检索结果-南通市图书馆

Advance in Pre-Clinical pharmacokinetics of Paeoniflorin, a Major Monoterpene Glucoside from the Root of <i>Paeonia lactiflora</i>

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Pharmacology & Pharmacy 2013年第7期4卷 4-14页

作者： Orleans N. K. Martey Xiaoyan Shi Xin He School of Chinese Materia Medica Tianjin University of Traditional Chinese Medicine Tianjin China School of Chinese Materia Medica Tianjin University of Traditional Chinese Medicine Tianjin China Centre for Scientific Re-search into Plant Medicine Akwapim-Mampong Ghana School of Chinese Materia Medica Tianjin University of Traditional Chinese Medicine Tianjin China Tianjin State Key laboratory of Modern Chinese Medicine Tianjin China.

Paeoniflorin (PF) is one of the main bioactive components of total glucosides of paeony (TGP) extracted from the root of Paeonia lactiflora Pall. TGP exhibit various biological activities such as improvement in memory, hepatoprotection, antimutagenic properties and platelet aggregation inhibition. The aim of this paper is to review the pharmacokinetics (PK) of PF as a pure compound and in single or multiple herb(s) of traditional Chinese medicine (TCM) prescriptions. The distribution of PF or PF in TCM fitted one or two compartmental model after oral administration or intravenous injection, respectively. However, PF has a low bioavailability (BA) in rabbit (7.24%) and rat (3.24%) after oral administration. The PK profiles and BA of PF were remarkably improved when co-administered with sinomenine or glycyrrhizin acid. The PK profiles and BA of PF in Radix Paeonia Rubra (RP-R) and Jing-zhi guan-xin were improved, but in co-administration of RP-R with Radix Angelicae Sinensis, the BA was significantly reduced. PK profiles and BA of PF in Shan yao gan-cao tang or Danggui-Shaoyao-San was either remarkably improved or not. However, neither the PK profiles nor the BA of PF in Radix paeonia alba, Huangqin-tang Si ni san or Tang-Min-Ling-Wan was improved. Metabolism in the liver did not play any role in the low oral BA of PF. The low BA was thus attributed to poor permeation due to low lipophilicity, P-glycoprotein mediated efflux, intestinal bacteria and hydrolytic degradation in the intestine by the intestinal brush border lactase phlorizin hydrolase (LPH) and certain esterases. These findings show the in vivo course of PF and provide information on the maximum biological actions of PF that may help traditional Chinese herbal medicinal practitioners.

关键词： Bioavailability Intestinal Bacteria pharmacokinetics Paeoniflorin (PF) P-glycoprotein (P-gp)

Enhanced permeability and retention effect based nanomedicine, a solution for cancer

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

World Journal of Pharmacology 2015年第2期4卷 168-171页

作者： Jun Fang Research Institute of Drug Delivery Science Sojo University laboratory of Microbiology and Oncology Faculty of Pharmaceutical Science Sojo University

Tumor-targeting is becoming more and more important for cancer chemotherapy. Though many molecular-target drugs have been developed in the past two decades which shed some light on targeted tumor therapy,clinical results of those molecular-target drugs are not so encouraging especially for solid tumors, problems mostly relating to the heterogeneity and mutations of target molecules in human solid tumors. More general tumor-targeting strategy is thus anticipated. In this regard, the enhanced permeability and retention(EPR) effect which is a unique phenomenon of solid tumors based on the anatomical and pathophysiological nature of tumor blood vessels, is receiving more and more attentions. This EPR effect now served as a standard for tumor-targeted macromolecular anticancer therapy, namely nanomedicine. Many nanoplatforms have been developed as targeted drug delivery systems, including liposome, polymeric micelles, polymer conjugate, nanoparticles. Ample macromolecular drugs are now approved for clinical use or in clinical stage development, all of which by taking advantage of EPR effect, show superior in vivo pharmacokinetics and remarkable tumor selectivity, resulting in improved antitumor effects with less adverse effects. We thus believe EPR-based nanomedicine will be a solution for cancer in the future, whereas further consideration of factors involved in EPR effect and strategies to augment/improve EPR effect are warranted.

