中国临床药理学杂志
中國臨床藥理學雜誌
중국림상약이학잡지
THE CHINESE JOURNAL OF CLINICAL PHARMACOLOGY
2010年
1期
23-27
,共5页
赵立子%钟国平%薛新平%欧志敏%曾桂雄%黄丽惠%马中富%陈孝%黄民
趙立子%鐘國平%薛新平%歐誌敏%曾桂雄%黃麗惠%馬中富%陳孝%黃民
조립자%종국평%설신평%구지민%증계웅%황려혜%마중부%진효%황민
头孢丙烯%高效液相色谱%药代动力学%生物等效性
頭孢丙烯%高效液相色譜%藥代動力學%生物等效性
두포병희%고효액상색보%약대동역학%생물등효성
cefprozil%HPLC%pharmacokinetics%bioequivalence
目的 研究2种国产头孢丙烯片(头孢类抗生素)在健康人体内的药代动力学过程,并评价这2种制剂的生物等效性.方法 20例健康成年男性受试者随机分组,自身对照,单次口服头孢丙烯片1 g后,用高效液相色谱法测定头孢丙烯顺式及反式异构体的血浆浓度,用非房室模型法计算各主要药代动力学参数,并进行方差分析和生物等效性评价.结果 顺式异构体:参比制剂与受试制剂的t_(max)分别为(2.4±1.0),(2.3±0.8)h;C_(max)分别为(15.4±3.5),(14.8±2.8)μg·mL~(-1);t_(1/2)分别为(1.4±0.1),(1.4±0.1)h;MRT分别为(3.4±0.6),(3.4±0.6)h;AUC_(0-1)分别为(61.2±10.6),(60.3±11.4)μg·h·mL~(-1);AUC_(0-∞)分别为(64.7±11.2),(64.5±11.7)μg·h·mL~(-1);受试制剂相对于参比制剂的生物利用度为(99.3±14.5)%.反式异构体:参比制剂与受试制剂的t_(max)分别为(2.4±0.9),(2.4±0.9)h;C_(max)分别为(1.6±0.3),(1.5±0.3)μg·mL~(-1);t_(1/2)分别为(1.2±0.2),(1.5±0.6)h;MRT分别为(3.2±0.7),(3.2±0.7)h;AUC_(0-t)分别为(6.1±1.4),(5.6±1.3)μg·h·mL~(-1);AUC_(0-∞)分别为(6.1±1.4),(5.6±1.3)μg·h·mL~(-1);受试制剂相对于参比制剂的生物利用度为(94.0±17.5)%.结论 受试制剂与参比制剂具有生物等效性.
目的 研究2種國產頭孢丙烯片(頭孢類抗生素)在健康人體內的藥代動力學過程,併評價這2種製劑的生物等效性.方法 20例健康成年男性受試者隨機分組,自身對照,單次口服頭孢丙烯片1 g後,用高效液相色譜法測定頭孢丙烯順式及反式異構體的血漿濃度,用非房室模型法計算各主要藥代動力學參數,併進行方差分析和生物等效性評價.結果 順式異構體:參比製劑與受試製劑的t_(max)分彆為(2.4±1.0),(2.3±0.8)h;C_(max)分彆為(15.4±3.5),(14.8±2.8)μg·mL~(-1);t_(1/2)分彆為(1.4±0.1),(1.4±0.1)h;MRT分彆為(3.4±0.6),(3.4±0.6)h;AUC_(0-1)分彆為(61.2±10.6),(60.3±11.4)μg·h·mL~(-1);AUC_(0-∞)分彆為(64.7±11.2),(64.5±11.7)μg·h·mL~(-1);受試製劑相對于參比製劑的生物利用度為(99.3±14.5)%.反式異構體:參比製劑與受試製劑的t_(max)分彆為(2.4±0.9),(2.4±0.9)h;C_(max)分彆為(1.6±0.3),(1.5±0.3)μg·mL~(-1);t_(1/2)分彆為(1.2±0.2),(1.5±0.6)h;MRT分彆為(3.2±0.7),(3.2±0.7)h;AUC_(0-t)分彆為(6.1±1.4),(5.6±1.3)μg·h·mL~(-1);AUC_(0-∞)分彆為(6.1±1.4),(5.6±1.3)μg·h·mL~(-1);受試製劑相對于參比製劑的生物利用度為(94.0±17.5)%.結論 受試製劑與參比製劑具有生物等效性.
