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1.
目的:研究氯雷他定血浆浓度测定方法及其在健康人体内的药动学.方法:18名健康男性志愿者单剂量口服氯雷他定片,在设计的时间点取静脉血,采用高效液相色谱-质谱法(HPLC-MS)测定血药浓度.药动学参数采用DAS程序计算.结果:单次口服20 mg氯雷他定片后的主要药动学参数AUC0-t、AUC0~∞、Cmax、tmax、t1/2分别为(32.26±21.54)μg/(L·h)、(37.18±22.53)μg/(L·h)、(12.00±7.50)μg/L、(1.56±0.70)h和(11.15±19.66)h.结论:本法适用于快速准确及高灵敏地测定血浆中的氯雷他定,其在研究人体内口服吸收较快,个体间差异较大,约1.5 h达血药浓度蜂值,平均消除半衰期为11 h.  相似文献   

2.
国产氯雷他定片人体生物等效性研究   总被引:2,自引:0,他引:2  
目的 :2 0名健康男性受试者随机交叉口服 2 0mg西南合成制药总厂研制的氯雷他定片 (LORAX)与上海先灵葆雅制药有限公司生产的氯雷他定片 (开瑞坦 ,LORAS)进行药代动力学和生物等效性研究。方法 :采用高效液相色谱法测定血中氯雷他定浓度。结果 :经 3p97程序拟合和计算 ,LORAX和LORAS的Cmax为 8.5 9± 6 .70和 9.5 9± 8.2 2ng/ml;Tmax为 1.0 8±0 .4 1和 1.2 1± 0 .2 8h ;AUC0 -t为 2 7.2 9± 2 4 .5 4和 2 7.12± 2 0 .6 4ng·h/ml。 结论 :经方差分析和双单侧检验 ,结果表明两者具有生物等效性 ,LORAX片的相对生物利用度为 10 0 .6 3± 14 .2 7%。  相似文献   

3.
西洛他唑片的人体生物等效性研究   总被引:2,自引:0,他引:2  
目的 研究西洛他唑片和培达片的人体生物等效性。方法  2 2例健康志愿受试者单剂量随机交叉给药 ,采用反相高效液相色谱法测定受试者体内西洛他唑血药浓度 ,用 3P97药动学程序计算药动学参数 ,并对AUC、Cmax进行分析。结果 西洛他唑片和培达片的主要药动学参数分别为 :AUC0 - Tn(12 2 2 2 .6± 3981.2 ) ng/(h· ml)和 (12 0 39.9± 4 181.0 ) ng/ (h· ml) ,AUC0→∞ (1312 1.0± 4 6 15 .8) ng/ (h· m l)和 (12 882 .1± 4 70 2 .6 ) ng/(h· ml) ,tmax(3.77± 0 .6 9) h和 (3.82± 0 .6 6 ) h,Cmax(70 0 .8± 179.7) ng/ m l和 (6 81.8± 189.3) ng/ m l,t1 /2α分别为(3.97± 1.82 ) h和 (3.70± 1.2 0 ) h,t1 /2β分别为 (2 0 .0 1± 8.80 ) h和 (19.18± 7.4 5 ) h。以培达片为参比 ,西洛他唑片生物利用度 F0 - Tn为 10 2 .6 %± 10 .4 % ,F0→∞ 为 10 2 .7%± 11.2 %。结论 两种制剂具有生物等效性。  相似文献   

4.
目的:研究地氯雷他定血清浓度测定方法及其在健康人体内的药动学.方法:18名健康男性志愿者单剂量口服地氯雷他定片, 在设计的时间点取静脉血,采用高效液相色谱-质谱法(HPLC-MS)测定血药浓度.药动学参数采用3P97程序计算.结果:单次口服10mg地氯雷他定片后的主要药动学参数tmax、Cmax、AUC0-t、AUC0-∞、t 1/2(ke)、Ke、CL,分别为(1.611±0.366)h 、(4.455±1.990)μg·L -1、(58.50±21.34)μg·L-1·h-1、(60.59±22.32)μg·L -1·h-1、(20.303±5.833)h、(0.0372±0.0116)h-1和(0.1 838±0.0563)L·h-1.结论:地氯雷他定在研究人体内口服吸收较快,约1.5 h达血药浓度峰值,平均消除半衰期为20 h.  相似文献   

