中国科技论文统计源期刊 中文核心期刊  
美国《化学文摘》《国际药学文摘》
《乌利希期刊指南》
WHO《西太平洋地区医学索引》来源期刊  
日本科学技术振兴机构数据库(JST)
第七届湖北十大名刊提名奖  

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    药物研究
  • 药物研究
    Ruidong XIA,Jialin SUN,Ruijuan YIN,Zhongguo SUI
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    Objective To study the effect of a new isothiourea modified curcumin pyrimidine derivative 1g on autophagy, invasion and migration ability of human colon cancer cells and its possible molecular mechanism. Methods CCK-8 method was used to detect the cell proliferation of HCT116 and HT29 cells at different concentrations of 1g. Transmission electron microscopy was used to observe the effect of 1g on the autophagy of HCT116 and HT29 cells. Transwell chamber was used to detectthe migration and invasion of HCT116 and HT29 cells;Western blotting was used to detect protein expression of CD147,p-PI3K/PI3K,p-AKT/AKT,LC3II/LC3Iincolon cancer cells. Results Compound 1g inhibited the proliferation of HCT116 and HT29 cells in a dose-dependent manner. It can induce colon cancer cell autophagy and LC3II/LC3I protein expression, inhibit colon cancer cell migration and invasion, and reduce the expression of CD147, p-PI3K/PI3K, and p-AKT/AKT proteins. Conclusion Isothiourea-modified curcumin-pyrimidine derivatives 1g may induce autophagy, and inhibit migration, invasion and proliferation of HCT116 and HT29 cells through CD147 and PI3K/AKT pathways.

  • 药物研究
    Wentao HUANG,Geng ZHANG,Song HU,Quanwei YANG
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    Objective To study the release of geniposide, paeoniflorins and hesperidin in anti-cancer cataplasm and determine the transdermal rate of isolated mice in vitro. Methods The modified France diffusion cell was used to simulate the human skin barrier with isolated mouse skin in vitro.The effective components were determined by the HPLC method. Results The cumulative releaserates of geniposide in the cataplasm at 10, 30, 60, 90 and 120 min were 12.75%, 39.27%, 48.76%, 67.84%, and 83.81%, respectively. The cumulative releaserates of paeoniflorin were 14.36%, 37.55%, 52.10%, 66.88%, and 84.17% respectively,and those of hesperidin were 10.27%, 36.74%, 49.10%, 58.22%, and 79.38%, respectively. The transdermal rates of geniposide, paeoniflorin, and hesperidin through the skin of isolated mice for 24 hours in the detoxification anti-cancer cataplasm were 26.55%, 23.64%, and 29.16%, respectively. Conclusion In vitro percutaneous osmotic behavior of detoxifying anti-cancer cataplasm in mice was optimized by Higuchi equation fitting, and the degree of fitting was the highest, indicating that the cataplasm was a skeleton controlled-release preparation.

