血浆中雷尼替丁和铋的药动学和生物等效性研究

目的建立高效液相色谱(HPLC)和电感耦合等离子体-质谱(ICP-MS)分别测定人血浆中雷尼替丁和铋质量浓度的方法 ,并应用该法进行雷尼替丁和铋在健康人体内的药动学特征研究和复方盐酸雷尼替丁片生物等效性评价。方法采用HPLC法和ICP-MS技术,分别测定20名健康男性受试者经口给予复方盐酸雷尼替丁片和复方雷尼替丁胶囊后不同时刻血浆中雷尼替丁和铋的质量浓度,分别绘制血药质量浓度-时间曲线,并计算主要药动学参数。结果受试制剂和参比制剂中雷尼替丁的主要药动学参数如下:tmax分别为(1.9±0.5)和(2.1±0.6)h,ρmax分别为(492.8±276.7)和(466.5±224.4)μg.L-1,t1/2分别为(2.9±1.6)和(2.8±1.0)h,用梯形法计算,AUC0-t分别为(2 548.3±895.6)和(2 377.5±887.0)μg.h.L-1,AUC0-∞分别为(2 562.9±912.8)和(2 377.5±887.0)μg.h.L-1,雷尼替丁的相对生物利用度平均为(111.6±35.4)%。受试制剂和参比制剂中铋的主要药动学参数如下:tmax分别为(0.4±0.2)和(0.3±0.1)h,ρmax分别为(56.0±40.2)和(53.3±37.9)μg.L-1,t1/2分别为(6.9±2.6)和(7.2±2.3)h,用梯形法计算,AUC0-t分别为(151.8±118.9)和(156.3±117.9)μg.h.L-1,AUC0-∞分别为(153.1±120.2)和(157.7±119.3)μg.h.L-1,铋的相对生物利用度平均为(95.3±16.2)%。结论复方盐酸雷尼替丁片与复方雷尼替丁胶囊两种制剂具有生物等效性。     

伪麻那敏渗透泵的药物动力学

目的建立一种同时测定动物血浆中盐酸伪麻黄碱和马来酸氯苯那敏方法,并进行伪麻那敏渗透泵的药物动力学研究。方法8只Beagle犬单次口服伪麻那敏渗透泵2片,用LC MS法测定血浆中各药物浓度,计算2种药物的药物动力学参数。结果单次口服伪麻那敏渗透泵2片后的主要药物动力学参数:盐酸伪麻黄碱t1/2为(3.36±1.05)h,tmax为(5.75±1.49)h,ρmax为(1110.86±200.61)μg.L-1,AUC0-t为(10 755.43±3 274.35)μg.h.L-1,马来酸氯苯那敏t1/2为(5.01±2.91)h,tmax为(4.06±1.70)h,ρmax为(5.02±1.81)μg.L-1,AUC0-t为(34.71±22.15)μg.h.L-1。结论本方法能测定口服伪麻那敏渗透泵的血药质量浓度,进行动物药物动力学研究。     

朝鲜族和汉族健康受试者单剂量口服盐酸曲马多的药物动力学

目的研究盐酸曲马多在中国朝鲜族和汉族健康受试者体内的药物动力学。方法朝鲜族和汉族健康受试者各10名,单剂量口服盐酸曲马多胶囊100 mg,用高效液相色谱荧光检测法测定受试者血浆中盐酸曲马多的血药浓度,研究其药物动力学,用DAS Ver 2.0药物动力学软件进行数据处理。结果汉族和朝鲜族健康受试者口服盐酸曲马多后的药-时曲线均符合一室开放模型,主要药物动力学参数分别为t1/2(6.2±1.0)h和(6.4±1.6)h,tmax(2.4±0.7)h和(2.0±0.9)h,ρmax(401.4±78)μg.L-1和(418.9±48)μg.L-1,AUC0-36(4297.1±1261.8)μg.h.L-1和(4071.8±1387.3)μg.h.L-1,AUC0-∞(4456.1±1318.5)μg.h.L-1和(4255.1±1548.2)μg.h.L-1。结论服用盐酸曲马多后,汉族和朝鲜族健康受试者的ρmax、AUC0-t、AUC0-∞个体间差异较大,但2组受试者之间药物动力学参数的差异无统计学意义(P>0.05)。     

