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pharmacokinetic
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  药动学
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  pharmacokinetic
Overall the pharmacokinetic properties of both isomers were similar in rats, monkeys and humans, with β-isomer exhibiting longer elimination half-life, MRT, volume of distribution and clearance, irrespective of the route of administration.
      
Because of their complimentary pharmacokinetic characteristics, the isomeric mixture of arteether can be therapeutically more beneficial than β- isomer used alone.
      
At present, however, side effects and/or insufficient pharmacokinetic profiles have made most of the drug candidates undesirable.
      
The genetic factors involved in Parkinson's and Alzheimer's diseases are conventionally divided into pharmacodynamic and pharmacokinetic.
      
The pharmacokinetic factors play a role in Parkinson's disease (PD) at the level of metabolism of DA, dioxyphenylalanine, and tyrosine and include polymorphisms of enzymes and proteins involved in the relevant metabolic reactions.
      
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A sensitive and specific method was developed for the isolation of puerarin from biological specimens and its quantitative determination by the application of polyamide thin layer chromatography and ultraviolet spectrophotometry. This method was adopted for the study of the metabolic fate of puerarin and its pharmacokinetics in rats, and also for the evaluation of drug elimination in humans.The blood level of puerarin following intravenous administration in rats was found to decrease in two phases, the distribution...

A sensitive and specific method was developed for the isolation of puerarin from biological specimens and its quantitative determination by the application of polyamide thin layer chromatography and ultraviolet spectrophotometry. This method was adopted for the study of the metabolic fate of puerarin and its pharmacokinetics in rats, and also for the evaluation of drug elimination in humans.The blood level of puerarin following intravenous administration in rats was found to decrease in two phases, the distribution phase and the elimination phase, with halflives of 3 and 18 min respectively. The pharmacokinetic parameters calculated according to the 2-compartment open model were as follows:α=0.23/min β=0.04/minK_(12)=0.08/min V_1=19.9 mlK_(21)=0.09/min V_2=33.7 mlK_e(K_2)=0.1/min V_d=53.7 mlClearance=2.0 ml/minThese results imply that puerarin is distributed widely in the body and eliminated in a fairly rapid rate which prevelits its serious accumulation in the body.Determination. of the drug in various organs revealed that drug levels were highest in the kidney, moderate in plasma, liver and spleen and lowest in the brain, indicating the existence of a partial blood-brain barrier.Absorption of the drug from the gastrointestinal tract was found to be fairly rapid but incomplete, 37.7% of the close could still be recovered from the gastrointestinal content and the faeces 24 hours after administration:In rate, the amount excreted in urine and faeces within 24 hours was about 1.85% and 35.7% respectively of the dose. administered orally, as compared with 37.6% and 7.39% administered intravenously. In normal human volunteers, however, only 0.78% of the dose was found in urine in 36 hrs, and 73.3% of the dose was present in the faeces collected for 72 hrs after oral administration.In vitro experiments provided evidence that puerarin was rather stable in the gastrointestinal tract, and might be metabolized by blood and various tissues such as liver, lung and kidney. The drug-plasma binding rate was found to be 24.6%.The metabolic characteristics of puerarin and daidzein were compared.

本文建立了一个用薄层及紫外光分光光度法分离并测定生物样品中葛根素的方法,并用该法研究了葛根素在大鼠体内的代谢,分析了其药代动力学特点,并观察了口服后在人体的排泄情况。 大鼠静脉注射后药物在肾脏含量较高,血浆、肝、脾次之,药物可通过血脑屏障进入脑组织,但脑中含量较低。血浆药-时曲线分快、慢两个时期。根据开放形二室模型数学公式计算葛根素各药代动力学参数为:t_(1/2)(α)=3.0分,t_(1/2)(β)=18.0分,V_1=19.9 ml,V_2=33.7ml,V_d=53.7ml,α=0.23/分,β=0.04/分,K_(12)=0.08/分,K_(21)=0.09/分,K_0=0.10/分,清除率=2.0 ml/分。此结果表明葛根素在体内分布广、消除快、不易积畜。体外实验证明,葛根素可被大鼠血及肝、肾等组织所代谢,且可与肝、肾、肺及血浆蛋白相结合,其与血浆蛋白的结合率达24.6%。 大鼠灌胃葛根素后药物吸收较快,但吸收程度较差,灌胃后24小时自粪及胃肠道内容物回收的药物为剂量的37.3%。体外实验证明,葛根素在胃肠道内破坏很少。 大鼠灌胃葛根素后24小时自尿及粪分别排出1.85%及35.70%,静脉注射后...

本文建立了一个用薄层及紫外光分光光度法分离并测定生物样品中葛根素的方法,并用该法研究了葛根素在大鼠体内的代谢,分析了其药代动力学特点,并观察了口服后在人体的排泄情况。 大鼠静脉注射后药物在肾脏含量较高,血浆、肝、脾次之,药物可通过血脑屏障进入脑组织,但脑中含量较低。血浆药-时曲线分快、慢两个时期。根据开放形二室模型数学公式计算葛根素各药代动力学参数为:t_(1/2)(α)=3.0分,t_(1/2)(β)=18.0分,V_1=19.9 ml,V_2=33.7ml,V_d=53.7ml,α=0.23/分,β=0.04/分,K_(12)=0.08/分,K_(21)=0.09/分,K_0=0.10/分,清除率=2.0 ml/分。此结果表明葛根素在体内分布广、消除快、不易积畜。体外实验证明,葛根素可被大鼠血及肝、肾等组织所代谢,且可与肝、肾、肺及血浆蛋白相结合,其与血浆蛋白的结合率达24.6%。 大鼠灌胃葛根素后药物吸收较快,但吸收程度较差,灌胃后24小时自粪及胃肠道内容物回收的药物为剂量的37.3%。体外实验证明,葛根素在胃肠道内破坏很少。 大鼠灌胃葛根素后24小时自尿及粪分别排出1.85%及35.70%,静脉注射后分别自尿、粪及胆汁排出剂量的37.62%,7.39%及3.65%。正常成人口服葛根素后36小时仅有0.78%自尿排出,72小时自粪排出剂量的73.3%。 本文对葛根素及黄豆甙元的代谢特点进行了讨论。

