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Physicochemical Properties and Evaluation of Microemulsion Systems for Transdermal Delivery of Meloxicam

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Chemical Research in Chinese Universities 2007年第1期23卷 81-86页

作者： YUAN Yue LI San-ruing YU Li-min DENG Pan zhong da-fang School of Pharmacy Shenyang Pharmaceutical University Shenyang 110016 P. R. China Center for Drug Metabolism and Pharmacokinetics Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 P. R. China

Microemulsion systems, composed of water, isopropyl myristate （IPM）, polyoxyethylene sorbitan trioleate （Tween 85 ）, and ethanol, were investigated as transdermal drug delivery vehicles for a lipophilic model drug（ meloxicam）. The purpose of this study was to investigate the physicochemieal properties of the tested microemulsion and to find the correlation between the physicoehemical properties and the skin permeation rate of the microemulsion. Pseudo-ternary phase diagram of the investigated system at a constant surfactant/cosurfactant mass ratio （ Km = 1 ： 1 ） was constructed by titration at 20℃, and the five fommlations were selected for further research in the o/w microemulsion domains. The values of electrical conductivity and viscosity showed that the selected systems were bicontinuous or non-spherical o/w microemulsion, and the electrical conductivity and viscosity were increased with increasing the content of water. These results suggest that the optimum formulation of microemulsion, containing 0. 375 meloxicam, 5% isopropyl myristate, 25% Tween 85. 25% ethanol, and water, showed the maximum permeation rate. It had a high electrical conductivity, small droplet size, and proper viscocity.

关键词： Microemulsion Physicochemical property Transdermal delivery Meloxicam Polyoxyethylene sorbitan triolcate

Quantification of Erdosteine in the Low-volume of Dog Plasma by Liquid Chromatography Tandem Mass Spectrometry

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Chemical Research in Chinese Universities 2007年第6期23卷 736-741页

作者： LIU dan WANG Yan TANG Yun-biao CHEN Xiao-yan zhong da-fang Laboratory of Drug Metabolism and Pharmacokinetics Shenyang Pharmaceutical University Shenyang 110016 P. R. China The First Hospital of Jilin University Changchun 130021 P. R. China Department of Pharmacy General Hospital of Shenyang Military Region Shenyang 110015 P. R. China Center for Drug Metabolism and Pharmacokinetics Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 P. R. China

Introduction Erdosteine [ N-（ carboxymethylthioacetyl ）-homocysteine thiolactone ] （ Fig. 1 ） is a synthetic derivative of natural amino acid methionine. It has been commonly used in clinical practice as a mucolytic drug and as an enhancer of respiratory ventilation in the treatment of patients with chronic obstructive respiratory disease. Erdosteine contains 2 blocked sulfhydryl groups, which are released after metabolic transformation in the liver. The liberated sulfhydryl groups break the disulphide bonds, which hold the glycoprotein fibres of mucus together; this makes the bronchial secretions more fluid and allows more rapid elimination. The reducing potential of these sulfhydryl groups accounts for the free radical scavenging and antioxidant properties of erdosteine.

关键词： Erdosteine Dog plasma Pharmacokinetics HPLC/MS/MS

Liquid Chromatography-Electrospray Ionization Mass Spectrometry Method for Determination of Protopanaxadiol in Rat Plasma

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Chemical Research in Chinese Universities 2009年第5期25卷 673-676页

作者： WU Yi TENG Guo-sheng LIANG Yong-tao zhong da-fang LIU Bing College of Pharmacy Jilin University Changchun 130021 P. R. China College of Life Science Jilin University Changchun 130012 P. R. China School of Chemistry and Life Science Changchun University of Technology Changchun 130012 P. R. China Jilin Provincial Corps Hospital Chinese People＇s Armed Police Forces Changchun 130052 P. R. China

A simple, rapid and sensitive method for the determination of protopanaxadiol in rat plasma with ginsenoside Rh2 as internal standard was developed and validated. The analyte and internal standard were extracted from plasma with ether-dichloromethane（3：2, volume ratio） and then were analyzed by reversed-phase HPLC on a short Zorbax Extend C18 column（50 mm×2.1 mm, 3.5 μm i. d.） eluted with a mobile phase consisting of acetonitrile/methanol 0.10 mmol/L ammonium acetate（45：45：10, volume ratio） at 0.4 mL/min. Detection was performed on an Applied Biosystems Sciex API 4000 mass spectrometer set at unit resolution in the multiple reaction monitoring mode. Electrospray ionization was used for ion production. The assay method shows linear over a range of 5-2000 ng/mL and intra- and inter-day precisions over this range were 〈10.0% with accuracy ranged from 86.3% to 114.1%. The limit of detection was 500 pg/mL in the plasma. The method was successfully applied to a preclinical pharmacokinetic study of protopanaxadiol（17.5 mg/kg） administered as a single oral dose.