  • 药物研究
    Huidong TIAN,Jing WANG,Lina GUO,Minglu JIA,Xueping CHEN,WANGRui
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    Objective To explore the mechanism of Rhizoma coptidis-Panax notoginsengagainst type 2 diabetes mellitus using network pharmacology. Methods The main active components and related targets of Rhizoma coptidis-Panax notoginseng were obtained by searching TCMSP database, and Cytoscape software (version 3.6.1) was used to build a network diagram between active components and targets. Secondly, “type 2 diabetes mellitus”targets was searched from CTD and TTD databases, and targets retrieved were used to build a PPI network based on the analysis from STRING database. To obtain type 2 diabetes mellitus targets of the active components, the PPI network was merged with the component-target network. Finally, the DAVID database was used to perform GO function and KEGG pathway enrichment analysis in order to explore the mechanism. Results Seventeen components with drug-likeness and good oral absorption were obtained, and 19 target proteins were selected including intestinal maltase glucoamylase (MGAM), dipeptidyl peptidase IV (DPP4), insulin receptor (INSR), peroxisome proliferator activated receptor gamma (PPARG), etc. According to the GO functional enrichment analysis,111 GO items were obtained (P<0.05),including 92 biological processes (BP) items,12 cell composition (CC),and 7 related items of molecular function (MF).There were 21 signal pathways (P<0.05) found in the KEGG pathway enrichment screening, involving HIF-1 signaling pathway, insulin resistance, regulation of lipolysis in adipocytes, and PI3K-Akt signaling pathway, etc. Conclusion Rhizoma coptidis-Panax notoginseng and its active components play therapeutic effect against type 2 diabetes mellitus through various targets and multiple pathways. This study laid a new foundation for the further study on the mechanism of Rhizoma coptidis-Panax notoginseng composition.
  • 药物研究
    Ling YUE,Yong WANG,Huiling SUN,Lizi YE,Ziyi ZHU,Jing LI,Zhiyang WANG
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    Objective To investigate the effect and mechanisms of Jinlida on the apoptosis of corpora cavernosum smooth muscle cells (CCSMCs) in high glucose-induced SD rats. Methods The primary CCSMCs of SD rats were cultured. The experiment was divided into four groups:the normal glucose group (NG), the high glucose group (HG), the high glucose +PD98059 group and the high glucose + Jinlida intervention group with different concentrations (50, 150, 300 mg·L-1). Cells were collected from each group after the culture for 48 h. Apoptosis rate was detected by flow cytometry, and the expression levels of ERK1/2, p-ERK1/2, caspase-3, and bcl-2 were determined by Western blotting. Results Compared with the normal glucose group, the expression levels of p-ERK1/2 and activated caspase-3 protein in the high glucose group were significantly increased (P<0.01);the expression of bcl-2 protein was significantly decreased (P<0.01), and the apoptosis rate of CCSMCs was significantly increased (P<0.01). Compared with the high glucose group, the expression of p-ERK1/2 and caspase-3 decreased after the high glucose + PD98059 and high glucose + Jinlida intervention(P<0.05);and the bcl-2 protein expression was up-regulated, and CCSMCs apoptosis was significantly decreased (P<0.05). Conclusion High glucose can induce apoptosis of CCSMCs in rats;Jinlida may ameliorate high glucose-induced apoptosis of CCSMCs by inhibiting ERK1/2 signaling pathway.

  • 药物研究
    Lei TANG,Chao AI
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    Objective To study the metabolism of vinpocetine in rats by LC-MS/MS, and its possible metabolic pathways, which provide references for the study of vinpocetine metabolism in vivo. Methods Vinpocetine were intragastricly administrated in Sprague-Dawley rats, and urine samples were collected. Metabolites in the urine sample were identified or confirmed through MS Scan, SIR, and daughter scan. Results Four metabolites were found in the urine including apovincaminic acid,hydroxyvinpocetine, dihydroxyvinpocetine, and vinpocetine hydrate. Conclusion By analyzing the results of vinpocetine metabolites in the urine of rats, the structure of one metabolite is identified, and the structures of the other three metabolites (M2, M3, M4) are inferred. This research provides information and reference for the further study on the metabolism of vinpocetine in vivo.

  • 药物研究
    Xiaodong LIU,Wenjing WEN,Zhijun ZHAO
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    Objective To investigate the protective effect and mechanism of total flavonoids from Lithocarpus polystachyus Rehd.(TFL) on CCl4-induced acute liver injury in mice. Methods Mice were randomly divided into 6 groups: normal control group, model control group (6% CCl4 olive oil solution), silymarin group (silymarin, 120 mg·kg-1), TFL low, medium and high dose group (50,100,150 mg·kg-1). The normal control group and the model control group were given equal volume of 0.9% of sodium chloride soution by gavage,while the other groups were administered with the corresponding dose of drugs according to the body mass. After 7 days, the acute liver injury model was established with 6% carbon tetrachloride olive oil solution (5 mL·kg-1). All of the mice were sacrificed to collect serum and liver tissues after 6 h. ALT and AST activities in serum were detected, and IL-1β, IL-6, TNF-α, SOD, GSH-Px, MDA levels in liver tissue were analyzed.Hematoxylin-eosin (HE) staining was used to observe the variation of liver histopathology.NLRP3, ASC, and Caspase-1 levelsin liver tissue were detected by Western blotting. Results Compared with the model control group, TFL decreased liver mass and liver index (P<0.05), down-regulated ALT and AST activities (P<0.05),decreased IL-1β, IL-6 and TNF-α levels in liver tissue (P<0.05), increased SOD and GSH levels, decreased MDA levels in liver tissue (P<0.05), and down-regulated NLRP3, ASC, and Caspase-1 protein levels in liver tissue (P<0.05). Microscopic observation showed that liver tissue injury was improved in different degrees. Conclusion The protective effect of TFL on CCl4-induced acuteliver injury was associated with attenuatedoxidative stress levels, reduced inflammatory factor levels, and regulated ROS/NLRP3/IL-1β signaling pathways.

