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
Chinese Journal of Pharmaceuticals

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    Perspectives & Review
  • Perspectives & Review
    Research Progress of Antibody Drug Conjugates
    Research Progress of Antibody Drug Conjugates
    2025, 56(10): 1243. https://doi.org/10.16522/j.cnki.cjph.2025.10.001
    Abstract ( )   Knowledge map   Save
    Antibody-drug conjugates(ADCs) are novel antineoplastics that combine the high targeting speciffcity of monoclonal antibodies with the potent cytotoxicity of small-molecule toxins. By selectively delivering cytotoxic payloads to tumor cells, ADCs achieve effective tumor cell killing while minimizing damage to healthy cells and reducing systemic toxicity. These innovative agents, often referred to as “biological missile”, are leading a new era in targeted cancer therapy. Although three generations of ADCs have been applied to cancer treatment, further optimization of the components of ADCs is still required to address challenges such as stability, cytotoxicity, and drug resistance. This article summarizes the approved ADCs and those under clinical research, outlines innovative directions for next-generation ADCs, to provide insights for advancing research and development of novel cancer treatments using ADC technology.
  • Perspectives & Review
    Research Progress of Co-delivery Systems Containing Paclitaxel and Traditional Chinese Medicine Components for Antitumor Applications
    ZHANG Yihong, XIE Yan
    2025, 56(10): 1252. https://doi.org/10.16522/j.cnki.cjph.2025.10.002
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    Various nature products have been veriffed to enhance the antitumor efffcacy of paclitaxel and mitigate its toxic and adverse reactions. However, the co-delivery of paclitaxel and natural products remains a signiffcant challenge in the pharmaceutical ffeld. In recent years, strategies such as drug self-assembly, drug carriers, and new formulation forms have been employed to concurrently deliver natural products and paclitaxel to tumor sites, aiming to exert their synergistic effects, thereby elevating antitumor activity of paclitaxel and circumventing drug resistance. This article systematically reviews relevant literature, focusing on the design strategies, release characteristics, and therapeutic effects of co-delivery systems, with the aim of providing insights and references for antitumor research combining paclitaxel and natural products.
    • Paper
  • Paper
    Synthesis and Impurity Study of Betrixaban
    WANG Haibo , JIN Hui , XIAO Yang , JIN Shiyuan , YU Ansheng
    2025, 56(10): 1261. https://doi.org/10.16522/j.cnki.cjph.2025.10.003
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    An optimized synthesis process of betrixaban(1) was reported in the paper. N-(5-Chloro-2-pyridinyl)- 5-methoxy-2-nitrobenzamide(6) was prepared by acylation of 5-methoxy-2-nitrobenzoic acid(8) and condensation with 2-amino-5-chloropyridine(7). 2-Amino-N-(5-chloro-2-pyridinyl)-5-methoxybenzamide(4) was prepared form 6 via reduction. Then compound 4 was condensed with 4-cyanobenzoic acid to obtain N-(5-chloro-2-pyridinyl)-2-[(4- cyanobenzoyl)amino]-5-methoxybenzamide(3). Next, N-(5-chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]- benzoyl]amino]-5-methoxybenzamide(2) was prepared from 3 by ammonolysis reaction. Finally, compound 2 was salted with maleic acid to obtain the target product 1, with an overall yield of 27.6％ and purity of 99.9％ . Meanwhile, the characteristic impurities generated in the process were synthesized, and their generation and removal were studied in detail. Among them, related substance D was reported at the ffrst time. By controlling the temperature of the reduction reaction, the drying temperature and the amounts of dimethylamine/n-butyllithium in the ammonolysis reaction, all characteristic impurities of the process were controlled below 0.15％ .
