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Transdermal delivery of 4-aminopyridine accelerates motor functional recovery and improves nerve morphology following sciatic nerve crush injury in mice 预览
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作者 Andrew RClark Chia George Hsu +2 位作者 M A Hassan Talukder Mark Noble John CElfar 《中国神经再生研究:英文版》 SCIE CAS CSCD 2020年第1期136-144,共9页
Oral 4-aminopyridine(4-AP)is clinically used for symptomatic relief in multiple sclerosis and we recently demonstrated that systemic 4-AP had previously unknown clinically-relevant effects after traumatic peripheral n... Oral 4-aminopyridine(4-AP)is clinically used for symptomatic relief in multiple sclerosis and we recently demonstrated that systemic 4-AP had previously unknown clinically-relevant effects after traumatic peripheral nerve injury including the promotion of re-myelination,improvement of nerve conductivity,and acceleration of functional recovery.We hypothesized that,instead of oral or injection administration,transdermal 4-AP(TD-4-AP)could also improve functional recovery after traumatic peripheral nerve injury.Mice with surgical traumatic peripheral nerve injury received TD-4AP or vehicle alone and were examined for skin permeability,pharmacokinetics,functional,electrophysiological,and nerve morphological properties.4-AP showed linear pharmacokinetics and the maximum plasma 4-AP concentrations were proportional to TD-4-AP dose.While a single dose of TD-4-AP administration demonstrated rapid transient improvement in motor function,chronic TD-4-AP treatment significantly improved motor function and nerve conduction and these effects were associated with fewer degenerating axons and thicker myelin sheaths than those from vehicle controls.These findings provide direct evidence for the potential transdermal applicability of 4-AP and demonstrate that 4-AP delivered through the skin can enhance in-vivo functional recovery and nerve conduction while decreasing axonal degeneration.The animal experiments were approved by the University Committee on Animal Research(UCAR)at the University of Rochester(UCAR-2009-019)on March 31,2017. 展开更多
关键词 4-AMINOPYRIDINE electron MICROSCOPY functional recovery NERVE conduction velocity PERIPHERAL NERVE injury PHARMACOKINETICS TRANSDERMAL administration
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More Rapid Sleep Onset with Lingual-Spray vs Oral-Tablet Delivery Zolpidem 预览
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作者 Robert B. Raffa Gerwin Westfield 《药理与制药(英文)》 2019年第7期329-342,共14页
