中国药业
中國藥業
중국약업
China Pharmaceuticals
2015年
21期
71-74
,共4页
杨自豪%刘嘉%龙远华%李卫平
楊自豪%劉嘉%龍遠華%李衛平
양자호%류가%룡원화%리위평
尼莫地平%药代动力学%大鼠%食物%高效液相色谱串联质谱法
尼莫地平%藥代動力學%大鼠%食物%高效液相色譜串聯質譜法
니막지평%약대동역학%대서%식물%고효액상색보천련질보법
nimodipne%pharmacokinetics%rat%food%HPLC-MS/MS
目的 建立高效液相色谱串联质谱(HPLC-MS/MS)法测定大鼠血浆中尼莫地平的质量浓度,并研究食物对大鼠体内尼莫地平药代动力学的影响.方法 将18只雄性SD大鼠随机分成3组,分别于空腹、进食标准餐和进食高脂餐后灌胃尼莫地平20 mg/kg,采用HPLC-MS/MS法测定大鼠血浆中尼莫地平浓度,用WinNonlin 6. 3软件计算主要药代动力学参数.结果 大鼠于空腹、进食标准餐和进食高脂餐后灌胃给予尼莫地平的主要药代动力学参数峰浓度( Cmax )分别为(19. 19 ± 4. 76)ng/mL,(30. 14 ± 7. 91)ng/mL,(34. 39 ± 8. 03)ng/mL,达峰时间( Tmax )分别为0. 96 h,0. 79 h和0. 75 h,药时曲线下面积( AUCinf )分别为(94. 47 ± 17. 24)ng/(mL·h),(139. 6 ± 32. 9)ng/(mL·h),(148. 1 ± 34. 2)ng/(mL·h);大鼠进食后给药的药代动力学参数与空腹相比,均有显著性差异( P<0. 05),而标准餐组和高脂餐组间的差异无统计学意义.结论 进食可显著提高尼莫地平在大鼠体内的吸收速度和程度.
目的 建立高效液相色譜串聯質譜(HPLC-MS/MS)法測定大鼠血漿中尼莫地平的質量濃度,併研究食物對大鼠體內尼莫地平藥代動力學的影響.方法 將18隻雄性SD大鼠隨機分成3組,分彆于空腹、進食標準餐和進食高脂餐後灌胃尼莫地平20 mg/kg,採用HPLC-MS/MS法測定大鼠血漿中尼莫地平濃度,用WinNonlin 6. 3軟件計算主要藥代動力學參數.結果 大鼠于空腹、進食標準餐和進食高脂餐後灌胃給予尼莫地平的主要藥代動力學參數峰濃度( Cmax )分彆為(19. 19 ± 4. 76)ng/mL,(30. 14 ± 7. 91)ng/mL,(34. 39 ± 8. 03)ng/mL,達峰時間( Tmax )分彆為0. 96 h,0. 79 h和0. 75 h,藥時麯線下麵積( AUCinf )分彆為(94. 47 ± 17. 24)ng/(mL·h),(139. 6 ± 32. 9)ng/(mL·h),(148. 1 ± 34. 2)ng/(mL·h);大鼠進食後給藥的藥代動力學參數與空腹相比,均有顯著性差異( P<0. 05),而標準餐組和高脂餐組間的差異無統計學意義.結論 進食可顯著提高尼莫地平在大鼠體內的吸收速度和程度.
목적 건립고효액상색보천련질보(HPLC-MS/MS)법측정대서혈장중니막지평적질량농도,병연구식물대대서체내니막지평약대동역학적영향.방법 장18지웅성SD대서수궤분성3조,분별우공복、진식표준찬화진식고지찬후관위니막지평20 mg/kg,채용HPLC-MS/MS법측정대서혈장중니막지평농도,용WinNonlin 6. 3연건계산주요약대동역학삼수.결과 대서우공복、진식표준찬화진식고지찬후관위급여니막지평적주요약대동역학삼수봉농도( Cmax )분별위(19. 19 ± 4. 76)ng/mL,(30. 14 ± 7. 91)ng/mL,(34. 39 ± 8. 03)ng/mL,체봉시간( Tmax )분별위0. 96 h,0. 79 h화0. 75 h,약시곡선하면적( AUCinf )분별위(94. 47 ± 17. 24)ng/(mL·h),(139. 6 ± 32. 9)ng/(mL·h),(148. 1 ± 34. 2)ng/(mL·h);대서진식후급약적약대동역학삼수여공복상비,균유현저성차이( P<0. 05),이표준찬조화고지찬조간적차이무통계학의의.결론 진식가현저제고니막지평재대서체내적흡수속도화정도.
Objective To develop an HPLC-MS/MS method for the determination of nimodipine in rat plasma, and to study the food effect on pharmacokinetics of nimodipine in rats. Methods 18 male SD rats were randomly divided into 3 groups, and were gavaged with nimodipine at a dose of 20 mg/kg under fasting conditions, with a standard meal or with a high-fat meal. The concentrations of nimodipine in rat plasma were analyzed with HPLC -MS/MS system, and WinNonlin 6. 3 software was utilized to perform the pharmacokinetic parameters calculation. Results The mean Cmax, Tmax and AUCinf were (19. 19 ± 4. 76), (30. 14 ± 7. 91) and (34. 39 ± 8. 03) ng/mL, 0. 96, 0. 79 and 0. 75 h, (94. 47 ± 17. 24), (139. 6 ± 32. 9) and (148. 1 ± 34. 2) ng/ (mL· h) under fasting conditions, with a standard meal or with a high-fat meal in rats. Administered with food showed influence on the pharmacokinetics of nimodipine, with Cmax, Tmax and AUCinf significantly increased compared with fasting group ( P < 0. 05 ) , but no significant differences were found be-tween the standard meal and high-fat meal group. Conclusion Administered with food can increase the rate and extent of nimodipine absorption in rats.
