Home Latest Articles
Latest Articles
  • Xiaoying HOU, Fan GAO, Lidong DU, Ruiqiong WANG, Guotai WU
    Chinese Pharmaceutical Journal. 2024, 59(24): 2299-2305.

    Ligustilide (LIG) is a phthalide compound found in Angelica sinensis (Oliv.) Diels and Ligusticum chuanxiong Hort, which has a wide range of pharmacological activities in clinical practice, including anti-inflammatory, antioxidant, analgesic, anti-tumor, neuroprotective, and vascular protective effects. However, LIG has poor stability and is easily affected by factors such as temperature, light, oxygen, pH value, and solvent type, leading to conformational changes. In addition, the low water solubility and low bioavailability of LIG limit its development and application in new drugs. The article reviews the research progress on natural sources, structural characteristics and structural modifications, degradation and transformation mechanisms, main degradation influencing factors, stabilization methods and bioactivity of LIG in recent years, in order to provide reference for the further development and applications of LIG.

  • Tongzhi TAI, Juan TANG, Jiazhen HU, Chenggang HU
    Chinese Pharmaceutical Journal. 2024, 59(24): 2322-2329.

    OBJECTIVE To use fingerprint combined with hierarchical clustering analysis (HCA), principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA) to identify chemical patterns. METHODS Chrom Core 120 C18 (4.6 mm×250 mm, 5 μm) chromatographic column, 0.1% phosphoric acid aqueous solution (A)-acetonitrile (B) as mobile phase for gradient elution, volume flow rate of 0.8 mL·min-1, detection wavelength of 280 nm, column temperature of 30 ℃ injection volume of 10 μL, HPLC method was used to establish the fingerprints of 30 batches of medicinal herbs from 12 origins, and similarity analysis, HCA, PCA and PLS-DA were used and other chemical pattern recognition technologies were used to screen and quantitatively analyze the differentially characteristic components. RESULTS The fingerprinting method established by the established fingerprint method met the methodological requirements, and 17 common peaks were indexed by HPLC fingerprint of 30 batches of Pterospermum chinensis, with a similarity of 0.863-0.975. HCA, PCA and PLS-DA were used to distinguish the PH from different origins, and combined with the previous experiments, three components, protocatechuic acid, proanthocyanidins B2 and epicatechins, were comprehensively analyzed and screened as the active ingredients of the PH, and the content ranges were 0.103-1.676, 0.141-5.556 and 0.144-3.381 mg·g-1, respectively. CONCLUSION The fingerprint of the medicinal materials and the determination of the contents of the three active ingredients established in this study are stable, reliable and reproducible, which provides a certain scientific basis for evaluating the quality of Pterospermum heterophyllum.

  • Jiangwei LÜ, Jingjing JIANG, Wei CHEN, Xueying ZHAO, Wenjun ZHANG, Youpeng QU
    Chinese Pharmaceutical Journal. 2024, 59(24): 2343-2353.

    OBJECTIVE In order to improve the solubility and dissolution of the insoluble drug fenofibrate (FNB) optimize, the prescription of the self-microemulsifying drug delivery system (SMEDDS) was optimized and its quality was evaluated. METHODS The prescription composition and proportion range of SMEDDS were determined by the solubility experiment, compatibility test and pseudoternary phase diagram. Star point design-response surface methodology was used to further optimize the formulation of fenofibrate self-microemulsifying drug delivery system (FNB-SMEDDS) by using solubility, average particle size and polydispersity index (PDI) as evaluation indicators. The physical and chemical properties, and preliminary stability of FNB-SMEDDS were evaluated. RESULTS The optimal prescription of FNB-SMEDDS was ethyl oleate (EO) 22.86% as oil phase, polyoxyethylene (40) hydrogenated castor oil (cremophor RH40) 51.07% as surfactant, diethylene glycol monoethyl ether (transcutol HP) 26.07% as co-surfactant. The obtained FNB-SMEDDS was uniform and transparent. The FNB-SMEDDS was self-emulsified in water with average particle size of (39.29±0.45) nm, PDI of (0.11±0.01), Zeta potential of (-7.7±0.9) mV, drug loading rate of 15 mg·g-1, encapsulation rate of (95.11±0.26)%, and emulsification time of (56.03±1.65) s. Stability experiments showed that after being stored at room temperature in the dark for 30 days, there was no significant change in its index components and appearance properties, indicating good stability. Compared with FNB API, FNB-SMEDDS significantly improved the in vitro dissolution of FNB. The cumulative release rates in water, pH 1.2 hydrochloric acid solution and pH 6.8 phosphate buffer solution for 120 min were (97.68±0.61)%, (92.23±4.07)% and (93.65±2.25)%, respectively. CONCLUSION FNB-SMEDDS has good appearance, high emulsification efficiency. It can significantly improve in vitro dissolution of the drug, and is expected to improve the in vivo bioavailability of FNB.

  • Xiaojun LI, Ting WANG, Wenjun FU, Chuanlan SANG
    Chinese Pharmaceutical Journal. 2024, 59(24): 2330-2336.

