Hoff S F, Fitzgerald R H, Kelly P J
J Bone Joint Surg Am. 1981 Jun;63(5):798-804.
The in vitro elution of penicillin and gentamicin from polymethylmethacrylate was studied qualitatively and quantitatively. Penicillin eluted poorly from Simplex P. Higher levels of penicillin eluted in sustained fashion from Palacos; concentrations of one microgram or more per gram of cement were recorded during the thirteen weeks of observation. Although the in vitro leaching of gentamicin from Palacos cement was similar to that of penicillin, there were two important differences: (1) most of the gentamicin leaching from the Palacos did so within the first twenty-four hours, and (2) the concentrations decreased to less than one microgram per gram of cement after the sixth week of observation. The in vivo elutions of penicillin and gentamicin from Palacos were studied in canine femora. The concentrations of penicillin and gentamicin in the endosteal bone at the bone-cement interface exceeded the concentrations found after intravenous administration of either agent. Bactericidal concentrations of gentamicin in osseous tissue persisted for seven months after implantation. Peak concentrations in serum following the depot administration of either penicillin or gentamicin occurred within thirty minutes of implantation. Concentrations of gentamicin in serum did not approach toxic levels. These data suggest that a high concentration of either penicillin or gentamicin can be obtained at the bone-cement interface--one of the vulnerable sites in total joint arthroplasty--for a prolonged period with the depot administration of these agents in acrylic bone cement. These osseous concentrations can be achieved without exposing the patient to elevated levels in serum and their potential toxic side effects.
对青霉素和庆大霉素从聚甲基丙烯酸甲酯中的体外洗脱情况进行了定性和定量研究。青霉素从Simplex P中的洗脱效果不佳。青霉素从Palacos中以持续的方式洗脱水平较高；在观察的十三周内，记录到每克骨水泥中有一微克或更高浓度的青霉素。虽然庆大霉素从Palacos骨水泥中的体外浸出情况与青霉素相似，但有两个重要差异：（1）从Palacos中浸出的大部分庆大霉素在最初的二十四小时内完成，（2）在观察的第六周后，浓度降至每克骨水泥低于一微克。在犬股骨中研究了青霉素和庆大霉素从Palacos中的体内洗脱情况。骨水泥界面处骨内膜骨中的青霉素和庆大霉素浓度超过了静脉注射这两种药物后发现的浓度。植入后，骨组织中庆大霉素的杀菌浓度持续了七个月。植入后三十分钟内，青霉素或庆大霉素长效制剂给药后血清中出现峰值浓度。血清中庆大霉素的浓度未接近毒性水平。这些数据表明，通过在丙烯酸骨水泥中使用这些药物的长效制剂，可以在全关节置换术中的一个易感染部位——骨水泥界面处，长时间获得高浓度的青霉素或庆大霉素。在不使患者暴露于血清中升高水平及其潜在毒性副作用的情况下，可以达到这些骨浓度。