5.
目的评价2种国产兰索拉唑片(抗溃疡药)的生物等效性.方法采用随机、双周期两制剂的自身交叉对照的试验设计,20名健康男性受试者单剂量口服两个不同厂家生产的兰索拉唑片试验制剂和参比制剂30mg,血样采用高效液相色谱-质谱-质谱联用(LC/MS/MS)方法测定,用奥美拉唑作内标,测定血浆中兰索拉唑的浓度,用DAS2.1.1软件进行药代动力学参数的计算及统计分析.结果兰索拉唑片试验制剂和参比制剂药代动力学参数分别为:t1/2:(1.99±1.55)h、(2.09±1.67)h;Tmax:(3.9±0.8)h、(4.0±0.7)h;Cmax:(733.6±294.9)ng/ml、(764.0±250.5)ng/ml;AUC0-t:(3103.6±1911.2)ng/ml*h、(3176.7±1730.4) ng/ml*h;AUC0-∞:(3694.9±3504.0)ng/ml*h、(3809.2±3416.3)ng/ml*h.以AUC0-t计算,与参比制剂相比受试制剂相对生物利用度为(95.1±9.8)%.结论试验制剂和参比制剂具有生物等效性.  相似文献   

6.
目的 对盐酸曲美他嗪胶囊进行健康人体生物等效性研究.方法 健康受试者20名,随机分成二组:一组服用盐酸曲美他嗪片(万爽力),另一组服用受试物盐酸曲美他嗪胶囊,剂量为20 mg/d;血样采集前,埋置肝素留置针头.用高效液相色谱-质谱联用法测定不同时点血浆中曲美他嗪的浓度,计算其药代动力学参数.结果 单剂量口服盐酸曲美他嗪胶囊及曲美他嗪片后,血浆的曲美他嗪AUC0-t分别为(667±119.7)和(652.3±121.9)ng·h/ml,AUC0-∞分别为(707.1±127.7)和(692±128.6)ng·h/ml,Cmax分别为(72.39±12.95)和(71.93±14.32)ng/ml;Tmax分别为2.289±0.561和(2.211±0.608)h,t1/2分别为(4.777±1.077)和(4.74±0.823)h,AUC0-∞的90%可信区间为98.99%-105.51%,Cmax的90%可信区间为98.60%-106.34%,AUC0-t的90%可信区间为99.10%-105.59%,两制剂药代动力学参数无统计学差异.结论 试验制剂盐酸曲美他嗪胶囊与盐酸曲美他嗪片(万爽力)具有生物等效性.  相似文献   

7.
目的比较黄连-吴茱萸药对提取液中盐酸小檗碱在急性胃溃疡模型大鼠与正常大鼠体内的药代动力学差异,探讨病理状态对盐酸小檗碱体内过程的影响。方法分别灌胃给予正常大鼠和急性胃溃疡模型大鼠黄连-吴茱萸(6:1)药对提取液,采用高效液相色谱方法测定大鼠体内盐酸小檗碱的血浆浓度,色谱柱:Diamonsil C18(150mm×4.6mm,5μm);流动相:乙腈-甲醇-0.05mol/L磷酸二氢钾溶液(23∶12∶65),流速:1.0ml/min;检测波长:345nm;柱温:30℃。结果盐酸小檗碱在正常组的药代动力学参数:Cmax=0.064±0.01μg/ml;Tmax=(0.42±0.13)h;t1/2=(5.96±1.16)h;AUC0-t=(0.42±0.08)μg/(ml.h);AUC0-∞=(0.45±0.09)μg/(ml.h)。盐酸小檗碱在模型组的药代动力学参数:Cmax=(0.069±0.01)μg/ml;Tmax=(0.54±0.11)h;t1/2=(5.11±1.78)h;AUC0-t=(0.60±0.17)μg/(ml.h);AUC0-∞=(0.63±0.18)μg/(ml.h)。结论黄连-吴茱萸药对在乙醇致急性胃溃疡模型大鼠中吸收减慢,但是吸收量多,体内滞留时间稍延长。  相似文献   

8.
帕罗西汀片在健康人体的药代动力学   总被引:1,自引:0,他引:1  
目的 研究帕罗西汀片在健康人体内的药代动力学.方法 20名健康志愿者单剂量121服40 mg帕罗西汀片后,用高效液相色谱法测定血浆中帕罗西汀浓度,并用3P97软件统计处理.结果 帕罗西汀片药-时曲线经拟合呈二室模型,其Cmax、Tmax 、AUC0.120、AUC0.inf分别为(64.74±18.43)ng/ml、(5.64±1.84)h、(20.03±5.33)h、(976.47±309.49)ng·h/ml和(1086.75±376.54)ng·h/ml.结论 帕罗西汀片在人体内的药代动力学呈二房室开放模型.  相似文献   

