Rectal absorption of lysozyme and heparin in rabbits in the presence of non-surfactant adjuvants.
作者:MASATOSHI MIYAKE、TOSHIAKI NISHIHATA、NORIKO WADA、EMIKO TAKESHIMA、AKIRA KAMADA
DOI:10.1248/cpb.32.2020
日期:——
Ethylacetoacetate enamines of phenylalanine and phenylglycine enhanced the rectal absorption of macromolecular drugs such as lysozyme and heparin in rabbits. Glycerine-1, 3-diacetoacetate, 1, 2-isopropylideneglyceryl-3-acetoacetate and ethylacetoacetylglycolate also enhanced the rectal absorption of lysozyme and heparin. Lysozyme is a basic compound and heparin is an acidic compound, so the non-surfactant adjuvants used in this study can promote the rectal absorption of macromolecular compounds irrespective of their electrochemical properties. The coadministration of calcium ion inhibited the adjuvant action, so complex formation of the adjuvant with calcium ion may occur, reducing the efficacy of these compounds as adjuvants.
苯丙氨酸和苯甘氨酸的乙酰乙酰乙酸烯胺能促进兔子对溶菌酶和肝素等大分子药物的直肠吸收。1,3-二乙酰乙酸甘油酯、1,2-异亚丙基甘油-3-乙酰乙酸酯和乙酰乙酰乙酸乙酯也能促进溶菌酶和肝素的直肠吸收。溶菌酶是碱性化合物,肝素是酸性化合物,因此本研究中使用的非表面活性佐剂可以促进大分子化合物的直肠吸收,而不受其电化学性质的影响。同时加入钙离子会抑制佐剂的作用,因此佐剂与钙离子可能会形成络合物,从而降低这些化合物作为佐剂的功效。