Feller K, le Petit G
Int J Clin Pharmacol Biopharm. 1977 Oct;15(10):468-9.
The equilibration of drug concentrations between blood plasma (unbound part) and saliva was studied for selected drugs with different physicochemical properties: Quinidine, sulfamerazine, paracetamol, diazepam and ethanol. From these and other experimental results it is suggested: 1. The concentration ratio between saliva and blood plasma (unbound) can only equal one for basic drugs with a pK a lower than 5.5 and acid drugs with a pK a higher than 8.5 and for pH indifferent drugs. 2. The drug must have a sufficient permeation ability through lipid membranes, valuable by the lipid water partition coefficient.
针对具有不同理化性质的特定药物(奎尼丁、磺胺甲基嘧啶、对乙酰氨基酚、地西泮和乙醇),研究了血浆(游离部分)与唾液之间药物浓度的平衡。根据这些及其他实验结果,提出以下建议:1. 对于pKa低于5.5的碱性药物、pKa高于8.5的酸性药物以及pH值不敏感药物,唾液与血浆(游离)之间的浓度比只能等于1。2. 药物必须具有足够的透过脂质膜的渗透能力,这可通过脂水分配系数来衡量。