  • 药物研究
    Feng LIANG,Biao YAN
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    Objective To investigate the potential protective effect and mechanism of curcumin (Cur) on KM mice induced by dibutyl phthalate (DBP). Methods Twenty-eight KM mice were randomly divided into 4 groups: normal control group, 50 mg·kg-1 DBP exposure group (DBP group), 2.5 mg·kg-1 Cur group, and 50 mg·kg-1 DBP + 2.5 mg·kg-1 Cur group (n=7). At the end of 4 weeks, the renal function indexes Urea and Crea levels of mice in each group were measured by automatic biochemical analyzer. Free radical (ROS) levels were analyzed by dichlorofluorescein diacetic acid (DCFH-DA) fluorescence, and the malondialdehyde (MDA)contents were detected by thiobarbituric acid (TBARS). The total antioxidant capacity (T-AOC) and cysteine protease-3 (Casp-3) levels were measured by Kits in renal homogenate. Additionly, Western blotting was used to detect the expressions of extracellular regulated protein kinases (ERKs) and its phosphorylated (p-ERKs) protein in renal tissue, and the expressions of Bcl-2 and Bax protein were detected by immunohistochemistry. Results Compared with the normal control group, the levels of Urea, Crea, ROS, MDA, and Casp-3 were significantly increased, and the levels of T-AOC were significantly decreased, and the expression levels of p-ERK and Bax were significantly up-regulated in DBP group. Compared with the DBP group, the levels of Urea, ROS, and Casp 3 decreased significantly, and the level of T-AOC and the ratio of Bcl-2 to Bax increased significantly. Conclusion Curcumin has protective effects on renal injury induced by DBP in KM mice.

  • 药物研究
    Tao CHEN,Jinglou CHEN,Wentao HUANG
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    Objective To investigate the potential protective effects of (-)-Epicatechin gallate (ECG) on benign prostatic hyperplasia (BPH) in male rats and its underlying mechanisms. Methods Rats were randomly divided into 4 groups (6 rats in each group):normal control group,model control group,ECG high dose group and ECG low dose group.BPH rat model was established by castration and daily subcutaneous injection of 10 mg·kg-1 testosterone propionate for 4 weeks.ECG groups were intragastricly administrated daily with 300 or 100 mg·kg-1 ECG for 4 weeks.Prostate tissues were separated after the experiment period.Prostatic collagen deposition and proliferation were evaluated by Masson and PCNA staining.The expression and mRNA levels of androgen receptor (AR) and estrogen receptor (ER) -α/β were detected by immunohistochemistry and real-time quantitative PCR.The prostatic levels of pro-inflammatory cytokines and growth factors were detected by ELISA. Results Compared to the normal control group,model control group showed obvious collagen deposition and proliferation.The prostate index increased from(2.13±0.18) mg·g-1 to (4.76±0.18) mg·g-1.The expression and mRNA levels of AR and ER-α were significantly increased (P<0.01),and the expression and mRNA level of ER-β were significantly decreased in model control group (P<0.01).Additionally,the prostatic levels of pro-inflammatory cytokines and growth factors were significantly enhanced (P<0.01).When compared to the model control group,both high dose and low dose ECG attenuated collagen deposition,significantly (P<0.01) inhibited prostate proliferation,reduced the prostate index to (3.27±0.20) mg·g-1 and (3.65±0.22) mg·g-1, reduced the mRNA levels of Col-1A1,Col-3A1,AR and ER-α,as well as significantly increased mRNA level of ER-β (P<0.05).Additionally,the high dose (P<0.01) and low dose (P<0.05) ECG significantly decreased the prostatic levels of pro-inflammatory cytokines.The high dose and low dose ECG also significantly decreased the prostatic levels of growth factors (P<0.05). Conclusion ECG can protect against BPH via regulating the expression of AR and ER-α/β,as well as the levels of pro-inflammatory cytokines and growth factors.

