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1.
采用RP-HPLC法,同时测定依普黄酮及其代谢物M-I血浆药物浓度并对16名健康志愿者进行了药代动力学研究,实验采用Waters公司HPLC系统,Nova-PakC18柱,以磷酸盐缓冲液(0.02mol/L,pH3.5)-乙腈(1:1)为流动相,克霉唑为内标,在254nm进行检测,依普黄酮及其代谢物M-I线性范围分别为4~200μg/L,4~250μg/L(r=0.9999),最低检测分别为0.0  相似文献   

2.
反相高效液相色谱法测定萘普生钠血浆浓度   总被引:2,自引:1,他引:1  
目的:建立用高效液相色谱法测定萘普生钠血浆浓度的方法。方法:血浆样品在酸性条件下,以1,2二氯乙烷提取,吲哚美辛为内标,采用LichrosorbC18(5μm)柱,流动相为甲醇∶醋酸醋酸铵缓冲液(pH4.5)=74∶26,流速为1.0ml·min-1,检测波长318nm,萘普生和内标的保留时间分别为3.35和4.71min。结果:线性范围在1~90μg·ml-1(r=0.9999,最低检测浓度为0.4μg·ml-1血浆,RSD%<3.5。结论:本方法可用于萘普生钠的药物动力学研究  相似文献   

3.
利多卡因缓释胶丸皮下植入的药代动力学   总被引:6,自引:0,他引:6  
目的:研究利多卡因缓释胶丸(LSRP)在兔和大鼠体内的药代动力学。方法:运用高效液相色谱法(HPLC)测定LSRP在血浆和组织中的浓度。结果:发现兔皮下植入LSRP(20,40,80mg·kg-1)后,血浆药物浓度—时间曲线符合缓释制剂的一室开放模型。3种剂量的LSRP吸收半衰期Ta1/2均较利多卡因注射液(LT,10mg·kg-1,sc)明显延长。3种剂量LSRP的峰浓度(Cmax)分别为0.24±0.09,1.25±0.23,5.65±0.10mg·L-1,而LI(10mg·kg-1,SC)的Cmax为2.18±0.32mg·L-1。40mg·kg-1LSRP经大鼠皮下植入后,在局部皮下组织中利多卡因浓度明显高于血浆、脑、心、肝和肾组织中浓度,并在给药后48h仍能维持在1.18μg·g-1水平。结论:LSRP经皮下植入后的缓释效果明显。提示LSRP能延长利多卡因的局麻、镇痛作用,并可能减轻其全身毒性。  相似文献   

4.
本文以2-萘磺酸钠为内标,建立了RP-HPLC法测定兔血浆中安乃近及其3种活性代谢物FAA、AA、MAA的浓度。Shim-PackCLC-ODS(15cm×6mmID)为分析柱;ODS预柱;流动相组成:甲醇-水-0.5mol/L磷酸二氢钠-三乙胺(35:63:2:0.01),磷酸调节pH6.0±0.5;流速:1.0ml/min;柱温:35℃;检测彼长:260nm。本法简便、快速、准确、灵敏,适用于安乃近及其活性代谢物的血药浓度测定及药物动力学研究。  相似文献   

5.
缓释微丸及血浆中酮洛芬的HPLC测定   总被引:4,自引:0,他引:4  
采用国产ODS柱,用0.05mol/LKH_2PO_4-甲醇(45:55)为流动相,以波长260nm检测缓释微丸中的酮洛芬(1)含量。采用无水乙醇一次萃取血浆样品中的1,以pH8.0的磷酸盐缓冲液溶解残渣后测定,平均回收率为91.4%。  相似文献   

6.
以高效液相色谱法测定血浆中的盐酸氟桂利嗪浓度。色谱条件:紫外检测波长210nm;柱SpherisorbC8150×4.6mm;流动相;甲醇(80%);水(15%):(0.05mol.L^-1NH4H2PO4+0.025mol.L^-1H3PO4)缓冲液(5%)。最低检测限10ng.ml^-1。药物动力学一室模型,其参数(T1/2(K)2.38-2.64h,Tmax2.30-2.43h,Cmax13  相似文献   

