中国新药与临床杂志
中國新藥與臨床雜誌
중국신약여림상잡지
CHINESE JOURNAL OF NEW DRUGS AND CLINICAL REMEDIES
2004年
4期
195-198
,共4页
戈升荣%王兰君%王晓珉%刘晓琰
戈升榮%王蘭君%王曉珉%劉曉琰
과승영%왕란군%왕효민%류효염
生物利用度%药动学%色谱法,高压液相%美洛昔康
生物利用度%藥動學%色譜法,高壓液相%美洛昔康
생물이용도%약동학%색보법,고압액상%미락석강
biological availability%pharmacokinetics%chromatography,high pressure liquid%meloxicam
目的:比较健康志愿者国产与进口美洛昔康片的人体药动学和相对生物利用度.方法:采用单次给药2周期交叉设计,HPLC法测定12名健康男性志愿者口服15 mg美洛昔康后血药浓度,计算药动学参数和国产片的相对生物利用度.结果:2种制剂的药时曲线符合一级吸收的一室开放模型.国产与进口片的药动学参数分别是AUC0-96 为 (67±s 14) mg·h·L-1和(64±15) mg·h·L-1;AUC0-∞为 (73±19) mg·h·L-1和(70±18) mg·h·L-1;Cmax 为(2.3±0.5) mg*L-1 和(1.6±0.3) mg·L-1;Tmax 为(2.0 ±1.6) h和(6±3) h;T(1)/(2)ke 为(25±6) h和(24±5) h;MRT 为(40±13) h and (39±8) h .方差分析表明两者AUC之间无显著差异(P>0.05),但两者的Cmax和Tmax之间有显著差异(P<0.05).结论:国产片的释药速率比进口片快,其相对生物利用度为(105±13) %.
目的:比較健康誌願者國產與進口美洛昔康片的人體藥動學和相對生物利用度.方法:採用單次給藥2週期交扠設計,HPLC法測定12名健康男性誌願者口服15 mg美洛昔康後血藥濃度,計算藥動學參數和國產片的相對生物利用度.結果:2種製劑的藥時麯線符閤一級吸收的一室開放模型.國產與進口片的藥動學參數分彆是AUC0-96 為 (67±s 14) mg·h·L-1和(64±15) mg·h·L-1;AUC0-∞為 (73±19) mg·h·L-1和(70±18) mg·h·L-1;Cmax 為(2.3±0.5) mg*L-1 和(1.6±0.3) mg·L-1;Tmax 為(2.0 ±1.6) h和(6±3) h;T(1)/(2)ke 為(25±6) h和(24±5) h;MRT 為(40±13) h and (39±8) h .方差分析錶明兩者AUC之間無顯著差異(P>0.05),但兩者的Cmax和Tmax之間有顯著差異(P<0.05).結論:國產片的釋藥速率比進口片快,其相對生物利用度為(105±13) %.
목적:비교건강지원자국산여진구미락석강편적인체약동학화상대생물이용도.방법:채용단차급약2주기교차설계,HPLC법측정12명건강남성지원자구복15 mg미락석강후혈약농도,계산약동학삼수화국산편적상대생물이용도.결과:2충제제적약시곡선부합일급흡수적일실개방모형.국산여진구편적약동학삼수분별시AUC0-96 위 (67±s 14) mg·h·L-1화(64±15) mg·h·L-1;AUC0-∞위 (73±19) mg·h·L-1화(70±18) mg·h·L-1;Cmax 위(2.3±0.5) mg*L-1 화(1.6±0.3) mg·L-1;Tmax 위(2.0 ±1.6) h화(6±3) h;T(1)/(2)ke 위(25±6) h화(24±5) h;MRT 위(40±13) h and (39±8) h .방차분석표명량자AUC지간무현저차이(P>0.05),단량자적Cmax화Tmax지간유현저차이(P<0.05).결론:국산편적석약속솔비진구편쾌,기상대생물이용도위(105±13) %.
AIM: To compare the pharmacokinetics and relative bioavailability of domestic and imported meloxicam tablets in healthy volunteers. METHODS: In a random two periods crossover study, 12 healthy male volunteers received a single dose of meloxicam 15 mg of two formulations respectively. The plasma concentration of meloxicam was determined by HPLC method. The pharmacokinetic parameters of the two preparations and the relative bioavailability of domestic tablets were calculated with statistical analysis. RESULTS: The concentration-time plots of the two preparations were in accordance with an open one-compartment model with first-order absorption. The main pharmacokinetic parameters of domestic and imported tablets were (67±s 14) mg·h·L-1 and (64±15) mg·h·L-1 for AUC0-96; (73±19) mg·h·L-1 and (70±18) mg·h·L-1 for AUC0-∞;(2.3±0.5) mg·L-1 and (1.6±0.3) mg·L-1 for Cmax;(2.0±1.6) h and (6±3) h for Tmax; (25±6) h and (24±5) h for T(1)/(2)ke; (40±13) h and (39±8) h for mean residence time (MRT), respectively. Variance analysis showed that there was significant difference in Cmax and Tmax but no significant difference in AUC between the two preparations. CONCLUSION: The release rate of the domestic meloxicam tablets is faster than that of the imported ones and the relative bioavailability of domestic tablets is (105±13) %.