  • 药物研究
    Chong LIU,Ningwei ZHU,Xiaomei JIANG
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    Objective The purpose of this study was to observe the effects and explore the underlining mechanisms of astaxanthin on the ability of learning and memory of vascular dementia mice. Methods Vascular dementia (VD) model was established by the permanent ligation of the rightcommon carotid artery. The mice were randomly divided into model control group, astaxanthin (50, 100 and 200 mg ·kg-1) group. After the intervention,the ability of learning and memory was explored by Morris water maze test. Forced swimming test was used to detect the depression degree.Using the Nissl staining, the morphological changes of hippocampal neurons were observed.The contents of SOD and MDA were tested by microplate reader in the hippocampus;DHE staining method was used to observe ROS fluorescence intensity in the hippocampus of mice. Results The permanent ligation of right common carotid artery model could cause the average escape latency time and the immobility time longer than sham operation group.And hippocampal neurons hierarchy was unclear and the arrangements were disordered (P<0.05).Moreover, the cell structure was destroyed seriously, and the space around the cells was enlarged, showing vacuole like changes. Astaxanthin (50, 100 and 200 mg·kg-1) reduced the average escape latency time and the immobility time, and improved the hippocampus neuron structure. The astaxanthin 200 mg·kg-1 group showed the best improvement among the three groups. Compared with model control group, the SOD activity significantly reduced, and MDA content and ROS fluorescence intensity increased in the hippocampus of model control group. Astaxanthin (50, 100 and 200 mg·kg-1) group increased SOD activity, decreased the MDA content and the ROS fluorescence intensity in the hippocampus, and the astaxanthin 200 mg·kg-1 group also had the best effects which was similar to those of sham operation group. Conclusion Astaxanthin could improve the ability of learning and memory of vascular dementia mice by the antioxidant effect, and play a role in protecting neurons in a dose-dependent relationship.

  • 防控新型冠状病毒肺炎专栏
  • 防控新型冠状病毒肺炎专栏
    Jun CAI,Weihong GE
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    Objective To explore the characteristics of dexamethasone in coronavirus treatment, and to provide a reference for the rational use of dexamethasone in coronavirus disease 2019 (COVID-19). Methods Literatures of dexamethasone in the treatment of coronavirus which was published until June 18, 2020 were retrieved from CNKI, Wanfang database and Pubmed, and analyzed by descriptive evaluation method. Results Five articles were included. Dexamethasone could reduce the mortality rate of by one third inpatients with severe COVID-19 using ventilator, and the mortality rate of the patients receiving only oxygen therapy decreased by 1/5. Dexamethasone could reduce the early stage of pulmonary lesions of porcine respiratory coronavirus (PRCV) infection, but aggravate the symptoms in the middle and late stage of infection. The level of IL-6 decreased first and then increased, while IFN-α, IFN-γ, IL-4, IFN-γ CSC, CD3+, CD4+, CD8+ decreased in the middle and late stages of infection. Dexamethasone significantly reduced the levels of IL-6, IL-10, and TGF-β1 in rats infected with SARS coronavirus N protein. Dexamethasone could not inhibit the production of RANTES in SARS-CoV-infected THP-1 cells. Conclusion Dexamethasone could reduce the mortality rate of patients with COVID-19. The timing of the initial therapy of dexamethasone, the duration of therapy and precautions for the use should be clear.

  • 防控新型冠状病毒肺炎专栏
    Dongyan LI,Jinwen ZHANG
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    Objective To investigate the characteristics of adverse drug reactions(ADR) in patients with COVID-19 in Tongji hospital,Tongji medical college,Huazhong university of Science and Technology (Tongji hospital) and provide references for rational drug use in clinic. Methods Using the method of retrospective analysis,the ADR report of 68 cases with COVID-19 reported by Tongji hospital from February 2020 to May 2020 were analyzed in terms of sex,age,proportions of new/ serious cases,involved drugs,organs/system injury,clinical manifestations,correlation evaluation and outcomes. Results The constituent ratio of ADR was higher in female than in male.Cases of ADR were mainly in the group of 61-80 years old,of which 35 cases (51.47%) were new and serious.The top three drug types causing ADR were antiviral drug with 32 cases (47.06%),immunosuppressants and anti-infective drugs with 4 cases (5.88%),respectively.Organs and system related ADR occured in a total of 80 cases.The most common organ/system injury involved was digestive system with 37 cases (46.25%),followed by skin injury with 17 cases (21.25%). Conclusion Off-label drug uses contributed to the adverse reactions caused by drugs used in the treatment of COVID-19,and the elderly patients with COVID-19 were more susceptible to ADR.Monitoring should be strengthened in off-label drug use and drug use in the elder to reduce the risk of drug use and ensure the safety.

