Wu W M, Murakami T, Higashi Y, Yata N
Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, Japan.
J Pharm Sci. 1987 Jul;76(7):508-12. doi: 10.1002/jps.2600760703.
The promoting efficacies of N-acyl derivatives of amino acids on the rectal absorption of sodium ampicillin were investigated using the rat rectal loop technique. N-Acyl derivatives with longer carbon chains in the acyl moiety showed a greater promoting potency. The promoting potencies of N-acyl derivatives of phenylglycine and phenylalanine were greater than those of glycine and alanine derivatives when compared at the same length of carbon chain in their acyl moieties. The promoting action of N-acylamino acids was not influenced by the presence of N-ethylmaleimide or ouabain. The promoting potencies of N-acylamino acids were depressed in the presence of calcium chloride in the rectal loop. The contribution of the calcium ion sequestration capacity of N-acylamino acids to their promoting efficacies is discussed.
采用大鼠直肠袢技术研究了氨基酸的N-酰基衍生物对氨苄西林钠直肠吸收的促进作用。酰基部分碳链较长的N-酰基衍生物显示出更大的促进效力。当在其酰基部分具有相同碳链长度时,苯甘氨酸和苯丙氨酸的N-酰基衍生物的促进效力大于甘氨酸和丙氨酸衍生物。N-酰基氨基酸的促进作用不受N-乙基马来酰亚胺或哇巴因的影响。在直肠袢中存在氯化钙的情况下,N-酰基氨基酸的促进效力降低。讨论了N-酰基氨基酸的钙离子螯合能力对其促进效力的贡献。