7.
以高效液相色谱法测定血浆中的盐酸氟桂利嗪浓度。色谱条件:紫外检测波长210nm;柱SpherisorbC8150×4.6mm;流动相:甲醇(80%)∶水(15%)∶(0.05mol·L-1NH4H2PO4+0.025mol·L-1H3PO4)缓冲液(5%)。最低检测限10ng·ml-1。药物动力学为一室模型,其参数(T1/2(K)2.38~2.64h,Tmax2.30~2.43h,Cmax135.13~143.96ng·ml-1。  相似文献   

8.
健康人单剂量口服茶碱控释胶囊的药物动力学   总被引:1,自引:0,他引:1  
目的:研究7 名健康志愿者单剂量口服茶碱控释胶囊( 简称CRTC)400 mg 后的药物动力学。方法:用紫外法测定健康人血清中茶碱的血药浓度。结果:CRTC的药物动力学参数分别为:Tmax = (7 .9 ±1.1)h,Cmax = (4.0 ±0 .9)μg·ml-1 ,T1/2e =(17 .2±2 .6)h,Ke =(0.04±0.06)h-1 ,T1/2a= (2 .1±0 .9)h,Ka=(0.23±0.04)h- 1 ,AUC072 = (138 .0±17 .6)μg·h·ml- 1 。结论:CRTC的药物动力学参数与国产茶碱控释片( 简称DCRTT)[1] 相比:其吸收减慢,导致达峰时间延长,达峰浓度降低。但其消除减慢,CRTC在体内蓄积,致使其药时曲线下的面积较DCRTT 大。  相似文献   

9.
高效液相色谱法测定人血浆依托泊苷浓度   总被引:4,自引:0,他引:4  
目的:建立一种快速、灵敏的高效液相色谱法测定人血浆中依托泊苷(Vp-16)浓度的方法。方法:以替尼泊苷(VM-26)为内标,采用惠普1100型高效液相色谱仪,以 HP Hypersil ODS column(125 min×4mm,5μm)为分析柱,前加HP Licro-sphere保护柱;流动相为甲醇∶水=48∶52(v/v),流速为1.5 ml/min;检测波长为220nm;室温25℃。血浆样品经甲醇沉淀蛋白等处理后进样。结果;色谱峰分离良好,无干扰。线性方程为Y=0.9921X+0.048 24,r=1.000;线性范围:0.l~10.00μg/ml;检测限:0.1μg/ml。利用本法检测了一例Vp-16 300mg、氟脲嘧啶1g、顺铂80mg的化疗患者血样,合并用药及代谢产物均对Vp-16色谱峰无干扰。结论:本法是一种可靠的、快速灵敏的检测血浆中Vp-16 浓度的方法,适用于含Vp-16的化疗方案的监测及药物动力学的研究。  相似文献   

10.
以高效液相色谱分析法测定按2mg·kg-1剂量给家兔皮下注射3-酮-地索高诺酮后0.25~24h的血药浓度,其血药浓度-时间曲线符合二室开放模型,药物动力学方程为C=257.07e-0.71t+42.23e-0.05t-299.30e-0.93t主要药物动力学参数:Tka0.78±0.17h,Tα1.20±0.30h,Tβ12.09±4.18h,AUC1312.90±387.45μg·h ̄(-1)·L ̄(-1),T_(max)1.69±0.39h,C(max)=128.21±50·71μg·L ̄(-1),V/F9.50±4.39L·kg(-1)。采用平衡透析法测得3-酮-地索高诺酮与兔血浆蛋白的结合率在81.09%~84.60%之间。  相似文献   

