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Table of Content

    03 March 2018, Volume 27 Issue 2
    Original articles
    A derivatization method to improve the assay of salinomycin sodium and its application in the liposomal formulation
    Jingying Zhang, Qian Luo, Jiarui Xu, Jing Bai, Lei Liu, Limin Mu, Yan Yan, Wanliang Lu
    2018, 27(2):  75-81.  DOI: 10.5246/jcps.2018.02.008
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    Salinomycin sodium (SAL-Na) is a type of antibiotic chemotherapeutic drugs with the potential to treat cancer stem cells. The assay method of SAL-Na included in the pharmacopoeia is a microbiological method, which is not suitable for the rapid detection in daily scientific research. Besides, the assay methods of SAL-Na reported by literature are not suitable for quantification due to the interference of various excipients. Consequently, the deep study on biological mechanism of SAL-Na is hindered by its assay method. In the present study, we aimed to establish an ultraviolet visible (UV-vis) spectrophotometric method to determine the content of SAL-Na in the liposomes. The first approach was a UV spectrophotometry, in which SAL-Na was dissolved in ethanol and then detected at 287 nm. Although the standard curve measured at 287 nm by UV method had good linearity, the quantification limitation was too high to meet the requirement in determining SAL-Na in the liposomes. In addition, the membrane materials in the liposomes severely affected the measurement. The second one was an improved UV-vis spectrophotometry by vanillin derivatization. In this method, SAL-Na was dissolved in 95% ethanol, mixed with vanillin test solution and heated at 72 °C for 40 min for derivatization. After cooling down to room temperature, the solution was detected using UV-vis spectrophotometer at 526 nm. This method could be used to accurately determine the content of SAL-Na at lower concentration, and the absorbance value was stable for 5 d at least. Moreover, the membrane materials of the liposomes did not affect the absorbance of SAL-Na at 526 nm. The precision and recovery studies demonstrated that the vanillin derivatization approach was stable and precise in assaying SAL-Na. In conclusion, the UV-vis spectrophotometry by vanillin derivatization could be used for measuring SAL-Na in the liposomes, thereby laying a foundation for deep study of the biological mechanism of SAL-Na in the liposomes.

    Process optimization for the enhanced stability of diclofenac potassium granules and capsules
    Jiangyan Liu, Xiunan Li, Xiaoxue Zhang, Haoyan Huang, Liqing Chen, Jinghao Cui, Qingri Cao
    2018, 27(2):  82-91.  DOI: 10.5246/jcps.2018.02.009
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    This study aimed to investigate the effects of different process parameters on the physical properties, in vitro dissolution rate, and short and long-term stability of diclofenac potassium (DFP) granules and capsules. DFP granules exhibited low total amounts of impurities when prepared through the wet granulation method using a granulating solvent with a low water/ethanol ratio. The impurities of the wet DFP mass dried at 70 °C were higher than those dried at 50 °C or 60 °C. DFP granules were stable under strong light exposure during preparation. DFP granules prepared using a granulating solvent with a 1:4 water/ethanol ratio had a relatively smaller particle size and higher angle of repose than those prepared using granulating solvents with other water/ethanol ratios. The dissolution rate of DFP capsules prepared using four different water/ethanol ratios was less than 2% after 10 min of dissolution and increased to 95% within 30 min of dissolution. The total amount of drug impurities of DFP capsules prepared using a granulating solvent with 1:4 water/ethanol ratio was considerably lower than those of DFP capsules prepared using a granulating solvent with a 1:0 water/ethanol solvent ratio. Regardless of the water/ethanol ratio, the capsules showed poor stability when exposed to high temperature (60 °C) and strong light (4500±500 Lux) for 10 days, but were relatively stable at high humidity (92.5% RH). The results of the long-term stability (25±2 °C and 60%±10% relative humidity) study showed that DFP granules were more stable than DFP capsules, and were stable for 12 months. The type of encapsulating material did not affect the 2-month stability of DFP. DFP granules are sensitive to granulating solvent and drying temperature and DFP capsules should be stored away from high temperature and strong light. 

