Koyama A, Mori J, Tokuda H, Waku M, Anno H, Katayama T, Murakami K, Komatsu H, Hirata M, Arai T
Jpn J Antibiot. 1986 Mar;39(3):761-71.
Cefotiam (CTM) is a new cephalosporin with a broad spectrum of activity against both Gram-positive and Gram-negative microorganisms. Cephalosporins are widely used for prophylaxis of infections in patients undergoing thoracotomy. Augmentation by serrapeptase on tissue permeation of CTM was examined in 35 thoracotomy patients with lung cancer. The subjects were divided into two groups according to the method of the administration of CTM. Group I consisted of 17 subjects, each of whom received a single dose of 2 g of CTM alone by an instillation for 30 minutes. Group II consisted of 18 subjects, each of whom received a combination of CTM and serrapeptase; serrapeptase was given 2 tablets (10 mg) each time for three times/day until the day before surgery, and then CTM was administered by the same procedure. The following results were obtained: Individual difference was observed for the permeation of CTM into tissues. Pathologic differences also affected the permeation. Nevertheless, the CTM levels in pulmonary tissues reached about a half of those in the blood in both the single dose group and the combination group, hence sufficient concentrations exceeding MIC80 for main microorganisms that caused infections in the lung were obtained. The concentrations of CTM in inflammatory tissues have showed lower levels than those of normal tissues in both CTM single dose and the combination groups. Decrease of blood flow volume may have contributed to the reduction in levels of CTM in the inflammatory tissues. The ratio of the concentration of the drug in pulmonary tissues to that in the blood was 29.1 +/- 2.5% in the single dose group, and 44.2 +/- 6.0% in the combination group, the latter showing quite a significant increase (P less than 0.05). Combined administrations of CTM and serrapeptase deserves more trials in the case when surgical treatments of the lung are performed. An antiinflammatory effect of serrapeptase in the respiratory system is expected, and in addition, the combined use of CTM and serrapeptase should stimulate permeation of the antibiotic into tissues.
头孢替安（CTM）是一种新型头孢菌素，对革兰氏阳性菌和革兰氏阴性菌均有广泛的抗菌活性。头孢菌素广泛用于开胸手术患者的感染预防。在35例肺癌开胸手术患者中研究了舍雷肽酶对CTM组织渗透的增强作用。根据CTM的给药方法将受试者分为两组。第一组由17名受试者组成，每人通过30分钟滴注单独接受2g CTM的单次剂量。第二组由18名受试者组成，每人接受CTM和舍雷肽酶的联合治疗；舍雷肽酶每次给予2片（10mg），每日3次，直至手术前一天，然后通过相同程序给予CTM。获得了以下结果：观察到CTM向组织渗透存在个体差异。病理差异也影响渗透。然而，单剂量组和联合组肺组织中的CTM水平均达到血液中CTM水平的约一半，因此获得了超过引起肺部感染的主要微生物的MIC80的足够浓度。在CTM单剂量组和联合组中，炎症组织中CTM的浓度均低于正常组织。血流量的减少可能导致炎症组织中CTM水平的降低。单剂量组肺组织中药物浓度与血液中药物浓度之比为29.1±2.5%，联合组为44.2±6.0%，后者显示出相当显著的增加（P＜0.05）。在进行肺部手术治疗时，CTM和舍雷肽酶的联合给药值得更多试验。预计舍雷肽酶在呼吸系统中具有抗炎作用，此外，CTM和舍雷肽酶的联合使用应能刺激抗生素向组织中的渗透。