Insomnia and related sleep disorders (somnipathies) affect a large segment of the population, and result in a significant negative impact on quality of life and reduced or lost productivity. The speed of sleep onset i... Insomnia and related sleep disorders (somnipathies) affect a large segment of the population, and result in a significant negative impact on quality of life and reduced or lost productivity. The speed of sleep onset is a critical characteristic of successful pharmacotherapeutic intervention for insomnia. Zolpidem, a non-benzodiazepine benzodiazepine receptor agonist (nBzRA) is widely used to treat insomnia. Although not itself a benzodiazepine (BZD), zolpidem has high binding affinity for the benzodiazepine receptor, which acts as a positive allosteric modulator of the GABAA receptor complex. It therefore increases the neuronal transmembrane influx of Cl- ions, thereby decreasing neuronal excitability and promoting sleep. In this four-way crossover, dose-ranging, multiple-treatment study, a lingual spray formulation of zolpidem was safe and well-tolerated and yielded more rapid pharmacokinetics (mean plasma concentration) and efficacy (visual analog scale and digit symbol substitution test) compared to oral tablets. 展开更多
关键词 ZOLPIDEM LINGUAL SPRAY PHARMACOKINETICS Efficacy Safety/Tolerability AMBIEN
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A Reliable Method to Quantify Trimethoprim and Sulfamethoxazole in Plasma of Children by HPLC with Application in Pharmacokinetic Studies 预览
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作者 Alejandra Toledo Ló pez +10 位作者 Hugo Juá rez Olguí n Ismael Lares-Asseff Fernanda Reyes Gonzá lez Radames Alemon Medina Gabriela Pé rez Guillé Francisca Trujillo Jimenez 《美国分析化学(英文)》 2019年第7期247-253,共7页
Aim: To develop a simple and sensitive high-performance liquid chromatography method to determine plasmatic levels of trimethoprim/sulfamethoxazole in paediatric population. Method: Chromatographic separation was carr... Aim: To develop a simple and sensitive high-performance liquid chromatography method to determine plasmatic levels of trimethoprim/sulfamethoxazole in paediatric population. Method: Chromatographic separation was carried out using a reverse phase column with detection ultraviolet at a wavelength of 225 nm. The mobile phase consists of phosphate buffer 0.1 M, acetonitrile and methanol, (65:20:15) with a flow of 1.0 ml/min. Results: Calibration curve was linear over the concentration range for trimethoprim of 0.25 to 5 μg/ml and 5 to 100 μg/ml for sulfamethoxazole. Precision were found to be within 15% for both compounds. The detection limits and quantifications for trimethoprim/sulfamethoxazole were 0.2 - 0.25 μg/ml and 3 - 5 μg/ml respectively. Conclusions: The developed method was applied for the quantification of both compounds in plasma samples of two patients resulting concentrations within the therapeutic ranges. The method is convenient for pharmacokinetic studies. 展开更多
关键词 CHILDREN Liquid Chromatography Phase REVERSE PHARMACOKINETICS
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A New Pharmacokinetic Model of Propofol for Japanese Patients 预览
