Josefsson K, Steinbakk M, Bergan T, Midtvedt T, Magni L
Chemotherapy. 1982;28(3):176-84. doi: 10.1159/000238073.
Pharmacokinetics of a new preparation of microencapsulated erythromycin base was studied in 16 healthy subjects. They received 250 mg base 6-hourly or 500 mg 12-hourly for 7 days. The mean maximal serum peaks (+/- SD) after morning doses on days 1, 2, 3, and 7 were 1.4 +/- 0.9, 3.2 +/- 1.1, 3.6 +/- 0.6, 3.5 +/- 1.2 mg/l after the 250-mg dose and 3.2 +/- 1.5, 3.7 +/- 2.1, 3.6 +/- 1.8, and 3.0 +/- 2.0 mg/l after the 500-mg dose. The mean 24-hour urine recoveries were 1.8 and 1.2%, the serum half-lives were (days 1-7) 1.4-2.1 h and 1.9-2.8 h for the 250-mg and 500-mg doses. The mean areas under the serum concentration curves (+/- SD) were 5.8 +/- 2.2, 11.9 +/- 2.2, and 15.3 +/- 5.1 mg . h . 1(-1) after 250 mg and 14.2 +/- 4.9, 16.4 +/- 7.6, and 14.3 +/- 9.0 mg . h . 1(-1) after 500 mg on days 1, 2, and 7. The inter- and intrasubject variability was larger after the 500-mg dose. The pharmacokinetic results indicate that both dosage alternatives are suitable and result in similar steady-state peak levels, but the initial dose should be 500 mg.
对16名健康受试者研究了一种新的微囊化红霉素碱制剂的药代动力学。他们每6小时服用250mg碱或每12小时服用500mg,共7天。第1、2、3和7天早晨给药后的平均最大血清峰浓度(±标准差),250mg剂量组分别为1.4±0.9、3.2±1.1、3.6±0.6、3.5±1.2mg/L,500mg剂量组分别为3.2±1.5、3.7±2.1、3.6±1.8、3.0±2.0mg/L。24小时尿回收率平均分别为1.8%和1.2%,250mg和500mg剂量组的血清半衰期(第1 - 7天)分别为1.4 - 2.1小时和1.9 - 2.8小时。第1、2和7天,250mg剂量后的血清浓度曲线下平均面积(±标准差)为5.8±2.2、11.9±2.2、15.3±5.1mg·h·L⁻¹,500mg剂量后的分别为14.2±4.9、16.4±7.6、14.3±9.0mg·h·L⁻¹。500mg剂量后的个体间和个体内变异性更大。药代动力学结果表明,两种给药方案均合适,且稳态峰水平相似,但初始剂量应为500mg。