关键词： Protopanaxadiol Ginsenoside Rh2 LC/MS

Rapid and Sensitive Liquid Chromatography-Tandem Mass Spectrometry for Quantification of Glycyrrhetic Acid in Human Plasma

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Chemical Research in Chinese Universities 2011年第2期27卷 185-189页

作者： TIAN Li GAO Xtao-li CHEN Xiao-yan zhong da-fang ZHANG Yi-fan daI Xiao-jian College of Trditional Chinese Medicine 2. College of Pharmacy Xinjiang Medical University Urumqi 830011 P R. China Center for Drug Metabolism and Pharmacokinetic Research Shanghai 201203 P. R. China

A simple, rapid and sensitive liquid chromatography-tandem mass spectrometry（LC-MS/MS） for the determination of glycyrrhetic acid in human plasma with ginsenoside Rh2 as internal standard was developed and validated. The plasma samples were prepared via liquid-liquid extraction with ethyl acetate. Chromatographic separation was accomplished on a Venusil MP-C18（50 mm×2.1 mm, 5 μm i.d.） column at 25 °C. The mobile phase consisted of acetonitrile/5 mmol？L-1 ammonium acetate（10：90, volume ratio） at a flow rate of 0.4 mL/min. Negative electrospray ionization was utilized as the ionization source. Glycyrrhetic acid and internal standard were determined via the mutiple reaction monitoring of precursor→production ion transitions at m/z 469→425, 409 and m/z 621→161, respectively. Each sample was chromatographed within 2.5 min. The lower limit of quantification was 0.50 ng/mL for 200 μL of plasma sample and the linear range was from 0.50 ng/mL to 800 ng/mL. The intra- and inter-day precisions were less than 8.76% in terms of relative standard deviation（RSD）, and the accuracy was within a range of -3.25%-1.32% in terms of relative error（RE）. The method was successfully applied to the pharmacokinetic studies of glycyrrhetic acid in healthy male Chinese volunteers after a single oral administration of 75 mg of glycyrrhizin.

关键词： Liquid chromatography-tandem mass spectrometry(LC-MS/MS) Glycyrrhetic acid Pharmacokinetics

Design and Synthesis of a Novel Peptidomimetic Inhibitor of Caspase-3

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Chemical Research in Chinese Universities 2006年第2期22卷 225-228页

作者： ZHANG Jin-liang LIU Lin-hua GUO Yang-hong YANG Jin-gang LI Wei zhong da-fang WANG Ji-dong College of Life Science Jilin University Changchun 130021 P. R. China

Caspases, a family of cysteine proteases, comprise of highly homologous enzymes that play an important role in apoptotic cell death. Caspase-3 shows key functions in apoptosis, mediating apoptotic cascade from the intrinsic and extrinsic activation pathways. Therefore, caspase-3 is an attractive target for therapeutic intervention. For instance, inhibitors of caspase-3 have been described as promising cardioprotectants, neuroprotectants and antiarthritic agents. A novel peptidomimetic inhibitor of caspase-3, has been designed, which still has the properties of a reversible inhibitor, while the P1 site at the C-terminal remains, and only L-amino acid has been replaced by D-amino acid. Also presented here is the synthesis of the inhibitor and its inhibitory activity against caspase-3, which was tested by the fluorescent activity assay.

关键词： Caspase-3 Inhibitor Retro-inverso Peptidomimetie Synthesis

Sensitive and Rapid Quantification of Felodipine by High-performance Liquid Chromatography-tandem Mass Spectrometry(HPLC-MS/MS) and Its Pharmacokinetics in Healthy Chinese Volunteers

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Chemical Research in Chinese Universities 2006年第4期22卷 479-483页

作者： LI Yan-yan YIN Yi-zi SUN Zhi-hui LI Xin HU Li-gang LI Peng-fei zhong da-fang The First Hospital Jilin University Changchun 130021 P.R. China Research Center for Drug Metabolism Jilin University Changchun 130021 P. R. China

To investigate the pharmacokinetics of felodipine in the plasma of healthy Chinese volunteers, 30 healthy volunteers received a single oral dose of 5 mg of extended release felodipine tablets. The felodipine was extracted from the matrix with a liquid-liquid extract procedure and analyzed by high-performance liquid chromatography-tandem mass spectrometry in the multiple reaction monitoring（MRM） mode using an electrospray ion source with positive ion detection. The method was validated over a felodipine concentration range of 0. 05-10.00 ng/mL in human plasma. Its main pharmacokinetic parameters values were： ρmax = （ 1.67 ± 0. 84 ） ng/mL, occurring at （ 3.93 3± 2. 49 ） h; the plasma elimination half-life：（23. 08 3± 9. 48） h and the area under the plasma concentration versus time curve：（29. 94 ± 14. 39） ng · h/mL. The validation results demonstrated that this method showed a satisfactory precision and accuracy across the calibration range. The procedure involved minimal drug administration, sample preparation, and a 2. 5-min chromatographic run time. It was well suited to clinical studies of the drug involving large numbers of samples.

