主办:上海医药工业研究院
   中国药学会
   中国化学制药工业协会
ISSN 1001-8255   CN 31-1243/R   ZYGZEA

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    Perspectives & Review
  • Perspectives & Review
    LIU Weiyuan, LIN Kuaile, XU Wenqian, YIN Xiaowei, ZHOU Weicheng
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    The U.S. Food and Drug Administration(FDA) approved 53 new drugs into the market in 2020, including 38 chemical small molecules and 15 biological products. According to the prescription information for professionals and the related literature as well as patent information, this review describes the descriptions, indications, mechanism of action, dosage form and strength, adverse reactions, and one synthetic route of the chemical small molecules, and brief information about the biological products.
  • Perspectives & Review
    ZHANG Qian, XIA Xuejun
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    The interactions between drugs and excipients in pharmaceutical formulations have positive or negative impacts on the solubility, stability and bioavailability of drugs. Therefore, it is indispensable to investigate the interactions between drugs and excipients, as well as excipients and excipients during the pharmaceutical development process. This paper focuses on the progress of the interactions between raw materials in solid preparations, liquid preparations and drug delivery systems as well as the analysis methods for compatibility study at home and abroad in recent years. It is expected to provide some references for formulation screening and dosage form design.
  • Perspectives & Review
    LUO Wenyan, DING Ying, QIN Feng, LIU Hao
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    Penem antibiotics have broad antibacterial spectrum and strong antibacterial activity, which are used for the treatment of multi-drug resistant bacteria infections. In order to strengthen the safety and effectiveness of the drugs, the progress in the quality research was reviewed in the paper, including assay, detection of the related substances, polymers and metal impurities, providing some references for quality control of penem antibiotics.
  • Paper
  • Paper
    CHEN Wang, DANG Yafeng, LIU Zhaopeng
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    Androst-4-ene-3,17-dione(2) were etherified in the presence of triethyl orthoformate and p-methylbenzenesulfonic acid in tetrahydrofuran and ethanol. The product without separation, underwent the Mannich reaction with N-methylaniline and 37% formaldehyde. And then the elimination reaction under acid conditions gave the key intermediate 6-methyleneandrost-4-ene-3,17-dione(3) in a yield of 71%. Exemestane(1) was obtained by palladium catalyzed 1,2 dehydrogenation in a purity of 99.46% and a total yield of 41%(based on 2). This route avoids the use of benzoquinones oxidant, and simplifies the subsequent purification process.
  • Paper
    BAO Guanglong, ZHANG Naihua, XIANG Yangguang, FEI Fan, ZHANG Guimin
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    A novel synthetic process of milrinone(1) was reported in this paper. 4-Methylpyridine(2) was reacted with acetyl chloride, followed by treatment with acetic anhydride, to afford 1-acetyl-4-(acetylmethylidene)-1,4- dihydropyridine(3), and 2-cyano-3-ethoxyacrylamide(5) was prepared from α-cyanoacetamide(4) via condensation with triethylorthoformate. Finally, the target compound 1 was obtained through cyclization of 3 and 5 with an overall yield of 74%(based on 2) and a purity of 99.96%. The synthetic method for 1 from 3 and 5 has not been found in literature. The new route has been tested in pilot scale, which is suitable for industrial production.
  • Paper
    MEI Yijiang, HU Kai, WENG Haijun, YANG Nonggang, GAO Zhaobo
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    In this paper, secondary exothermic phenomena was found in the preparation of diethyl isonitrosomalonate from diethyl malonate and sodium nitrite, the intermediate of favipiravir. And the dosage of sodium nitrite was far higher than the theoretical amount. The reaction process was studied by on-line infrared and thermodynamic data, the causes of secondary exothermic phenomena were discussed, and the possible reaction mechanism was explained, and the key risk points were identified, which could provide a strong support for the safety research of this nitrosation reaction.
