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Table of Content

    28 February 2018, Volume 27 Issue 1
    Original articles
    Protective effects of tanshinone IIA derivative on myocardial ischemia/reperfusion injury in rats
    Wanli Shen, Fei Yu, Lu Xu, Cong Chen, Yini Cao, Shu Liu, Nanyin Han, Chao Wang, Rong Qi
    2018, 27(1):  1-13.  DOI: 10.5246/jcps.2018.01.001
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    Tanshinone IIA (TSIIA) is the major bioactive constituent of Salvia miltiorrhiza Bunge, a Chinese herbal medicine, which has protective effects on myocardial ischemia/reperfusion (MIR) injury. However, the cardioprotective effects of TSIIA as well as its clinical use were limited due to its poor water solubility. The objective of this study was to evaluate whether Tanshinone IIA derivative (TD), a new water soluble compound synthesized by TSIIA and N-Methyl-D-Glucamine, had protective effects on MIR injury and what the related mechanism was. The cardioprotective effects of TD were evaluated and compared with TSIIA in a rat MIR model. The results show that pretreatment with TD significantly alleviated inflammatory infiltration and exhibited antioxidant effect in MIR injury by reducing the activity of lactate dehydrogenase (LDH) and malondialdehyde (MDA), decreasing expression of nuclear factor-κ-gene binding (NF-κB) and upregulating expression of heme oxygenase (HO-1), but having no effect on the content of total superoxide dismutase (T-SOD) and mRNA expression of superoxide dismutase (SOD-1). Thus, our study reveals that TD exerted significant protective effects on MIR injury through attenuating oxidative stress and inflammatory responses.

    Influence of CYP2C9*2 genetic polymorphism on pharmacokinetics of losartan and its active metabolite E-3174 on the background of CYP3A4 wild genotype in healthy Chinese Hui subjects
    Lu Yang, Tao Guo, Xuemei Zhuang, Hongyan Gu
    2018, 27(1):  14-21.  DOI: 10.5246/jcps.2018.01.002
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    In the present study, we aimed to investigate the influence of CYP2C9*2 genetic polymorphism on pharmacokinetics of losartan and its active metabolite E-3174 on the background of CYP3A4 wild genotype in healthy Chinese Hui subjects. Blood samples were collected from subjects for CYP2C9 and CYP3A4 genotyping using a polymerase chain reaction-restriction fragmentlength polymorphism (PCR-RFLP) assay. A pharmacokinetic study was then carried out in two groups with CYP2C9*1/*1 (n = 8) andCYP2C9*1/*2 (n = 6) genotypes at the same time, and all the 14 subjects were CYP3A4 wildgenotype. Plasma levels of losartan and E-3174 were determined by high-performance liquid chromatography-fluorescence (HPLC-FLD) method before and after a single oral dose of 50-mg dose of losartan in tablet form. The pharmacokinetic parameters were calculated by DAS 2.0 software and analyzed by SPSS 16.0 software. Pharmacokinetic parameters, including area under the curve from 0 h to the last measured point 24 h (AUC0–24), area under the curve from 0 h to infinite time (AUC0–∞), peak plasma concentration (Cmax), time to reach Cmax (tmax), oral clearance (CL), oral volume of distribution (Vd) and elimination half-life (t1/2), were determined. Compared with the CYP2C9*1/*2 group, the AUC0–24, AUC0–∞ and Cmax of E-3174 in CYP2C9*1/*1 group of Hui subjects were respectively 1.36, 1.32 and 1.64 times more, and the statistic differences were significant (P<0.05). The CYP2C9*2 mutant allele played an important role in the pharmacokinetics of losartan after oral administration, and itmight decrease the generationof E-3174. However, large-sample clinical trials are required to validate whether the dose adjustment according to CYP2C9 genotype is necessary.

    Study on the interactions of pharmacokinetics and liver distributions between rosuvastatin and repaglinide in rats
    Dujuan Zhang, Keguang Chen, Rui Zhang, Guiyan Yuan, Benjie Wang, Ruichen Guo
    2018, 27(1):  22-30.  DOI: 10.5246/jcps.2018.01.003
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    In the present study,we aimed to investigate the interactions of pharmacokinetics and liver distributions between rosuvastatin and repaglinide in rats.Coadministration of repaglinide (0.5 mg/kg, 1 mg/kg and 2 mg/kg) for 7 d significantly increased the AUC0–24 and Cmax of rosuvastatin (P<0.01), but dramatically decreased the CL/F of rosuvastatin (P<0.01) after a single dose of rosuvastatin (10 mg/kg). There were no obviously changes in the parameters of Tmax and t1/2. Coadministration of repaglinide also decreased the liver distribution of rosuvastatin (P<0.01). Coadministration of rosuvastatin (20 mg/kg) for 7 days significantly increased the AUC0–12 and Cmax of repaglinide (P<0.05), and decreased the CL/F of repaglinide (P<0.01) after a single dose of repaglinide (1 mg/kg). The liver distribution of repaglinide was also decreased (P<0.01). Our animal study indicated that repaglinide could significantly affect the pharmacokinetics and liver distribution of rosuvastatin in rats and vice versa.

