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  • SU Feng, XIONG Feng, CAO Junru, CHU Xiaoqin, HE Guangwei, YIN Lifang
    Chinese Pharmaceutical Journal. 2024, 59(4): 285-295.

    In recent years, central nervous system (CNS) diseases have become serious threat to human life and health. The existence of the blood-brain barrier (BBB), which prevents most drugs from entering the brain, has made the treatment of CNS diseases a major problem in the field of medicine and pharmacy. The advent of nanotechnology has given drugs the potential to penetrate the blood-brain barrier, and the rapid development of siRNA drugs has brought light to patients with CNS disorders. However, the delivery of nanocarriers to the brain encounters many obstacles and the conditions that can be met for brain delivery as siRNA nanocarriers are also very demanding. This paper therefore reviews the research progress and the advantages and disadvantages of lipokinase nanoparticles, chitosan nanoparticles, polyethyleneimine nanoparticles, dendrimer nanoparticles, nanogels, nanomicelles, nanoemulsions, exosomes, cells, and siRNA adducts as siRNA brain delivery systems, with a view to exploring a suitable siRNA nanodelivery system for blood-brain barrier penetration.

  • HE Fengyan, NIE Lixing, ZHENG Xiaowei, WANG Qi, GAO Yan, GUO Rixin, GUO Lin, DAI Zhong, MA Shuangcheng
    Chinese Pharmaceutical Journal. 2024, 59(4): 346-352.

    OBJECTIVE To analyze the quality status of Xinnaojing Tablets by multi-index comprehensive evaluation. METHODS Samples were tested according to the statutory standards. Several new methods were established and adopted for multi-index comprehensive evaluation. RESULTS All samples were qualified in statutory tests. But quality defects were found in some samples by multi-index comprehensive exploratory studies. The main problems involved poor quality of raw materials, low feeding, or lack of process control. CONCLUSION Multi-index comprehensive evaluation is more capable of evaluating the real quality status of Xinnaojing Tables. To ensure the safety and effectiveness of the midication, manufacturers should pay attention to the quality of raw materials and process control, especially on Borneolum Syntheticum, Aucklandiae Radix, and Uncariae Ramulus Cum Uncis.

  • XIA Tianli, WANG Yan, WANG Di, ZHAO Deping, SU Ting, ZHAO Jihui, LEI Xia, ZHANG Ning
    Chinese Pharmaceutical Journal. 2024, 59(4): 330-337.

    OBJECTIVE To study the components of Rhizoma Anemarrhenae-Cortex Phellodendri Chinesis (RA-PC) herb-pair absorbed into blood in normal rabbits. METHODS Rabbits were fed with the decoction of RA-PC herb pair (4.5 g·kg-1) once a day for 7 days, then blood samples were taken. High-performance liquid chromatography-quadrupole-electrostatic field orbital trap (UPLC-Q-Exactive Orbitrap-MS) technique was applied for the analysis, and fragments were split in both positive and negative ion modes. The compositions into blood were determined according to retention time, accurate relative molecular mass, and secondary mass spectra. RESULTS A total of 54 components were identified in the drug-containing serum of rabbits, including 46 prototype components, which were alkaloids, flavonoids, saponins, glycosides, phenolic acids, phenylpropanoids, lactones, and phenolic derivatives. The nine metabolites were derived from berberine, jatrorrhizine, berberrubine, and mangiferin, respectively. CONCLUSION RA-PC contains 46 chemical components that can enter blood of normal rabbits, and may also contains four chemical components which are metabolized into nine metabolites.

  • ZHANG Fan, LU Boyu, BAI Xue, ZOU Yuzhen, ZHANG Xinyue, ZHAO Bin, MEI Dan
    Chinese Pharmaceutical Journal. 2024, 59(3): 281-284.