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作者 Masahito Omote Shunsuke Tachibana +1 位作者 Yasuyuki Tokinaga Michiaki Yamakage 《麻醉学期刊(英文)》 2019年第9期179-188,共10页
Target-controlled infusion (TCI) of propofol is used for general anesthesia. However, the only pharmacokinetic parameter commercially used for Japanese patients is weight, and pharmacokinetic models are based on Europ... Target-controlled infusion (TCI) of propofol is used for general anesthesia. However, the only pharmacokinetic parameter commercially used for Japanese patients is weight, and pharmacokinetic models are based on European physical attributes. Drug metabolism also differs in races. This study aimed to identify optimal continuous doses of propofol for Japanese patients and to create a simulated pharmacokinetic (PK) model. Thirty Japanese patients were enrolled. Patients received a constant infusion of 9 mg/kg/h of propofol. Arterial blood samples were collected and the time course of plasma propofol concentrations was modeled using the nonlinear mixed effects model (NONMEM) three-compartmental PK model. We validated the model by intravenously injecting 10 patients with a TCI driver system programmed with the NONMEM model. Our model’s performance was evaluated using the median prediction error (MDPE), median absolute prediction error (MDAPE), and Wobble. We analyzed 320 blood samples for model building and 160 samples for validating our new model. The calculated parameters for the three-compartmental PK model were volume [V1, 3.58;V2, 13.0 + 0.49 × (Age—64);and V3, 186] and elimination clearance [CL1, 0.77 + (WT—54) × 0.04 + (HT—158) × 0.03;CL2, 0.89 + 0.12 × (Age—64);and CL3, 0.98 × exp ((Age—64)/10)]. The new model improved MDPE, MDAPE, and Wobble values (11.5% ± 43.8%, 14.3% ± 33.0%, and 25.0% ± 21.3%, respectively). We created a new pharmacokinetic model for Japanese patients, which is more accurate than the three existing models applied to Japanese populations. Electronic document is a “live” template. The various components of your paper [title, text, heads, etc.] are already defined on the style sheet, as illustrated by the portions given in this document. 展开更多
关键词 PROPOFOL PHARMACOKINETICS Target-Controlled INFUSION JAPANESE
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成人应用伏立康唑的群体药动学研究进展 预览
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作者 刘思敏 蔡俊 +3 位作者 李慧馨 杨立 赵燕 张晋萍 《中国临床药理学与治疗学》 CAS CSCD 2019年第9期1015-1023,共9页
目的:伏立康唑抗真菌活性强,抗真菌谱广,但其药动学呈现高度变异性。本文基于群体药动学模型对伏立康唑的药动学特征进行描述,为伏立康唑的个体化用药提供理论依据。方法:通过对中国知网、Pubmed、Web of Science等数据库查找伏立康唑... 目的:伏立康唑抗真菌活性强,抗真菌谱广,但其药动学呈现高度变异性。本文基于群体药动学模型对伏立康唑的药动学特征进行描述,为伏立康唑的个体化用药提供理论依据。方法:通过对中国知网、Pubmed、Web of Science等数据库查找伏立康唑群体药动学研究文献进行汇总分析,描述伏立康唑药动学特征。结果:9篇文献报道伏立康唑的群体药动学模型为一房室模型,4篇文献为二房室模型。伏立康唑代谢的主要影响因素为年龄、体质量、CY2C19基因型、肝功能和合并用药。结论:伏立康唑个体间存在相当大的差异性。对于特殊人群,制定个性化给药方案尤为重要。 展开更多
关键词 伏立康唑 药动学 群体药动学 影响因素
