Iwasawa T
Jpn J Antibiot. 1975 Aug;28(4):584-94.
As the results of laboratory and clinical investigation with a new tetracycline derivate, PT-122M (doxycycline) was performed with the results which may lead to the following conclusions. 1) In vitro antibacterial activity: The minimal inhibitory concentration of doxycycline (DOTC) was measured by an agar plate dilution method. The MIC of DOTC against 60 strains of coagulase-positive Staphylococcus aureus isolated from otorrhoea was distributed over a range of 0.2 approximately 1.56 mcg/ml and 12.5 approximately 50 mcg/ml. Furthermore, Escherichia coli, Proteus mirabilis and Klebsiella pneumoniae was 3.13 to 100 mcg/ml. 2) Concentration in blood: The blood level of DOTC in healthy adults who were given 100 mg of DOTC intravenous reached maximum of 1.97 mcg/ml on the average 15 minutes after injection. Even at 12 hours after intravenous injection clinically effective serum DOTC concentration of 0.47 mcg/ml was still demonstrable. 3) CLINICAL RESULTS: PT-122M (DOCT) was intravenously injected into 30 cases with typical infection in the field of otorhinolaryngology. It was excellent in 15 cases, good in 10 cases, fair in 3 cases, and poor in 2 cases. When the cases in which it was excellent and good were considered together, good results were obtained in 25 cases, a ratio of effectiveness being 83 per cent. 4) Side effect: The comparative examination of hepatic function, electrolyte and auditory acuity before and after injection showed no significant disturbance. No side effect was shown with the intravenous injection.
作为对一种新型四环素衍生物PT - 122M(强力霉素)进行实验室和临床研究的结果,得到了可能导致以下结论的结果。1)体外抗菌活性:采用琼脂平板稀释法测定强力霉素(DOTC)的最低抑菌浓度。DOTC对从耳漏中分离出的60株凝固酶阳性金黄色葡萄球菌的MIC分布在0.2至约1.56 mcg/ml和12.5至约50 mcg/ml范围内。此外,大肠杆菌、奇异变形杆菌和肺炎克雷伯菌的MIC为3.13至100 mcg/ml。2)血液中的浓度:给健康成年人静脉注射100 mg DOTC后,血液中DOTC水平在注射后平均15分钟达到最高值1.97 mcg/ml。即使在静脉注射12小时后,仍可检测到临床有效血清DOTC浓度为0.47 mcg/ml。3)临床结果:将PT - 122M(DOCT)静脉注射到30例耳鼻喉科典型感染病例中。其中15例效果极佳,10例良好,3例尚可,2例较差。将效果极佳和良好的病例合并考虑,25例取得了良好效果,有效率为83%。4)副作用:注射前后肝功能、电解质和听力的对比检查未显示明显干扰。静脉注射未显示副作用。