  • Paper
    WANG Yanquan, LI Cailin, NAJIB Mohammerd, PENG Fang, WU Dingyu
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    The effect and mechanism of periplaneta American polypeptide PAE2 in reversing the multi-drug resistance of hepatocellualar carcinoma resistant BEL-7402/5-FU cells were studied in this paper. Hepatocellualar carcinoma sensitive cells of BEL-7402, hepatocellualar carcinoma resistant 5-fluorouracil(5-FU) cells of BEL-7402/5- FU and Balb/c-nude mice were used as the research objects. MTT method was used to detect the multi-drug and crossdrug resistance of BEL-7402/5-FU cells, and the accumulation of doxorubicin in BEL-7402/5-FU cells was observed by laser confocal microscope. In order to determine the mechanism of the periplaneta American polypeptide PAE2 in reversing multi-drug resistance, real-time fluorescent quantitative polymerase chain reaction and immunocytochemical staining method were used to detect the mRNA and protein relative expression of P-glycoprotein 1(P-gp1), multi-drug resistance protein 1(MRP1), lung resistance protein 1(LRP1) and breast cancer resistance protein 1(BCRP1) in BEL- 7402/5-FU cells. In addition, an axillary tumor model of BEL-7402/5-FU cells was established in Balb/c-nude mice to observe the effects of periplaneta American polypeptide PAE2 on immune organs, liver and kidney function, tumor inhibition and induction of tumor cell apoptosis, as well as regulation of multi-drug resistance related proteins in tumor tissues. The results showed that the periplaneta American polypeptide PAE2 could effectively reverse the multi-drug and cross-drug resistance of BEL-7402/5-FU cells. The mechanism might be related to the down-regulation of the expression of multi-drug resistance related proteins, which reduced the efflux ability of multi-drug resistant cells on anti-tumor drugs and intervene molecular metabolism of anti-tumor drugs, reversing the multi-drug resistance of hepatocellualar carcinoma finally.
  • Paper
    HAN Huijing, WU Qiangdong, HE Jiang, CHENG Bo
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    A method was established to identify the Uighur medicine Lavandula Angustifolia and its adulterants(Dracocephalumn integrifolium and Prunella vulgaris) based on the internal transcribed spacer(ITS2) sequence. The ITS2 sequences of the Uighur Medicine Lavandula Angustifolia and its adulterants were subjected to PCR amplification and Bi-directional sequencing. CodonCode Aligner software was used to splice sequence of the sequence peak maps, and the MEGA 6.0 software was used to perform multiple alignment of the assembled sequences. In addition, the genetic distances of interspecies and intraspecies were calculated, the NJ system clustering tree was constructed, and ITS2 secondary structure of Uighur medicine Lavandula Angustifolia and its adulterants was predicted. The results showed that the ITS2 sequence comparison of eighteen Uighur Medicine Lavandula Angustifolia showed no difference after PCR amplification and sequencing, with the sequence lengths were all 235 bp, and the GC content was 67.23% - 69.36%. The sequence lengths of nine Dracocephalumn integrifolium were all 218 bp, and the GC content was 66.21% - 69.51%. And the sequence lengths of nine Prunella vulgaris were all 234 bp, and the GC content was 66.24% - 67.09%. In addition, the intraspecific distance of Uighur Medicine Lavandula Angustifolia was more less than the interspecific distance. The ITS2 sequence could be used as a DNA barcode to identify the Uighur Medicine Lavandula Angustifolia and its adulterants, which provided an effective scientific and technological reference for the safety of the Uighur Medicine Lavandula Angustifolia.
  • Paper
    ZHANG Xiaowen, SUN Jingmeng, NING Jintao, WANG Zhuoming, ZHANG Weiyu
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    Pantoprazole sodium(1) enteric solid dispersion was prepared by solvent freeze-drying method. Taking the cumulative release at 45 min in pH 6.8 phosphate buffer as the index, fishbone analysis method combined with Plackett-Burman design(PBD) were adopted to select the key influence factors from six factors, namely pH value of the solution of enteric carrier, mass ratio of drug to enteric carrier, mass ratio of enteric carrier to lyoprotectant, stirring speed, adsorption of filter membrane and mixing time. According to the results, a Box-Behnken design(BBD) with response surface methodology was used for further investigation. The optimal parameters were as follows: the mass ratio of drug to enteric carrier was 1∶4, stirring speed was 370 r/min, and the mixing time was 20 min. The results of infrared spectroscopy, Raman spectroscopy and differential scanning calorimetry showed that the drug existed in an amorphous form in the carrier. The self-made tablets based on the optimal enteric solid dispersion were prepared by direct compression, then the release behavior of the drug from the tablets in pH 6.8 media were investigated with the commercial enteric tablets as the control. The results showed that the self-made tablets exhibited higher rate and extent of drug release.