  • Paper
    New Synthesis of Iguratimod
    LIU Li , HUANG Jing , ZHU Xiaoyu , JI Tingting , WANG Chen
    2025, 56(10): 1271. https://doi.org/10.16522/j.cnki.cjph.2025.10.004
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    A new synthetic process of iguratimod(1) was reported. Firstly, in the presence of aluminum chloride, the starting material 3-methylsulfonylamino-4-phenoxyphenyl methyl ether(2) reacted with acetyl chloride to generate N-(4-acetyl-5-hydroxy-2-phenoxyphenyl)methanesulfonamide(3). Then, the key intermediate N-(3-bromo-4-oxo6-phenoxy-4H-chromen-7-yl)methanesulfonamide(19) was synthesized by the addition-cyclization reaction of N,Ndimethylformamide dimethyl acetal/N-bromosuccinimide and 3. Compound 7 was obtained by amination of 19 with ammonium hydroxide. Finally, 1 was synthesized from 7 by formylation. The yield increased from 27.4％ to 33.0％ (based on 2), and the HPLC purity of the target 1 reached 99.9％ . The new synthetic process has the advantages of short steps, avoiding the use of flammable, explosive, and toxic chemical reagents, and mild reaction conditions, less side reaction, which is suitable for industrial production.
  • Paper
    Synthesis of Related Substances of Stiripentol
    XIAO Hu, ZHOU Hao, SHI Xiaoyu, DOU Jianwei, ZHANG Daizhou
    2025, 56(10): 1277. https://doi.org/10.16522/j.cnki.cjph.2025.10.005
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    In order to control the quality of stiripentol(1), four related substances were synthesized, namely (Z)-4,4-dimethyl-1-[(3,4-methylenedioxy)phenyl]-1-penten-3-ol(related substance A), bis[(E)-4,4-dimethyl-1-(3,4- methylenedioxy)phenyl-1-pentene-3-yl]ether(related substance B), (E)-4,4-dimethyl-1-[(3,4-methylenedioxy)phenyl]- 3-ethoxy-1-pentene(related substance C), (E)-4-methyl-1-[(3,4-methylenedioxy)phenyl]-1-hexen-3-ol(related substance D). Among them, related substances C and D were reported at the ffrst time. Their structures were conffrmed by 1 H NMR, 13 C NMR and MS.
  • Paper
    Comparative Study of Recombinant Trypsin and TPCK-treated Trypsin Applied to Trastuzumab Peptide Mapping Analysis
    LIU Qiao , LIU Xiao , WEN Xuemei , LI Suxia , PAN Hongjuan
    2025, 56(10): 1282. https://doi.org/10.16522/j.cnki.cjph.2025.10.006
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    This study utilized trastuzumab as a model sample for peptide mapping analysis to comprehensively compare the performance of recombinant trypsin and N-tosyl-L-phenylalanyl chloromethyl ketone(TPCK)-treated trypsin across three aspects: rapid digestion with conventional enzyme amounts, overnight digestion with low enzyme amounts, and enzyme activity assays. The results demonstrated that both trypsins achieved 100％ sequence coverage for the light chain of the monoclonal antibody. However, recombinant trypsin provided superior heavy chain sequence coverage compared to TPCK-treated trypsin. Results of rapid digestion tests revealed that recombinant trypsin achieved more complete antibody digestion within shorter timeframes, though with relatively higher abundances of missed cleavages and non-specific cleavages than TPCK-treated trypsin. Conversely, under low-enzyme overnight digestion conditions, recombinant trypsin generated lower abundances of missed cleavages and non-specific cleavages than TPCK-treated trypsin. Additionally, digests with TPCK-treated trypsin contained chymotrypsin cleavage sites(F, phenylalanine). Further enzyme activity assays conffrmed that recombinant trypsin exhibited better activity and stability than TPCK-treated trypsin. In conclusion, while both trypsins are suitable for standard peptide mapping protocols using conventional enzyme amounts and digestion times, recombinant trypsin demonstrates superior activity, cleavage speciffcity, and stability, making it the preferred choice for peptide mapping analysis and other structural characterization sample preparations of biologics.
  • Paper
    Preparation and in vitro Release of Indapamide Push-pull Osmotic Pump Controlledrelease Tablets
    YIN Hui
    2025, 56(10): 1293. https://doi.org/10.16522/j.cnki.cjph.2025.10.007
    Abstract ( )   Knowledge map   Save
    This study employed a single-factor method to optimize the formulation of indapamide(1) singlechamber double-layer push-pull osmotic pump controlled-release tablets. Systematic investigations were conducted on the drug-containing layer formulation, push layer composition, and coating weight gain. The ffnal optimized formulation was determined as follows: drug-containing layer containing 1.5 mg of 1 and 100 mg of polyethylene oxide(relative molecular weight: 300 000); push layer containing 65 mg of polyethylene oxide(relative molecular weight: 5 000 000) and 20 mg of sodium chloride; coating weight gain of 4％ . The 1 push-pull osmotic pump controlled-release tablets were prepared according to the optimized formulation, and their release behaviors in various media of different pH value were evaluated. The results demonstrated that the optimized tablets achieved zero-order release over 24 h, with drug release behavior independent of external environmental factors. This study provides a valuable reference for developing novel sustainedrelease formulations of 1.
