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８名健康男性志愿者单剂静注和肌注１ｇ国产阿洛西林后的药物动力学、生物利用度的研究及阿洛西林对β－内酰胺酶的稳定性的测定结果显示：静注和肌注后药物在体内的转运过程符合二室开放模型。静注后即刻血药浓度为２１９．８４μｇ／ｍｌ。肌注后５ｍｉｎ血药浓度为１０．７９μｇ／ｍｌ，约３０ｍｉｎ达峰，峰浓度为４３．２４μｇ／ｍｌ。静注和肌注后分布相半衰期分别为０．１７和０．２９ｈ，消除相半衰期为１．６０和１．８４ｈ，药—时曲线下面积为１１５．９７和７１．８８μｇｈ／ｍｌ，生物利用度为６１．９８％。２４ｈ尿排泄率为７０．３１％和６８．５６％。本品对质粒和染色体介导的β－内酰胺酶均不稳定。
Eight healthy male volunteers single intravenous and intramuscular injection of 1g domestic azlocillin pharmacokinetics, bioavailability and azlocillin β-lactamase stability of the results showed that: intravenous and After intramuscular injection of drugs in vivo transport process in line with the two-compartment open model. Immediate intravenous plasma concentration of 219.84μg / ml. 5min after intramuscular injection of plasma concentration of 10.79μg / ml, about 30min peak, the peak concentration of 43.24μg / ml. The half-lives of 0.17 and 0.29 h after intravenous injection and intramuscular injection respectively, the elimination half-lives were 1.60 and 1.84 h, and the area under the drug-time curve was 115.97 and 71.88 μg / ml, respectively. The degree is 61.98%. 24h urinary excretion rate of 70.31% and 68.56%. This product is plasmid and chromosome-mediated β-lactamase are not stable.