尿中氧氟沙星药代动力学的测定

氧氟沙星为喹诺酮类药物 ,对革兰阳性及阴性菌有强大的抗菌作用 ,临床广泛用于治疗各种感染性疾病。我们采用紫外分光光度法测定１２例腹腔感染与５例对照 ,氧氟沙星尿药浓度对氧氟沙星的药代动力学进行了研究。１资料和方法１ １一般资料 :随机选择１２例腹腔感染患者为感染组 :男８例 ,女４例 ,年龄１８～５７岁 ,平均３８ ６岁。正常对照组５例 ,男３例 ,女２例。年龄２５～４３岁 ,平均４０ ２岁 ,均无肝肾疾病史。１ ２检测方法 :按文献方法采用紫外分光光度法 ,检测感染组和对照组氧氟沙星尿药浓度 ,氧氟沙星为０ １ｇ／片 ,珠海丽珠…     

口服胃舒平对茶碱药物动力学的影响

以６只家兔单服氨茶碱（Ａ）和同服胃舒平（Ｂ）后茶碱的血药浓度及药物动力学进行研究。结果表明两药同服时，茶碱的血药浓度明显偏低，所得药动学参数经配对ｔ检验，Ｃｍａｘ和ＡＵＣ具有显著性差异（Ｐ＞０．０５），Ｂ与Ａ的ＡＵＣ之比约为８０％，而Ｔ１／２（Ｋａ）、Ｔ１／２（Ｋ）、Ｔｍａｘ无显著性差异（Ｐ＞０．０５）。表明：胃舒平对茶碱的代谢消除无显著影响。但可影响茶碱的吸收，致使茶碱的生物利用度降低约２０％。因此在临床应避免两者同时服用     

氧氟沙星对人体内氨茶碱药物动力学的影响

本文采用荧光偏振免疫法测定8名健康志愿者单用氨茶碱和联合应用氧氟沙星后血药浓度的变化。结果表明,氧氟沙星对氮茶碱药动学参数有影响。其单用和联合应用氮茶碱的各药动学参数:半衰期T_(1/2)分别为7.79和10.14,峰浓度C_(max)分别为4.64和5.37,曲线下面积AUC 分别为56.37和100.5。经统计学处理有显著意义(P<0.05)。     

用尿药法比较氧氟沙星两种片剂的生物利用度

本文用尿药浓度法测定六名志愿者单剂量口服国产、进口两种氧氟沙星片剂的尿药浓度,结果表明:国产与进口两种片剂具有相同的药动学特征及生物等效性。其药动学参数分别为:k(h~(-1)):0.1185、0.1180;T_(1/2)(h):5.94、6.11;(?)—24(mg):174.66、167.79;排泄率:87.33%、83.89%     

氧氟沙星对健康人茶碱药物动力学的影响

本文应用均相酶免疫法，测定了６名健康志愿者多剂量口服氧氟沙星前后口服茶碱的稳态血清浓度，以ＰＫＢＰ－Ｎ１程序包按一室模型对数据进行处理并对结果进行统计分析。结果：氧氟沙星对茶碱的达峰时间、峰浓度、消除速率常数、清除率及曲线下面积未见影响（Ｐ＞０．０５），但对茶碱的分布容积有显著增加（Ｐ＜０．０５）。     

左旋氧氟沙星对氨茶碱药物动力学的影响

采用荧光偏振免疫分析法(FPIA),在7名志愿者身上,对氨茶碱单用及与左旋氧氟沙星合用后,血中氨茶碱浓度的变化进行观测.结果表明,合用左旋氯氟沙星后氨茶碱消除速率常数k降低13.6%,清除率CL下降15.6%,半衰期T_1/2延长16.5%(P<0.05),但对峰浓度C_(max)、曲线线下面积AUC,表观分布容积V_d无显著影响(P相似文献   

氧氟沙星三种给药途径的药物动力学

本报道４２例呼吸道感染病人用ｉｎｆ，ｉｍ和ｐｏ三种途径给氧氟沙星后的药物动力学特性。血药浓度经３Ｐ８７程序拟合，ｉｎｆ和ｉｍ药物动力学模型符合二房室，ｐｏ为一房室。ｉｎｆ，ｉｍ，ｐｏ后氧氟沙星的主要药物动力学参数为Ｔ１２β６．０±１．３，５．０±１．０和Ｔ１２ｋ５．０±０．７ｈ；Ｖｃ５８±１６，６８±２７和Ｖｄ９４±２５ｌ；Ｃｍａｘ３．９±１．０，２．８±０．９和１．９±０．７μｇ．ｍｌ＾－１；     

