中国药师
中國藥師
중국약사
CHINA PHARMACIST
2014年
9期
1463-1466
,共4页
尼美舒利颗粒%生物等效性%药动学%高效液相色谱法
尼美舒利顆粒%生物等效性%藥動學%高效液相色譜法
니미서리과립%생물등효성%약동학%고효액상색보법
Nimesulide granules%Bioequivalence%Pharmacokinetics%HPLC
目的：评价2种国产尼美舒利颗粒在中国健康人体的生物等效性。方法：18名健康男性受试者随机交叉单剂量口服试验制药或参比制剂各200 mg。用高效液相色谱法测定血浆中尼美舒利的浓度；用DAS2.1软件计算主要药动学参数，并对2种药物进行生物等效性评价。结果：试验制药和参比制剂的主要药动学参数：Cmax分别为(9.28±2.05)和(9.41±2.31)μg·ml-1；Tmax分别为(3.50±1.86)和(3.56±1.65)h； T1/2分别为(3.43±0.85)和(3.38±0.68)h；AUC0-24分别为(77.78±18.42)和(81.69±23.50)μg·ml·h-1；AUC(0-∞)分别为(79.07±19.21)和(82.92±24.11)μg·ml·h-1。 ln(AUC0-24)、ln (AUC0-∞)、ln(Cmax)的90%可信区间分别为90.7%~107.9%、90.6%~111.2%和90.7%~103.0%。试验制药相对于参比制剂的生物利用度F为(96.7±37.6)%。结论：受试制剂和参比制剂生物等效。
目的：評價2種國產尼美舒利顆粒在中國健康人體的生物等效性。方法：18名健康男性受試者隨機交扠單劑量口服試驗製藥或參比製劑各200 mg。用高效液相色譜法測定血漿中尼美舒利的濃度；用DAS2.1軟件計算主要藥動學參數，併對2種藥物進行生物等效性評價。結果：試驗製藥和參比製劑的主要藥動學參數：Cmax分彆為(9.28±2.05)和(9.41±2.31)μg·ml-1；Tmax分彆為(3.50±1.86)和(3.56±1.65)h； T1/2分彆為(3.43±0.85)和(3.38±0.68)h；AUC0-24分彆為(77.78±18.42)和(81.69±23.50)μg·ml·h-1；AUC(0-∞)分彆為(79.07±19.21)和(82.92±24.11)μg·ml·h-1。 ln(AUC0-24)、ln (AUC0-∞)、ln(Cmax)的90%可信區間分彆為90.7%~107.9%、90.6%~111.2%和90.7%~103.0%。試驗製藥相對于參比製劑的生物利用度F為(96.7±37.6)%。結論：受試製劑和參比製劑生物等效。
목적：평개2충국산니미서리과립재중국건강인체적생물등효성。방법：18명건강남성수시자수궤교차단제량구복시험제약혹삼비제제각200 mg。용고효액상색보법측정혈장중니미서리적농도；용DAS2.1연건계산주요약동학삼수，병대2충약물진행생물등효성평개。결과：시험제약화삼비제제적주요약동학삼수：Cmax분별위(9.28±2.05)화(9.41±2.31)μg·ml-1；Tmax분별위(3.50±1.86)화(3.56±1.65)h； T1/2분별위(3.43±0.85)화(3.38±0.68)h；AUC0-24분별위(77.78±18.42)화(81.69±23.50)μg·ml·h-1；AUC(0-∞)분별위(79.07±19.21)화(82.92±24.11)μg·ml·h-1。 ln(AUC0-24)、ln (AUC0-∞)、ln(Cmax)적90%가신구간분별위90.7%~107.9%、90.6%~111.2%화90.7%~103.0%。시험제약상대우삼비제제적생물이용도F위(96.7±37.6)%。결론：수시제제화삼비제제생물등효。
Objective:To evaluate the bioequivalence of two kinds of domestic nimesulide granules in healthy volunteers. Meth-ods:In self-control and two-way crossover design, 18 healthy male volunteers were divided into two groups randomly. Each subject was given 100 mg test or reference nimesulide granules with single dose. The concentration of nimesulide in plasma was determined by HPLC. The concentration of nimesulide in plasma was calculated and compared statistically to evaluate the bioequivalence between the two kinds of granules by DAS 2. 1 software. Results:The main pharmacokinetic parameters of test and reference preparations were as follows:Cmax was(9. 28 ± 2. 05) and(9. 41 ± 2. 31)μg·ml-1;Tmax was(3. 50 ± 1. 86)and(3. 56 ± 1. 65)h;T1/2 was (3. 43 ± 0. 85) and(3.38 ±0.68)h;AUC0-24 was(77.78 ±18.42)and(81.69 ±23.50)μg·ml·h-1;AUC(0-∞) was (79.07 ±19.21)and(82.92 ± 24. 11)μg·ml·h-1, respectively. The 90% confidential interval of ln(AUC0-24), ln(AUC0-∞) and ln(Cmax) of the test preparation was 90. 7%-107. 9%,90. 6%-111. 2% and 90. 7%-103. 0%, respectively. The relative bioavailability was (96. 7 ± 37. 6)%. Con-clusion:The two nimesulide granules are bioequivalent.