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东莨菪内酯的药理活性及药代动力学研究进展 预览
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作者 褚子璇 卢敏 熊山 《化学研究》 CAS 2019年第4期434-440,共7页
东莨菪内酯是一种香豆素类化合物,具有抗肿瘤、抗炎、降血糖、降血压、抗神经退行性疾病等多种药理活性.药代动力学方面,东莨菪内酯具有吸收快,组织分布广等特点.本文总结了近年来东莨菪内酯的药理作用及药代动力学的研究进展,以期为其... 东莨菪内酯是一种香豆素类化合物,具有抗肿瘤、抗炎、降血糖、降血压、抗神经退行性疾病等多种药理活性.药代动力学方面,东莨菪内酯具有吸收快,组织分布广等特点.本文总结了近年来东莨菪内酯的药理作用及药代动力学的研究进展,以期为其深入研究和开发利用提供参考. 展开更多
关键词 东莨菪内酯 药理活性 药代动力学
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2018年药物代谢和药物动力学国家自然科学基金资助项目简介
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作者 曾苏 《中国现代应用药学》 CAS CSCD 北大核心 2019年第4期389-391,共3页
本文对2018年批准的药物代谢和药物动力学学科国家自然科学基金30个资助项目进行分析和分类,总结其重要研究方向,为药物代谢和药物动力学科研人员撰写和评审国家自然科学基金项目提供参考,以期为我国药物代谢和药物动力学研究提出和选... 本文对2018年批准的药物代谢和药物动力学学科国家自然科学基金30个资助项目进行分析和分类,总结其重要研究方向,为药物代谢和药物动力学科研人员撰写和评审国家自然科学基金项目提供参考,以期为我国药物代谢和药物动力学研究提出和选出高水平项目,从而加快追赶国际先进水平。 展开更多
关键词 药物代谢 药物动力学 国家自然科学基金 资助项目
Development and validation of an LC-MS/MS method for tyrphostin A9 预览
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作者 Lyndsey F. Meyer Dhaval K. Shah 《药物分析学报:英文版》 CAS CSCD 2019年第3期163-169,共7页
Here we have presented a sensitive and selective LC-MS/MS method for the quantification of tyrphostin A9, which is a selective inhibitor for platelet derived growth factor receptor tyrosine kinase and has been investi... Here we have presented a sensitive and selective LC-MS/MS method for the quantification of tyrphostin A9, which is a selective inhibitor for platelet derived growth factor receptor tyrosine kinase and has been investigated in vitro as a potent oxidative phosphorylation uncoupler. The murine analytical method was developed for three biological matrices: cell culture media, 3T3-L1 cell lysate, and murine plasma. For each matrix the limit of detection and the limit of quantification were found to be 0.5 ng/mL and 1.0 ng/ mL, respectively. The range of standard curve for each matrix was 1.0-100 ng/mL, linearity was >0.99, and the precision and accuracy were within 20%. 3-(3,5-di-tert-butyl-4-hydroxyphenyl) propanoic acid was found to be the most suitable internal standard. The validated LC-MS/MS method was used to investigate stability and in vitro pharmacokinetics of tyrphostin A9. It was found that tyrphostin A9 is susceptible to hydrolysis, and the degradation product was identified as 3,5-di-tert-butyl-4- hydroxybenzaldehyde. Tyrphostin A9 was not stable in biological matrices, and the rate of its degradation in murine plasma was faster than that in cell culture media. In vitro pharmacokinetic studies revealed that tyrphostin A9 concentrations in the cell culture media declined in a bi-exponential manner and the concentrations inside the adipocytes remained constant, suggesting tyrphostin A9 has an intracellular binding site and is retained within the cell. The LC-MS/MS method presented here paves the way for further quantitative investigations involving tyrphostin A9. 展开更多