环丙沙星和氧氟沙星对氨茶碱药代动力学的影响

本文观察２２例患者加用环丙沙星或氧氟沙星前后血清茶碱药代动力学的变化。患者开始口服氨茶碱１００ｍｇ，每８ｈ１次；第４ｄ起Ａ组加服环丙沙星５００ｍｇ，Ｂ组加服氧氟沙星３００ｍｇ，均为每１２ｈ１次，至第９ｄ。结果显示：Ａ组患者加用环丙沙星后，血清茶碱浓度显著增加，消除半衰期延长３６．１％（Ｐ＜０．０１），清除率下降２９．６％（Ｐ＜０．０５）；Ｂ组患者加用氧氟沙星后，血清茶碱浓度亦有增加，消除半衰期延长     

国产氧氟沙星药代动力学研究

本文报道国产氧氟沙星药代动力学研究结果。用ＨＬＣ法测定血清药物浓度。８名健康志愿者口服４００ｍｇ氧氛沙星后，体内过程符合一室开放模型。血峰浓度于１．４７ｈ到达，为３．４８±０．７７μｇ／ｍｌ。ＡＵＣ为２５．３１±６．５０μｇ·ｈ／ｍｌ。半衰期为４．１３±０．８５ｈ。     

用尿药法研究诺氟沙星的药物动力学

用紫外分光光度法测定了诺氟沙星胶囊在5名健康受试者体内的尿药浓度。该法简便、可靠、重现性好(回收率100.984±2.30％,CV=2.27％,日内差,日问差均<3％)。通过尿药速度法求其药动学参数,结果表明:诺氟沙星的消除速度常数K为0.1870h~(-1),半衰期T_(1/2)为3.70h,24h内尿药排泄率为43.09％。     

双膦酸盐类药物的药动学及药物相互作用研究进展

双膦酸盐类药物用于预防与治疗骨吸收相关疾病,包括第1代的依替膦酸二钠、替鲁膦酸二钠、氯膦酸二钠,第2代的帕米膦酸二钠、阿仑膦酸钠,第3代的利塞膦酸钠、伊班膦酸钠、唑来膦酸等。该类药物口服达峰时间较短,吸收率偏低,生物利用度很低;骨结合部分的半衰期较长,药物留存时间也较长。与双膦酸盐联用产生相互作用的药物主要为：含有二价阳离子药物、其他双膦酸盐药物、华法林、苯妥英、非甾体类抗炎药、抗癌药、激素、H2受体拮抗剂以及肾毒性药物。从药动学角度解释双膦酸的药物相互作用,以避免不良反应发生。     

Comparative pharmacokinetics of theophylline following two fluoroquinolones co-administration

Summary Pretreatment for 3 days with oral ofloxacin or norfloxacin had no significant effect on the disposition of a single i.v. dose the theophylline in healthy volunteers.     

Simple method for determination of hydrochlorothiazide in human urine by high performance liquid chromatography utilizing narrowbore chromatography

A simple high performance liquid chromatographic (HPLC) method utilizing narrowbore chromatography was developed for the determination of hydrochlorothiazide in human urine. A mobile phase of 0.1% aqueous acetic acid—acetonitrile (93:7, v/v) pH 3 was used with a C18 analytical column and ultraviolet detection (UV). The method demonstrated linearity from 2 to 50 μg ml⁻¹ using 50 μl of urine with a detection limit of 1 μg ml⁻¹. The method was utilized in a study evaluating if racial differences are present in the pharmacokinetic and pharmacodynamic effects of hydrochlorothiazide.     

联苯双酯对环孢素A经大鼠小肠给药药动学影响的研究

目的:阐明联苯双酯(bifendate,BFD)对环孢素A(cyclosporin,CsA)经大鼠小肠给药药动学的影响。方法:两组大鼠分别给予0.5%CMC-Na和BFD(20mg.kg-1)连续灌胃6d,第7天分别从十二指肠幽门端注入CsA(1mg.kg-1)或CsA(1mg.kg-1) BFD(20mg.kg-1),从门静脉采血,用荧光偏振免疫法测定全血CsA浓度。结果:与单用CsA组相比,联用BFD组的Cmax平均降低55.7%(P<0.01),AUC平均降低49.7%(P<0.01)。联用BFD组的t1/2β、CL/F、V/F与单用CsA组相比明显升高(P<0.01或0.05)。其余参数在两组间差异无显著性(P>0.05)。结论:BFD可明显降低CsA的生物利用度,肠道可能是此相互作用发生的部位之一。     

