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     

环丙沙星的人体药代动力学研究

健康志愿者8名,静脉恒速滴注乳酸环丙沙星200mg(30min)后,其体内过程符合二室开放模型,主要药动学参数分别为:滴注完时浓度Co为4.14±0.82μg/ml,消除相半衰期t1/2为3.35± 0.30h,AUC为7.225±0.814μg·h/ml。另外8名志愿者分别口服500mg盐酸环丙沙星胶囊或片剂后,其体内过程符合一室模型,主要药动学参数分别为;C_(max)为2.47± 0.33及2.28±0.30μg/ml;t1/2为3.13±0.44及3.51±0.35h,Tp为1.53±0.36及1.28±0.31h;AUC为17.08±2.17及15.91±2.01μg·h/ml。绝对生物利用度为78.8％及72.7％。血浆药物浓度采用微生物法测定。     

环丙沙星药代动力学和体外抗菌活性研究

本文报道环丙沙星体外抗菌活性及药代动力学研究结果。用HPLC法测定血清药物浓度。6名健康志愿者环丙沙星400mg口服后,体内过程符合一室开放模型。血峰浓度于2小时到达,为2.52±0.82μg/ml。表现分布容积为2.47L/kg,AUC为14.10μg·h/ml,消除半衰期为2.93小时。体外抗菌活性研究结果表明,本品抗菌谱广,抗菌活性强。对金葡菌、大肠杆菌、肺炎杆菌、痢疾杆菌、伤寒杆菌MIC90分别为0.125、0.5,0.06、<0.03和0.25μg/ml。对绿脓杆菌抑苗率达87％。上述资料表明,环丙沙星口服400mg后,峰浓度明显高于多种细菌的MIC90值,预期临床可取得较好疗效。     

环丙沙星肛栓的尿药动力学研究

目的 :研究环丙沙星肛栓和环丙沙星片剂的药代动力学 ,为环丙沙星肛栓治疗慢性细菌性前列腺炎提供依据。方法 :健康成人分别口服250mg 环丙沙星片剂和使用剂量为250mg 的肛塞栓剂 ,留量尿液 ,用双波长分光光度法测定其中环丙沙星的含量 ,计算药代动力学参数。结果 :主要药代动力学参数 :口服组尿中环丙沙星24h回收率 (70 3±11 2) % ,k= (0 161±0 059)h ,Tp=(1 71±0 556)h ;栓剂组24h尿中环丙沙星回收率 (17 2±3 6) % ,栓剂类似于缓释制剂 ,在体内近似于零级速率过程。结论 :环丙沙星肛栓用于治疗慢性细菌性前列腺炎 ,每天1枚即可。     

环丙沙星在急慢性肝炎患者中药物动力学变化

环丙沙星(Ciprofloxacin, CLPX)是第三代氟喹诺酮类合成抗菌药。其在正常人及肾功衰竭病人中药物动力学变化国外已有报告,但对该药在肝病病人中的变化的研究还很少。另外,对该药在腹水中变化尚未见有报道。我们采用HPLC外标法测定口服CPLX在各型肝炎病人血和(或)腹水中药物浓度变化,并进行药物动力学分析,从而确定肝损害时药物代谢情况及调整给药方案。 一、材料及方法 1.药品:环丙沙星片剂及标准品(cif-     

抗生素在糖尿病患者体内的药代动力学

糖尿病是一种严重危害人类健康的全身性疾病 ,其并发症特别多 ,几乎可涉及到全身各组织器官 ,是导致患者病情恶化并死亡的重要因素。目前 ,对糖尿病并发症的预防和治疗已经成为治疗糖尿病的重要内容 ,其治疗效果如何直接关系到糖尿病患者的健康及其生活质量。感染是糖尿病的常见并发症之一 ,发生率比较高 ,尤其在创伤条件下更易发生。有资料表明 ,糖尿病并发感染的发生率为３６ ８ % ,其中呼吸道感染最常见 ;其次为尿路感染、皮肤感染、结核病等。引起感染的病原菌以革兰阴性菌为多 ,占７３ ２５ % ,尤以肺炎杆菌、大肠杆菌最常见 ;其次为绿…     