9.
目的 建立高效液相色谱-串联质谱(HPLC-MS/MS)法测定大鼠血浆中人参皂苷Rg3的浓度,用于大鼠体内人参皂苷Rg3的药代动力学研究.方法 血浆样品经乙酸乙酯液-液提取.色谱柱为Inertsil ODS-3(2.1 mm×50 mm,5μm),流动相:乙腈:10 mmol/L乙酸铵水溶液(含0.1%甲酸,90:10);流速:0.4 mL/min;ESI离子源,负离子模式监测.6只大鼠灌胃给予人参皂苷Rg3 20 mg/kg后按预定时间点眼眶采血.采用DAS 3.3.1软件统计其药代动力学参数.结果 血浆中人参皂苷Rg3的线性范围为2 ~ 400 ng/mL,日内、日间精密度及基质效应RSD均小于15%,主要的药代动力学参数:AUC0-t为(821.659±170.125)ng·h/mL,AUC0-∞为(912.468±190.653)ng·h/mL,Cmax为(138.803±28.997) ng/mL,t1/2为(2.803±0.263)h.结论 建立的方法快速、灵敏、准确.适用于大鼠血浆中人参皂苷Rg3浓度的测定.  相似文献   

10.
苯磺酸氨氯地平分散片药代动力学与相对生物利用度   总被引:1,自引:0,他引:1  
目的 建立人体血浆中苯磺酸氨氯地平的高效液相色谱-质谱测定方法,用于研究苯磺酸氨氯地平分散片在人体的药代动力学及相对生物利用度.方法 20例健康男性志愿者单剂量口服苯磺酸氨氯地平分散片受试制剂或参比制剂10mg后,用高效液相色谱-质谱测定方法测定氨氯地平的血药浓度,用DAS 2.0药动学软件求算药动学参数,以双单侧t检验进行生物等效性评价.结果 受试制剂与参比制剂的主要药动学参数:Tmax为6.1±1.2小时, 6.9±1.7小时; Cmax分别为8.0±2.2 ng/(ml·h),8.0±2.0ng/ml;t1/2为30.4±5.9小时, 26.5±6.2小时; AUC0-t为259.1±37.8小时, 270.7±53.7ng/(ml·h), AUC0-∞为275.4±40.1 ng/(ml·h), 283.1±56.2 ng/(ml·h).相对生物利用度F=97.6%±14.8%.结论 两制剂为等效制剂.  相似文献   

11.
Objective: To evaluatel the value of D-dimers in patients with acute aortic dissection (AAD). Methods: This study consisted of 16 patients with AAD and 27 non-AAD patients. Serum D-dimets were measured by Sta-Liatest D-DI immunoturbidimetric assay. Results: D-dimer level was higher (P < 0.001) in patients with AAD(7.91 ± 5.52 μg/ml) than that in non- AAD group(1.57±1.24 μg/ml). D-dimer was positive (>0.4 μg/ml) in all patients with AAD and in 10 control group patients (37%). Among patients with acute AAD, D-dimers tended to be higher in Stanford A than in Stanford B (8.67 ± 4.31 μg/ml vs. 3.24±1.27 μg/ml, P <0.01). D-dimer values tended to be higher in more extended disease(3.84 ± 1.65 μg/ml, 8.57 ± 3.58 μg/ml and 11.87 ± 5.69 μg/ml in thoracic aorta, thoracic and abdominal aorta, thoracic and abdominal aorta and iliacal arteries, respectively, P < 0.05 for both 8.57 ± 3.58 and 11.87 ± 5.69 vs. 3.84 ± 1.65 ). Including the control group into the analysis, we found a sensitivity of 100%, a negative predictive value of 100%, and a specificity of 66% and a positive predictive value of 64% for D-dimer in diagnosis of AAD in our patients with suspected AAD. Conclusion: D-dimer was elevated in patients with AAD. A negative D-dimer test result could be useful in excluding AAD.  相似文献   

12.
Objective: To set up a simple and reliable rat model of combined liver-kidney transplantation. Methods: SD rats served as both donors and recipients. 4℃ sodium lactate Ringer's was infused from portal veins to donated livers,and from abdominal aorta to donated kidneys, respectively. Anastomosis of the portal vein and the inferior vena cava (IVC) inferior to the right kidney between the graft and the recipient was performed by a double cuff method, then the superior hepatic vena cava with suture. A patch of donated renal artery was anastomosed to the recipient abdominal aorta. The urethra and bile duct were reconstructed with a simple inside bracket. Results: Among 65 cases of combined liver-kidney transplantation, the success rate in the late 40 cases was 77.5%. The function of the grafted liver and kidney remained normal. Conclusion: This rat model of combined liver-kidney transplantation can be established in common laboratory conditions with high success rate and meet the needs of renal transplantation experiment.  相似文献   