关键词：肿瘤靶向治疗化疗治疗方法

Research progress and quality markers prediction analysis of Dysosma versipellis

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Traditional Medicine Research 2023年第3期8卷 36-50页

作者： Yuan-Hui Guo Peng Lu Jia-Xing He Bao-Nan Ma Ebuka-Olisaemeka Nwafor Wen-Xin Wang Chuan-Xin Liu Endocrine and Metabolic Disease Center First Affiliated Hospitaland College of Clinical Medicine of Henan University of Science and TechnologyMedical Key Laboratory of Hereditary Rare Diseases of HenanLuoyang Sub-center of National Clinical Research Center for Metabolic DiseasesLuoyang 471000China Department of Pharmacy Suzhou TCM Hospital Affiliated to Nanjing University of Chinese MedicineSuzhou 215009China College of Traditional Chinese Medicine Beijing University of Traditional Chinese MedicineBeijing 100029China School of Health&Biomedical Sciences RMIT University–Bundoora CampusMelbourne 3083Australia School of Biological and Medical Engineering Beihang UnivesityBeijing 100083China

Dysosma versipellis is the rhizome of Bajiaolian in *** is a unique medicinal plant in China and it was the first to be recorded in Shennong’s Classic of Materia Medica(unknown author,25–220 C.E.).It has complex chemical components as well as complex,pharmacological and toxicological effects are *** on the recent research progress,the chemical constituents,pharmacological activities and toxicological effects of Dysosma versipellis were *** with the core concept of quality markers of traditional Chinese medicine,the prediction and analysis were carried out from the aspects of phytogenetics and the source pathway of specific chemical constituents,traditional medicinal properties,traditional efficacy,chemical composition measurability,blood components,and pharmacokinetics,in order to provide reference for further study of Dysosma versipellis.

关键词： Dysosma versipellis lignans flavonoids chemical composition pharmacological activity toxicological effect quality marker podophyllotoxin kaempferol quercetin

Harnessing pharmacological knowledge for personalized medicine and pharmacotyping: Challenges and lessons learned

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

World Journal of Pharmacology 2014年第4期3卷 110-119页

作者： Ioannis S Vizirianakis laboratory of Pharmacology Department of Pharmaceutical Sciences School of Health Sciences Aristotle University of Thessaloniki GR-54124 Thessaloniki Greece

The contribution of the genetic make-up to an individual's capacity has long been recognized in modern pharmacology as a crucial factor leading to therapy inefficiency and toxicity, negatively impacting the economic burden of healthcare and restricting the monitoring of diseases. In practical terms, and in order for drug prescription to be improved toward meeting the personalized medicine concept in drug delivery, the maximum clinical outcome for most, if not all, patients must be achieved, i.e., pharmacotyping. Such a direction although promising and of high expectation from the society, it is however hardly to be afforded for healthcare worldwide. To overcome any existed hurdles, this means that practical clinical utility of personalized medicine decisions have to be documented and validated in the clinical setting. The latter implies for drug delivery the efficient implementation of previously gained in vivo pharmacology experience with pharmacogenomics knowledge. As an approach to work faster and in a more productive way, the elaboration of advanced physiologically based pharmacokinetics models is discussed. And in better clarifying this topic, the example of tamoxifen is thoroughly presented. Overall, pharmacotyping represents a major challenge in modern therapeutics for which pharmacologists need to work in successfully fulfilling this task.

关键词：遗传组成现代药理学治疗方法临床分析

棉酚旋光异构体在牛体内代谢动力学研究:从日粮向血浆中转移及瘤胃微生物的降解作用(英文)

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Journal of Zhejiang University-Science B(Biomedicine & Biotechnology) 2018年第6期19卷 471-480页

作者： Chao-hua TANG Jia LIU Qing-yu ZHAO Jun-min ZHANG State Key laboratory of Animal Nutrition Institute of Animal Science Chinese Academy of Agricultural Sciences Scientific Observing and Experiment Station of Animal Genetic Resources and Nutrition in North China Ministry of Agriculture and Rural Affairs College of Pastoral Agriculture Science and Technology Lanzhou University

目的:比较研究棉酚旋光异构体从日粮向血浆中转移以及瘤胃微生物的降解作用。创新点:从饲粮向血浆中吸收代谢以及瘤胃微生物降解角度揭示了棉酚旋光异构体在牛体内代谢差异,为棉酚毒理学评价、棉籽类产品在畜牧生产中合理应用提供科学... 详细信息