목적 연구2충국산두포병희편(두포류항생소)재건강인체내적약대동역학과정,병평개저2충제제적생물등효성.방법 20례건강성년남성수시자수궤분조,자신대조,단차구복두포병희편1 g후,용고효액상색보법측정두포병희순식급반식이구체적혈장농도,용비방실모형법계산각주요약대동역학삼수,병진행방차분석화생물등효성평개.결과 순식이구체:삼비제제여수시제제적t_(max)분별위(2.4±1.0),(2.3±0.8)h;C_(max)분별위(15.4±3.5),(14.8±2.8)μg·mL~(-1);t_(1/2)분별위(1.4±0.1),(1.4±0.1)h;MRT분별위(3.4±0.6),(3.4±0.6)h;AUC_(0-1)분별위(61.2±10.6),(60.3±11.4)μg·h·mL~(-1);AUC_(0-∞)분별위(64.7±11.2),(64.5±11.7)μg·h·mL~(-1);수시제제상대우삼비제제적생물이용도위(99.3±14.5)%.반식이구체:삼비제제여수시제제적t_(max)분별위(2.4±0.9),(2.4±0.9)h;C_(max)분별위(1.6±0.3),(1.5±0.3)μg·mL~(-1);t_(1/2)분별위(1.2±0.2),(1.5±0.6)h;MRT분별위(3.2±0.7),(3.2±0.7)h;AUC_(0-t)분별위(6.1±1.4),(5.6±1.3)μg·h·mL~(-1);AUC_(0-∞)분별위(6.1±1.4),(5.6±1.3)μg·h·mL~(-1);수시제제상대우삼비제제적생물이용도위(94.0±17.5)%.결론 수시제제여삼비제제구유생물등효성.
Objective To study the pharmacokineties and bioequiva-lenee of two demostic cefprozil tablets.Methods Twenty healthy volun-teers were randomized into two groups,whose plasma concentrations of cis and trans isomers of eefprozil were determined at different time after single oral dose of 1 g cefprozil tablets by own control by HPLC method.The pharmacokinetic pammeters were computed and which were experi-enced variance analysis.Results Gis cefprozil:the main pharmaeoki-netic parameters of refe:rence and trial cefprozil tablets were as follows:t_(max) were(2.4±1.0),(2.3±0.8)h;C_(max) were(15.4±3.5),(14.8±2.8)μg·mL~(-1);t_(1/2) were(1.4±0.1),(1.4±0.1)h;MRT were (3.4±0.6),(3.4±0.6)h;AUC_(0-t) were(61.2±10.6),(60.3±11.4)μg·h·mL~(-1);AUC_(0-∞) were(64.7±11.2),(64.5±11.7)μg·h·mL~(-1),respectively.Trans cefprozil:the relative bioavailability of the trial preparation was(99.3±14.5)%.Trans cefprozil:the main pharmacokinetic parameters of reference and trial cefprozil tablets were as follows:t_(max) were(2.4±0.9),(2.4±0.9)h;C_(max) were(1.6±0.3),(1.5±0.3)μg·mL~(-1);t_(1/2) were(1.2±0.2),(1.5±0.6)h;MRT were(3.2±0.7),(3.2±0.7)h;AUC_(0-t) were(6.1±1.4),(5.6±1.3)μg·h·mL~(-1);AUC_(0-∞) were(6.1±1.4),(5.6±1.3)μg·h·mL~(-1),respectively.The relative bioavailability of the trial preparation was(94.0±17.5)%.Conclusion The results shows that the trial preparation and the reference prepara-tion of cefprozil were bioequivalent.