13.
FOR anesthesiologis s ,treatingpostoperativepainhas alwaysbeen a problem.Althoughopioidshave been provedtobe effective,theirsideeffectscouldnotbeignored.With thedevelopmentofscienceand pharmacology,many drugs with aspectsof satisfactoryanalgesicefficacyand couldbe welltoleratedby patientshave been developed.And lornoxicamisone of them, which isa non-steroidalanti-inflammatorydrug (NSAID ), with analgesic, anti-infl-ammatory,andantipyreticproperties.Itseliminationhalf-time(3 to 5 hours) isle…  相似文献   

14.
Objective To observe blood pressure change with age in salt-sensitive teenagers whose salt sensitivity were determined by repeated testing.Methods Salt sensitivity was determined through intravenous infusion of normal saline combined with volume-depletion by oral diuretic furosemide in 55 teenagers. After five years, salt sensitivity was re-examined and subject blood pressure was followed up. Blood pressure changes in salt-sensitive teenagers were compared to that of non-salt sensitive teenagers over five years.Results After 5 years, the repetition rate of salt sensitivity determined by intravenous saline loading is 92.7%. In teenagers with salt sensitivity on the baseline, both the systolic blood pressure increments and increment rates were much higher than non-salt sensitive teenagers (12.7±12.1 mmHg vs. 2.8±5.2 mmHg, P< 0.01; 12.2%± 12.0% vs. 2.5% ±4.4%, P< 0.001,respectively). There was a similar trend for diastolic blood pressure (8.4 ± 6.4 mmHg vs. 3.7 ± 6.4 mmHg, P = 0.052; 13.2% ±10.6 % vs. 6.8%± 10.1%, P = 0.053, respectively).Conclusions Salt sensitivity determined by intravenous saline loading showed good reproducibility. Blood pressure increments with age were much higher in salt-sensitive teenagers than non-salt sensitive teenagers, especially in terms of systolic blood pressure.  相似文献   

15.
Shock wave lithotripsy (SWL) is a treatment of choice for upper urinary stones. However, this procedure is inappropriate for obese patients because the focus is often unable to reach the target owing to the limited focal distance in shock wave source. Although treating such patients in a blast path may increase the application length of shock wave source, it's difficult to find this path on the lithotripter monitor. For this reason, we invented an adjustable calibration marker in order to set an effective focus in the shock wave hath.  相似文献   

16.
Excess production of reactive oxygen species(ROS)of mitochondrion mediated by hyperglycemia is the common pathogenesis of angiopathic complications of diabetes.TCM holds that the damp from the dysfunction of spleen.kidney and liver is the causative factor of complications of diabetes.This is similar to the mechanism of Ros resulting in angiopathic complications of diabetes.When the angiopathic complications of type II diabetes mellitus(T2DM)are difierentiated as caused by turbid damp in TCM can be explained as ROS.Since the obstruction of pathogenic damp in channels and collaterals is said to be the main pathogenesis,the treating principle should be dissolving the damp to remove the obstruction.  相似文献   

17.
INTRODUCTION Obesity is a complex emergent problem, which can be possibly solved not only by the diet but also by the life style and promotion of a constant physical exercise. 1, 2 No doubt careful attentions must be given to the nutritional condition of obese people, the dietary habits, the somatic build (i.e. distribution of fat mass) and the organic functions linked to formation of the fat mass. All the parameters should be constantly monitored before, during and after a diet treatment. 3, 4, 5  相似文献   

18.
People with dysglycemia are at high risk for atherosclerotic diseases. This study aims at investigating the atherosclerotic vascular damage in dysglycemia and its metabolic origin in Tibetan population.  相似文献   

19.
Objective: To observe the therapeutic effects in acupunture treatment of primary dysmenorrhea combined with spinal Tui Na, and study its mechanism. Methods: Thirty cases of the treatment group were treated by acupuncture combined with spinal Tui Na, and thirty cases in the control group were treated by routine acupuncture. Results: The total effective rate was 93.3% in the treatment group, and 73.3% in the control group, with a significant difference between the two groups (P<0.05). Conclusions: Acupuncture combined with spinal Tui Na has good prospects for treatment of primary dysmenorrhea.  相似文献   

20.
In treating chronic nephropathy,Luo Lingjie,a chief physician,pays attention to regulating the balance between yin and yang,treating infection if present,and removing pathogenic factors.He prescribes gentle drugs and uses carefully strongly warming-tonifying ones,emphasizes the importance of persuading the patient to persist in treatment with medication and nurse one's health for recuperation,and is good at combined use of TCM and western medicine therapy and brings the merits of various therapies into full play,with obvious theraoeutic effects.  相似文献   

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