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  • Lihua LU, Yizhuo CHANG, Lixin WANG, Xiaomeng CHONG, Hui XU, Baoming NING
    Chinese Pharmaceutical Journal. 2024, 59(23): 2258-2265.

    OBJECTIVE To establish an evaluation method for the release of mupirocin ointment in vitro, according to the quality research of ointment preparations at home and abroad and the technical guidelines for generic drugs. METHODS The diffusion cell method was adopted, the release membrane was polyethersulfone membrane, the receiving medium was sodium dihydrogen phosphate buffer solution with pH 7.4, the rotation speed was 600 r·min-1, and the sample size was 300 mg. The concentration of mupirocin in the receiving solution at different time points was determined by HPLC method, and the cumulative release and release rate were calculated. The particle size morphology and particle size distribution of mupirocin ointment from different manufacturers were determined by particle size analyzer. The viscosity of preparations from different manufacturers was determined by rheometer. RESULTS The determination method for the release of mupirocin ointment in vitro was established, and the precision, durability and discrimination of this method were good, and the consistency evaluation was made for preparations from different manufacturers. There were great differences in particle size distribution and viscosity between different manufacturers. CONCLUSION The differences in particle size distribution between different manufacturers reflect the differences in preparation production process, and the differences in viscosity reflect the differences in preparation prescription, both of them can affect the release rate of mupirocin ointment in vitro.

  • Minmin LIU, Jiazhe HU, Jiawen HE, Qiao CHEN, Jiaxin WEN, Hua LI, Qunyue WU
    Chinese Pharmaceutical Journal. 2024, 59(23): 2266-2271.

    OBJECTIVE To provide reference and suggestions for the quality control of this variety, evaluate the quality of xiaojianzhong preparations and preparations analyze the existing problems based on the national drug sampling. METHODS A total of 160 batches of samples were tested according to the statutory standard. In the exploratory study, ochratoxin A and zearalenone residues were detected by liquid chromatography-tandem mass spectrometry; paeoniflorin sulfite in xiaojianzhong preparation was detected by ultra performance liquid chromatography-tandem high resolution mass spectrometry; cinnamaldehyde was determined by high performance liquid chromatography; the overall quality of Xiaojianzhong preparation was evaluated by fingerprint analysis. The pH value of the mixture was investigated. RESULTS The qualified rate of 160 batches of samples was 100% according to statutory standard. Exploratory studies showed that ochratoxin A or zearalenone was detected in 33.1% of the samples, and paeoniflorin sulfite was detected in 83.5% of the samples.The pH value of 9% mixture was beyond the range of benzoic acid inhibitory effect. Cinnamaldehyde in 95.4% of the samples was below the proposed limit. Fingerprint analysis showed that the similarity of 14.6% of samples was lower than the proposed limit. CONCLUSION It is suggested to unify the quality control items of the four dosage forms, increase the pH limit, monitor the quality of the raw materials of licorice and dextrin, standardize the use of cerealose, and strengthen the system specification for the development of ancient classic prescriptions.

  • Xueting LIU, Haofeng LÜ, Lina ZENG, Xiaojuan DU, Yifen YE, Ziyu GUO, Yaoxuan XIE, Shuhong WANG, Chang SU
    Chinese Pharmaceutical Journal. 2024, 59(23): 2272-2277.

    OBJECTIVE To establish a method for determining the transformation of pesticide residues in honeysuckle and the development of limit standards in accordance with the requirements of GB 2763-2021 Food Safety Standards for Maximum Residue Limits of Pesticides in Food and the Chinese Pharmacopoeia. METHODS According to “the Principle of Conversion of Limit Standards of Traditional Chinese Medicine in <GB 2763-2021 National food safety standard-Maximum residue limits for pesticides in food>”, using a risk assessment model that is in line with the characteristics of traditional Chinese medicine, the maximum residual limit value of the pesticide to be transformed from honeysuckle was evaluated. Using acetonitrile as the extraction solvent and direct extraction as the pre-treatment method. LC-MS/MS methods were used to screen three commonly used pesticides in 57 batches of honeysuckle. RESULTS Combined with the relevant requirements of GB 2763-2021 and the Chinese Pharmacopoeia,the maximum residue limit regulations for three pesticides in honeysuckle were proposed to be formulated through sample determination,namely imidacloprid (1 mg·kg-1), avermectin benzoate (0.1 mg·kg-1),and imidacloprid (15 mg·kg-1). CONCLUSION This study screened three commonly used pesticides in 57 batches of honeysuckle and establishes a method and limit standard for the determination of conversion pesticide residues in combination with GB 2763-2021, which has guiding and important significance for further research on the standardization, quality standards, and market circulation supervision of pesticide use during the planting process.