万古霉素在危重患者体内的药代动力学研究

目的 研究万古霉素在危重患者体内的药代动力学特点.方法 入选8例肝肾功能正常的危重病患者,给予万古霉素0.5g溶解100 ml 0.9％氯化钠溶液中静脉滴注1h后多次留取血液标本和尿液标本,利用高效液相色谱分析得到万古霉素的血、尿药代动力学参数.结果 在危重病患者体内万古霉素仍符合二室模型,血样回归方程:A =5315.3p+ 1176.4(r =0.9998,A为峰面积,为万古霉素浓度),尿样回归方程:A= 10 368p -7150.3.血浆药代参数药物浓度-时间曲线下面积(AUC)( 162.72±84.23)μg(h·ml);二室模型分布相的半衰期(t1/2α)(0.49±0.30)h,二室模型消除相的半衰期(t1/2β)(7.08±4.01)h,总清除率(Cl)(63.09±31.09) ml/min,一次给药后的最大血药浓度(Cmax)(44.46 ±28.60) μg/ml,tmax(1.0±0)h,表观分布容积(0.28±0.15) L/kg,尿液药代参数tmax(3.50±3.16)h,Cmax(74 889.86±83 277.71) μg/h,t1/2β( 10.47±9.61)h,AUC[ (31 5464.1±284 428.3)μg/(h·ml)].结论 对于危重病患者,给予0.5g万古霉素,AUC约为健康人的2倍;t1/2β也长于健康人.这可能与危重患者组织灌注不足,药物从循环向组织扩散减慢,体温异常而使药物代谢的酶活性降低等有关.同时对于重症患者因万古霉素谷浓度易高于正常而应更关注万古霉素的不良反应.     

微生物法测定环丙沙星片在人体中的药物动力学和生物利用度

8名健康受试验者交叉口服单剂量德国产及国产环丙沙星片(750mg)后,用微生物法测定血药浓度,按单室模型处理分析得各药物动力学参数。结果表明二者基本相似其相对生物利用度为97±20%。     

环丙沙星3种剂型在62名健康志愿者的药物动力学研究

用微生物测定法对环丙沙星３种剂型在６２名男性健康志愿者身上进行药物动力学研究。在１６名受试者静滴环丙沙星注射液（２００ｍｇ／１００ｍｌ）后，０、１、４、１２ｈ的血药浓度分别为３．６８±０．６３、≤１、０．３３～０．４３及０．１μｇ／ｍｌ，药动学参数Ｔ１／２为３．２４ｈ，总清除率３９３．５ｍｌ／ｍｉｎ，ＡＵＣ０～２４６．２１ｈ·μｇ／ｍｌ，Ｖｓｓ１５５．０±３４．２Ｌ。单次口服环丙沙星１００及５００ｍｇ，体内平均药动学参数Ｃｍａｘ分别为２．３１±０．２８及２．４９±０．２４μｇ／ｍｌ，Ｔｍａｘ分别为１．２６±０．１８及１．４７±０．２１ｈ，Ｔ１／２为２．６９±０．４８及３．８７±０．５３ｈ，ＡＵＣ０～２４为１２．８１±０．８５及１５．０２±２．１１ｈ·μｇ／ｍｌ，结果与文献报道相同。此外，对静滴及口服两种给药途径的血药浓度与临床疗效关系以及统计矩法与房室模型在药物动力学研究中的选用进行了讨论。     

Clinical pharmacokinetics of ciprofloxacin in patients with major burns

Objective: To better master the use of ciprofloxacin (CPF) in burn patients, a clinical study, including pharmacokinetics in serum and urine, was undertaken in a pathophysiologically homogeneous population of major-burn subjects. Methods: Twelve major-burn patients who were infected with Pseudomonas aeruginosa, enterobacteria and gram-positive cocci, received CPF (600 mg t.i.d.). The mean body surface area affected by third-degree burns was 31.8 ± 14.5%. Two series of blood samples were drawn after the first and seventh doses; urine was collected during the first infusion. Levels of CPF in serum and urine were measured by means of high-performance liquid chromatography. A non-compartmental method was used for kinetic and graphic analysis of concentration–time pairs. Results: No adverse effects were noted. Trough concentrations measured on day 3 (mean ± SD) were above the minimum inhibitory concentration (MIC) for the organism responsible for infection; i.e., 2.0 ± 1.2 μg · ml⁻¹, and maximum concentrations were high 9.9 ± 3.4 μg · ml⁻¹. An area under the concentration–time curve (AUC)/MIC ratio above 125 SIT⁻¹ (where SIT is the serum inhibitory titer), which has been strongly correlated with clinical response and time to bacterial eradication, was achieved in 11 patients with a MIC of 0.5 μg · ml⁻¹. There was a statistically significant difference between C_min and AUC determined on day 1 and day 3. In contrast to healthy volunteers, CPF clearance rates were notably decreased. Conclusion: The pharmacokinetics of CPF was altered in major-burn patients. The recommended dosage regimen for administration of CPF, i.e. 600 mg t.i.d. shows no adverse effects and a good microbiological efficacy. Received: 13 October 1998 / Accepted in revised form: 8 June 1999     

Pharmacokinetics of intravenously administered ciprofloxacin in intensive care patients with acute renal failure

The pharmacokinetics of ciprofloxacin after a single intravenous administration of 100 mg were studied in intensive care patients with an acute renal impairment. There was no correlation found between the creatinine clearance and the renal clearance of ciprofloxacin. This applies to the entire group of patients. The decrease in renal clearance of ciprofloxacin was, however, more pronounced than the change in the elimination half-life, suggesting an important extra-renal elimination of the drug.     

