Peters J H, Murray J F, Gordon G R, Gelber R H
Pharmacology. 1981;22(3):162-71. doi: 10.1159/000137486.
Concentrations of dapsone (DDS) and its metabolite, monoacetyl dapsone (MADDS) were measured in plasma and saliva samples collected concurrently from volunteers receiving a 50-mg oral dose of DDS. A liquid chromatographic technique was employed to separate the compounds from each other and from endogenous materials. Fluorescence detection provided limited sensitivities to 0.1 ng/ml of sample. Saliva levels of DDS were consistently 15-20% of the plasma levels of DDS during the study period, which ranged from 4 to 48 h. Decay rates for DDS from saliva and plasma were nearly identical. In 4-hour samples of plasma subjected to equilibrium dialysis, we found amounts of DDS in the dialysates nearly identical to levels found in saliva collected at that time. Saliva levels of MADDS ranged from 0.8 to 2.6% of their plasma levels at all times. Decay rates of MADDS from the two fluids were nearly identical and saliva levels of MADDS in 4-hour samples were nearly identical to levels found in paired plasma dialysates. Nevertheless, levels of MADDS were so low that a reliable definition of the subjects' acetylator phenotype from levels of MADDS in saliva only was impossible.
在接受50毫克口服剂量氨苯砜(DDS)的志愿者同时采集的血浆和唾液样本中,测定了氨苯砜(DDS)及其代谢产物单乙酰氨苯砜(MADDS)的浓度。采用液相色谱技术将这些化合物彼此分离,并与内源性物质分离。荧光检测对0.1纳克/毫升的样本灵敏度有限。在4至48小时的研究期间,唾液中DDS的水平始终为血浆中DDS水平的15%至20%。唾液和血浆中DDS的衰减率几乎相同。在经过平衡透析的4小时血浆样本中,我们发现透析液中DDS的量与当时采集的唾液中的水平几乎相同。MADDS的唾液水平始终为其血浆水平的0.8%至2.6%。两种液体中MADDS的衰减率几乎相同,4小时样本中MADDS的唾液水平与配对血浆透析液中的水平几乎相同。然而,MADDS的水平非常低,仅根据唾液中MADDS的水平无法可靠地定义受试者的乙酰化表型。