  • Xiaoming GAO, Kangwei XU, Xu LU, Zhizhong QIAO, Yaru QUAN, Changgui LI, Xinhua XIANG
    Chinese Pharmaceutical Journal. 2024, 59(23): 2288-2292.

    OBJECTIVE To evaluate the testing capability of the vaccine quality control laboratories and vaccine manufacturer laboratories which participated in the proficiency testing of pH, osmotic pressure molar concentration and aluminum content of inactivated COVID-19 vaccine. METHODS Samples of inactivated COVID-19 vaccine were tested for uniformity and stability by F-test and t-test, and then distributed to participating laboratories by cold chain transportation. The abilities of the participating laboratories for determination of pH, osmotic pressure molar concentration, and aluminum content were evaluated by Z ratio. RESULTS A total of 30 laboratories across the country participated in this proficiency testing, and the pH and aluminum content assessment results were all satisfactory, while the osmotic pressure molar concentration results of two laboratories were unsatisfactory. After participating in measurement audits, satisfactory results were obtained. CONCLUSION The provincial vaccine quality control laboratories, and vaccine production enterprises participating in this proficiency testing have good testing capabilities and quality control levels.

  • Furui HUANG, Chunlei MIAO, Kun HOU, Benben ZHU, Yaodong PING, Shikui WU
    Chinese Pharmaceutical Journal. 2024, 59(23): 2293-2298.

    OBJECTIVE To summarize the research progress and beneficiary population of immune re challenge in the treatment of non-small cell lung cancer (NSCLC), and provide reference for the treatment of NSCLC in clinical practice. METHODS Using keywords such as “non- small cell lung cancer”, “immune checkpoint inhibitor”, “rechallenge”, etc., a combination of topic words and free words was used to search relevant literature from PubMed、Cochrane Library、embase、self-built databases such as China National Knowledge Infrastructure until February 1, 2024. RESULTS A total of 526 relevant literature were retrieved, with over 40 valid articles. Among them, there are 6 systematic reviews/Meta analyses on NSCLC rechallenge, 5 clinical studies, and most of the rest are retrospective real-world studies. CONCLUSION The effectiveness and controllable irAEs of immune rechallenge therapy for NSCLC were analyzed, and it was preliminarily believed that patients with high programmed cell death ligand 1 (PD-L1) expression (TPS ≥ 50%), good performance status (PS) score in the Eastern Cooperative Oncology Group (ECOG) in the United States (ECOG-PS≤1) and longer initial immunotherapy time were more likely to benefit from ICIs rechallenge.

  • Hui LU, Ying YU, Jianya LING, Xiaorui CHENG
    Chinese Pharmaceutical Journal. 2024, 59(22): 2099-2106.

    The discovery of drug targets is crucial for understanding the mechanism of drug action and facilitating the development of novel drug therapeutics. Microscale thermophoresis (MST), renowned for its minimal sample consumption, rapid detection speed, high sensitivity, and the absence of the need for protein immobilization, has emerged as a pivotal tool in drug target research. This article outlines the strategies for identifying drug targets, with a focus on elucidating the principles of MST and its application in drug target discovery. Furthermore, it summarizes the promising prospects of MST in this field. The applications of MST are found in both forward and reverse strategies for target discovery, enabling the identification of target proteins for compounds, single herbal ingredients, and compound prescriptions, as well as facilitating drug screening. Additionally, the integration of MST with other molecular interaction techniques, such as surface plasmon resonance (SPR), provides a potent arsenal for studying the interactions between drugs and their targets. Despite certain limitations, MST holds immense potential for application in the realms of novel drug development and drug mechanism research.

  • Xiaomin HAN, Mingyue YIN, Jie SONG, Tao ZHUANG
    Chinese Pharmaceutical Journal. 2024, 59(22): 2107-2115.

    Pain management remains as a global public health issue, with 20% of the adult population worldwide impacted and many patients still suffer from unrelieved or undertreated pain. Classic opioids exert antinociceptive effects by activating μ opioid receptor (MOR), but they are associated with many side effects (including respiratory depression, addiction, and constipation) which have aggravated the ongoing and escalating opioid crisis in worldwide. Therefore, there is an urgent need for the development of novel analgesics free of MOR-mediated unwanted adverse effects. Multi-target therapeutics target two or more related targets in a disease network system simultaneously, which can potentially provide greater efficacy and improve treatment outcomes compared with single-target therapies. Due to the key role of MOR in regulating pain signal transmission, MOR-based multi-target ligands have been accepted as one of the mainstream strategies for designing new potent analgesics without side effects. In this review, recent advances in multitarget-directed drugs toward MOR are summarized, which may provide references for the development of potent and safer analgesics.