Pharmacokinetics and Pharmacodynamics of Nitrendipine

ＰｈａｒｍａｃｏｋｉｎｅｔｉｃｓａｎｄＰｈａｒｍａｃｏｄｙｎａｍｉｃｓｏｆＮｉｔｒｅｎｄｉｐｉｎｅＰｈａｒｍａｃｏｋｉｎｅｔｉｃｓａｎｄＰｈａｒｍａｃｏｄｙｎａｍｉｃｓｏｆＮｉｔｒｅｎｄｉｐｉｎｅＭａｒｓｔｅｒ＇ｓＤｅｇｒｅｅＺｈｅｎ－ＬｉＬｉｎＳｕ...     

氧氟沙星、环丙沙星抗胆道感染作用的实验研究

目的观察喹诺酮类抗生素(环丙沙星、氧氟沙星)在胆汁中的代谢过程,为临床医师提供胆道感染时合理选用有效抗生素的理论依据。方法犬为实验动物,行胆总管造瘘,以备留取胆汁标本。静脉滴注氧氟沙星(Ofloxacin)、环丙沙星(Ciprofloxacin)后,留取静脉及胆汁标本,用微生物法测定药物浓度,3P87软件数据处理,得出药物动力学参数。结果静脉滴注氧氟沙星、环丙沙星后,胆汁中主要的代谢参数峰值时间(Tpeakmin)分别为58、72;峰值浓度(Cmaxμg/ml)分别为8.02、8.81;半衰期(T     

家兔静注环丙沙星后血液与眼组织分布及其药代动力学研究

研究家兔静注环丙沙星 (CPL X)后血液与眼组织分布及药代动力学参数。用高效液相色谱法测定血液和眼内各组织中药物浓度。结果给药 30 min后泪液、角膜、房水、虹膜 -睫状体、晶状体和玻璃体组织内峰浓度值 (Cmax)分别为 (8.92± 2 .88)、(14 2 .84± 2 5 .0 2 )、(11.0 6± 2 .80 )、(99.32± 10 .6 0 )、(30 .2 8± 1.91)和(8.10± 1.71) μg/ ml或 μg/ g;其血液和各组织中消除半衰期 (T1 /2β)分别为 (1.2 1± 0 .2 3)、(1.4 8± 0 .97)、(1.6 6± 0 .13)、(2 .0 9± 0 .5 1)、(2 .0 1± 0 .4 4 )、(1.5 2± 0 .92 )和 (1.2 1± 0 .6 6 ) h。表明家兔静注 CPL X后能穿透到眼内各组织中。     

兔单剂静注替考拉宁的药物动力学

本文报道健康兔６只静注替考拉宁后的药物动力学。血药浓度用微生物法测定。剂静注替考拉宁２０ｍｇ／Ｋｇ后，体内药物转运过程符合二室开放模型。     

Pharmacokinetics of oral diltiazem and five of its metabolites in patients with chronic renal failure

The pharmacokinetics of oral diltiazem were studied in 10 patients with chronic renal failure not requiring dialysis and in five healthy volunteers after a single dose of 120 mg. We found that patients with chronic renal failure had lower amounts of unchanged diltiazem and of its main metabolite (MA) in urine and a trend to have slightly higher values of plasma concentration. Since the terminal elimination phase is not affected by chronic renal failure we conclude that this trend is probably the result of alterations in the volume of distribution of diltiazem in these patients.     

氧氟沙星和环丙沙星在老年人中的药物动力学

对氧氟沙星和环丙沙星在老年和年轻健康志愿者中的药物动力学进行同期比较研究。上述两药全部血、尿浓度均以高效液相色谱法测定。老年组单剂口服氧氟沙星３００ｍｇ后的平均血清Ｔ＿（１／２β）为７．０８±０．８１ｈ，Ｃｌ＿ｒ为９５．９±２１．０ｍｌ／ｍｉｎ，ＡＵＣ为３２．６±４．１ｈ·ｍｇ／Ｌ，与年轻组相比，血清Ｔ＿（１／２β）延长，Ｃｌ＿ｒ降低以及ＡＵＣ增大。老年组与年轻组的Ｃ＿（ｍａｘ）则相近，分别为４．６７±０．９８和４．７２±０．５１ｍｇ／Ｌ。老年组每１２ｈ口服氧氟沙星３００ｍｇ连续７天后的Ｃ＿（ｍａｘ）和ＡＵＣ较单剂者明显增高。老年组和年轻组单剂口服环丙沙星５００ｍｇ后的Ｔ＿（１／２ｋｅｌ）分别为３．３２±０．４３和２．７６±０．４３ｈ，Ｃｌ＿ｒ分别为２３１．４±６８．８和２５６．９±６４．０ｍｌ／ｍｉｎ，ＡＵＣ分别为１７．７±４．９和１５．９±３．５ｈ·ｍｇ／Ｌ。根据本研究结果，对上述两药在治疗老年人感染时给药方案的调整提出了建议。