目的:比较研究棉酚旋光异构体从日粮向血浆中转移以及瘤胃微生物的降解作用。创新点:从饲粮向血浆中吸收代谢以及瘤胃微生物降解角度揭示了棉酚旋光异构体在牛体内代谢差异,为棉酚毒理学评价、棉籽类产品在畜牧生产中合理应用提供科学依据。方法:利用高效液相色谱法(HPLC)测定全棉籽、血浆及瘤胃发酵液中棉酚旋光异构体含量。结论:三个调研牛场奶牛日粮右旋、左旋棉酚摄入量分别在5.6~8.5和3.8~5.9g/(d·herd)之间。血浆棉酚含量与日粮棉酚摄入量呈正相关,右旋、左旋棉酚浓度分别在0.31~0.48和0.39~0.59μg/ml之间。奶牛摄入棉酚中右旋棉酚比率(58.8%~59.8%)高于左旋棉酚,血浆中左旋棉酚比率(54.6%~55.9%)高于右旋棉酚。体外静态培养试验发现:500和1000μg/g组左旋棉酚的降解率在6小时后分别为67.4%和85.7%,12小时后降解率分别升高到83.6%和92.5%;同时,棉酚旋光异构体之间降解规律相似。结果表明:相比于右旋棉酚,左旋棉酚在奶牛体内吸收率更高,瘤胃微生物对棉酚旋光异构体的降解没有选择性。

关键词：棉酚旋光异构体代谢动力学牛

Therapeutic Evaluation of Monoclonal Antibody-Maytansinoid Conjugate as a Model of RON-Targeted Drug Delivery for Pancreatic Cancer Treatment

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Therapeutic Evaluation of Monoclonal Antibody-Maytansinoid C...

Regulatory effects of the combination of berberine and ginsenoside Rb1 on high-fat diet-induced nonalcoholic fatty liver disease via AMPK pathway and improved pharmacokinetics

浙江省免疫学会第十次学术大会

作者： Hang-Ping Yao Liang Feng Jianwei Zhou Ruiwen Zhang Ming-Hai Wang State Key laboratory for Diagnosis & Treatment of Infectious Diseases Collaborative Innovation Center for Diagnosis and Treatment of Infectious Diseases First Affiliated Hospital of Zhejiang University School of Medicine Cancer Biology and Therapeutics Research Center Department of Biomedical Sciences Texas Tech University Health Sciences Center School of Pharmacy Department of Molecular Cell Biology & Toxicology Nanjing Medical University School of Public Health Department of Pharmaceutical Sciences Texas Tech University Health Sciences Center School of Pharmacy

Aberrant expression of the RON receptor tyrosine kinase,a member of the MET proto-oncogene family,contributes significantly to pancreatic cancer tumorigenesis and *** we validate RON as a target for pancreatic cancer therapy using a novel anti-RON antibody Zt/g4-drug maytansinoid conjugates(Zt/g4-DMl) as a model for RON-targeted drug delivery to kill pancreatic cancer *** pancreatic cancer cell lines overexpressing RON,Zt/g4-DM1 rapidly induced receptor endocytosis,arrested cell cycle at G2/M phase,reduced cell viability,and subsequently caused massive cell *** in vitro observations help to establish a correlation between the number of the cell surface RON receptors and the efficacy of Zt/g4-DM1 in reduction of cell *** mice,Zt/g4-DM1 pharmacokinetics in the linear dose range fitted into a two-compartment model with clearance in 0.21 ml/day/kg and terminal half-life at 6.05 *** results helped to confirm a concentration-activity relationship for the BxPC-3 and other pancreatic cancer cell xenograft model with a tumoristatic dose at 3.02 mg/***/g4-DM1 was effective in vivo against various xenograft PDAC growth but efficacy varied with individual cell *** of Zt/g4-DM1 with gemcitabine had a complete inhibition of xenograft pancreatic cancer *** conclude from these studies that increased RON expression in pancreatic cancer cells is a suitable targeting moiety for anti-RON ADC-directed drug delivery and anticancer ***/g4-DM1 is highly effective alone or in combination with chemotherapeutics in inhibition of pancreatic cancer xenograft growth in preclinical *** findings justify the use of humanized Zt/g4-DM1 for targeted pancreatic cancer therapy in the future.

关键词： receptor tyrosine kinase antibody-drug conjugate pancreatic cancer pharmacokinetics xenograft tumor model therapeutic efficacy combination therapy

来源： cnki会议评论

在线全文

cnki会议

学校读者我要写书评

暂无评论

TMR Integrative Medicine 2018年第2期2卷 76-86页

作者： Lv Zhou Xiu-Teng Zhou Wen-Bo Xu Yi-Dan Chen Ni-Hua Wang Jiao Guo Hui Fan Guangdong Research Center of Metabolic Diseases of Integrated Western and Chinese Medicine Guangdong Pharmaceutical University Guangzhou 510006 China Joint laboratory between Guangdong and Hong Kong on Metabolic Disease Guangdong Pharmaceutical University Guangzhou 510006 China National Resource Center for Chinese Materia Medica China Academy of Chinese Medical Sciences State Key Laboratory Breeding Base of Daodi Herbs Beijng 100700 China