    Tissue distribution and pharmacokinetics of brucine niosomal gels in rats after topical and oral application
    Zhenzhen Wu, Hengchun Ren, Yanying Li, Jiajia Fu, Xiaojun Liu, Jie Hu
    2018, 27(2):  92-98.  DOI: 10.5246/jcps.2018.02.010
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    Brucine has anti-inflammatory and analgesic effects and is the main active compound of the seeds of Strychnos nux-vomica L. To study brucine niosomal gels, a reliable and rapid LC-MS/MS method was established to quantify brucine levels in rats. Tissue distribution and pharmacokinetics of brucine were investigated after topical and oral application of brucine niosomal gels to rats. The plasma concentration versus time profiles suggested that systemic exposure of brucine for oral administration of brucine niosomal gels was higher than that for topical administration, and topical administration showed a relatively sustained release. There was a considerable amount of brucine distributed in the knee joint. These results provided a strong basis for the follow-up study of this preparation.

    Preparation, characterization and pharmacokinetic studies of total paeony glycoside nanocrystals
    Jinfeng Zhang, Fan Wu, Jiayi Han, Jinghong Rong, Yi Li, Yu Liu, Xiao Liang, Xin Wang, Hao Pan, Hongsheng Liu, Lijiang Chen
    2018, 27(2):  99-108.  DOI: 10.5246/jcps.2018.02.011
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    Total paeony glycoside (TPG) is obtained from Radix Paeoniae Rubra with a variety of bioactivities. However, the low solubility and bioavailability limit its application. The present study aimed to develop TPG nanocrystals to increase the dissolution and then improve the oral bioavailability. TPG nanocrystals were prepared via precipitation and high-pressure homogenization method. The physical-chemical properties of the optimal TPG nanocrystals in terms of particle size, zeta potential, morphology and crystallinity were evaluated. The results showed that TPG nanocrystals had a mean particle size of (210.2±2.5) nm, a polydispersity index of 0.191±0.033 and a zeta potential of (–22.4±1.2) mV. The result of differential scanning calorimetry showed that the nanocrystals were still in crystalline state after the preparation procedure. Transmission electron microscopy (TEM) results showed that the nanosuspension was in spherical shape. The pharmacokinetics of TPG nanocrystals for rats was investigated by liquid chromatography-tandem mass spectroscopy (LC-MS/MS). Compared with the TPG coarse suspension, TPG nanocrystals exhibited significant increase in AUC0–∞ (approximately 1.85-fold). Taken together, TPG nanocrystals could be used as a promising drug delivery system due to the enhanced oral bioavailability of TPG. 

    Quality evaluation of heat stress treated Radix saposhnikoviae using pharmacokinetic and pharmacologic methods
    Hua Jiang, Jingming Yang, Ling Cao, Guizhi Jia, Hongliang Dai, Xiangcai Meng
    2018, 27(2):  109-115.  DOI: 10.5246/jcps.2018.02.012
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    The quality of Radix saposhnikoviae (RS) had deteriorated due to the adoption of cultivated plants rather than wild plants. High temperature treatment increases the content of several chromones, however using one or more individual constituents would be difficult to determine the medical quality of RS. In this paper, we used pharmacokinetic and pharmacologic approaches to evaluate the quality of RS. The active constituents were analysed using pharmacokinetic parameters of the chromone derivatives, and  the antipyretic, analgesic, and anti-inflammatory effects were evaluated by pyretic animal model, hot plate test, and ear edema model, respectively. Only cimifugin was found in plasma after RS and heat-stress-RS were administered to rats, with a 50.6% increase in AUC0–24 h of cimifugin in the latter. Likewise, more potent anti-pyretic, analgesic, and anti-inflammatory activities were also found in the latter. Exposure of S. divaricata fresh roots to high temperatures enhanced the antipyretic, analgesic, and anti-inflammatory effects of RS by promoting the absorption of cimifugin.

    Cardioprotective effects of combination of notoginseng total saponins and safflower total flavonoids against myocardial infarction in rats
    Yuqing Meng, Lichao Wang, Yan Li, Jinyang Song, Zhiyong Du, Chun Li, Yong Jiang, Pengfei Tu, Xiaoyu Guo
    2018, 27(2):  116-122.  DOI: 10.5246/jcps.2018.02.013
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    In this study, the cardioprotective mechanism of the combination of notoginseng total saponins and safflower total flavonoids (CNS) was investigated due to its excellently efficacy against myocardial infarction (MI) in rats. After the left anterior descending coronary artery (LADCA) ligation, rats were orally administered with CNS for 7 consecutive days. CNS prevented MI-induced pathophysiological changes and significantly decreased plasma levels of myocardial enzymes, including creatine kinase MB isoenzyme (CK-MB), lactate dehydrogenase (LDH) and aspartate aminotransferase (AST). Further investigation revealed that CNS attenuated the production of inflammatory factors in plasma, including tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6) and interleukin-1β (IL-1β). Moreover, CNS treatment decreased the expression of caspase-3 at the mRNA level in infarct tissue. Our findings demonstrated that the anti-inflammatory and anti-apoptotic properties of CNS might confer its cardioprotection against MI in rats.  

