Cooper C E, Slocombe B, White A R
Beecham Pharmaceuticals Research Division, Betchworth, Surrey, UK.
J Antimicrob Chemother. 1990 Sep;26(3):371-80. doi: 10.1093/jac/26.3.371.
Concentrations of amoxycillin/clavulanic acid achievable in the respiratory tract following oral dosage were assessed for in-vitro activity against beta-lactamase-producing strains of Branhamella catarrhalis and Haemophilus influenzae. In agar-dilution studies, 8 mg amoxycillin/l was required to inhibit 45 strains of beta-lactamase-producing B. catarrhalis, whereas all the strains were inhibited by 0.5 mg amoxycillin/l in the presence of 0.01 mg clavulanic acid/l. Similarly, 0.1 mg amoxycillin plus 0.05 mg clavulanic acid/l were bactericidal against beta-lactamase-producing strain of B. catarrhalis and prevented regrowth within 24 h. In tests against 43 beta-lactamase-producing strains of H. influenzae, concentrations of up to 128 mg amoxycillin/l were required for inhibition, whereas 32 strains (75%) were fully sensitive to amoxycillin (MIC 0.5 mg/l) in the presence of 0.12 mg clavulanic acid/l. These concentrations of amoxycillin/clavulanic acid were also bactericidal for a beta-lactamase-producing strain of H. influenzae. The study therefore showed that amoxycillin/clavulanic acid, at concentrations similar to those likely to be achieved in the respiratory tract following oral dosage, was bactericidal in vitro for beta-lactamase-producing isolates of B.catarrhalis and H. influenzae.
评估了口服给药后呼吸道中可达到的阿莫西林/克拉维酸浓度对产β-内酰胺酶的卡他莫拉菌和流感嗜血杆菌菌株的体外活性。在琼脂稀释研究中,抑制45株产β-内酰胺酶的卡他莫拉菌需要8mg/L的阿莫西林,而在存在0.01mg/L克拉维酸的情况下,所有菌株均被0.5mg/L的阿莫西林抑制。同样,0.1mg阿莫西林加0.05mg/L克拉维酸对产β-内酰胺酶的卡他莫拉菌菌株具有杀菌作用,并能在24小时内防止其再生长。在针对43株产β-内酰胺酶的流感嗜血杆菌菌株的试验中,抑制作用需要高达128mg/L的阿莫西林浓度,而在存在0.12mg/L克拉维酸的情况下,32株(75%)对阿莫西林完全敏感(MIC为0.5mg/L)。这些阿莫西林/克拉维酸浓度对产β-内酰胺酶的流感嗜血杆菌菌株也具有杀菌作用。因此,该研究表明,阿莫西林/克拉维酸在口服给药后呼吸道中可能达到的浓度下,对产β-内酰胺酶的卡他莫拉菌和流感嗜血杆菌分离株在体外具有杀菌作用。