  • Zhuo KONG, Demeng SUN, Yanmei JIANG, Yun HU
    Chinese Pharmaceutical Journal. 2024, 59(22): 2116-2125.

    OBJECTIVE To design, synthesize and evaluate a series of 3', 4'-ethylendioxy chalcone derivatives as monoamine oxidase B (MAO-B) inhibitors, and summarize the structure-activity relationship (SAR). METHODS The targeted compounds were synthesized via Claisen-Schmidt condensation reaction starting from 6-acetyl-1, 4-benzodioxan and corresponding benzaldehydes. The inhibition of these compounds on human MAO-B (hMAO-B) was determined, and the inhibiting selectivity, dynamics and reversibility were investigated as well. The binding mode between active compounds and hMAO-B was revealed by molecular docking study. Additionally, the inhibitory effect of active compounds on the proliferation of BV2 cell line was determined by MTT assay. RESULTS Sixteen targeted compounds were successfully prepared. Most compounds showed good inhibitory effects on hMAO-B. Representative compounds 9 and 13 exhibited IC50 values of 0.021 and 0.042 μmol·L-1, respectively, which showed high inhibiting selectivity towards hMAO-B. Both compounds acted as competitive and reversible hMAO-B inhibitors. The main interactions between active compounds and hMAO-B were hydrophobic interaction and hydrogen bond. The most active compound 9 exhibited low cytotoxicity in BV2 cells. CONCLUSION This class of 3', 4'-ethylendioxy chalcone derivatives represent potential novel inhibitors of hMAO-B, and compound 9 could be further investigated as a potent lead for future studies.

  • Yuzhuo ZHU, Fei XUE, Yang JIAO, Weiliang CUI, Juan CHEN, Bing WANG, Yongqiang LIN
    Chinese Pharmaceutical Journal. 2024, 59(22): 2126-2131.

    OBJECTIVE To accurately distinguish deer-derived medicinal materials from four different position: Cervi Cornu Pantotrichum, Cervi Cornu, Cervi Cornu Degelatinatum and Deer hide. METHODS The extraction efficiency of two extraction solvent systems for four different kinds of deer-derived medicinal materials was compared, and the optimum enzymatic hydrolysis conditions of the samples were optimized to form an efficient and simple sample pretreatment process. A specific analysis method, combining chemical markers and characteristic polypeptides was established to identify four different position of deer-derived medicinal materials by using liquid chromatography-triple quadrupole mass spectrometry and mass spectrometry multi-reaction monitoring technology (MRM). And methodological experiments were conducted as part of this analysis method. RESULTS The optimized sample pretreatment method with high extraction efficiency and good enzymatic effect was successfully applied, and the corresponding characteristic polypeptide ion pairs were successfully detected in 24 batches of samples. CONCLUSION The distinction and identification method with high-level specificity, sensitivity and robustness of deer-derived medicinal materials were established. The innovative analysis method can be effectively used to evaluate the quality of deer-derived medicinal materials, which provides a reference for ensuring and improving the quality of deer-derived medicinal materials.

  • Xintong YU, Qian CAO, Lanlan ZHANG, Kaidong WANG, Zaoshu CHEN, Ling PAN, Zheng ZHANG
    Chinese Pharmaceutical Journal. 2024, 59(22): 2132-2139.

    OBJECTIVE To determine the antioxidant activities of Gossampim Flos waterextracts,establish UPLC fingerprints and study the spectral effect relationship. METHODS Based on the scavenging rates of 2, 2-diazo-di (3-ethyl-benzothiazolin-6-sulfonic acid) diamiammonium salt (ABTS) and 1, 1-diphenyl-2-picrohydrazyl radical (DPPH), the fingerprint of different parts (petal, calyx and stamen) of 12 batches of Gossampim Flos were established by UPLC method, and similarity analysis were carried out. Grey correlation analysis (GRA), Spearman analysis, stepwise regression analysis and partial least squares regression(PLSR) analysis were used to study the relationship between antioxidant spectrum effect. RESULTS Eight chromatographic peaks were identified by fingerprint identification of water extracts from different parts of 12 batches of Gossampim Flos. Mangiferin, quercetin, rutin, vitexin and other compounds were the main active components of Gossampim Flos and its different parts for antioxidant activities. CONCLUSION The antioxidant activity of Gossampim Flos and its different parts are the result of the combined effect of multiple components. This study can provide a comprehensive reference for the basis and quality control of antioxidant active substances of Gossampim Flos and its different parts.