11.
Several biochemical and cellular effects have been described for methylxanthines under in vitro conditions. However, it is unknown, whether threshold concentrations required to exert these effects are attained in target tissues in vivo. We therefore employed the microdialysis technique for measuring theophylline concentrations in peripheral tissues under in vivo conditions.Following in vitro and in vivo calibration, microdialysis probes were inserted into the medial vastus muscle and into the periumbilical subcutaneous adipose layer of healthy volunteers. Following single oral dose administration of 300 mg or i.v. infusion of 240 mg theophylline, in vivo time courses of theophylline concentrations were monitored in tissues and plasma. Major pharmacokinetic parameters (cmax, tmax, AUC) were calculated for plasma and tissue time courses. The mean AUCtissue /AUCplasma-ratio was 0.56 (p.o.) and 0.55 (i.v.) for muscle and 0.55 (p.o.) and 0.72 (i.v.) for subcutaneous adipose tissue.We conclude that microdialysis provides important information on the distribution and the tissue pharmacokinetics of theophylline.Abbreviations FPIA Fluorescence polarisation immuno assay - AUC Area under the curve - tmax Time to peak concentration - cmax Peak concentration  相似文献   

12.
In assessing interindividual variability in metabolic activation, the toxic metabolite is often too unstable for conventional analysis. Possible alternatives include a stable product of the reactive metabolite e.g. cysteinyl derivatives of N-acetyl-4-benzoquinoneimine, the toxic metabolite of paracetamol, adducts with DNA or protein, and indirect measurement of the activity of the enzyme(s) producing the active metabolite. An example of the last approach is the use of furafylline, a highly specific inhibitor of human CYP1A2, to determine the extent of the metabolic activation of the cooked food mutagens PhIP and MeIQx. The extent of inhibition, determined from levels of unchanged amine in urine, is an indirect measure of the activity of the activation pathway. Further refinement of this approach, allied to improved measures of the biological process of interest should prove of value in evaluating interindividual variability and its role in the risk assessment process.  相似文献   

13.
1. The pharmacokinetics of the antimalarial compound artemisinin were compared in the male and female Sprague-Dawley rat after single dose i.v. (20 mg.kg) or i.p. (50 mg.kg) administration of an emulsion formulation. 2. Plasma clearance of artemisinin was 12.0 (95% confidence interval: 10.4, 13.0) l.h. kg in the male rat and 10.6 (95% CI: 7.5, 15.0) l.h. kg in the female rat suggesting high hepatic extraction in combination with erythrocyte uptake or clearance. Artemisinin half-life was 0.5 h after both routes of administration in both sexes. Values for plasma clearance and half-lives did not statistically differ between the sexes. 3. After i.p. administration artemisinin AUCs were 2-fold higher in the female compared with male rat (p 0.001). Artemisinin disappearance was 3.9-fold greater in microsomes from male compared with female livers and it was inhibited in male microsomes by goat or rabbit serum containing antibodies against CYP2C11 and CYP3A2 but not CYP2B1 or CYP2E1. 4. The unbound fraction of artemisinin in plasma was lower (p 0.001) in plasma obtained from the male (8.8 2.0%) compared with the female rat (11.7 2.2%). 5. The possibility of a marked sex difference, dependent on the route of administration, has to be taken into account in the design and interpretation of toxicological studies of artemisinin in this species.  相似文献   

14.
本实验测定10名休克患者血浆和红细胞的丙二醛(MDA)、血浆总抗的氧化活性(AOA)的含量。结果表明:休克病人红细胞膜和血浆 MDA 含量(4.298±0.722;5.348±0.834)与对照组(3.235±0.682;4.356±1.081)比较明显增高(P<0.05);血浆 AOA(39.65±7.858)与对照组(48.21±10.81)比较明显降低(P<0.01)。提示:休克时,患者机体内自由基反应增强是引起组织细胞损伤的原因之一。  相似文献   

