CAJ | 학술논문

目的：建立测定人体血浆中头孢地尼浓度的UPLC－MS／MS方法，评价3种头孢地尼口服药物在健康人体内的生物等效性。方法随机、自身前后三交叉的试验设计。24名健康男性受试者单剂量口服3种头孢地尼100 mg，用UPLC－MS／MS法测定其血药浓度，计算主要药代动力学参数及相对生物利用度，评价3种药物的生物等效性。结果头孢地尼的线性范围为11.50～2300.00 ng· mL－1，批内、批间精密度（ RSD）均小于10％。受试药物（片剂，分散片）与参比药物（胶囊）的主要药代动力学参数为， tmax分别为（3.00±0.80），（3.20±0.90）和（3.50±0.70） h； Cmax分别为（548.96±184.58），（607.09±236.38）和（570.18±172.37） ng· mL－1；t1／2分别为（2.00±0.30），（1.90±0.40）和（1.90±0.30） h， AUC0－t分别为（2755.35±956.10），（3037.49±1014.42）和（2756.43±804.06） ng· mL－1· h。头孢地尼片和头孢地尼分散片分别以胶囊为对照，相对生物利用度分别为（104.2±37.5）％和（111.8±30.3）％。结论建立的分析方法灵敏、快速、准确。3种头孢地尼在健康人体内的生物等效。
목적：건립측정인체혈장중두포지니농도적UPLC－MS／MS방법，평개3충두포지니구복약물재건강인체내적생물등효성。방법수궤、자신전후삼교차적시험설계。24명건강남성수시자단제량구복3충두포지니100 mg，용UPLC－MS／MS법측정기혈약농도，계산주요약대동역학삼수급상대생물이용도，평개3충약물적생물등효성。결과두포지니적선성범위위11.50～2300.00 ng· mL－1，비내、비간정밀도（ RSD）균소우10％。수시약물（편제，분산편）여삼비약물（효낭）적주요약대동역학삼수위， tmax분별위（3.00±0.80），（3.20±0.90）화（3.50±0.70） h； Cmax분별위（548.96±184.58），（607.09±236.38）화（570.18±172.37） ng· mL－1；t1／2분별위（2.00±0.30），（1.90±0.40）화（1.90±0.30） h， AUC0－t분별위（2755.35±956.10），（3037.49±1014.42）화（2756.43±804.06） ng· mL－1· h。두포지니편화두포지니분산편분별이효낭위대조，상대생물이용도분별위（104.2±37.5）％화（111.8±30.3）％。결론건립적분석방법령민、쾌속、준학。3충두포지니재건강인체내적생물등효。
Objective To establish a high performance liquid chroma-tography-tandem mass spectrometry ( UPLC-MS/MS) method to deter-mination the plasma concentration of cefdinir and to study the pharmaco-kinctics and bioequivalence of three kinds of cefdinir formulations in healthy volunteers.Methods In a randomized, 3 way-crossover and self-control study, 24 healthy male volunteers were orally administrated with three kinds of cefdinir formulations ( test sample and reference sam-ple) 100 mg.The concentrations of cefdinir in plasma were determined by LC-MS/MS.The main pharmacokinetic parameters were calculated.Results The method was validated by investigating the accuracy and precision for intra and inter -day runs in a linear concentration from 11.50-2300.00 ng· mL-1.The main pharmacokinetic parameters of test (cefdinir tables A drug, cefdinir dispersible tables B drug ) and reference (cefdinir capsules, C drug ) formulations in plasma were shown as follows:tmax were (3.00 ±0.80),(3.20 ±0.90) and (3.50 ±0.70) h ; Cmax were (548.96 ±184.58 ), ( 607.09 ±236.38 ) and ( 570.18 ±172.37 ) ng· mL-1;t1/2 were ( 2.00 ±0.30),(1.90 ±0.40)and (1.90 ±0.30) h; AUC0-t were ( 2755.35 ±956.10 ) , ( 3037.49 ±1014.42 ) and (2756.43 ±804.06 ) ng · mL-1 · h, respectively.The relative bioavailability F were ( 104.20 ±37.50 )% and (111.50 ±29.70)%.Conclusion The method was proved to be accurate, rapid and sensitive.The three kinds of cefdinir formulations are bioequivalent in healthy volunteers.