  • 防控新型冠状病毒肺炎专栏
    Shengnan LIU,Zhaoshuai JI,Xuan LIU,Jizhang YANG,Qiantai MAO,Cao AI
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    Objective To analyze the current situation of off-label and compassionate drug uses during the epidemic period of coronavirus disease 2019 (COVID-19), so as to provide references for improving the relevant systems of our country. Methods The off-label use and compassionate use of drugs for the COVID-19 treatment were combed and analyzed by consulting instructions, guidelines, literature research and other methods. Results The therapeutic drugs recommended by the latest guidelines for the diagnosis and treatment of COVID-19 are all off label drugs, which may cause certain risks in clinical use.And the use of "compassionate drugs" can improve the symptoms in some critical ill patients.However, it is a case study, and the effectiveness of drugs still needs to be verified by large-scale rigorous clinical trials. Conclusion The off-label use and compassionate use are feasible ways to explore more functions of drugs in clinic, and have positive significance for treating patients, carrying out clinical trials and expanding new indications of drugs. However, it is necessary to continuously construct and improve the supervision system of drug use.

  • 防控新型冠状病毒肺炎专栏
    Jing XIA,Bi SHENG,Li WU,Yonggang CHEN,Jinhu WU
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    Objective To analyze the relationship of drugs for treating coronavirus disease 2019 (COVID-19) patients with the drug-induced liver injury. Methods The hospital information management system (HIS) was used to collect COVID-19 cases diagnosed in the third hospital of Wuhan city.The patients with abnormal liver function during hospitalization were screened, and the general situation, clinical characteristics and medication status of the patients were collected. Results A total of 78 patients with drug-induced liver injury were collected during the hospitalization(1326 cases,5.88%).Moxifloxacin, cefoperazone sulbactam, abidor, and ganciclovir were used in high rates. The most common two-drug combination was moxifloxacin + cefoperazone sulbactam, and the most common three-drug combination was cefoperazone sulbactam + ganciclovir + moxifloxacin. Long hospital stay and drug combinations were the risk factors for drug-induced liver injury. Conclusion The clinical drug varieties for patients with COVID-19 in this hospital were relatively focused. The safety and rationality of the combination of two or more drugs especially broad-spectrum antibiotics, which may cause liver injury, should be concerned.

  • 生物医药发展与临床应用
  • 生物医药发展与临床应用
    Wenqing FANG,Xinglu XU,Huizhen DAI,Xin LI
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    Objective To evaluate the effect of the implementation of national medical insurance admittance negotiation policy on the utilization of innovative anticancer drugs and the medical insurance payment in Nanjing city. Methods Based on the purchase data by medical insurance in Nanjing city from 2016 to 2019.To compared and analyzed the drug utilization and expenditure of medical insurance fund by calculating the frequency of drug utilization,consumption amount,defined daily dose consumption,ranking ratio and amount of medical insurance payment. Results After being included in the medical insurance,the innovative anticancer drug DDDs and the consumption amount increased significantly,the overall B/A increased,and the synchronization of drugs were becoming better.However,the consumption amount was separated from DDDs for some drugs.Innovative anticancer drugs in the medical insurance account for a higher proportion of the total amount of anticancer drugs paid,but their proportion in the total drugs amount of medical insurance payment was low. Conclusion National medical negotiation and medical reimbursement effectively promote the utilization and availability of innovative anticancer drugs and it didn’t have a great impact on the medical insurance fund.

  • 生物医药发展与临床应用
    Hui SU,Cheng LI
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    Rheumatoid arthritis (RA) is a multi-joint chronic autoimmune disease. It is characterized by severe cartilage destruction and a large amount of inflammatory infiltration, which induce systemic complications and disability and eventually reduce the quality of life. Currently, the drugs used for the treatment of RA have several disadvantages, such as large dosage, frequent administration and serious side effects. These limitations have greatly promoted the research and application of targeted drugs in RA therapy. In this article, we review the recent progress of targeted drugs in the treatment of RA and discuss the application of various targeting strategies. Finally,the challenges needed to be solved and outlook for the futurewas discussed.