关键词 TYRPHOSTIN 9/ A9/AG-9/Malonoben/SF6847 LC-MS/MS Stability PHARMACOKINETICS TYROSINE KINASE inhibitor
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GC-MS测定莪术中β-榄香烯的血药浓度及大鼠体内药代动力学研究
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作者 李婧 刘文静 《药物分析杂志》 CAS CSCD 北大核心 2019年第5期846-851,共6页
目的:建立快速灵敏的气质联用(GC-MS)法测定莪术中β-榄香烯在大鼠血浆中血药浓度,并研究β-榄香烯在大鼠体内的药代动力学特征。方法:血浆样品的处理采用正己烷液-液萃取方法,萘为内标。色谱柱:DB-5毛细管柱(30 m×0.25 mm,0.25μ... 目的:建立快速灵敏的气质联用(GC-MS)法测定莪术中β-榄香烯在大鼠血浆中血药浓度,并研究β-榄香烯在大鼠体内的药代动力学特征。方法:血浆样品的处理采用正己烷液-液萃取方法,萘为内标。色谱柱:DB-5毛细管柱(30 m×0.25 mm,0.25μm);程序升温:初始60℃,保持1 min,再以30℃·min^-1的速度升温至160℃,保持3 min,再以10℃·min^-1的速度升温至200℃,保持2 min。采用电子轰击离子源及选择离子扫描模式(SIM);选择监测离子:β-榄香烯m/z 93,内标m/z 128。按β-榄香烯10 mg·kg^-1灌胃给药后,测定大鼠血浆中β-榄香烯的浓度,并用DAS 2.0软件计算药代动力学参数。结果:血浆中β-榄香烯质量浓度在0.05~200.0μg·mL^-1浓度范围内线性关系良好(r2=0.999 1),定量下限为0.05μg·mL^-1;低、中、高3个浓度准确度、日内及日间精密度均小于5%;提取回收率分别为91.7%、105.1%、108.8%;低、中、高3个浓度血浆样品在室温放置12 h,4℃冰箱中放置24 h及反复冻融4次后均能保持稳定。大鼠灌胃莪术提取液后β-榄香烯药-时曲线符合二室模型;主要药代学参数:AUC0-t为(9.83±1.07)μg·L^-1·h,t1/2α为(0.47±0.05)h,t1/2β为(1.82±3.11)h,Tmax为(2.06±0.37)h,Cmax为(2.61±0.17)μg·mL^-1。结论:该方法简便、准确,专属性强,适用于莪术中β-榄香烯在大鼠体内的药代动力学研究。 展开更多
关键词 莪术 Β-榄香烯 液-液萃取 挥发油 大鼠血浆 血药浓度 药代动力学 气相色谱质谱联用
头孢噻呋在动物呼吸道感染的应用 预览
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作者 孙达 米坤 +1 位作者 袁宗辉 黄玲利 《中国抗生素杂志》 CAS CSCD 2019年第10期1140-1147,共8页
头孢噻呋作为第一个畜禽专用的第三代头孢类抗生素,其抗菌谱广,抗菌活性强,对革兰阳性细菌和革兰阴性细菌都有较强的抗菌活性。本文概述了头孢噻呋对呼吸道细菌的抗菌活性,药动学,动物呼吸道的临床应用与安全性等方面。通过对头孢噻呋... 头孢噻呋作为第一个畜禽专用的第三代头孢类抗生素,其抗菌谱广,抗菌活性强,对革兰阳性细菌和革兰阴性细菌都有较强的抗菌活性。本文概述了头孢噻呋对呼吸道细菌的抗菌活性,药动学,动物呼吸道的临床应用与安全性等方面。通过对头孢噻呋的发展以及临床的应用概述,有利于促进头孢噻呋在兽医临床中合理应用,有效缓解食品安全和减少细菌耐药性等问题。 展开更多
关键词 头孢噻呋 抗菌活性 药动学 呼吸道 临床应用
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Pharmacological and analytical aspects of artemisinin for malaria: Advances and challenges
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作者 Sravani Karri Sanjay Sharma Ginpreet Kaur 《亚太热带医药杂志:英文版》 SCIE CAS 2019年第8期339-346,共8页
Malaria remains a major tropical health burden owing to the development of resistance and decreased sensitivity to the frequently used conventional antimalarial drugs. The drug like artemisinin possesses potent antima... Malaria remains a major tropical health burden owing to the development of resistance and decreased sensitivity to the frequently used conventional antimalarial drugs. The drug like artemisinin possesses potent antimalarial activities, but has some limitations. Therefore, new strategies are to be implemented for optimal utilization of artemisinin to improve its therapeutic effectiveness and to overcome its limitations. The present review focuses on present scenario of malaria and pharmacological as well as analytical aspects of artemisinin. Data from 2000 to 2018 were collected from NCBI for understanding the various analytical techniques used for estimation of artemisinin. This review will reveal the facts about artemisinin which can be utilized to develop novel drug delivery system either in a combination or as alone for the wellbeing of the patients suffering from malaria. 展开更多