    OBJECTIVE To explore an evaluation method of sterile operation in pharmacy intravenous admixture services(PIVAS). OBJECTIVE The US intravenous quality assurance(IVQA) media fill test kit was used to verify the aseptic operation of the mixed dispensing personnel in our hospital, and the feasibility of applying the media fill test in the PIVAS was preliminarily explored. RESULTS The media fill test was easy to operate without harsh culture conditions and testing equipment. The test results were different under two different mixing conditions, which can verify the operation of personnel. CONCLUSION The media fill test is applicable to the quality control of personnel in sterile dispensing operations.

  • YAN Qinying, WANG Yan, WAN Aiqun, SHEN Shulin, WENG Jiaqi, FANG Min, YANG Gensheng
    Chinese Pharmaceutical Journal. 2024, 59(3): 193-199.

    In recent years, transdermal delivery has proven to be one of the most favorable methods among novel drug delivery systems due to avoiding the gastrointestinal tract and reducing systemic side effects. Skin is one of the most immunologically active organs due to the presence of immune cells, such as Langerhans cells(LCs), dermal dendritic cells(dDCs), and T cells. Unique immune properties of the skin offer excellent opportunities for transdermal treatment of autoimmune diseases(ADs). This review highlights the pathogenic mechanism of ADs caused by various reasons such as loss of immune self-tolerance and abnormal autoreactive T cells, and the advantages of transdermal drug delivery for the treatment of ADs, as well as expounds on the application of transdermal drug delivery systems(TDDS) in the treatment of several typical ADs. TDDS will provide new ideas and methods for the treatment and research of autoimmune diseases.

  • ZHAO Zhuang, FAN Qiang, SU Wu, CHEN Lerong, LI Hua, GE Shuai, KONG Yu, LONG Jiangang
    Chinese Pharmaceutical Journal. 2024, 59(3): 210-219.

    Cell membrane chromatography is a bioaffinity chromatography method which has been developing rapidly in recent years, where the carriers coated with receptor-containing biomembrane are packed to stationary phase and the bioaffinity between compound and membrane receptor presents in chromatography process. This method has the advantages of biomimetic, high efficiency and low cost, and has been widely used in drug screening and identifying the affinity between membrane receptor and candidate ligand. Mitochondria, a crucial functional intracellular membrane system, with various drug targets residing in membrane. Recently, significant research advancements have been made in mitochondrial membrane chromatography technology. In this paper, the recent progresses and applications of cell membrane chromatography and mitochondria membrane chromatography are reviewed.

  • DING Hao
    Chinese Pharmaceutical Journal. 2024, 59(3): 270-274.

    OBJECTIVE To establish a method for the determination of 32 elements in COVID-19 vaccine. OBJECTIVE The 32 elements were determined by inductively coupled plasma optical emission spectrometer(ICP-OES) through semi-quantitative screening and quantitative detection, and the specificity, linearity, limit of quantification, detection limit and recovery rate of the ICP-OES method were investigated to evaluate the feasibility of the method for the detection of trace elements in vaccines. RESULTS The linear relationship of each element was good within the detection mass concentration range, and the recoveries of element added were 94.06%-115.50%. When applied to the detection of the samples at each accelerated placement point, except for the trace contents of B and Si elements, which did not increase significantly after long-term placement, the contents of other elements were far less than the prescribed limits. CONCLUSION The ICP-OES method is established. And the method has good specificity, reliable results, simple and rapid, and is suitable for the determination of 32 elements in COVID-19 vaccine.

  • XIE Yule, YANG Yijing, ZHAO Shengxian, HU Hongyu
    Chinese Pharmaceutical Journal. 2024, 59(3): 227-234.