  • 生物医药发展与临床应用
    Shengzhao ZHANG,Na SU,Ting XU,Ling WANG,Zhou QIN
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  • 生物医药发展与临床应用
    Kefu YU,Jiadan YE,Yue TIAN,Bei XU,Yong CUI,Zhigang ZHAO
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  • 生物医药发展与临床应用
    Hao WANG,Chenxin ZENG,Li LI,Weihong GE
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    Objective To evaluate the cost-effectiveness of osimertinib and gefitinib/erlotinib in the first-line treatment of EGFR-mutation positive non-small-cell lungcancer (NSCLC) from the perspective of health care payers in China. Methods Based on a high-quality, multi-center Phase III randomized clinical trial (FLAURA), the three-state Markov model was established according to the progression of the disease. In this model, each state transition probability and adverse reaction rate were collected and calculated based on theclinical trial data;the effectiveness values were calculated from those of the Chinese population in the literature references;the direct medical costs were calculated based on the fees charged locally or related literature.The total population and the subgroup of patients with brain metastasis were assessed for cost effectiveness over a 10-year period, and the stability of the results from the model was analyzed for both deterministic and probabilistic sensitivity. Results In the foundation analysis, the osimertinib group gained 0.41 more quality-adjusted life years (QALYs) than the gefitinib/erlotinib group. The incremental cost-effectiveness ratio (ICER) of the osimertinib schedule and the gefitinib/erlotinib schedulein the total population and in the central nervous system (CNS) metastasis subgroup population were CNY 340,645.44/QALY and CNY 246,175.55/QALY, respectively. The ICER values of both groups were higher than the willingness-to-pay (WTP) threshold in China, i.e., CNY 198,018/QALY, indicating that osimertinib are less economically efficient than gefitinib/erlotinib.Sensitivity analysis shows that drug price, utility value at the stage of disease progression, and treatment cost after progression had a significant impact on the outcome stability. Conclusion Osimertinib can prolong the QALYs of patients suffering from EGFR-mutation positive NSCLC and improve the quality of life, but medical costs also increase accordingly. Currently in China, osimertinib has no economic advantage over gefitinib/erlotinib for patients suffering from EGFR-mutation-induced NSCLC.

  • 生物医药发展与临床应用
    Dana LYU,Suqiu PANG
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    Objective To reduce the incidence rate of immune-related adverse events induced by PD-1 inhibitors through the pharmaceutical care. Methods Clinical pharmacist participated in the analysis of the immune-related adverse events of 2 patients after the application of PD-1 inhibitors and carried out pharmaceutical care. Results Based on the literatures and guides, the clinical pharmacist offered suggestions on rational drug use and prevention measures, which were adopted by the physicians, to ensure the safety for patients. Conclusion There are many kinds of immune-related adverse events caused by PD-1 inhibitors. Clinical pharmacists should strengthen pharmaceutical care and remind physicians to do the relevant medical examinations to improve the safety and effectiveness of PD-1 inhibitor treatment, and avoid negative impact on patients' quality of life.

  • 药物与临床
  • 药物与临床
    Peng LI,Ying GAO,Peng YAO
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  • 药学进展
  • 药学进展
    Jinfang ZHANG,Xiaorui ZHANG,Minsi ZHENG,Zhiyong LI,Tao YUAN,Xiulan HUANG
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    Cucurbitacins are highly oxidized cucurbitane tetracyclic triterpenoids.They are widely found in folk medicinal plants,such as Cucumis melopedicle, Citrullus colocynthis(L.) Schrad, Hemsleya chinensis and Momordica grosvenorii. Cucurbitacins have many pharmacological effects such as anti-tumor, anti-inflammatory, immune regulation, liver protection,antidiabetic and anti-cardiac hypertrophy, which mainly used to treat a variety of tumors, liver diseases, inflammation, diabetes and cardiovascular diseases and so on. In order to find a cucurbitacin with better biological activity, and explore the medicinal potential, molecular mechanism and possible molecular targets of cucurbitacins,this review mainly aimed at summarizing the pharmacological effects and mechanism of frequent reported cucurbitacins for providing some valuable references for the research and development of lead compounds and new drugs of cucurbitacins.

  • 药学进展
    Yong XU,Hao WANG,Jiguo ZHANG
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    Glycogen synthase kinase-3β (GSK-3β) as a multifunctional serine/threonine protein kinase is widely expressed in eukaryotic cells, such asin mammalian muscles, fat, liver, and brain.GSK-3β is involved in many pathophysiological processes such as cell differentiation, embryonic development, inflammatory response, and cell cycle in vivo.In recent years, it has been found that GSK-3β participates in the pathogenesis of Alzheimer's disease (AD) by regulating abnormal aggregation of Aβ, phosphorylation of tau protein, neuronal apoptosis and inflammation.This paper reviews the role of GSK-3β in AD and its possible mechanism.