目的：评价小檗碱（BBR）联合人参皂苷Rb1（G-Rb1）对高脂饮食（HFD）诱导的大鼠非酒精性脂肪肝病（NAFLD）的保护作用并阐明其作用机制.方法：大鼠给予高脂饮食6周,然后分别给予BBR（50mg/kg）,G-Rb1（100mg/kg）,BBR（50mg/kg）＋G-Rb... 详细信息

目的：评价小檗碱（BBR）联合人参皂苷Rb1（G-Rb1）对高脂饮食（HFD）诱导的大鼠非酒精性脂肪肝病（NAFLD）的保护作用并阐明其作用机制.方法：大鼠给予高脂饮食6周,然后分别给予BBR（50mg/kg）,G-Rb1（100mg/kg）,BBR（50mg/kg）＋G-Rb1（100mg/kg）和非诺贝特（40mg/kg）治疗.通过组织学检查染色评估肝组织.在人肝癌细胞HepG2细胞系中,通过蛋白质印迹检测AMP-活化蛋白激酶（AMPK）和乙酰辅酶A羧化酶（ACC）蛋白的表达,定量PCR检测肉毒碱棕榈酰转移酶1和3-羟基-3-甲基戊二酰辅酶A还原酶mRNA的水平.药代动力学评估包括体内BBR和G-Rb1的生物利用度,以及体外肠道细菌的G-Rb1代谢.结果：根据肝脏甘油三酯含量分析和肝脏切片组织学评价,与单用组相比,BBR联合G-Rb1可显著改善HFD诱导的肥胖大鼠的肝脏脂肪堆积.在用BBR和G-Rb1处理的肝癌细胞HepG2中,肝脏AMPK的活化和ACC的磷酸化显着升高.与AMPK的活化一致,肉毒碱棕榈酰转移酶1的mRNA表达被刺激,而3-羟基-3-甲基戊二酰辅酶A还原酶的转录被抑制.药代动力学分析显示BBR增加了SD大鼠G-Rb1的生物利用度.此外,BBR在体外防止粪便溶液中G-Rb1的降解.结论：BBR联合G-Rb1通过作用于AMPK信号通路改善NAFLD,BBR可通过促进G-Rb1在肠道吸收来增强G-Rb1生物利用度,小檗碱联用人参皂苷Rb1可能是治疗NAFLD的有效药物.

关键词：非酒精性脂肪肝 AMP活化蛋白激酶小檗碱人参皂苷Rb1 药代动力学肠道细菌

Phase 1 studies comparing safety, tolerability, pharmacokinetics and pharmacodynamics of HLX01(a rituximab biosimilar) to reference rituximab in Chinese patients with CD20-positive B-cell lymphoma

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Chinese Journal of Cancer Research 2021年第3期33卷 405-416页

作者： Yuankai Shi Qingyuan Zhang Xiaohong Han Yan Qin Xiaoyan Ke Hang Su Li Liu Jinxiang Fu Jie Jin Jifeng Feng Xiaonan Hong Xiaohong Zhang Depei Wu Bin Jiang Xiaodong Dong National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital Chinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing Key Laboratory of Clinical Study on Anticancer Molecular Targeted DrugsBeijing 100021China Harbin Medical University Cancer Hospital Harbin 150081China Peking University Third Hospital Beijing 100191China The 307th Hospital of Military Chinese People's Liberation Army Beijing 100071China Tangdu Hospital of the Fourth Military Medical University Xi'an 710038China The Second Affiliated Hospital of Soochow University Suzhou 215004China The First Affiliated Hospital Zhejiang University College of Medicine Hangzhou 310006China Jiangsu Cancer Hospital Nanjing 210009China Fudan University Shanghai Cancer Center Shanghai 200032China The Second Affiliated Hospital Zhejiang University School of Medicine Hangzhou 310003China The First Affiliated Hospital of Soochow University Suzhou 215006China Peking University People's Hospital Beijing 100034China Shanghai Henlius Biotech Inc.Shanghai 200233China

