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单剂量及重复剂量服用依托红霉素和硬脂酸红霉素后的血浆水平。

Plasma levels following single and repeated doses of erythromycin estolate and erythromycin stearate.

作者信息

Welling P G, Elliott R L, Pitterle M E, Corrick-West H P, Lyons L L

出版信息

J Pharm Sci. 1979 Feb;68(2):150-5. doi: 10.1002/jps.2600680208.

Abstract

The pharmacokinetics of erythromycin and erythromycin 2'-propanoate were studied in healthy male volunteers following single and repeated doses of erythromycin stearate tablets, erythromycin estolate capsules, and a suspension. Estolate dosages gave rise to higher plasma levels of total drug than the stearate. However, the stearate yielded higher plasma levels of erythromycin base. Absorption of all dosage forms, except the suspension, was delayed, and pharmacokinetic interpretation of both single- and multiple-dose data required incorporation of an absorption lag time. The absorption of erythromycin stearate was inhibited by food and also by low fluid volumes in fasted subjects. Absorption of erythromycin estolate was increased in the presence of food and was not greatly affected by fluid volume. Although single-dose data poorly predicted circulating levels of erythromycin following repeated doses, trends observed after single doses were maintained during chronic treatment.

摘要

在健康男性志愿者中,对单次和重复剂量的硬脂酸红霉素片、依托红霉素胶囊及混悬液给药后,研究了红霉素和2'-丙酸红霉素的药代动力学。依托红霉素剂型产生的总药物血浆水平高于硬脂酸红霉素剂型。然而,硬脂酸红霉素剂型产生的红霉素碱血浆水平更高。除混悬液外,所有剂型的吸收均延迟,单剂量和多剂量数据的药代动力学解释都需要纳入吸收延迟时间。食物以及禁食受试者低液体量均会抑制硬脂酸红霉素的吸收。食物存在时依托红霉素的吸收增加,且不受液体量的很大影响。尽管单剂量数据难以预测重复给药后红霉素的循环水平,但单剂量后观察到的趋势在长期治疗期间得以维持。

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