0.1至20微克/毫升范围内呈线性，相关系数为0.999。批内和批间变异系数均小于9%。测量值平均在目标值的8%以内。萃取回收率在87%至106%之间。三名患有隐球菌性脑膜炎的艾滋病患者每天接受200毫克氟康唑治疗，其稳态血浆氟康唑水平（均值±标准差）在8.95±1.32至11.41±0.63微克/毫升之间，根据先前的研究，该水平在该给药速率的预期范围内。一名每天接受400毫克氟康唑治疗的患者，其脑脊液中氟康唑浓度与血浆中氟康唑浓度之比在稳态时为0.73，与已发表的报告一致。
