Kramer W G, Rensimer E R, Ericsson C D, Pickering L K
J Clin Pharmacol. 1984 Apr;24(4):181-6. doi: 10.1002/j.1552-4604.1984.tb01828.x.
The comparative bioavailability of chloramphenicol from intravenous succinate, oral palmitate, and oral base preparations was studied in a crossover manner in 12 adult patients. Chloramphenicol was administered at a dose of 1 Gm every 6 hours, and blood samples were collected at steady state. For the succinate study, total urine output was also collected. The bioavailability of active chloramphenicol from the succinate preparation averaged 85.8 +/- 42.3 and 78.8 +/- 50.1 per cent of the free base and palmitate forms, respectively. This lower availability appeared to be due to variable excretion of unchanged succinate in the urine, averaging 27 +/- 11 per cent of the dose. Regardless of dosage form or route of administration, plasma chloramphenicol concentrations remained in the therapeutic range (5 to 25 mg/liter) for the entire dosage interval, implying that no change needs to be made when changing dosage form or route of administration. The interpatient variability, however, supports the need for monitoring of plasma chloramphenicol concentrations, especially in newborn infants, persons with liver disease, or those receiving other medications that alter chloramphenicol metabolism.
在12名成年患者中，采用交叉试验的方式研究了琥珀酸氯霉素、棕榈酸氯霉素口服制剂和氯霉素口服碱制剂的相对生物利用度。氯霉素的给药剂量为每6小时1克，并在稳态时采集血样。在琥珀酸氯霉素的研究中，还收集了总尿量。琥珀酸氯霉素制剂中活性氯霉素的生物利用度分别平均为游离碱形式和棕榈酸形式的85.8±42.3%和78.8±50.1%。生物利用度较低似乎是由于尿液中琥珀酸未变化部分的排泄量可变，平均占剂量的27±11%。无论剂型或给药途径如何，在整个给药间隔期内，血浆氯霉素浓度均保持在治疗范围内（5至25毫克/升），这意味着在改变剂型或给药途径时无需进行调整。然而，患者间的变异性支持监测血浆氯霉素浓度的必要性，尤其是在新生儿、肝病患者或正在接受其他改变氯霉素代谢的药物治疗的患者中。
