Pharmacokinetics of four different brands of colistimethate and formed colistin in rats

被引:69
作者
He, Hui [1 ]
Li, Ji-Chang [1 ,2 ]
Nation, Roger L. [1 ]
Jacob, Jovan [1 ]
Chen, Gong [1 ]
Lee, Hee Ji [1 ]
Tsuji, Brian T. [3 ]
Thompson, Philip E. [1 ]
Roberts, Kade [1 ]
Velkov, Tony [1 ]
Li, Jian [1 ]
机构
[1] Monash Univ, Monash Inst Pharmaceut Sci, Parkville, Vic 3052, Australia
[2] Northeast Agr Univ, Coll Vet Med, Harbin 150030, Peoples R China
[3] SUNY Buffalo, Sch Pharm & Pharmaceut Sci, Buffalo, NY 14260 USA
基金
中国国家自然科学基金;
关键词
elemental analysis; HPLC; intravenous administration; colistin base activity; CRITICALLY-ILL PATIENTS; PERFORMANCE LIQUID-CHROMATOGRAPHY; GRAM-NEGATIVE BACTERIA; HUMAN PLASMA; POPULATION PHARMACOKINETICS; BAD BUGS; METHANESULFONATE; STABILITY; DRUGS; POLYMYXINS;
D O I
10.1093/jac/dkt207
中图分类号
R51 [传染病];
学科分类号
100401 ;
摘要
Objectives: Very different labelling conventions are employed by different products of colistimethate (CMS), an inactive prodrug of colistin that is used as a last-line defence against Gram-negative 'superbugs'. This study examined the chemical composition and pharmacokinetics in rats of four commercial parenteral products of CMS. Methods: Contents per vial of four brands of CMS from three different continents were weighed (n = 3). Elemental analysis and HPLC examination were conducted. The pharmacokinetics of CMS and formed colistin were investigated for each product after intravenous administration in rats (28.1 mg/kg CMS; n = 4). Blood was collected over 180 min, and concentrations of CMS and colistin were measured followed by pharmacokinetic analysis. Results: X-GEN, Paddock and Atlantic products, labelled with 150 mg 'colistin base activity', contained 366.8 +/- 0.80, 340.6 +/- 0.08 and 380.0 +/- 5.97 mg CMS (sodium) per vial, respectively; while the Forest product (labelled with 2000000 IU) contained 159.3 +/- 1.75 mg CMS (sodium). The elemental compositions of the four products were similar; however, the HPLC profile of the Atlantic CMS was different from those of the other three products. The pharmacokinetics of CMS were generally comparable across brands; however, the molar ratios (%) of the AUC(0-180min) of colistin to CMS (1.68%+/- 0.35% to 3.29%+/- 0.43%) were significantly different (P = 0.0157). Conclusion: This is the first study to demonstrate that although different brands of CMS from various parts of the world have similar elemental compositions, they lead to different exposures to the microbiologically active formed colistin. The study has significant implications for the interpretation of pharmacological studies of CMS conducted in different parts of the world.
引用
收藏
页码:2311 / 2317
页数:7
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