15.
Polymorphisms in genes involved in neurotransmission in relation to smoking   总被引:4,自引:0,他引:4  
Smoking behavior is influenced by both genetic and environmental factors. The genetic contribution to smoking behavior is at least as great as its contribution to alcoholism. Much progress has been achieved in genomic research related to cigarette-smoking within recent years. Linkage studies indicate that there are several loci linked to smoking, and candidate genes that are related to neurotransmission have been examined. Possible associated genes include cytochrome P450 subfamily polypeptide 6 (CYP2A6), dopamine D1, D2, and D4 receptors, dopamine transporter, and serotonin transporter genes. There are other important candidate genes but studies evaluating the link with smoking have not been reported. These include genes encoding the dopamine D3 and D5 receptors, serotonin receptors, tyrosine hydroxylase, trytophan 2,3-dioxygenase, opioid receptors, and cannabinoid receptors. Since smoking-related factors are extremely complex, studies of diverse populations and of many aspects of smoking behavior including initiation, maintenance, cessation, relapse, and influence of environmental factors are needed to identify smoking-associated genes. We now review genetic polymorphisms reported to be involved in neurotransmission in relation to smoking.  相似文献   

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18.
1.?Pradigastat is a potent and specific diacylglycerol acyltransferase-1 (DGAT1) inhibitor effective in lowering postprandial triglycerides (TG) in healthy human subjects and fasting TG in familial chylomicronemia syndrome (FCS) patients.

2.?Here we present the results of human oral absorption, metabolism and excretion (AME), intravenous pharmacokinetic (PK), and in vitro studies which together provide an overall understanding of the disposition of pradigastat in humans.

3.?In human in vitro systems, pradigastat is metabolized slowly to a stable acyl glucuronide (M18.4), catalyzed mainly by UDP-glucuronosyltransferases (UGT) 1A1, UGT1A3 and UGT2B7. M18.4 was observed at very low levels in human plasma.

4.?In the human AME study, pradigastat was recovered in the feces as parent drug, confounding the assessment of pradigastat absorption and the important routes of elimination. However, considering pradigastat exposure after oral and intravenous dosing, this data suggests that pradigastat was completely bioavailable in the radiolabeled AME study and therefore completely absorbed.

5.?Pradigastat is eliminated very slowly into the feces, presumably via the bile. Renal excretion is negligible. Oxidative metabolism is minimal. The extent to which pradigastat is eliminated via metabolism to M18.4 could not be established from these studies due to the inherent instability of glucuronides in the gastrointestinal tract.  相似文献   

19.
Based on blood and cerebrospinal fluid samples collected in a full-term neonate, the penetration of tramadol in the central nervous system is described. Following intravenous administration of tramadol, a lag time of about 4 h was observed until full blood–brain equilibration was achieved. This pharmacokinetic observation is in line with a recent pharmacodynamic evaluation of the central opioid effects of tramadol in adults.  相似文献   

20.
Diclofop-methyl (DM) is a chlorophenoxy derivative used in large quantities for the control of annual grasses in grain and vegetable crops. In this study, the genotoxic effects of DM were investigated by measuring chromosomal aberrations (CAs) in mouse bone-marrow cells and CA and the comet assay in human peripheral lymphocytes. Mice were treated with 15.63, 31.25, 62.5, and 125?mg/kg body weight of DM intraperitoneally for 24 hours, and 15.63-, 31.25-, 62.5-, 125-, and 250-µg/mL concentrations were applied to human lymphocytes for both 24 and 48 hours. In in vivo treatments, DM significantly, but not dose dependently, increased the total chromosome aberrations, compared to both negative and solvent controls. Cell proliferation was significantly, but not dose dependently, affected by all doses. In in vitro treatments, DM (except 15.63 µg/mL) significantly and dose dependently increased the frequency of chromosome aberrations. Also, 250 µg/mL of 48-hour treatment was found to be toxic. Cell proliferation was significantly and dose dependently affected by DM applications, when compared to negative control. In in vitro treatments, DM significantly decreased the mitotic index only at the highest concentration for 24 hours, and 62.5- and 125-µg/mL concentrations for 48 hours. In the comet assay, a significant and dose-dependent increase in comet-tail intensity was observed at 62.5-, 125-, and 250-µg/mL concentrations. The mean comet-tail length was significantly increased in all concentrations. Our results demonstrate that DM is genotoxic in mammalian cells in vivo and in vitro.  相似文献   

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