CAJ | 학술논문

目的：研究左氧氟沙星4种晶型在SD大鼠体内药动学差异，评价其优势药用晶型，探讨药物晶型物质状态对临床用药的影响。方法 SD大鼠灌胃给予不同晶型左氧氟沙星固体原料药，高效液相色谱法测定血左氧氟沙星浓度，非房室模型计算大鼠体内药动学参数并在不同晶型之间进行比对。结果大鼠灌胃给予左氧氟沙星晶Ⅰ、Ⅱ、Ⅲ、Ⅳ型后，血液中峰浓度（ Cmax ）分别为6.984，9.692，9.405，6.424 mg·L-1；达峰时间（ tmax ）分别为0.6，0.9，1.0，1.0 h；半衰期（t1/2）分别为4.207，2.970，4.857，1.695 h；药-时曲线下面积（AUC（0→12h））分别为31.478，42.385，32.406，31.636 mg·h·L-1。结论大鼠口服不同晶型左氧氟沙星后，利用专业软件DAS 3.0对测得的血药浓度数据进行药动学参数计算，左氧氟沙星4种晶型未发现差异有统计学意义，但检测结果表明晶Ⅱ型血药浓度最高，血药浓度维持时间长，可能作为优势药用晶型用于产品生产。
목적：연구좌양불사성4충정형재SD대서체내약동학차이，평개기우세약용정형，탐토약물정형물질상태대림상용약적영향。방법 SD대서관위급여불동정형좌양불사성고체원료약，고효액상색보법측정혈좌양불사성농도，비방실모형계산대서체내약동학삼수병재불동정형지간진행비대。결과대서관위급여좌양불사성정Ⅰ、Ⅱ、Ⅲ、Ⅳ형후，혈액중봉농도（ Cmax ）분별위6.984，9.692，9.405，6.424 mg·L-1；체봉시간（ tmax ）분별위0.6，0.9，1.0，1.0 h；반쇠기（t1/2）분별위4.207，2.970，4.857，1.695 h；약-시곡선하면적（AUC（0→12h））분별위31.478，42.385，32.406，31.636 mg·h·L-1。결론대서구복불동정형좌양불사성후，이용전업연건DAS 3.0대측득적혈약농도수거진행약동학삼수계산，좌양불사성4충정형미발현차이유통계학의의，단검측결과표명정Ⅱ형혈약농도최고，혈약농도유지시간장，가능작위우세약용정형용우산품생산。
Objective To study the pharmacokinetics difference of levofloxacin polymorphs in rats, evaluate the advantageous medical polymorph,and explore the effects of different polymorphs on clinical medicine. Methods Four crystal forms of levofloxacin were administered intragastrically to rats,and high performance liquid chromatography( HPLC)was used to measure the contents of levofloxacin in rat plasma. The pharmacokinetic parameters were calculated and compared Results After a single oral dose,the peak plasma concentration(Cmax)of crystal forms ofⅠ,Ⅱ,ⅢandⅣof levofloxacin was 6. 984,9. 692,9. 405,6.424 mg·L-1;the time to peak(tmax)was 0.6,0.9,1.0,1.0 h;the half-life(t1/2)was 4.207,2.97,4.857,1.695 h;theareaunderthecurve(AUC0→12h)was31.478,42.385,32.406,31.636mg·h·L-1. Conclusion Thereisnostatistically significant difference in pharmacokinetic parameters. However,compared with other crystal forms,plasma concentration of crystal form II is higher and maintained longer. Therefore,crystal form II of levofloxacin is an advantageous polymorph for medicine.