  • 药物制剂与药品质量控制
  • 药物制剂与药品质量控制
    Ming CHEN,Ping DUAN,Zuogang XU,Hongcai WAN,Xiaoyan LIU
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    Objective A dual wavelength high performance liquid chromatography (HPLC) method was established for the simultaneous determination of protocatechuic acid, protocatechuic aldehyde, orientin, oramnosylvitexin, vitexin, and luteolin-7-o-glucoside in Stenoloma chusanum (L.) Ching. Methods The analysis was performed on a Thermo-Finnegan C18 (250 mm×4.6 mm,5 μm) column with mobile phase of acetonitrile (A)-0.4% phosphoric acid solution(B) at the flow rate of 1.0 mL·min-1for gradient elution.The determintion wavelength was 280 nm for protocatechuic acid and protocatechui caldehyde, and 350 nm for orientin, oramnosylvitexin, vitexin and luteolin-7-o-glucoside.The column temperature was 30 ℃ and injection volume was 5 μL. Results The six compounds were well separated. The linear ranges were from 0.161 9 to 1.214 4, 0.0637 to 0.477 9, 0.083 5 to 0.626 5, 0.238 5 to 1.788 5, 0.077 8 to 0.583 7, and 0.0263 to 0.197 0 μg for protocatechuic acid, protocatechuic aldehydeorientin, orientin, oramnosylvitexin, vitexin, luteolin-7-o-glucoside, respectively,with the correlation of r≥0.999 9. The average recoveries were 100.42% (RSD 2.38%), 101.78% (RSD 2.53%), 99.17% (RSD 2.31%), 105.12% (RSD 3.06%), 97.86% (RSD 2.13%) and 101.54% (RSD 3.87%). Conclusion The method is simple, accurate, reproducible and stable, which can provide reference for the quality control standard of Stenoloma chusanum (L.)Ching.

  • 用药指南
  • 用药指南
    Hui XIE,Zhao WU,Linying WU,Kai ZHAO,Shuang LI,Bin OUYANG,Weiqing HUANG
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    Objective To develop a LC-MS/MS method for determination DADLE in brain tissue of rats. Methods The rats’ brain homogenates were precipitated by acetonitrile.And the separation was carried out by a reversal C18 (2.0 mm×50 mm,5 μm)column in water-menthol system with 0.1% formic acid, the flow rate was 0.4 mL·min-1 followed by mass spectrometry quantitation.Rats with global cerebral ischemia reperfusion were injected with 2,5,10 mg·kg-1 DADLE through jugular vein.And the concentrations in brain tissue were tested 10 and 20 minutes after injection. Results DADLE in rat brain tissue has a good linearity from 0.1 to 1000 ng·mL-1 with the LOQ of 0.1 ng·mL-1.Both the intra- and inter- batch precisions of RSD were within 11.6%.And the accuraues were in the range of 95.81%-99.19%.DADLE concentrations in rats' brain tissue were not varied significantly 10 minutes after injection,and were (1.3±0.45),(2.2±1.1),(2.9 ±1.4) ng·mL-1 20 minutes after injection of 2,5,10 mg·kg-1 DADLE. Conclusion A rapid and simple quantitation method of DADLE is well established and validated,which applied to determination of the DADLE concentration in rat brain tissue.

  • 用药指南
    Kejia LE,Yingjie SU
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    Objective To evaluate and analyze the drug-drug interactions (DDI) of different drugs for lung cancer treatment. Methods Pharmaceutical information databases, Lexicompand Micromedex, were used to evaluate DDI for 25 drugs for lung cancer treatment recommended by guidelines for lung cancer (2018). Results Nine hundred and thirty one DDIs were identified in Lexicomp and 349 in Micromedex. 170 (Lexicomp) and 47 (Micromedex) medication combinations were classified as category X, which should be avoided to use together. The quantities of DDIs in plants products was the most. Conclusion Patients with cardiovascular diseases or infectious diseases and those who use tyrosine kinase inhibitors had high risk to occur DDI. Clinical pharmacists should pay more attention on these patients to avoid the adverse drug reactions during therapy.

