PHARMACOKINETICS AND SUCTION BLISTER FLUID PENETRATION OF A SEMISYNTHETIC INJECTABLE STREPTOGRAMIN RP-59500 (RP-57669 RP-54476)

被引:11
作者
BERNARD, E [1 ]
BENSOUSSAN, M [1 ]
BENSOUSSAN, F [1 ]
ETIENNE, S [1 ]
CAZENAVE, I [1 ]
CARSENTIETESSE, E [1 ]
LEROUX, Y [1 ]
MONTAY, G [1 ]
DELLAMONICA, P [1 ]
机构
[1] RHONE POULENC RORER,F-92165 ANTONY,FRANCE
关键词
D O I
10.1007/BF02276064
中图分类号
R51 [传染病];
学科分类号
100401 [流行病与卫生统计学];
摘要
RP 59500 is a new semisynthetic injectable streptogramin with excellent activity against most gram-positive bacteria. In order to assess its potential for the treatment of tissue infections, the pharmacokinetics and penetration into suction blister fluid were studied in a pilot phase I study in six male volunteers following a single infusion of 12 mg/kg over 1 h. Plasma and suction blister fluid concentrations were determined by microbiological assay. The mean peak concentration in plasma was 8.65 mg/l at the end of infusion. The mean plasma elimination half-life was 1.48 h. The mean peak concentration in interstitial fluid was 2.41 mg/l and was reached after Ih in two volunteers and after 2 h in the other four. The mean percentage penetration for the interval 0-6 h was 82.5 %. RP 59500 was still detectable in interstitial fluid at 6 h at a mean concentration of 0.92 +/- 0.25 mg/l. The data of this pilot study demonstrate good penetration of RP 59500 into non-inflammatory interstitial fluid.
引用
收藏
页码:768 / 771
页数:4
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