    A subchronic toxicity test of ethyl acetate extract from endophytic fungus Penicillium sp. of kunyit putih (Curcuma zedoaria) against Swiss albino mice
    Muharni, Heni Yohandini
    2018, 27(2):  123-130.  DOI: 10.5246/jcps.2018.02.014
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    Ethyl acetate extract of endophytic fungus from Penicillium sp. of kunyit putih showed antibacterial activity in vivo but no acute toxicity. However, the extract may have toxic effects on major organs for long-term consumption. This study was carried out in order to test sub-chronic toxicity of the ethyl acetate from endophytic fungus Penicillium sp. of kunyit putih against mice (Mus musculus). A total of 50 male mice were divided into five groups. Groups I, II, III and IV were orally administered with ethyl acetate extracts of 250, 500, 1000 and 2000 mg/kg body weight (BW), respectively. Group V was used as a control without extract treatment. A toxic symptom was observed by analyzing several parameters, namely change in BW, hematologic and biochemical properties (SGOT & SGPT), macroscopic organs, and relative organ weight. The results showed that there was toxic symptom and statistically significant difference in the parameters of SGOT, SGPT and heart weight between treated and control groups. Based on analysis, we concluded that ethyl acetate extract from endophytic fungus Penicillium sp. of kunyit putih had subchronic toxicity effect.

    Drug administration and clinical pharmacy column
    Investigations and feedback on the training mode of professional master’s degree of clinical pharmacy in Peking University and the preliminary exploration of Pharm. D. Education
    Zhiyan Liu, Xiaoyan Nie, Qian Xiang, Luwen Shi, Yimin Cui
    2018, 27(2):  131-137.  DOI: 10.5246/jcps.2018.02.015
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    In order to carry out the comprehensive reform of the professional master’s degree training mode of clinical pharmacy, we carried out interviews among 91 persons on the professional master's degree of clinical pharmacy in Peking University School of Pharmaceutical Sciences and collected extensive feedback. We preliminaries explore the mode of Doctor of Pharmacy (Pharm. D.) Education, laying the foundation for Doctor’s education of professional clinical pharmacy in China. We conducted investigations and interviews among 91 clinical pharmacists and students of Peking University School of Pharmaceutical Sciences on the training of professional master’s degree and Pharm. D. education mode, which includes 67 postgraduates and 24 clinical pharmacists. Respondents put forward the problems of training mode and corresponding suggestions and opinions from different aspects during the investigation and interview. The results mainly divide into four aspects: curriculum setting, clinical practice, assessment system and teaching resources. Respondents put forward effective feedback on the above four aspects, which are beneficial to the comprehensive reform of the training mode of professional master degree in clinical pharmacy and preliminary exploration of Pharm. D. Education in China.

    Others
    Information from US FDA——Impact of Severe Weather Conditions on Biological Products & FDA Drug Safety Communication: FDA review finds additional data supports the potential for increased long-term risks with antibiotic clarithromycin (Biaxin) in patients with heart disease
    http://www.fda.gov
    2018, 27(2):  138-140. 
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    The U.S. Food and Drug Administration today approved Imfinzi (durvalumab) for the treatment of patients with stage III non-small cell lung cancer (NSCLC) whose tumors are not able to be surgically removed (unresectable) and whose cancer has not progressed after treatment with chemotherapy and radiation (chemoradiation). This is the first treatment approved for stage III unresectable non-small cell lung cancer to reduce the risk of the cancer progressing, when the cancer has not worsened after chemoradiation,” said Richard Pazdur, M.D., director of the FDA’s Oncology Center of Excellence and acting director of the Office of Hematology and Oncology Products in the FDA’s Center for Drug Evaluation and Research. “For patients with stage III lung cancer that cannot be removed surgically, the current approach to prevent progression is chemoradiation. Although a small number of patients may be cured with the chemoradiation, the cancer may eventually progress. Patients now have an approved therapy that has been shown to keep the cancer from progressing for a longer time after chemoradiation.”

    The research on Autism related molecules by group of Heli Liu was reported in the journal Nature Communications
    Jianmei Liu
    2018, 27(2):  141-142. 
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    The research on Autism related molecules by group of Heli Liu was reported in the journal Nature Communications.