关键词 MALARIA ARTEMISININ PHARMACOKINETICS Mechanism ANALYTICAL techniques
HPLC-MS/MS测定大鼠血浆中普萘洛尔的含量及其药动学研究
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作者 魏娟 贾琪 +3 位作者 姚广哲 欧阳慧子 常艳旭 何俊 《中国现代应用药学》 CAS CSCD 北大核心 2019年第18期2241-2244,共4页
目的建立大鼠血浆中普萘洛尔的高效液相色谱-质谱联用(HPLC-MS/MS)定量分析方法,考察大鼠口服给药后,普萘洛尔在其体内的药动学特征。方法血浆样品用甲醇沉淀蛋白法处理后,以盐酸美西律为内标,采用LC-MS/MS分析方法,测定大鼠血浆中普萘... 目的建立大鼠血浆中普萘洛尔的高效液相色谱-质谱联用(HPLC-MS/MS)定量分析方法,考察大鼠口服给药后,普萘洛尔在其体内的药动学特征。方法血浆样品用甲醇沉淀蛋白法处理后,以盐酸美西律为内标,采用LC-MS/MS分析方法,测定大鼠血浆中普萘洛尔的浓度。色谱柱为ZORBAX Eclipse Plus C18柱(2.1 mm×100 mm,3.5μm),流动相为0.1%甲酸水溶液-乙腈(70∶30)等度洗脱;采用ESI离子源,正离子模式,多反应离子监测(MRM)m/z 260.2→116.2(普萘洛尔)和m/z 180.2→58.2(内标盐酸美西律)。结果普萘洛尔在5~1 000 ng·mL^-1内线性关系良好;日内、日间精密度RSD为0.36%~6.39%,准确度为96.19%~113.38%;提取回收率为86.82%~96.12%;基质效应为100.1%~103.1%。结论本方法经方法学验证,可用于大鼠血浆中普萘洛尔的测定及其药动学研究。 展开更多
关键词 普萘洛尔 高效液相色谱-质谱联用 大鼠 血浆 药动学
介孔二氧化硅在药物递送系统及其体内外研究进展 预览
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作者 张文君 吴梦婷 +2 位作者 吕春艳 王晴 陈泳霖 《生物技术通报》 CAS CSCD 北大核心 2019年第12期159-168,共10页
介孔二氧化硅纳米粒因比表面积大、孔隙率高、介孔结构可调、表面易修饰等特点,近年来在生物医学领域受到广泛的关注。介孔二氧化硅作为一种新型载体,相比于传统的纳米载体不仅可以改善难溶性药物的溶解度,有效地提高药物的生物利用度,... 介孔二氧化硅纳米粒因比表面积大、孔隙率高、介孔结构可调、表面易修饰等特点,近年来在生物医学领域受到广泛的关注。介孔二氧化硅作为一种新型载体,相比于传统的纳米载体不仅可以改善难溶性药物的溶解度,有效地提高药物的生物利用度,还可以通过修饰或包覆功能性物质实现对肿瘤细胞的靶向性及控制药物的吸附、释放,且其稳定的框架结构可以递送和保护核酸分子,达到基因治疗的目的。然而,要将介孔二氧化硅纳米粒应用于临床,还需要做进一步的工作来预测和评估潜在的毒性和不良反应,明确介孔二氧化硅纳米粒在体内的吸收、分布、代谢、排泄及生物相容性和毒性,以确保其在患者中的有效性和安全性。综述了介孔二氧化硅纳米粒在药物递送系统及基因治疗的应用,着重介绍了靶向型介孔二氧化硅以及刺激响应型介孔二氧化硅的一些研究成果,并对介孔二氧化硅的药物代谢动力学、生物相容性和毒性的研究情况进行了深入的总结,旨为介孔二氧化硅在生物医学的应用提供参考。 展开更多
关键词 介孔二氧化硅 药物递送系统 基因治疗 药物代谢动力学 生物相容性 毒性
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淫羊藿化学成分分析及其药代动力学研究进展 预览
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作者 欧阳慧子 何俊 《天津中医药大学学报》 CAS 2019年第3期219-227,共9页
淫羊藿作为补肾阳中药,具有悠久的用药历史。通过回顾淫羊藿化学成分分析及其药代动力学研究,发现淫羊藿成分复杂多样(如黄酮类、生物碱类、酚酸类等),易受到品种、产地、部位、加工炮制等因素的影响,且淫羊藿各类成分的体内过程差异较... 淫羊藿作为补肾阳中药,具有悠久的用药历史。通过回顾淫羊藿化学成分分析及其药代动力学研究,发现淫羊藿成分复杂多样(如黄酮类、生物碱类、酚酸类等),易受到品种、产地、部位、加工炮制等因素的影响,且淫羊藿各类成分的体内过程差异较大,疾病、组方配伍、炮制加工及中西药联用对其药代动力学参数均有不同程度的影响。文章归纳淫羊藿成分分析及体内过程的研究思路和方法,探讨了目前研究中存在的一些问题,以期为淫羊藿质量控制、新药开发与临床应用研究提供参考。 展开更多
关键词 淫羊藿 化学成分 分析方法 药代动力学 研究进展
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何首乌的入血成分、药动学及肝毒性代谢组学研究进展
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作者 蒙钟经 丁选胜 《药学进展》 CAS 2019年第5期379-383,共5页
中药何首乌为蓼科植物何首乌Polygonum multiflorum Thunb.的干燥块根,是一种常用的补益中药,并兼有药食同源的应用基础。但近年来,何首乌及其制剂导致药源性肝损伤的报道日益增多,其安全性问题已成为人们关注的焦点。基于此,对近年来... 中药何首乌为蓼科植物何首乌Polygonum multiflorum Thunb.的干燥块根,是一种常用的补益中药,并兼有药食同源的应用基础。但近年来,何首乌及其制剂导致药源性肝损伤的报道日益增多,其安全性问题已成为人们关注的焦点。基于此,对近年来何首乌入血成分、药动学及肝毒性代谢组学的研究进展进行综述,以期为何首乌在临床上安全、合理应用提供参考。 展开更多
关键词 何首乌 肝毒性 入血成分 药动学 代谢组学
Development of a method to quantify total and free irinotecan and 7-ethyl-10-hydroxycamptothecin(SN-38)for pharmacokinetic and bio-distribution studies after administration of irinotecan liposomal formulation 预览
