Tinkler A E, Shannon R
Bull World Health Organ. 1966;35(6):857-62.
In order to investigate the reliability with which a given dose of benzathine penicillin will result in predictable ranges of penicillinaemia on any particular day during the week after injection, ambulant adult males were injected with 2 400 000 IU of "all-purpose" penicillin (600 000 IU potassium penicillin G, 600 000 IU procaine penicillin G and 1 200 000 IU of benzathine penicillin). Penicillin serum assays were performed, 24 each day, from the third to the seventh day after injection (120 assays in all).Statistical evaluation of the results showed that the means of the groups of 24 assays fell within narrow ranges, indicating that the long-acting component (benzathine penicillin) gives reliable daily ranges in a high proportion of cases. The results of a previous trial, using half the present dosage (1.2 mega-units of "all-purpose" penicillin) were compared statistically with those of the present trial. A very satisfactory degree of correlation between dosage and resulting daily serum concentration was observed-in general double the dose yielded double the daily concentration. The many factors which affect absorption rate are discussed and it is suggested that preparations which depend on an oily gel to delay absorption add an avoidable factor to the list of variables which may play an important part in producing the significant differences in serum levels commonly reported after the use of PAM preparations. The narrow ranges of penicillinaemia observed after 1.2 mega-units and 2.4 mega-units of benzathine penicillin and the degree of correlation observed in general between dose and resulting serum levels suggest that a large-scale controlled series of parallel trials should be undertaken to compare the relative long-acting qualities of PAM and benzathine penicillin.
为了研究注射苄星青霉素后一周内的任何一天,给予特定剂量的苄星青霉素能使青霉素血症达到可预测范围的可靠性,对能自由活动的成年男性注射240万国际单位的“通用”青霉素(60万国际单位青霉素G钾、60万国际单位普鲁卡因青霉素G和120万国际单位苄星青霉素)。在注射后的第三天至第七天,每天进行24次青霉素血清检测(共120次检测)。结果的统计评估表明,24次检测组的平均值落在狭窄范围内,这表明长效成分(苄星青霉素)在很大比例的病例中能给出可靠的每日范围。将之前使用当前剂量一半(120万国际单位“通用”青霉素)的试验结果与当前试验结果进行了统计学比较。观察到剂量与每日血清浓度之间具有非常令人满意的相关性——一般来说,剂量加倍会使每日浓度加倍。讨论了影响吸收速率的诸多因素,并指出依赖油性凝胶来延缓吸收的制剂在可能导致使用青霉素普鲁卡因酰胺(PAM)制剂后血清水平常见显著差异的变量清单中增加了一个可避免的因素。120万国际单位和240万国际单位苄星青霉素后观察到的青霉素血症狭窄范围以及一般观察到的剂量与血清水平之间的相关性程度表明,应该进行大规模的对照平行试验系列,以比较PAM和苄星青霉素的相对长效特性。