Fix J A, Leppert P S, Porter P A, Caldwell L J
J Pharm Sci. 1983 Oct;72(10):1134-7. doi: 10.1002/jps.2600721006.
The rectal absorption of gentamicin sulfate in rats, both in the presence and absence of sodium salicylate, was facilitated by the use of high ionic strength aqueous formulations. The relative order of effectiveness in promoting gentamicin absorption was sodium dihydrogen phosphate congruent to sodium chloride much greater than potassium chloride, indicating a preferential effect of sodium ions. The increased gentamicin bioavailability in response to sodium salicylate adjuvant activity appeared to be independent of and additive to the increased gentamicin absorption due to high ionic strength conditions. The inability of sorbitol to increase gentamicin bioavailability above control levels indicated that elevated osmotic pressure was not a major determinant of rectal gentamicin absorption.
在大鼠中,无论有无水杨酸钠存在,通过使用高离子强度的水性制剂可促进硫酸庆大霉素的直肠吸收。促进庆大霉素吸收的有效性相对顺序为磷酸二氢钠等同于氯化钠远大于氯化钾,表明钠离子具有优先作用。水杨酸钠辅助活性导致的庆大霉素生物利用度增加似乎独立于高离子强度条件下庆大霉素吸收的增加,且二者具有相加性。山梨醇无法使庆大霉素生物利用度高于对照水平,这表明渗透压升高不是直肠庆大霉素吸收的主要决定因素。