米诺环素的药效学研究

Pharmacodynamics study on minocycline

国产米诺环素（ｍｉｎｏｃｙｃｌｉｎｅ，ＭＩＮＯ）的体内外抗菌活性研究结果表明：ＭＩＮＯ是一个对革兰氏阳性菌和革兰氏阴性菌均有较强抗菌活性的广谱抗生素，对金葡球菌、表葡球菌的抗菌活性优于四环素（ＴＣ）、青霉素（ＰＣＧ）、麦迪霉素（ＭＤＭ）、庆大霉素（ＧＭ）和依诺沙星（ＥＮＸ），并对耐四环素金葡球菌和表葡球菌有很强的抗菌活性。ＭＩＮＯ对化脓性链球菌的抗菌活性优于ＴＣ、ＭＤＭ、ＧＭ、ＥＮＸ，弱于ＰＣＧ；对大肠杆菌、肺炎克雷伯氏菌的抗菌活性优于ＴＣ、ＧＭ，弱于ＥＮＸ；对变形杆菌的抗菌活性优于ＴＣ，弱于ＧＭ、ＥＮＸ。口服ＭＩＮＯ对金葡球菌感染小鼠的ＥＤ５０为０．９９ｍｇ／ｋｇ，优于强力霉素（ＤＯＸＹ）和ＴＣ；对大肠杆菌感染小鼠的ＥＤ５０为１０．９６ｍｇ／ｋｇ，优于ＴＣ，与ＤＯＸＹ的ＥＤ５０无显著性差异；对耐ＴＣ金葡球菌感染小鼠的ＥＤ５０为０．６５ｍｇ／ｋｇ，明显优于ＤＯＸＹ和ＴＣ。杀菌试验表明：ＭＩＮＯ在２～４ＭＩＣ时，对金葡球菌和大肠杆菌具有杀菌作用。

The in vitro and in vivo antimicrobial activities of minocycline (MINO) have been studied in this paper. The experimental results indicated that: MINO is a broad spectrum antibiotic highly active against both Gram postitive and Gram negative bacteria. The antibacterial potency of MINO was superior to those of tetracycline (TC), benzy lpenicillin (PCG), midecamycin (MDM), gentamicin (GM) and enoxacin (ENX) against S.aureus and S.epiderimidis . MINO also has a antibacterial activity against TC resistant S.aureus and TC resistant S.epidermidis . Against S.pyogenes the activity of MINO was superior to those of TC、MDM、GM、ENX and inferior to that of PCG. The antibacterial activity of MINO was superior to those of TC、GM and inferior to that of ENX against E.coli and K.pneumoniae , superior to that of TC and inferior to those of GM, ENX against proteus. For experimental infection with S.aureus and E.coli in mice, MINO showed a superior protective efficacy to TC and DOXY. The ED 50 s of MINO were 0.99 and 0.65mg/kg against S.aureus 15 and TC resist S.aureus 1206, and 10.96mg/kg against E.coli 1515, respectively. The MBCs of MINO ranged from two to four times the MICs against S.aureus and E.coli .