盐酸小檗碱单次和多次给药在Beagle犬体内的药动学

目的研究盐酸小檗碱胶囊单次和多次给药后在Beagle犬体内的药动学。方法 6条Beagle犬按150 mg单次和多次口服盐酸小檗碱胶囊,多次给药每天1次,共7 d。采用UPLC-MS/MS色谱法测定犬血浆中盐酸小檗碱的浓度。用DAS 2.0药动学软件处理血药浓度数据。用SPSS统计软件对所得的药动学数据进行显著性差异分析。结果单次给药后主要药动学参数t1/2为(18.85±10.54)h,ρmax为(4.18±2.59)μg.L-1,AUC0-t为(110.04±70.22)μg.h.L-1,AUC0-∞为(121.51±74.19)μg.h.L-1,CL为(1 593.57±745.01)L.h-1,V为(44 509.1±34 995.4)L,tmax为(20.42±22.98)h;多次给药达稳态后主要药动学参数t1/2为(18.53±9.99)h,ρmax为(9.92±7.01)μg.L-1,AUC0-t为(164.51±119.70)μg.h.L-1,AUC0-∞为(172.34±125.03)μg.h.L-1,CL为(1 280.19±709.95)L.h-1,V为(33 655.7±27 632.2)L,tmax为(6.08±4.90)h。结论盐酸小檗碱单次和多次给药后在Beagle犬体内血药浓度均较低,盐酸小檗碱多次给药在Beagle犬体内无明显蓄积现象。     

单剂量口服奥美拉唑在中国维吾尔族和汉族健康人体内药物动力学考察

目的研究维吾尔族和汉族健康受试者单剂量口服奥美拉唑肠溶片的药物动力学,旨在为战时救治和平时临床合理应用奥美拉唑提供依据。方法健康维吾尔族和汉族受试者各10名,男、女各半,单剂量口服奥美拉唑肠溶片40 mg后,于不同时间点采集静脉血,血浆样品经处理后用HPLC法测定奥美拉唑的质量浓度。用DAS 2.0药物动力学软件处理数据,用SPSS11.5软件统计分析。结果奥美拉唑在维吾尔族受试者体内的主要药物动力学参数分别为:ρmax(728.4±214.3)μg.L-1,tmax(2.8±0.5)h,t1/2(1.2±0.5)h,AUC0-12(1 837.0±861.8)μg.h.L-1,AUC0-∞(1 847.6±869.1)μg.h.L-1;在汉族受试者体内的主要药物动力学参数分别为:ρmax(760.5±581.2)μg.L-1,tmax(2.7±0.8)h,t1/2(1.6±1.3)h,AUC0-12(1 437.6±798.1)μg.h.L-1,AUC0-∞(1 470.1±769.5)μg.h.L-1。结论奥美拉唑在维吾尔族、汉族受试者体内的ρmax、AUC(0-12)、AUC(0-∞)个体间差异较大,但统计学分析结果显示两民族人体内主要药物动力学参数差异无统计学意义。     

琥珀酸美托洛尔缓释片在中国人体的药动学特性

目的研究琥珀酸美托洛尔缓释片在中国人体的药动学特性.方法采用HPLC荧光检测法测定血浆中美托洛尔的浓度.结果22名健康受试者口服单剂量50mg琥珀酸美托洛尔缓释片后的AUC0-t为(173.15±99.52)μg·h·L-1,AUC0-∞为(237.44±162.11)μg·h·L-1,cmax为(15.67±7.69)μg·L-1,tmax为(6.14±2.55)h,MRT为(14.17±4.01)h;多剂量口服50mg缓释片后的AUCss0-t为(335.42±235.19)μg·h·L-1,cmax为(23.03±15.16)μg·L-1,tmax为(5.8±2.2)h,cmin(6.73±4.98)μg·L-1,平均稳态血药浓度cav是(13.98±9.80)μg·L-1,血药浓度波动度DF(%)(122.55±53.93)%.结论单剂量给予缓释片的结果与美托洛尔普通片相比,tmax明显延长(5.8vs 1.1 h),cmax明显降低(15.67×2vs 186.2μg·L-1).琥珀酸美托洛片缓释片与普通片相比在中国健康受试者中的缓释特征明显,安全性良好.在整个试验过程中监测血压、心率,无低血压、血晕等不良反应发生.     