Objective: This study aimed to compare the pharmacokinetic, pharmacodynamic and safety profiles of HLX01(a rituximab biosimilar) and reference rituximab sourced from China(Mab Thera?;rituximab-CN).Methods: Here we report the results of two phase 1 studies. In the phase 1 a, open-label, dose-escalation study(NCT03218072, CTR20140400), eligible patients received 250, 375 and 500 mg/m^(2) HLX01 sequentially at 7-day intervals, after confirming no dose-limiting toxicity(DLT). In the phase 1 b, double-blind study(NCT02584920,CTR20140764), eligible patients were given a single dose of 375 mg/m^(2) HLX01 or rituximab-CN. The primary endpoints included safety and tolerability parameters for the phase 1 a and the area under the plasma concentrationtime curve from time zero to day 91(AUC0-91 d) for the phase 1 b study. Equivalence was concluded if 90%confidence interval(90% CI) for the geometric least squares mean ratio(GLSMR) fell in the pre-specified equivalence criteria(80%-125%).Results: Between June 20, 2014 and January 5, 2015, 12 patients were enrolled in the phase 1 a study. The pharmacokinetics of HLX01 showed dose proportionality and accumulation to steady state. HLX01 was well tolerated, with no serious adverse events(AEs), discontinuations or DLTs. Between November 8, 2014 and August13, 2015, 87 eligible patients were enrolled in the phase 1 b study, including 43 who received HLX01 and 44 who were treated with rituximab-CN. The equivalence endpoint was met with GLSMR for AUC0-91 d being 89.6%(90% CI: 80.4%-99.8%). AEs, anti-drug antibodies, and CD19+ and CD20+ B lymphocyte counts were similar between the HLX01 and rituximab-CN treatment ***: Treatment with HLX01 was safe and well tolerated in Chinese patients with B-cell ***01 and rituximab-CN have similar pharmacokinetic, pharmacodynamic and safety profiles.

关键词： Biosimilar lymphoma monoclonal antibody pharmacokinetics safety

Safety, Tolerability, pharmacokinetics and Pharmacodynamics of E3024, a Novel and Selective Dipeptidyl Peptidase-IV Inhibitor, in Healthy Japanese Male Subjects: Rash Development in Men and Its Possible Mechanism

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Pharmacology & Pharmacy 2013年第9期4卷 663-678页

作者： Yutaka Takeuchi Masayuki Namiki Yasumi Kitahara Setsuo Hasegawa Akihiro Ohnishi Nobuyuki Yasuda Takashi Inoue Richard Clark Kazuto Yamazaki Clinical Development Japan/Asia Clinical Research PCU Eisai Co. Ltd. Tokyo Japan Clinical Development Japan/Asia Clinical Research PCU Eisai Co. Ltd. Tokyo Japan Clinical Pharmacology Clinical Science SOCS CFU Eisai Co. Ltd. Tokyo Japan Department of laboratory Medicine Daisan Hospital Jikei University School of Medicine Tokyo Japan Sekino Clinical Pharmacology Clinic Tokyo Japan Present Address: Pharmaspur Inc. Tokyo Japan Tsukuba Research Laboratories Eisai Co. Ltd. Tsukuba Japan.

E3024 (3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate) is a dipeptidyl peptidase-IV (DPP-IV) inhibitor that was expected to be an antidiabetic agent. Its safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) were investigated in a randomized, double-blind, placebo-controlled, ascending single-dose study in 48 healthy Japanese male subjects. Fasted subjects were orally administered E3024 (5, 10, 20, 40, or 80 mg) or placebo. E3024 was rapidly absorbed, with tmax values ranging between 0.33 and 3 h after dosing. The mean t1/2 ranged from 5.34 to 11.68 h. AUC0-inf and Cmax increased dose-proportionately. PK-PD relationship of E3024 was evaluated by using an Imax model, indicating that plasma E3024 concentrations and inhibitory effects of plasma DPP-IV activity were well correlated. The IC50 value was calculated as 33.7 ng/mL, which was consistent with in vitro data. Thus, E3024 showed a good PK profile and inhibited DPP-IV dose-dependently. Of 30 subjects administered E3024, 12 (40%) experienced adverse events (AEs). Dose escalation to 160 mg was abandoned owing to undesired subjective/objective findings in 4 of 6 subjects receiving 40 mg and 5 of 6 subjects receiving 80 mg. The most prominent AE was rash, but there were no serious AEs or deaths. The maximum tolerated dose was considered to be 20 mg. We hypothesized that histamine was a cause of the rash induction, and examined blood histamine levels of normal Fischer rats treated with E3024. Blood histamine levels were increased significantly by E3024 at 500 mg/kg (p < 0.001), but not by vildagliptin or valine-pyrrolidide (DPP-IV inhibitors) at the same dose. No blood histamine increases were observed in genetically mast cell-deficient Ws/Ws rats treated with E3024 at 500 mg/kg. In in vitro assays, E3024 induced histamine release from normal rat peritoneal mast cells in a concentration-dependent manner, but not from basophils. The structure-activity relati

关键词： Dipeptidyl Peptidase-IV Inhibitor Rash Histamine Structure-Activity Relationship