    Development and optimization of nanoemulsion gel for topical delivery of imiquimod
    Gurvinder Kaur, Tanurajvir Kaur, Deepak N. Kapoor
    2018, 27(1):  31-39.  DOI: 10.5246/jcps.2018.01.004
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    In the present study, we aimed to formulate, optimize and characterize nanoemulsion-based gel of imiquimod for its topical administration and to improve the drug permeation. Nanoemulsions were prepared by the aqueous phase titration method and spontaneously formed by mixing specific fractions of oil phase:Smix:water. The nanoemulsion formulations were optimized by response surface methodology (RSM) using mixture design, Scheffe model. The formulated nanoemulsion was incorporated into 0.5% Carbopol 934 (w/v) to enhance convenience in superficial application of the drug. The nanoemulsions were characterizedin terms of droplet size, zeta potential, TEM, DSC and in vitro drug permeation. The vesicle size was 113.6 nm with polydispersity index of 0.251. The zeta potential was 34 mV. The spherical droplet shape was confirmed by TEM analysis. The drug permeation from the diffusion membrane was 73.67% in 6 h for the optimized formulation. An optimized nanoemulsion gel formulation of imiquimod was successfully developed with improved permeation using experimental design technique. The developed formulation could be further explored as a potential alternate to currently available topical formulations for the treatment of genital warts.

    Chemical constituents from the leaves of Cistus parviflorus
    Xinyu Fang, Rongrong Wang, Shiwei Sun, Xiaoxiao Liu, Xiaohong Liu, Wei Wang, Yoshihito Okada, Wei Wang
    2018, 27(1):  40-50.  DOI: 10.5246/jcps.2018.01.005
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    A phytochemical investigation on the leaves of Cistus parviflorus led to the isolation of 18 compounds. The structures of the isolated compounds were elucidated as kaempferol 3-O-(3′′,6′′-di-O-E-p-coumaroyl)-β-D-glucopyranoside (1), scopoletin (2),kaempferol 3-O-(3′′-O-E-p-coumaroyl)-β-D-glucopyranoside (3), kaempferol 3-O-(6′′-O-E-p-coumaroyl)-β-D-glucopyranoside (4), kaempferol 3-O-β-D-glucopyranoside (5), kaempferol 3-O-α-L-rhamnopyranosyl-(1→2)-(6′′-O-E-p-coumaroyl)-β-D-glucopyranoside (6), methyl flavogallonate(7), quercetin 3-O-β-D-glucopyranoside (8), quercetin 3-O-β-D-galactopyranoside (9), hydroquinone (10), arbutin (11), methyl β-glucopyranoside (12), shikimic acid (13), (S)-1,2-propandiol-1-O-β-D-glucopyranoside (14), benzyl-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside (15), 2-phenethyl-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside (16), corchoionoside C (17), kaempferol 3-O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside (18) by the analysis of the MS and NMR spectroscopic data and comparison with the literature. Compounds 12, 67, 1012, and 1416 were isolated from Cistus genus for the first time. 

    Drug administration and clinical pharmacy column
    An analysis on the factors associated with reuse of insulin pen needles in type 2 diabetic patients in China
    Xiaodong Guan, Lili Ma, Guoying Wang, Haishaerjiang Wushouer, Chunxia Man, Sheng Han, Luwen Shi
    2018, 27(1):  51-58.  DOI: 10.5246/jcps.2018.01.006
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    Incorrect injection technique of insulin is a common problem worldwide, which can reduce the efficacy of insulin therapy and lead to poor glucose control. A cross-sectional, multiple-center survey from 44 hospitals was conducted from Nov. 2015 to Dec. 2015. Non-parametric Kruskal–Wallis analysis of variance and Mann-Whitney U test were used for multi-parametric analysis. Multivariable logistic regressions were performed to identify the factors associated with independent variables. Overall, a single needle was used at an average of 3.79 times, with the highest of 60 times. Analysis across all study participants showed that the frequency of a single needle was positively correlated with age (P = 0.029), duration of diabetes (P≤0.001) and number of complications (P≤0.001). Multivariable logistic regressions analysis of insulin pen needle reuse and needle compliance showed that age, income, education, marital status, duration of diabetes, quality of life and cost of drug were significantly related to needle reuse. From this survey, we found that reuse of insulin pen needle was common in China. Frequency of needle reuse was related to the patients’ demographic characteristics (income level, age, region, education, employment status and self-care), health-related variables (duration of diabetes, number of complications and EQ-5D index scores) and utilization of health services (clinical visits, hospitalization and cost of medications). 

    Clinical development of tumor necrosis factor-alpha inhibitors for ankylosing spondylitis
    Zhou Linguang, Jiang Bin
    2018, 27(1):  59-63.  DOI: 10.5246/jcps.2018.01.007
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    There is no radical cure for ankylosing spondylitis, a chronic inflammation in joint, till now. Tumor necrosis factor-alpha (TNF-α) inhibitors can block the cascade in inflammatory chain and improve clinical symptom. Among these biological agents, three of them are marketed in China: etanercept, infliximab and adalimumab. Some of the research progresses between 2014 and 2016 are summarized including treatment application, side effects of drugs, and comprehensive research of TNF-α inhibitors. 

    Others
    Information for Authors
    Journal of Chinese Pharmaceutical Sciences
    2018, 27(1):  64-73. 
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    Prof. Xinshan Ye was awarded “Weishan Chemistry Prize of Natural Products Synthesis”, Prof. Ning Jiao was awarded “Chinese Chemical Society-BASF SE Youth Knowledge Innovation Award”
    Shuxiang Song
    2018, 27(1):  74-74. 
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    Prof. Xinshan Ye was awarded “Weishan Chemistry Prize of Natural Products Synthesis”, Prof. Ning Jiao was awarded “Chinese Chemical Society-BASF SE Youth Knowledge Innovation Award”