ショ糖脂肪酸エステルの研究 (第3報)

薬物の消化管からの吸収に及ぼす影響

抄録

Effect of various types of surface active agents on the absorption of drugs was investigated using perfusion technique by rat small intestine.
Tetracycline (TC), sulfanilamide (SF), isoniazid, and salicylic acid (SA) were used as test drugs, and sodium laurylsulfate (SLS), benzethonium chloride, polysorbate 80 (PS-80), sucrose monostearate, and sucrose distearate were used as surface active agents.
It was found that: (1) ionic nature of the surfactants substantially influenced the absorption, (2) a rate of absorption of TC was accelerated by the presence of SLS, benzethonium chloride or sucrose esters, (3) PS-80 showed a marked reduction in the absorption of SA and TC, (4) benzethonium chloride reduced the absorption of SA, and (5) sucrose esters within the concentrations tested did not decrease the absorption of all the drugs tested. They were explained by the low thermodynamic activity of the drugs in the vehicles due to complexing or other forms of interactions and/or by the correlation with organic solvent/isotonic buffer solution partition ratios.
Amount of the drug excreted into urine was measured, following to oral administration of the solution of the drug-surfactant combination to adult human subjects. The results supported the foregoing conclusions that sucrose esters greatly enhanced, while PS-80 markedly reduced the absorption of TC, and that the absorption of SF was not affected significantly by the presence of sucrose esters.