Pharmacokinetics and tolerance of a new penem antibiotic,FCE 22101, in healthy volunteers after a single intravenous dose

Summary The clinical tolerance and pharmacokinetics of FCE 22101 (sodium (5R, 6S)-6-[(1R)-hydroxyethyl]-2-carbamoyloxymethyl-2-penem-3-carboxylate), a new penem antibiotic, have been studied after giving a single i.v. dose of 4 mg·kg^–1 to ten healthy male volunteers. The pharmacokinetics was estimated according to a two-compartment open model. The peak plasma concentration (C_max) was 15.5 (1.08) µg·ml^–1, mean (SEM). FCE 22101 was rapidly cleared from the systemic circulation [ =44.2 (4.2) min; CL=7.21 (0.47) ml·kg^–1·min^–1]. The mean apparent volume of distribution at steady-state was 246 (16.9) ml·kg^–1. The mean residence time relative to the 10 min infusion was 39.4 (1.5)min. Urinary recovery of FCE 22101 showed wide inter-subject variation, ranging from 10.2 to 53.6% of the dose. No subject complained of adverse effects.     

几种典型综合评价方法的比较

目的探讨几种评价方法的优缺点及适用范围。方法通过陈述TOPSIS法、层次分析法、模糊评价法等几种评价方法的基本思想及其差别,并举实例论证。结果列表得出了各种方法的优缺点及适用范围,为评价工作提供方法学参考。结论应根据不同的资料类型采取不同的方法,使得分析评价的结果最接近于真实结果;并注意多种评价方法的联合应用。     

右旋糖酐与氟碳乳剂稀释血液对心肌缺血时全血粘度与侧支循环影响的比较

用麻醉开胸狗对比观察了低分子右旋糖酐与氟碳乳剂稀释血液对急性心肌缺血时全血粘皮与侧支血流量变化的影响。结果表明,氟碳乳剂稀释血液除具有与右旋糖酐稀释血液相同的降低全血粘度、增加侧支血流量、提高缺血区心肌供血量/需血量比值等作用外,还可使血氧分压与活性氧明显增加,因而使缺血区心肌供氧量增加。     

3-偶氮甲基利福霉素抗结核作用的实验研究

3-偶氮甲基利福霉素又称FCE22250,在国内首先由四川抗菌素工业研究所研制成功,本文报道它的体内外抗结核菌活性及其在小鼠体内血药浓度的变化。 实验表明:(一)FCE22250对人型结核分枝杆菌H37Rv的抑菌作用与利福平、利福喷丁相近或略强。(二)FCE22250体内抗结核菌活性显著强于利福平,略优于利福喷丁。(三)FCE22250呈显著长效抗结核活性,给小鼠一次灌胃12mg/kg其抗结核活性的有效浓度可维持10～12天,而利福平在同样条件下最长维持1天,利福喷丁可维持7天。(四)FCE22250的小鼠血浆半衰期达37.7小时,利福平为4.0小时,利福喷丁为31小时。FCE22250给小鼠灌胃12mg/kg,9天后血浆中药物浓度的实测值为0.19微克/毫升(仍可达到其体外最小抑菌浓度)。FCE22250是迄今血浆半衰期最长的抗结核菌药物。     

Effects of FCE 20700, a new PGE2 derivative,on gastric acid secretion and cytoprotective processes in man

Summary The pharmacodynamic effects of FCE20700, a new PGE₂ derivative, have been investigated in 6 healthy volunteers given single intragastric (i.g.) and intraduodenal (i.d.) doses of 1 and 2 mg and placebo, according to a double-blind, within — subjects design. For 30–270 min following i.g. administration the effect of FCE20700 on peptone-stimulated gastric acid secretion (AS) was assessed by i.g. titration, and serum gastrin (G) levels were also determined. For the same period after i.d. dosing the effect of the compound on pentagastrin-stimulated AS and on mucoproteins and bicarbonate content in the gastric juice was measured. Blood pressure (BP), heart rate and possible side-effects were monitored. Following i.g. administration there was a moderate, dose-related, significant inhibition of AS; significant inhibition of G levels was observed only after the highest dose. After i.d. administration there was a very modest through dose-related and significant inhibition of AS; a brief maximal increase in mucoproteins and in bicarbonate levels was apparent after the 1 mg dose. After i.d. but not after i.g. administration of 2 mg there was a modest but significant decrease in BP. No side-effects of clinical relevance were reported. The results appear to suggest a major activity of FCE20700 on cytoprotection rather than in inhibiting gastric acid secretion. The observed change in BP may indicate that after i.d. administration there will be some systemic effects of FCE20700.