关键词： Felodipine Liquid chromatography-tandem massspectrometry Pharmacokinetics

靶向抗肿瘤药物的ESI-MS/MS解析和代谢物鉴定

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质谱学报 2021年第5期42卷 804-818,I0007页

作者：田倩倩钟大放中国科学院上海药物研究所上海201203

靶向抗肿瘤药物是新药研发的热点,也是我国近年来批准上市的新药中数目最多的一类药物。电喷雾质谱(ESI-MS)在当前新药研发中发挥着重要作用,质谱碎裂信息是建立药动学生物样品分析方法的基础,也是鉴定药物代谢产物结构的主要依据。本... 详细信息

靶向抗肿瘤药物是新药研发的热点,也是我国近年来批准上市的新药中数目最多的一类药物。电喷雾质谱(ESI-MS)在当前新药研发中发挥着重要作用,质谱碎裂信息是建立药动学生物样品分析方法的基础,也是鉴定药物代谢产物结构的主要依据。本文总结了我国研发的靶向抗癌药物埃克替尼、阿帕替尼、吡咯替尼、氟马替尼、伏美替尼、法米替尼等及其主要代谢产物的电喷雾质谱碎裂途径,探讨质谱特征,并与其结构类似的药物进行比较。该综述对于如何选择合适的离子对进行定量分析,以及如何通过特征产物离子鉴定代谢产物具有参考意义。

关键词：靶向抗肿瘤药物电喷雾质谱裂解代谢产物鉴定

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抗体药物LC-MS法生物分析进展

药学学报 2020年第3期55卷 453-462页

作者：高宇雄钟大放中国科学院上海药物研究所上海201203

在抗体药物的生物分析中,液相色谱-质谱联用(LC-MS)技术已经成为传统配体结合分析(LBA)的一种重要的替代或补充方法。其方法开发中替代肽的选择、样品制备、灵敏度和定量准确性是值得关注的问题。本文对抗体药物LC-MS法生物分析的进展... 详细信息

在抗体药物的生物分析中,液相色谱-质谱联用(LC-MS)技术已经成为传统配体结合分析(LBA)的一种重要的替代或补充方法。其方法开发中替代肽的选择、样品制备、灵敏度和定量准确性是值得关注的问题。本文对抗体药物LC-MS法生物分析的进展进行综述,介绍LC-MS法分析抗体药物的原理,说明LC-MS法定量抗体过程中面临的挑战与当前可用于应对这些挑战的新策略,包括:替代肽的选择、样品纯化与富集、提高酶解效率、肽段富集与应用低速LC等方面。本文最后展示了LC-MS技术在抗体药物生物分析中的应用实例,并对抗体药物LC-MS法的发展提出了展望。

关键词：抗体药物 LC-MS 生物分析

抗新型冠状病毒肺炎(COVID-19)药物的代谢和药动学

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药学学报 2020年第11期55卷 2570-2579页

作者：潘露露钟大放中国科学院上海药物研究所上海201203

以我国新型冠状病毒肺炎诊疗方案(试行第七版)推荐的抗病毒治疗的药物为基础,本文对临床上用于治疗抗新型冠状病毒肺炎(COVID-19)的药物包括瑞德西韦、氯喹和羟氯喹、洛匹那韦/利托那韦、法匹拉韦进行了药物代谢和药动学性质的综述,同... 详细信息

以我国新型冠状病毒肺炎诊疗方案(试行第七版)推荐的抗病毒治疗的药物为基础,本文对临床上用于治疗抗新型冠状病毒肺炎(COVID-19)的药物包括瑞德西韦、氯喹和羟氯喹、洛匹那韦/利托那韦、法匹拉韦进行了药物代谢和药动学性质的综述,同时对作者实验室的研究成果包括阿比朵尔、黄芩苷和连花清瘟胶囊主要成分连翘苷的代谢和药动学进行了回顾,以期为治疗COVID-19药物的药效评价和合理用药提供参考。

关键词：新型冠状病毒肺炎药物代谢药动学