盐酸氟桂利嗪两种制剂的生物等效性

目的评价2种盐酸氟桂利嗪制剂人体生物等效性。方法用双周期交叉实验设计,采用液相色谱-质谱-质谱联用法测定了20名健康男性受试者口服盐酸氟桂利嗪口腔崩解片和盐酸氟桂利嗪胶囊后血浆中氟桂利嗪的浓度,绘制了血药质量浓度-时间曲线并计算药动学参数。结果20名受试者口服含盐酸氟桂利嗪20 mg的受试制剂和参比制剂后血浆中氟桂利嗪的tmax分别为(2.7±0.6)和(2.5±0.6)h,ρmax分别为(55.85±20.66)和(56.74±21.40)μg.L-1,t1/2分别为(6.70±2.46)和(6.89±1.98)h,用梯形法计算,AUC0-t分别为(419.0±126.7)和(428.1±175.2)μg.h.L-1,AUC0-∞分别为(465.3±147.8)和(477.0±202.3)μg.h.L-1。以AUC0-t计算,盐酸氟桂利嗪口腔崩解片的相对生物利用度平均为(104.6±22.0)%。结论盐酸氟桂利嗪两制剂生物等效。     

石杉碱甲缓释贴片和片剂人体药动学比较

目的比较2种石杉碱甲制剂在正常人体内的药动学情况。方法 20名健康受试者分为2组(每组10名),分别单剂量贴用石杉碱甲缓释贴片10 mg和口服石杉碱甲片0.2 mg后,用液相色谱-串联质谱法(LC-MS/MS)检测血浆中石杉碱甲浓度,并经DAS药动学程序进行数据处理,计算药动学参数。结果石杉碱甲缓释贴片与片剂的tmax分别为(40.2±13.2)、(0.6±0.3)h;t1/2分别为(28.4±7.4)、(13.6±1.3)h;ρmax分别为(0.7±0.4)、(1.9±0.5)μg.L-1;MRT0-t分别为(74.1±8.5)、(18.7±1.6)h;AUC0-t分别为(70.4±53.1)(0～168 h)、(19.9±2.7)(0～48 h)μg.h.L-1。结论石杉碱甲缓释贴片的药动学参数较普通片剂ρmax降低,tmax显著延长,t1/2延长,从而达到缓释效果。     

每日1次美斯地浓缓释片体内药代动力学与生物等效性研究

目的研究美斯地浓缓释片在兔体内单剂量和多剂量的药代动力学和生物等效性,为临床研究提供参考和依据。方法 6只兔采用自身交叉给药方案,分别单剂量及多剂量口服美斯地浓缓释片和普通片后,采用高效液相色谱法(HPLC)测定血浆中美斯地浓浓度。结果单次口服缓释片和普通片后主要药动学参数为:Tmax分别为(6±0)和(2±0)h;Cmax分别为(14.446±0.279)和(17.944±0.919)μg.L-1;T 12分别为(5.449±2.779)和(2.733±0.652)h;AUC0-t分别为(231.076±4.408)和(196.127±4.009)μg.h.L-1;AUC0-∞分别为(254.644±6.49)和(198.385±3.934)μg.h.L-1,相对生物利用度F为(117.3±11.0)%。多次口服缓释片和普通片达稳态后主要药动学参数:Cmax分别为(18.391±0.16)和(25.477±0.177)μg.L-1;Cmin分别为(3.421±0.186)和(6.612±0.254)μg.L-1;Cav分别为(12.99±0.055)和(16.088±0.132)μg.L-1;AUCss分别为(155.881±0.655)和(193.057±1.591)μg.h.L-1;DF分别为(1.152±0.012)和(1.173±0.019),相对生物利用度F为(106.7±6.4)%。结论美斯地浓缓释片与普通片两种制剂生物等效,且美斯地浓缓释片具有明显的缓释特征。     

单剂量口服硝苯地平缓释片的药动学及生物等效性

目的研究单剂量口服硝苯地平缓释片在人体内的药动学特点和国产硝苯地平缓释片的生物等效性.方法22名健康男性志愿者采用双周期交叉、自身对照试验设计.以尼群地平为内标,采用高效液相色谱-大气压化学源-质谱联用(HPLC-MS)的方法,测定人血浆中硝苯地平的浓度.结果单剂量口服20mg受试和参比制剂后血浆中硝苯地平的Cmax分别为(52.9±31.5)ug·L-1和(52.1±35.6)μg·L-1,Tmax分别为(4.1±1.2)h和(4.7±1.9)h,t1/2分别为(6.9±3.5)h和(7.7±4.5)h,AUC0-36 h分别为(410.7±188.1)μg·h·L-1和(440.4±271.7)μg·h·L-1,AUC0-∞分别为(437.6±206.8)μg·h·L-1和(477.9±290.4)μg·h·L-1.将22名受试者的经时血药浓度录入DAS(ver 1.0)程序,Tmax进行非参数秩和检验,Cmax、AUC0-36h、AUC0-∞、t1/2经对数转换后做方差分析,并经双向单侧t检验,两制剂的tmax、Cmax、AUC0-36h、AUC0-∞、t1/2差异均无显著性,两种制剂的相对生物利用度为(104.4±40.1%)(AUC0-36h.T/AUC0-36h.R×100%).结论两种制剂具有生物等效性.     

