PHARMACOKINETIC STUDIES OF CLINDAMYCIN PHOSPHATE
PHARMACOKINETIC STUDIES OF CLINDAMYCIN PHOSPHATE
复制标题
DOI：
10.1002/j.1552-4604.1973.tb00208.x
复制
发表时间：
1973-01-01
影响因子：
2.9
通讯作者：
VANDENBOSCH, WD
中科院分区：
文献类型：
--
作者：
DEHAAN, RM;METZLER, CM;VANDENBOSCH, WD
C LINDAMYcmN 磷酸盐是抗生素克林霉素[7(S)-氯-7-脱氧林可霉素]的肠胃外制剂，作为治疗住院患者严重感染的药物，正在进行深入研究。克琳达-。霉素比母体化合物林可霉素对革兰氏阳性需氧菌活性更高，对革兰氏阳性和革兰氏阴性厌氧病原体（包括脆弱拟杆菌）也具有高活性；体外对敏感生物体（梭菌属除外）的最低抑菌浓度 (MIC) 一般低于 0.5 g/ml。’8 在体外，磷酸酯本身对细菌没有活性，但在体内很容易水解成具有微生物活性的克林霉素。 91#{176} 本文介绍了针对健康男性的六项药代动力学研究的结果以及一项测量一名患者的胆汁排泄生物活性的研究的结果。其中五项研究还被设计为耐受性研究；耐受性数据将在别处描述。这些研究的药代动力学方面的主要目的是为推荐克林霉素磷酸酯的剂量方案奠定基础。
C LINDAMYcmN phosphate, a parenteral preparation of the antibiotic clindamycin[7 (S)-chloro-7-deoxylincomycin], has been undergoing intensive investiga-tion as an agent for treating serious infections in hospitalized patients. Clinda-. mycin is more active than the parent compound, lincomycin, against gram-positive aerobes and highly active against both gram-positive and gram-negative anaerobic pathogens, including Bacteroides fragilis; the minimum inhibitory concentration (MIC) in vitro for susceptible organisms (except Clostridia spp.) is generally less than 0.5 g/ml.’8 In vitro the phosphate ester is itself inactive against bacteria, but in vivo it is readily hydrolyzed to microbiologically active clindamycin. 91#{176} This paper presents the results of six pharmacokinetic studies in healthy men and a study in which biliary excretion of bioactivity was measured in one patient. Five of the studies were also designed as tolerance studies; tolerance data will be described elsewhere. The chief aims of the pharmaeokinetic aspects of the studies were to establish a basis for recommending dosage regimens of clindamycin phos-