Inui K I, Tabara K, Hori R, Kaneda A, Muranishi S
J Pharm Pharmacol. 1977 Jan;29(1):22-6. doi: 10.1111/j.2042-7158.1977.tb11231.x.
Black lipid membranes were generated in isotonic buffer (pH 4-5 and pH 6-5) from egg phosphatidylcholine and intestinal lipid, and the permeability to salicylamide, salicylic acid, p-aminobenzoic acid and tryptophan of these membranes was studied. Electrical resistance of intestinal lipid membranes was higher than that of phosphatidylcholine membranes. The presence of cholesterol produced an increase in the electrical resistance of black lipid membranes and a small decrease in the permeability of membranes to drugs. The permeability coefficient of salicylamide, an uncharged drug, was much larger than the coefficients of the charged drugs examined. The values for salicylic acid and p-aminobenzoic acid were much larger than comparable values predicted from their partition coefficients. Intestinal lipid membranes were more permeable to acidic drugs than phosphatidylcholine membranes. It is suggested that phospholipids and other lipid components of the small intestine may play an important role in the membrane permeability to acidic drugs. This method may be of interest in studying the complex processes of drug absorption from intestine.
采用卵磷脂和肠脂质在等渗缓冲液(pH 4 - 5和pH 6 - 5)中制备黑色脂质膜,并研究了这些膜对水杨酰胺、水杨酸、对氨基苯甲酸和色氨酸的通透性。肠脂质膜的电阻高于卵磷脂膜。胆固醇的存在使黑色脂质膜的电阻增加,且膜对药物的通透性略有降低。不带电荷的药物水杨酰胺的通透系数远大于所检测的带电荷药物的通透系数。水杨酸和对氨基苯甲酸的值远大于根据其分配系数预测的可比数值。肠脂质膜对酸性药物的通透性高于卵磷脂膜。提示小肠中的磷脂和其他脂质成分可能在膜对酸性药物的通透性方面发挥重要作用。该方法对于研究药物从肠道吸收的复杂过程可能具有重要意义。