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作者 Wenqian Yang Zimeng Yang +2 位作者 Jieru Liu Dan Liu Yongjun Wang 《亚洲药物制剂科学(英文)》 2019年第6期687-697,共11页
In 2015,liposomal formulation of irinotecan(ONIVYDE)has been approved by FDA and widely applied in the treatment of pancreatic cancer.ONIVYDE is a novel liposome formulation,entrapping CPT-11 in the aqueous core of ve... In 2015,liposomal formulation of irinotecan(ONIVYDE)has been approved by FDA and widely applied in the treatment of pancreatic cancer.ONIVYDE is a novel liposome formulation,entrapping CPT-11 in the aqueous core of vesicles using a modified gradient loading method.Due to toxicity concerns,it is essential to explore a rapid and reliable method to effectively isolate and quantify the non-liposomal,namely,free CPT-11and total CPT-11 in plasma.This study focuses on separation of non-liposomal CPT-11,evaluation of the pharmacokinetics of free CPT-11 and total CPT-11 and bio-distribution after intravenous administration of CPT-11 liposome.Free CPT-11 in plasma was separated by solid-phase extraction(SPE).The amount of total CPT-11 and main metabolite 7-ethyl-10-hydroxycamptothecin(SN-38)in plasma was quantified by ultra-performance liquid chromatography–MS/MS.The calibration curves fitted well and lower limit of quantitation for SN-38,free CPT-11,total CPT-11 and CPT-11 in tissue and were 5 ng/ml,10 ng/ml,4.44 ng/ml and 25 ng/ml respectively.The recoveries,precision and accuracy of the method appear satisfactory.Using this method,the pharmacokinetics and bio-distribution of CPT-11 liposome formulation after an intravenous dose of 2.5 mg/kg were then investigated. 展开更多
关键词 IRINOTECAN Liposome UPLC-MS-MS SPE Pharmacokinetics Bio-distribution
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动物专用药物氟苯尼考的研究进展
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作者 张春辉 邢广旭 +5 位作者 胡骁飞 邓瑞广 王方雨 张改平 吕全建 张卫宪 《中兽医医药杂志》 2019年第5期95-98,共4页
从氟苯尼考的构效关系、药物效应动力学及药物动力学等方面进行综述,为更科学地指导临床使用氟苯尼考,延长氟苯尼考的使用期限,保障动物源食品的安全提供参考。
关键词 氟苯尼考 药效学 药代动力学 体内过程 检测方法
重症患者万古霉素谷浓度达标情况及其影响因素分析
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作者 王金龙 王皓飞 +5 位作者 石梦娟 徐静媛 黄丽丽 李卿 刘松桥 黄英姿 《中华内科杂志》 CAS CSCD 北大核心 2019年第8期572-576,共5页
目的探讨重症患者万古霉素谷浓度的达标情况及其影响因素。方法纳入2015年1月至2017年12月入住东南大学附属中大医院ICU,接受静脉滴注万古霉素治疗的成人重症患者(年龄≥18岁)。记录万古霉素给药方案,监测稳定状态时万古霉素谷浓度。观... 目的探讨重症患者万古霉素谷浓度的达标情况及其影响因素。方法纳入2015年1月至2017年12月入住东南大学附属中大医院ICU,接受静脉滴注万古霉素治疗的成人重症患者(年龄≥18岁)。记录万古霉素给药方案,监测稳定状态时万古霉素谷浓度。观察不同肌酐清除率的重症患者万古霉素谷浓度的达标情况。采用线性回归分析重症患者万古霉素谷浓度的影响因素。结果共纳入85例患者,仅23.5%(20/85)的重症患者达到万古霉素目标谷浓度(15~20 mg/L);肾功能正常的重症患者,仅11.4%(4/35)的患者达到万古霉素目标谷浓度,80.0%(28/35)的肾功能正常患者万古霉素谷浓度低于15 mg/L。简单线性回归分析结果显示,急性生理与慢性健康状况评分Ⅱ(APACHE Ⅱ)、序贯器官功能衰竭评分(SOFA)、感染性休克、去甲肾上腺素剂量、超敏C反应蛋白、降钙素原、尿素氮、血肌酐、估算肾小球滤过率(eGFR)与万古霉素谷浓度显著相关(P<0.05)。多元线性回归分析显示,降钙素原、eGFR、APACHE Ⅱ是万古霉素谷浓度的独立影响因素(P<0.05)。结论重症患者万古霉素谷浓度的不达标率高,降钙素原、eGFR、APACHE Ⅱ是重要的影响因素。 展开更多