  • Paper
    Inffuence of Component Concentration on the Binding Afffnity and Entrapment Efffciency of Three Volatile Oil Components of Wenjing Decoction with β-cyclodextrin
    SHEN Wen , SHI Run , LI Zhuoyuan , TAO Lin , LI Junsong , LI Wen, WANG Honglan
    2025, 56(10): 1299. https://doi.org/10.16522/j.cnki.cjph.2025.10.008
    Abstract ( )   Knowledge map   Save
    The aim of this study is to investigate the correlation between the binding afffnity of cinnamaldehyde, paeonol and ligustilide(main volatile components of Wenjing decoction) with β-cyclodextrin (β-CD) and the encapsulation efffciencies of their β-CD inclusion complexes. The volatile oil(or volatile parts) of Cinnamomi Cortex, Angelicae sinensis Radix/Chuanxiong Rhizoma and Moutan Cortex was extracted by steam distillation. Based on the molar ratios of the complete formula of Wenjing decoction, a series of concentrations of volatile oil with different molar ratios of above three componets were prepared. And the β-CD inclusion complexes were prepared by saturated aqueous solution method. The thermal stability test was carried out to investigate the stability of the inclusion complexes, and a HPLC method was used to determine the encapsulation efffciency. The binding afffnity of β-CD to the three volatile components was analyzed by phase solubility test and molecular docking. The results showed that in the mixed volatile oils with molar ratios of 1 ∶ 2 ∶ 4 and 1 ∶ 1 ∶ 1 for cinnamaldehyde, paeonol and ligustilide(with the total concentrations of 0.1％ , 0.2％ and 1.0％ ) as well as in the mixed volatile oils with molar ratios of 2 ∶ 4 ∶ 1 and 4 ∶ 2 ∶ 1(with the total concentration of 0.1％ ), the encapsulation efffciency was mainly affected by the binding afffnity of each component with β-CD itself. While in the mixed volatile oils with molar ratios of 4∶2∶1 and 2∶4∶1 for above three components(with the total concentrations of 0.2％ and 1.0％ ) encapsulation efffciency was mainly inffuenced by the molar ratios of the components themselves. This study provides ideas for the inclusion process regulation of the synchronous and consistent transfer of volatile oil components in the preparation of granules of Wenjing decoction．
  • Paper
    Establishment of Speciffc Chromatogram and Content Determination of Shufu Plaster Based on GC-MS
    ZUO Jie, XIONG Wei, JIANG Jiashu, GUO Li, HU Can
    2025, 56(10): 1308. https://doi.org/10.16522/j.cnki.cjph.2025.10.009
    Abstract ( )   Knowledge map   Save
    Different batches of Shufu plaster were determined by the combination of characteristic map, multiindex component content determination and chemical pattern recognition analysis. A GC-MS method was established to determine seven components(camphor, trans-nerolidol, isoborneol, borneol, menthol, α-zingiberene, α-farnesene) in Shufu plaster. A HP-INNOWax chromatography column(30 m×0.25 mm×0.5 μm) was used, and the injection port temperature was 230 ℃ , carrier gas was helium, and ion source temperature was 230 ℃ . The cluster analysis results showed that the components of 15 batches of Shufu plaster were clustered into two categories. Principal component analysis further screened out seven representative components contributing to the batch differences. Multi-index content determination revealed variations in chemical component contents among batches. The established method is speciffcity, accuracy, and feasibility. When combined with chemical pattern recognition, it can be effectively used for quality control of Shufu plaster.