    OBJECTIVE To design and synthesize N-substituted methylene-3-(4-(pyridin-3-yl)pyrimidin-2-yl)amino)benzohydrazide derivatives, and evaluate their anticancer activities. OBJECTIVE Using 3-aminobenzoic acid ethyl ester as the starting reagent, a series of target compounds 4a-4p were synthesized in a 4-step reaction, and all of the target compounds were structurally characterized by 1H-NMR, 13C-NMR and HRMS. MTT assay was used to detect the inhibitory effect of synthetic compounds on breast cancer cells. RESULTS It's showed that the target compounds had certain inhibitory activity on the growth of breast cancer cells, among which compound 4e was the best one, showing obvious inhibitory effect on breast cancer cells. The IC50 value of breast cancer cell line MCF-7 was (2.30±0.34)μmol·L-1, and the toxicity of 4e to normal mammary epithelial cells was low(IC50>100 μmol·L-1). Thus, 4e is better than the positive drug cisplatin. In addition, 4e could significantly up-regulate the protein expression level of Nur77 and induce the S-phase arrest of MCF-7. CONCLUSION This series of compounds have good anti-cancer activity and are of interest for further study.

  • YAO Mingli, GAO Dingjia, ZHANG Jie, LI Shan, WU Song, SI Xinxin, XIA Jie
    Chinese Pharmaceutical Journal. 2024, 59(3): 249-255.

    OBJECTIVE To build a text-convolutional neural network(Text-CNN)-based prediction model for anti-Staphylococcus aureus(S.aureus) activity and identify anti-S.aureus hits by virtual screening. OBJECTIVE A dataset containing 26327 compounds annotated with S.aureus activity data was collected and curated from the ChEMBL database. Ten pairs of training and test sets were generated by random partition for 10 times and then 10 models were built using the Text-CNN algorithm. The best-performing model was determined by model evaluation and further studied by Y-randomization test and applicability domain analysis. Following that, the best-performing model was used to virtually screen the in-house chemical library, by which the potential antibacterial agents were determined. The micro-broth dilution method was used to test anti-S.aureus activity of the potential hits. RESULTS The machine-learning model(named Text-CNN3) performed well in classification. Evaluated on the test set, its Mathews correlation coefficient was 0.573 and the area under the ROC curve was 0.881. With this model for virtual screening as well as antibacterial screening, compounds Y5 and Y7 were identified as antibacterial compounds, with minimum inhibitory concentrations(MIC) of 8 and 4 μg·mL-1, respectively. CONCLUSION The Text-CNN3 model in this study is effective to identify anti-S.aureus compounds, while the antibacterial hits Y5 and Y7 are worthy of further study.

  • GUO Haonan, LI Huahua, JIANG Miaomiao, MI Zhuoxin, ZHENG Qi, ZHANG Peng
    Chinese Pharmaceutical Journal. 2024, 59(3): 235-240.

    OBJECTIVE To study the chemical constituents of Pinellia ternata(Thunb).Breit.. OBJECTIVE The 60% ethanol extract of Pinellia ternata(Thunb). Breit. was isolated and purified by silica, MCI, ODS and preparative HPLC, and the structures of obtained compounds were identified by physico-chemical properties and MS、NMR data. RESULTS The compound are kaempferol-3-O-β-D-rutinoside(1), inosine(2), lactariolide I(3), (2E,4E,1'S,2'R,4'S,6'R)-dihydrophaseic acid(4), tryptophan(5), 1-oleoyl-3-O-β-D-galactopyranosyl-sn-glycerol(6), 6'-O-linoleylsucrose(7), 6'-O-palmitoylsucrose(8), gingerglycolipid C(9), (2S)-1-O-6'-O-(α-D-galactopyranosyl)-β-D-galactopyranosyl-3-O-palmitoyl glyceride(10), 1-O-hexadecanoyl-3-O-β-D-galatopyranosylglycerol(11), tianshic acid(12), 4-(2-hydroxyethyl)phenol(13), phenylpropionic acid(14), 3-phenyllactic acid(15), trans-cinnamic acid(16). CONCLUSION Compound 1, 2, 3, 4, 6-13, 15-16 are firstly isolated from the genus Pinellia.