Cefathiamidinum is a new broad-spectrum semisynthetic cephalosporin antibiotic developed in china. In this paper the pharmacokinetics of cefathiamidinum and the effect of probenecid were studied in seven healthy adults.Post-infusion serum drug concentration versus time curve was fitted to two-compartment open model with first order elimination. However, the serum drug level data after intramuscular administration was adequately fitted to one-compartment open model with first order absorption and elimination....

Cefathiamidinum is a new broad-spectrum semisynthetic cephalosporin antibiotic developed in china. In this paper the pharmacokinetics of cefathiamidinum and the effect of probenecid were studied in seven healthy adults.Post-infusion serum drug concentration versus time curve was fitted to two-compartment open model with first order elimination. However, the serum drug level data after intramuscular administration was adequately fitted to one-compartment open model with first order absorption and elimination. The pharmacokinetics of cefathiamidinum was complicated with the simultaneous administration of probenecid. After pharmacokinetic analysis it was considered that probenecid can competitively inhibit the urinary excretion of cefathiamidimum. The peak trevel and the area under Cxt curve increased significantly in the presence of prebenecid, and its probable clinical significance was discussed.The pharmacokinetic characteristics of cefathiamidinum were discussed and compared with those of other members, of the commonly used cephalosporin series.

本文对硫脒头孢菌素在7例健康受试者体内的药物代谢动力学过程,以及合用丙磺舒的影响,进行了初步的分析。 静脉注射后的血药浓度-时间曲线符合开放型二室模型;但肌内注射时可以简化为开放型单室模型。 合用丙磺舒对硫脒头孢菌素药代动力学过程的影响比较复杂。对计算的主要结果进行分析讨论后认为:丙磺舒能够抑制硫脒头孢菌素的经尿排泄,表现在尿药排泄量减少,血药峰浓度及血药浓度-时间曲线下总面积增加。对合用丙磺舒的临床意义也进行了讨论。 与常用头孢菌素的药代动力学特性,进行了讨论比较。

Metabolic studies of a new non-antimonial antischistosome agent-Nithiocyamine were carried out on animals and reviewed together with some human results. In rabbits, the blood concentration reached a peak at the 4th hour after oral administration, then fell gradually, pharmacokinetic parameters were assessed by the two compartment open model where three biological half-lives t_(1/2)ka, t_(1/2)α and t_(1/2)β were shown to be 0.855, 0.924 and 105.8 hours respectively; and the three rate constants k_(el),...

Metabolic studies of a new non-antimonial antischistosome agent-Nithiocyamine were carried out on animals and reviewed together with some human results. In rabbits, the blood concentration reached a peak at the 4th hour after oral administration, then fell gradually, pharmacokinetic parameters were assessed by the two compartment open model where three biological half-lives t_(1/2)ka, t_(1/2)α and t_(1/2)β were shown to be 0.855, 0.924 and 105.8 hours respectively; and the three rate constants k_(el), k_(21), and k_(12), 0.0127, 0.398 and 0.356 hour~(-1) respectively. The apparent volume of distribution (V_f)was calculated as 0.934L/kg.Nithiocyamine distributed widely in many tissues after absorption. In rats, at the 4th hour after oral administration, the drug occurred in the following tissues in concentrations of ascending order: the liver kidney, spleen, lung, muscle, heart, brain and blood. In infected rabbits, the schistosomes took up more drug than tissues of the host animal, and female schistosomes more than the male. Nithiocyamine was excreted only slowly through the urine and bile. Urinary excretion in human usually lasted more than 3 days after a single oral administration, and lasted more than 19 days after three consecutive dosages.The metabolites occurred in urine were extracted and separated by TLC, Chemical methods UV an. HPLC, examination revealed that it was the NCS group first reduced into amino, and then conjugated with glucuronic acid to form a N-glycoside.. This metabolic change is one of its biotransformation pathways.

硝硫氰胺是一非锑类治疗血吸虫病的新药。在动物和人体研究了该药的代谢。家兔口服给药后4小时达到高峰血浓度。由二室模型对血浓度数据作药物动力学参数计算,得t_((1/2)ka)、t_((1/2)α)和t_(1/2)β分别为0.815,0.924和105.8小时,Kel、K_(21)和K_(12)分别为0.0127、0.398和0.356小时~(-1),V_f为0.934升。大鼠口服给药后4小时药物在各组织的浓度大小依次为:肝、肾、脾、肺、肌肉、心、脑和血。血吸虫浓度高于肝和血浓度,而且雌虫高于雄虫。该药由尿和胆汁排泄,大鼠一次口服的尿排泄持续3天以上,人连服三次排泄持续超过19天。尿代谢产物由层析、高速液相色谱、紫外光谱和化学方法检测,硝硫氰胺转化成氨基物再转化成N-葡萄糖醛酸甙,这种代转变化是其生物转化途径之一。

 
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