硝苯地平缓释片在中国健康人体的生物等效性

目的评价硝苯地平缓释片在健康人体的生物等效性。方法 20名男性健康志愿者进行随机双交叉试验,分别单次和多次口服硝苯地平受试药物和参比药物,用液相色谱-串联质谱法测定血浆中硝苯地平的血药浓度,DAS2.1软件计算药代动力学参数。结果单次口服2种硝苯地平缓释片,受试药物和参比药物的主要药动学参数分别如下:Cmax为(92.68±34.98),(112.39±47.98)ng.mL-1,tmax为(2.68±0.69),(2.70±0.57)h;t1/2为(5.01±1.65),(4.83±2.16)h;AUC0-36 h为(648.09±332.98),(659.62±376.95)ng.h.mL-1;F为(104.1±25.6)%。AUC0-36 h,AUC0-∞,Cmax的[1-2α]置信区间分别为94.6%～108.29%,93.9%～106.9%,72.8%～100.6%。多次口服2种硝苯地平缓释片,达稳态时受试药物和参比药物的体内药代动力学参数分别如下:Cmax为(122.85±45.46),(141.29±53.51)ng.mL-1;tmax为(2.55±0.65),(2.70±0.66)h;t1/2为(5.57±1.91),(3.83±1.25)h;Cav为(57.36±26.31),(59.26±25.25)ng.mL-1;AUCss为(688.26±315.67),(711.10±303.01)ng.h.mL-1;F为(99.8±29.9)%。AUCss,Cmax的[1-2α]置信区间分别为85.8%～107.3%,73.5%～103.2%。结论受试药物与参比药物具有生物等效性。     

双氯芬酸钠缓释片在健康人体的药代动力学和生物等效性

目的:评价双氯芬酸钠缓释片受试制剂和参比制剂在健康人体的药代动力学和生物等效性。方法:24例健康男性志愿者分别行单剂量和多剂量交叉口服双氯芬酸钠缓释片受试与参比制剂,用高效液相色谱-串联质谱法测定血浆中双氯芬酸钠的血药浓度,计算药代动力学参数及相对生物利用度。结果:单剂量口服受试制剂和参比制剂的主要药动学参数如下:Cmax分别为(568.38±271.26)和(458.64±173.96)ng.mL-1,Tmax分别为5(0.5,12)和1.5(0.5,7)h,AUC0～24 h分别为(2 557.72±659.43)和(2 364.14±698.08)ng.h.mL-1,AUC0～∞分别为(2 655.25±635.48)和(2 843.62±808.61)ng.h.mL-1,MRT分别为(6.3±1.8)和(7.0±1.7)h;多剂量口服受试制剂和参比制剂的主要药代动力学参数为:T(ss,max)分别为5(1,7)和4(0.5,8)h,C(ss,max)分别为(520.58±245.89)和(522.98±234.36)ng.mL-1,C(ss,min)分别为(24.96±20.79)和(22.68±17...     

The kinetics of nifedipine release from porous hydrophilic matrices and the pharmacokinetics in man

Porous hydrophilic tablets of nifedipine were prepared with hydroxypropyl methylcellulose as swellable polymer, as well as with the addition of a solid dispersion of the drug in polyethylene glycol, a water soluble system. The kinetic data conformed with the Higuchi square root equation and first order release for in vitro release from a single planar surface of the tablet, as well as release from the whole tablet. The addition of a soluble fraction to the porous swellable release system increased the nifedipine release rate constant. This shows that the dosage form may be formulated as a drug-polymer system which exhibits constant release at a desired rate. In the bioequivalence study with five volunteers, the pharmacokinetic parameters of a sustained release hydrophilic tablet of nifedipine and of immediate release capsules were determined. Although the bioavailability of the two preparations is similar, the therapeutic effects may differ. The rate of absorption, the maximum concentration levels, the time of the peak and the period of maintenance of the therapeutic serum levels after single oral doses are different after the administration of the two tested formulations. The hydrophilic tablets of nifedipine may be useful as a sustained release formulation for long term treatment of hypertension.     

