Niazi S, Chiou W L
J Pharm Sci. 1977 Jan;66(1):49-53. doi: 10.1002/jps.2600660111.
A three-compartment open model was proposed for the disposition of dichlorodifluoromethane in dogs with average half-lives of 1.47, 7.95, and 58.5 min for the three disposition phases. This proposal is contrary to several studies that monitored blood levels for a shorter period. An analysis of the tissue compartment distribution following a single dose showed that about 1.5 hr was required to achieve pseudodistribution equilibration, following which more than 90% of the dose remaining in the body was retained in the tissue compartments. The pulmonary clearance and volumes of distribution were calculated considering the first-pass effect through the lungs. The volume of distribution after reaching pseudodistribution equilibrium was approximately 10 times the body weight in terms of the blood concentration, and about 68% of the propellant was cleared from the blood passing through the lungs in each cycle. Disposition of the propellant followed dose-independent kinetics after multiple dosing. No volatile metabolites were detected in the blood using GC.
针对犬体内二氯二氟甲烷的处置提出了一个三室开放模型,三个处置阶段的平均半衰期分别为1.47、7.95和58.5分钟。这一观点与几项监测血液水平时间较短的研究相反。单次给药后对组织室分布的分析表明,达到假分布平衡大约需要1.5小时,此后体内剩余剂量的90%以上保留在组织室中。考虑到通过肺部的首过效应,计算了肺清除率和分布容积。达到假分布平衡后的分布容积以血药浓度计约为体重的10倍,每个循环中约68%的推进剂从流经肺部的血液中清除。多次给药后推进剂的处置遵循非剂量依赖性动力学。使用气相色谱法未在血液中检测到挥发性代谢物。