Padfield J M, Kellaway I W
J Pharm Pharmacol. 1975 May;27(5):348-52. doi: 10.1111/j.2042-7158.1975.tb09453.x.
The self-diffusion coefficients of penicillin G and ampicillin have been determined at 25 degrees in water and in the presence of a swamping concentration of electrolyte. The antibiotics diffused through phospholipid dispersions at a reduced rate due to interaction with the lipid aggregates. Ampicillin diffused through the phosphatidylcholine and phosphatidylethanolamine dispersions more rapidly than penicillin G, whereas the latter diffused more rapidly through the lysophosphatidylcholine dispersions. Estimates of binding have been made from these data and compared with those obtained from equilibrium dialysis studies. Surface tension measurements indicated that the antibiotics exhibited minimal surface activity. These results have been correlated with data obtained in other studies and a possible explanation has been advanced for the reported differences in vivo activity of penicillin G and ampicillin.
已测定青霉素G和氨苄西林在25摄氏度的水中以及在过量电解质存在下的自扩散系数。由于与脂质聚集体相互作用,抗生素在磷脂分散体中的扩散速率降低。氨苄西林在磷脂酰胆碱和磷脂酰乙醇胺分散体中的扩散速度比青霉素G快,而后者在溶血磷脂酰胆碱分散体中的扩散速度更快。已根据这些数据进行结合估计,并与平衡透析研究获得的数据进行比较。表面张力测量表明,抗生素表现出最小的表面活性。这些结果已与其他研究中获得的数据相关联,并对报道的青霉素G和氨苄西林体内活性差异提出了一种可能的解释。