  • Paper
    WANG Hongwei, TIAN Bing*, Li Lei, ZHU Haichao
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    In order to improve the stability of reduced glutathione for injection and shorten the freeze-drying cycle, single factor test was carried out to select the solvent and drying temperature of freeze-drying process with several key quality attributes such as freeze-drying time, product appearance and moisture as indicators. The optimal conditions were as follows. First, glutathione and sodium bicarbonate were dissolved in 1% tert-butanol aqueous solution. Next, the solution was pre-frozen at –50 ℃ for 3 h until the drug was completely frozen. Then, the drying temperature of primary drying was adjusted to –36 ℃ and the vacuum degree was kept at 20 Pa for 21 h until the solvent was completely sublimated. After maintaining for 2 h, the temperature of second drying was adjusted to 50 ℃ and the vacuum degree was kept below 10 Pa for 4 h. The obtained freeze-dried product had a white appearance with low moisture and residual solvents. The results of preliminary stability test suggested that the sample had good stability with quality attributes remaining constant. Moreover, the freeze-drying cycle was significantly shortened.
  • Paper
    ZHU Jiaojiao, MENG Yingcai, WANG Shengfeng
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    According to the oxidative self-polymerization of dopamine and 5-hydroxytryptamine under alkaline conditions, the pH-responsive charge-reversal copolymer nanoparticles(PDH NPs) were prepared in this paper. The nanoparticles were characterized by transmission electron microscopy(TEM), ultraviolet absorption spectroscopy(UV) and infrared spectroscopy(IR). The charge-reversal ability and photothermal property of the prepared nanoparticles were also investigated. The results showed that PDH NPs had uniform spherical shapes with particle size of about 100 nm. The copolymer nanoparticles were negatively charged in pH 7.6 medium and positively charged in pH 6.0 medium, showing the pH-responsive charge-reversal ability in vitro. Meanwhile, the PDH NPs had obvious photothermal effect with repeatability. This study would provide a new idea for the construction of multifunctional nanoparticles with synergistic effects of tumor targeting and photothermal therapy.
  • Paper
    CAO Linxiao, ZHAO Jinwei, ZHU Meng, YAO Jingchun, ZHANG Guimin
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    In this study, tricopterid Ⅱ(1) was hydrolyzed in the catalysis of b-glucosidase, and a new iridoid compound [named Y012(2)] was obtained, which was identified as tricopterid Ⅱ aglycon by physical and chemical property inspection, mass spectrometry, 1H NMR, and 13C NMR. The pharmacodynamic test showed that 2 had a good therapeutic effect on cerebral ischemia-reperfusion injury, and it could effectively reduce rat behavior score and cerebral infarction area ratio. In addition, it could also significantly reduce the level of inflammatory factors.
  • Paper
    BAI Xiaoping, LUO Huan, CHEN Jianqiu, JI Yibing
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    In this study, dodecanoyl-β-cyclodextrin was used as a chiral selector to prepare a dodecanoyl- β-cyclodextrin polysulfone blend membrane by immersion precipitation phase inversion method. The stability and performance of the membrane were investigated, and the membrane was used for the chiral resolution of tryptophan racemates. In addition, a chiral ligand exchange liquid chromatography method, which was capable of resolving tryptophan racemates, was established to evaluate the chiral resolution of the blended membrane, and the methodological investigation was conducted. A BaseLine C18 column(4.6 mm×250 mm, 5 μm) was used, with the mobile phase of aqueous phase(0.375 mmol/L L-phenylalanine and 0.075 mmol/L copper sulfate solution, adjusted to pH 4.3 with glacial acetic acid)-methanol(80∶20). The detection wavelength was 278 nm, the column temperature was 35 ℃, and the flow rate was 1 ml/min. The established method provided a reference for chiral resolution of tryptophan enantiomers.
  • Paper
    XU Guili, ZHOU Ainan, HE Qi, WAN Bo, ZHANG Qingwei
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    An high performance liquid chromatography-ultraviolet detection method (HPLC-UV) with dualwavelength was established for the determination of seven related substances in tetrabenazine. A Welch Ultimate XBC18 chromatographic column was used, with 0.005 mol/L dipotassium hydrogen phosphate and 0.005 mol/L potassium dihydrogen phosphate solution(pH 7.0) as mobile phase A, and acetonitrile as mobile phase B(gradient elution). The detection wavelengths were 284 nm and 220 nm. The results showed that it was linear for the related substances in the range of 0.5~10.0 μg/ml. The recoveries were 90%~108%. The sensitivity, selectivity and repeatability of this method were good. In addition, the unknown oxidative degradation impurity (related substance B) was identified by mass spectrometry and nuclear magnetic resonance as 1-hydroxy-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydropyrido [2,1-α] isoquinoline-2-ketones.
  • Pharmaceutical Management & Information
  • Pharmaceutical Management & Information
    XUE Feng, XI Quan
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  • Pharmaceutical Management & Information
    YANG Weichao, CAO Yinhu
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  • Pharmaceutical Management & Information
    WANG Wei
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