  • 用药指南
    Wanqing WANG,Liang ZHOU,Rong CHEN
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    Objective To explore pharmaceutical care model of chronic diseases for asthma and chronic obstructive pulmonary disease (COPD) patients by establishing a special dispensing counterin the outpatient pharmacy. Methods By means of information technology, a special dispensing counterfor asthma and COPD in outpatient pharmacy was established. One hundred and seventy six patients with asthma or COPD who visited the respiratory department of the First Affiliated Hospital of Soochow University from January 2019 to July 2019 were collected, and randomly divided into control group (n=88) and intervention group (n=88). Various forms of pharmaceutical care were conducted in the intervention group (face-to-face demonstration, video tutorial, paper materials, online consultation and guidance, and follow-up), while the control group patients only received usual pharmaceutical care when they entered the group. After 3 months, the inhaler usage score, compliance[Morisky Drug Compliance scale (MMAS-8)] score, rate of correct inhaler operation of each step, clinical effective control rate, incidence of adverse reactions, times of acute attack/aggravation (≥ 2 times), and beliefs about medicines questionnaire (BMQ) of two groups were evaluated, and patient satisfaction in the intervention group was also evaluated. Results Compared with those in the before intervention and control group, the inhaler usage score, MMAS-8 score, rate of correct inhaler operation of each step, and clinical effective control rate in the intervention group significantly increased, while the number of patients with acute attack/ exacerbation more than 2 times and BMQ score significantly decreased (P<0.05 or P<0.01). The incidence of adverse reactions in the intervention group decreased by 10%. Patient satisfaction with pharmaceutical care in the intervention group was basically above 93.18%. Conclusion Providing pharmaceutical care by establishing a special dispensing counter in outpatient pharmacy can help asthma and COPD patients to use inhaler device correctly, resulting in improving compliance of inhaler usage and better disease control, and reducing the occurrence of adverse drug reactions. It is a positive attempt and exploration of pharmaceutical care model for patients with asthma and COPD.

  • 临床药师交流园地
  • 临床药师交流园地
    Maochang LIU,Hua XU,Jia ZHOU,Wei XIE
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    Objective To explore the key points of perioperative pharmaceutical care for children with severe congenital diaphragmatic hernia. Methods In the retrospective analysis of the perioperative treatment of a child with congenital diaphragmatic hernia,the clinical pharmacist provided strategies of pharmaceutical care for children with this disease, from the aspects of optimizing sedation and analgesia, anti-infection regimen and vasoactive medication selection. Results Clinical pharmacists provided pharmaceuticall technical support to maintain the stability of respiratory circulation and to control postoperative infections of the child, and assisted in clinical medication decision-making, so that the child can successfully pass the postoperative risk period. Conclusion Clinical pharmacists actively participate in the pharmaceutical care of children with congenital diaphragmatic herniaand comprehensively analyze the pharmacological characteristics of different medications and the pathophysiological characteristics of the patients, which can improve the level of individualized medication for severely ill children.

  • 药品不良反应与不良事件
  • 药品不良反应与不良事件
    Mengxia LI,Zhixun GUO,Huan LIU,Xiaoyan TIAN,Yan LI,Zhineng MAN,Gang LI
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    Objective To analyze the occurrence regularity and characteristics of platinum-based adverse drug reactions (ADR) in a cancer hospital from 2012 to 2018, and to explore the causes of ADR, so as to provide references for clinical rational application of drugs. Methods A retrospective analysis method was used to summarize the information on 404 cases of platinum-based ADR reported in the hospital from 2012 to 2018. Statistical analysis was performed from the basic condition of the patient, drug names, the original disease, the time of ADR, the organ or system involved, the severity and the outcome of ADR. The data mining method was used to analyze the correlation of ADR related factors. Results In the ADR report, the proportion of patients aged 41-50 was the highest;the number of ADR cases was the highest in cisplatin;the most common ADR in platinum-containing chemotherapy regimens was myelosuppression;51.83% of ADR occurred several days after the administration. Cisplatin is closely related to the damage of blood system and gastrointestinal system;Lobaplatin has a strong correlation with blood system damage;ADR occurred within 2-10 d, which was strongly associated with blood system damage;the association rules show that the severity of ADR which occurred within 1-24 h or caused by oxaliplatin was low. Conclusion In daily clinical work, medical staff should pay attention to ADR information reporting, summarize the regularity and characteristics of different ADR occurrences, give reasonable monitoring advice, reduce the occurrence of ADR and ensure the safety of patients' medication.

  • 世界新药信息
  • 世界新药信息
    zuozhe
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  • 世界新药信息
    Ying ZHAO,Huan GAO,Xing LIU,Yanqing SONG
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    Obeticholic acid (OcalivaTM) is a farnesoid-X receptor (FXR) agonist that is being developed by Intercept Pharmaceuticals for the treatment of various liver diseases, and has recently been granted accelerated approval in the USA for the treatment of primary biliary cholangitis in combination with ursodeoxycholic acid in adults with an inadequate response to ursodeoxycholic acid, or as monotherapy in adults who is unable to tolerate ursodeoxycholic acid. This indication has been approved by the European Union. In this paper, we describe the mechanism, pharmacokinetics and clinical studiesandadverseevents of obeticholic acid.