关键词 万古霉素 谷浓度 药代动力学 肾毒性
LC-MS/MS法测定人血浆中霉酚酸浓度及其在心脏移植患者药动学研究中的应用 预览
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作者 赵晓亚 王艺茸 +5 位作者 周红 蔡杰 张菁 向红平 张敏 韩勇 《医药导报》 CAS 北大核心 2019年第10期1326-1330,共5页
目的建立一种液相色谱-质谱串联(LC-MS/MS)法测定人血浆中霉酚酸(MPA)浓度,用于心脏移植患者药动学研究及治疗药物浓度监测。方法取血浆样品200μL,加入MPA-d3内标(2μg·mL-1)20μL,乙腈沉淀,取上清液进样。Agilent ZORBAX SB-C18(... 目的建立一种液相色谱-质谱串联(LC-MS/MS)法测定人血浆中霉酚酸(MPA)浓度,用于心脏移植患者药动学研究及治疗药物浓度监测。方法取血浆样品200μL,加入MPA-d3内标(2μg·mL-1)20μL,乙腈沉淀,取上清液进样。Agilent ZORBAX SB-C18(2.1 mm×50 mm, 3.5μm)色谱柱进行分离;5 mmol乙酸铵(0.25%甲酸)溶液(A)-乙腈(B)为流动相,梯度洗脱,流速0.2 mL·min^-1。用多反应监测进行定量,ESI负离子方式进行检测,用于定量分析的离子对为m/z 319.1→191.0 (MPA)与m/z 322.1→191.1 (内标MPA-d3)。6例心脏移植患者采用他克莫司+吗替麦考酚酯(MMF)+泼尼松的三联免疫抑制方案,测定首次服用MMF后0~12 h的MPA浓度并计算药动学参数。30例患者服用MMF 0.5 g,q12h,至少7 d,检测达稳态后的谷浓度。结果 MPA在0.1~40μg·mL^-1范围内线性良好(R2>0.99)。MPA日内及日间变异均小于10%,提取回收率为96.3%~97.9%,基质效应为99.7%~106.5%。6例心脏移植患者单次给予MMF1 g后,MPA的主要药动学参数:峰浓度(Cmax)为(7.58±5.09)μg·mL^-1,峰时间(tmax)为(1.83±1.13) h,AUC0-12为(26.58±7.23)μg·mL^-1·h,AUC0-∞为(37.41±14.42)μg·mL^-1·h,t1/2为(7.53±8.01) h。CL/F为(29.36±7.78)L·h^-1,Vd为(258.80±177.96)L。30例患者血浆MPA稳态谷浓度为0.37~3.832μg·mL^-1,个体间变异高达59.2%。结论该研究所建立的方法简单、准确、灵敏、专属性强,适用于心脏移植患者MPA药动学研究及治疗药物浓度监测。 展开更多
关键词 霉酚酸 心脏移植 药动学 血药浓度监测 LC-MS/MS法
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Characteristics of the traditional Liu-Wei-Di-Huang prescription reassessed in modern pharmacology
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作者 CHENG Xiao-Rui QI Chun-Hui +2 位作者 WANG Tong-Xing ZHOU Wen-Xia ZHANG Yong-Xiang 《中国天然药物:英文版》 SCIE CAS CSCD 2019年第2期103-121,共19页
Liu-Wei-Di-Huang(LW) is a Yin nourishing and kidney tonifying prescription in traditional Chinese medicine with promising pharmacological characteristics that can be further exploited and developed in modern medicine.... Liu-Wei-Di-Huang(LW) is a Yin nourishing and kidney tonifying prescription in traditional Chinese medicine with promising pharmacological characteristics that can be further exploited and developed in modern medicine. We provide a comprehensive and detailed literature report on the clinical and experimental pharmacology of LW,including its quality control parameters, phytochemistry, pharmacokinetics, and toxicology. Our literature review indicates that the LW prescription possesses a unique combination of pharmacological characteristics that can be safely used for treating very different diseases. Quality control and pharmacokinetic parameters of LW are mostly based on its major bioactive phytochemical constituents. We postulate that modulating or rebalancing the neuroendocrine immunomodulation network in the body is the underlying mechanism of the multiple pharmacological activities displayed by LW. 展开更多
关键词 Liu-Wei-Di-Huang TRADITIONAL Chinese medicine Pharmacology PHYTOCHEMISTRY Pharmacokinetics Toxicology
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