硝苯地平缓释片对高血压昼夜节律的作用

本文用24h动态血压监测方法观察了硝苯地平缓释片对高血压病人血压昼夜节律的作用，结果表明，与硝苯地平片相比，硝苯地平缓释片能选择性降低非构型高血压病人的夜间高血压，而对构型的夜间血压无显著影响。认为硝苯地平缓释片有改善高血压昼夜节律的作用。     

基于粉末直接压片工艺的硝苯地平缓释片：制备、体外释放度及比格犬体内药动学评价

目的选用粉末直接压片工艺,以羟丙基甲基纤雏素为骨架材料制备日服1次的硝苯地平缓释片。方法建立24h的释放度测定方法并进行硝苯地平缓释片的体外评价;应用液相色谱-质谱联用技术研究缓释片在比格犬体内药代动力学,与市售参比制剂对比并计算相对生物利用度。结果受试制剂和参比制剂有相似的药代动力学参数,相对生物利用度为（100．9±12．4）％;药物体外累积释放百分数与体内吸收百分数有较好的相关性,r=0．9625。结论本工艺制得的硝苯地平缓释片可以达到缓释24h的要求。     

多剂量口服硝苯地平缓释片的药动学及生物等效性研究

目的研究多剂量口服硝苯地平缓释片在人体内的药动学特点和两种硝苯地平缓释片的生物等效性.方法22名健康男性志愿者采用双周期交叉、自身对照试验设计.以尼群地平为内标,采用高效液相色谱-大气压化学源-质谱联用(HPLC-MS)的方法,测定人血浆中硝苯地平的浓度.将22名受试者的经时血药浓度录入DAS(ver 1.0)程序,得到药代动力学参数,并进行统计分析和生物等效性评价.结果多剂量口服 20 mg×7 d 受试和参比制剂后血浆中硝苯地平的Cmax分别为 52.5±27.4、54.0±31.2 ng·ml-1,Cmin分别为 5.4±4.1、6.2±5.9 ng·ml-1,Cav分别为 16.8±9.2、19.3±12.4 ng·ml-1,Tmax分别为 3.7±0.9、4.1±1.1 h,t1/2分别为 8.9±4.9、8.5±3.1 h,AUC0-τ分别为 403.4±221.0、461.9±296.6 ng·h·ml-1,AUC0-36h分别为 444.4±256.1、503.1±330.9 ng·h·ml-1,AUC0-∞分别为 482.1±268.9、542.3±348.4 ng·h·ml-1 ,DF分别为(299.8±117.7)%、(279.2±97.5)%.Tmax进行非参数秩和检验,Cmax、Cmin、Cav、DF、AUC0-τ、AUC0-36h、AUC0-∞经对数转换后做方差分析,并经双向单侧t检验,两制剂的Tmax、Cmax、Cmin、Cav、DF、AUC0-τ、AUC0-36h、AUC0-∞均无显著性差异(P＞0.05),受试制剂的Cav、DF、AUC0-36h、AUC0-τ、AUC0-∞的90%可信限落在参比制剂的80%～125%范围内;Cmax、Cmin的90%可信限落在参比制剂的70%～143%范围内.两种制剂的相对生物利用度为(100.6±38.6)%(AUC0-36h,T/AUC0-36h,R×100%).结论两种制剂具有生物等效性.     

Formulation and comparative bioavailability of 2 ciprofloxacin sustained release tablets

BACKGROUND AND THE PURPOSE OF THE STUDY: The aim of this study is to formulate and evaluate the quality of ciprofloxacin (CAS number: 85721-33-1) sustained release tablet (Ciprocare?XR) 1 000 mg ciprofloxacin (test formulation) by comparing its pharmacokinetic parameters with Cipro?XR sustained release tablet (reference formulation). For this purpose ciprofloxacin SR tablets were developed using the 2-layer method. To assess the quality of the produced sustained release tablets a randomized, 2-way, crossover, bioequivalence study was performed in 24 healthy, male volunteers. The selected Middle Eastern volunteers were divided into 2 groups of 12 subjects. One group was treated with the reference formulation and the other one with the test formulation, with a cross-over after a drug washout period of 7 days. Blood samples were collected at fixed time intervals and Ciprofloxacin concentrations were determined by a validated HPLC assay method. The pharmacokinetic parameters AUC0-48, AUC0-∞, Cmax, Tmax, Ke and T1/2 were determined for both sustained release tablets and were compared statistically to evaluate the bioequivalence between the 2 formulations of ciprofloxacin, using the statistical model recommended by the FDA. The analysis of variance (ANOVA) did not show any significant difference between the 2 formulations and 90% confidence intervals (CI) fell within the acceptable range for bioequivalence. According to the obtained results it was concluded that the test and reference formulations are bioequivalent, since they exhibit comparable pharmacokinetic parameters.     