阿霉素对去甲斑蝥素在大鼠体内药动学的影响

目的研究大鼠静脉给予阿霉素（ADM）对去甲斑蝥素（NCTD）体内药物动力学的影响。方法用HPLC-MS方法测定ADM和NCTD合并给药与NCTD单独给药大鼠血浆中的NCTD浓度,比较两者的药动学参数。结果ADM和NCTD合并给药组与NCTD单独给药组相比在分布速度常数（α）、分布相半衰期（t1/2α）、中央室向周边室的转运速度常数（k12）3个药动学参数有统计学差异（P〈0.05）,其余药动学参数之间无显著差异（P〉0.05）。结论NCTD与ADM合用时,ADM不会显著影响NCTD在大鼠体内的药动学过程,两药合用增效的原因主要在于药效学上的协同作用。     

Effect of single- and multiple-dose carbamazepine on the pharmacokinetics of diphenylhydantoin

Summary A three-phase trial has been done in 11 volunteers. They were given 600 mg phenytoin (Dilantin capsules) in each phase after an overnight fast. In the first study, phenytoin was given alone. In the second phase 400 mg carbamazepine (CBZ) was given at the same time as the phenytoin, and in the third part, 200 mg CBZ t. d. s. was given for one week prior to the phenytoin. Blood samples were taken for 72 h in each phase. Plasma levels of phenytoin and CBZ were determined by HPLC, and plasma protein binding was determined by equilibrium dialysis.The unbound fraction of phenytoin was 0.082, 0.085, and 0.077 in the control, single-dose CBZ, multi-dose CBZ phases, respectively. Single and multiple doses of CBZ decreased the plasma level of phenytoin. The 72-h AUC of phenytoin was 276, 237, and 176 mg h·l^–1 in the 3 phases, respectively, and the 72-h AUC of unbound phenytoin was 22.8, 20.5, 13.0 mg h·l^–1. The AUC of phenytoin (unbound and total) after multiple doses of CBZ was significantly lower than in the other two phases. The apparent volume of distribution (V_z/f) was 89.9, 110.3, and 121.3 l in the 3 phases, respectively.Through pharmacokinetic analyses, the decreased AUC and increased V_z/f were attributed to decreased bioavailability of phenytoin when CBZ was co-administered.     

Effect of itraconazole on the pharmacokinetics and pharmacodynamics of zopiclone

Objective: We studied the possible interaction between itraconazole, a potent inhibitor of CYP3A, and zopiclone, a short-acting hypnotic. Methods: A double-blind, randomized, two-phase crossover design was used. Ten healthy young subjects received daily either 200 mg itraconazole or placebo for 4 days. On day 4 they ingested a single 7.5-mg oral dose of zopiclone. Plasma concentrations of zopiclone and itraconazole were determined and pharmacodynamic responses were measured up to 17 h. Results: Itraconazole significantly increased the C_max of zopiclone from 49 to 63 ng ⋅ ml⁻¹. The t_1/2 of zopiclone was prolonged from 5.0 to 7.0 h. The AUC(0–∞) of zopiclone was increased from 415 to 719 ng ⋅ ml⁻¹ h by itraconazole. No statistically significant differences were observed in the pharmacodynamic responses between the groups. Conclusion: Itraconazole has a statistically significant pharmacokinetic interaction with zopiclone but this is only of limited clinical importance, at least in young adults. Received: 15 April 1996 /Accepted in revised form: 4 June 1996     

Effect of mequitazine on the pharmacokinetics of theophylline in asthmatic patients

Summary The effect of an oral anti-allergic drug, mequitazine, on the pharmacokinetics of theophylline has been investigated in seven asthmatic patients. They received chronic theophylline therapy (a sustained-release theophylline tablet 200–400 mg b.d. at 12 h intervals) and coadministered mequitazine 6 mg for 3 weeks. Plasma theophylline concentration-time curves and the urinary excretion of theophylline and its major metabolites before and after coadministration of mequitazine were compared.No significant change in the pharmacokinetic parameters of theophylline or in the urinary recovery of unchanged drug and its metabolites was observed.Thus, mequitazine did not influence the pharmacokinetics of theophylline and it should be safe for coadministration to asthmatic patients on chronic theophylline therapy.