  • Paper
    Determination of Sixteen Elemental Impurities in Zinc Gluconate Oral Solution by ICP-MS
    FENG Xialan, YANG Mei, ZHANG Rongqin, CHEN Hong, ZHAO Xinqing
    2025, 56(10): 1316. https://doi.org/10.16522/j.cnki.cjph.2025.10.010
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    An inductively coupled plasma mass spectrometry(ICP-MS) method was established for the simultaneous determination of sixteen elemental impurities(B, Mg, Al, V, Cr, Mn, Fe, Co, Ni, Cu, As, Cd, Sb, Ba, Hg, Pb) in zinc gluconate oral solution(1), and the reasons for content differences were analyzed. The samples were diluted and analyzed by collision mode(kinetic energy discrimination), with Sc, Ge, In, Bi as the internal standard elements.The results showed that all 16 elements exhibited good linearity within their concentration range with detection limit of 0.001 - 0.177 μg/mL. The spiking recoveries(n=9) ranged from 91.4％ to 104.8％ , with RSDs all below 9.5％ . All sixteen elemental impurities were detected, and safety evaluation confirmed that their maximum daily intake were below the permitted daily exposure limits. The analysis showed that the elemental content difference in 1 was mainly caused by batchto-batch quality variations of the active pharmaceutical ingredients. The method is simple, accurate and sensitive, which can be used for the content determination and source analysis of element impurities, and drug packaging material screening for 1.
    • Proficiency Testing of Enviromental Test in Pharmaceutical Production Cleanroom
  • Proficiency Testing of Enviromental Test in Pharmaceutical Production Cleanroom
    Proffciency Test for Airffow Detection of Clean Environment of 54 Inspection and Testing Institutes in China
    ZHAO Yanjun, AI Lun, XIE Langui, TIAN Lin, WU Hui, ZHAO Xia
    2025, 56(10): 1322. https://doi.org/10.16522/j.cnki.cjph.2025.10.011
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  • Proficiency Testing of Enviromental Test in Pharmaceutical Production Cleanroom
    Proffciency Test for the High Efffciency Filter Integrity Testing of Class Ⅱ Biological Safety Cabinets
    ZHAO Yanjun, AI Lun, XIE Langui, TIAN Lin, WU Hui, ZHAO Xia
    2025, 56(10): 1327. https://doi.org/10.16522/j.cnki.cjph.2025.10.012
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    • Pharmaceutical Management & Information
  • Pharmaceutical Management & Information
    Proficiency Test for Inflow Velocity Testing of a Class Ⅱ Biological Safety Cabinet
    ZHAO Yanjun, AI Lun, XIE Langui, TIAN Lin, WU Hui, ZHAO Xia
    2025, 56(10): 1331. https://doi.org/10.16522/j.cnki.cjph.2025.10.013
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  • Pharmaceutical Management & Information
    Key Points of Non-clinical Research and Evaluation of Nasal Sprays
    LIAO Ping , FENG Zhen , CAO Meng , CHEN Yifei , TANG Liming
    2025, 56(10): 1336. https://doi.org/10.16522/j.cnki.cjph.2025.10.014
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  • Pharmaceutical Management & Information
    Key Points of Clinical Research and Evaluation of Nasal Sprays
    ZHANG Wanjing , LIAO Ping, ZHAN Huizhong , ZHANG Jing
    2025, 56(10): 1343. https://doi.org/10.16522/j.cnki.cjph.2025.10.015
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  • Pharmaceutical Management & Information
    Thoughts on the Application of MES in Biopharmaceuticals and Compliance Inspections in the Context of Smart Supervision
    MA Yinlin , KONG Liya , LEI Dong , HE Xuefeng , HU Min
    2025, 56(10): 1349. https://doi.org/10.16522/j.cnki.cjph.2025.10.016
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  • Pharmaceutical Management & Information
    Patent Analysis for Erdafftinib
    WEI Bei , XIE Xiaoni
    2025, 56(10): 1356. https://doi.org/10.16522/j.cnki.cjph.2025.10.017
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  • Pharmaceutical Management & Information
    Analysis of Patent Declarations and Patent Registrations of the Early Resolution Mechanism for Drug Patent Disputes in China
    SONG Jiemei, WANG Huaping, XU Dan
    2025, 56(10): 1365. https://doi.org/10.16522/j.cnki.cjph.2025.10.018
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