Reproducibility of nifedipine absorption from GITS tablets: comparison of single-dose pharmacokinetics using 10, 20, 40 and 60 mg nifedipine

OBJECTIVE: To examine the reproducibility of nifedipine absorption from gastrointestinal therapeutic system (GITS) tablets by comparing the single-dose pharmacokinetic profiles of 4 different dosages administered orally. METHODS: Twelve healthy male volunteers, aged between 22 and 29 years were enrolled in the open, 4-way, dose escalation study with single oral doses of 10, 20, 40 and 60 mg (two 30 mg) nifedipine GITS tablets. Each administration was separated by a 1-week washout period. Coefficients of variation (CV) of dose-corrected area under the concentration-time curve (AUC) and peak plasma drug concentrations (Cmax) were calculated from the pharmacokinetic profiles. RESULTS: Mean AUC and mean Cmax were dose-proportional from 10 to 60 mg. Although the CV of 4 mean dose-corrected AUC and Cmax were 5.5% and 17.5%, respectively, CV of dose-corrected AUC and Cmax in each subject varied from 5.1 to 37.4% (mean 11.0%) and from 14.1% to 46.4% (mean 25.8%), respectively. CONCLUSIONS: Whereas mean plasma nifedipine concentration remained markedly stable over a 16- to 24-hour interval and mean dose-corrected AUC showed good reproducibility with nifedipine GITS, the CV of dose-corrected AUC of the nifedipine GITS tablets in each subject showed large variability.     

Development and characterization of buccoadhesive nifedipine tablets.

The buccoadhesive controlled-release tablets for delivery of nifedipine were prepared by direct compression of carboxymethyl cellulose (CMC) with carbomer (CP), which showed superior bioadhesion properties compared to polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA), hydroxypropylmethyl cellulose (HPMC), and acacia in a modified tensiometry method in vitro. The tablets containing 30mg of nifedipine and various amounts of CMC and CP showed a zero-order drug release kinetic. The adhesion force was significantly affected by the mixing ratio of CP:CMC in the tablets. The weakest and highest adhesion force was observed at the mixing ratios of 1:0 and 8:2 of CP:CMC, respectively. The tablets containing 15% CMC and 35% CP adhered for over 8h to the upper gums of six healthy human volunteers. These tablets released about 56% of the loaded drug after 8h in vivo with a rate of 2.17h(-1) and were perfectly tolerated, while they released about 100% of their content after the same time with a rate of 3.49h(-1) in vitro. A good correlation (r(2)=0.989) was observed between drug-released in vitro and in vivo.     

氨茶碱缓释片与普通片在健康人体内药动学的比较

目的研究氨茶碱缓释片与普通片在健康人体内的药动学和生物等效性。方法采用双交叉试验设计,将20例健康志愿者随机分为2组,分别进行单次给药和多次给药试验。交叉单次(缓释片和普通片各200 mg)和多次服用氨茶碱缓释片(200 mg,qd×10 d)或普通片(100 mg,bid×10 d),采用荧光偏振免疫分析法检测不同时间点血药浓度,DAS2.0药动学程序软件计算主要药动学参数及相对生物利用度,判断生物等效性。结果单次口服氨茶碱缓释片的Ka、Ke、ρmax均小于普通片;而tmax和t1/2均大于普通片,差异均有显著意义(P<0.05)。连续多次服用氨茶碱缓释片和普通片的ρmax、ρmin及DF相比均无显著差异(P>0.05),而缓释片的tmax较普通片延长(P<0.05)。以AUC0-t计算,缓释片单次或多次给药的F分别是普通片的(105.9±12.7)%和(103.4±15.2)%。结论氨茶碱缓释片具有显著的缓释效果,和普通片具有生物等效性。