    OBJECTIVE To explore the effect and possible mechanism of Xiaoyao San in chronic stress depression mice. METHODS The antidepressant effects of Xiaoyao San (XYS, low-dose 1.40 g·kg-1, high-dose 2.79 g·kg-1), mifepristone (1.73 mg·kg-1) and fluoxetine (2.9 mg·kg-1) were assessed in chronic unpredictable mild stress (CUMS)-exposed male mice. After the intervention, the depressive-like behaviors of mice were evaluated by open-field test (OFT), sucrose preference test (SPT), forced swimming test (FST), and tail suspension test (TST). Hematoxylin eosin (HE) staining experiment was used to observe the pathological changes of the hippocampal tissue. Enzyme linked immunosorbent assay (ELISA) was used to detect the level of corticosterone (CORT) in serum of mice. Western blot (WB) experiment was used to detect the protein expression of nuclear and cytoplasmic glucocorticoid receptor (GR), phosphorylation GR, FK506 binding protein 51 (FKBP51), brain-derived neurotrophic factor (BDNF) in hippocampal tissue. RESULTS Compared with the control group, mice in the model group showed it was significantly deteriorated behavioral performance (P<0.01) and pathological changes in the hippocampal tissue, indicating the successful establishment of the CUMS model. After XYS treatment, the behavioral performance (P<0.05) of mice and pathologic manifestation of the hippocampal tissue were significantly improved, and the serum CORT level was significantly reduced (P<0.05). In addition, WB examination demonstrated that XYS treatment significantly increased the expression of GR, BDNF, pGR-S211, and nuclear GR in hippocampal tissue (P<0.05), while significantly decreased the expression of FKBP51 and pGR-S226 (P<0.05). CONCLUSION XYS may exert its anti-depressant effects by regulating the expression of FKBP51, phosphorylation GR and BDNF, improving the function of GR and regulating the homeostasis of the hypothalamic-pituitary-adrenal (HPA) axis.

  • 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.

  • 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.

  • Meixiu LUO, Zhi PAN, Lianyun DU, Lu TANG, Yinghang WANG
    Chinese Pharmaceutical Journal. 2024, 59(23): 2241-2248.

    OBJECTIVE To investigate the mechanism by which Danggui Buxue Decoction (DBD) regulates oxidative stress in rats with rheumatoid arthritis based on phosphatidylinositol 3-kinase (PI3K)/protein kinase B(Akt)/nuclear factor E2-related factor 2(Nrf2) signaling pathway. METHODS Forty-eight Wistar rats were randomly divided into 6 groups [normal group, model group, tripterygium glycosides tablets group(9.45 mg·kg-1), DBD low dose (3.75 g·kg-1), medium dose(7.5 g·kg-1) and high dose group(15 g·kg-1)]. In addition to the normal group, the other groups were constructed collagen-induced arthritis (CIA) rat model, and given the corresponding drug treatment for 28 days. During the period, the body weight of the rats, the degree of ankle swelling, and the arthritis score were recorded regularly. The levels of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), catalase (CAT) and malondialdehyde (MDA) in serum of rats were determined by ELISA. The spleen index and thymus index were calculated. HE staining and safranin O-fast green staining were used to observe the pathological morphology of synovial membrane of knee joint in rats. The expression of PI3K, AKT, Nrf2 and HO-1 mRNA in synovial tissue was determined by qPCR. The expression of p-PI3K/PI3K, p-Akt/Akt, Nrf2 and HO-1 protein in synovial tissue was determined by Western blot. RESULTS Compared with the normal group, the body weight of the rats in the model group was lower (P<0.05), and the bilateral hind limbs were obviously red and swollen or even deformed. Compared with the model group, the body weight of rats in each administration group increased gently (P<0.05), the swelling degree of bilateral hind limbs was significantly reduced (P<0.05), and the arthritis score was significantly decreased (P<0.05). The level of MDA in joint tissue decreased (P<0.05), and the levels of GSH-Px, CAT and SOD increased (P<0.05). The expression of PI3K, Akt, Nrf2 and HO-1 mRNA in PI3K/Akt/Nrf2 pathway was increased (P<0.05). The ratio of p-PI3K/PI3K, p-Akt/Akt and the expression of Nrf2 and HO-1 protein were significantly increased (P<0.05). CONCLUSION DBD may inhibit the level of oxidative stress, attenuate the oxidative damage of synovial tissues and improve the pathological changes of synovium by regulating the PI3K/Akt/Nrf2 pathway in CIA rats, thus exerting an anti-RA effect.

  • 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.

  • Pan WANG, Fusong LIU, Delin ZHANG, Jie PENG, Sha LIU, Faming WU
    Chinese Pharmaceutical Journal. 2024, 59(23): 2226-2240.

    OBJECTIVE To provide reference for reasonable protection, development and utilization of Codonopsis pilosula germplasm resources. METHODS Variation analysis, correlation analysis, principal components analysis, cluster analysis, piecewise linear regression analysis, and stepwise multiple regression analysis were conducted on the main agronomic traits and representative components of 106 Codonopsis pilosula germplasm resources. RESULTS The genetic variability of the 106 Codonopsis pilosula germplasm resources was rich, with the coefficients of variation of the 106 Codonopsis pilosula trait indexes ranging from 9.331% to 86.948%, among which the coefficient of variation of the degree of variability of atractylenolide Ⅲ was the highest, 86.948%; the indexes of genetic diversity ranged from 1.587 to 2.039, with syringin 1.587, and root length, number of branches, and Codonopsis polysaccharide were 2.027,2.039 and 2.032, respectively. Correlation analysis showed that most of the 14 traits had significant or highly significant relationships with each other. The seven principal component factors available for principal component analysis could explain most of the information of the 14 indicators, with eigenvalues of 4.172, 2.427, 1.646, 1.196, 0.943, 0.872 and 0.75, respectively, and the cumulative contribution rate reached 85.760%. Using the DTOPSIS method to score the germplasm resources of Codonopsis pilosula, the top 15 were No.13, No.20, No.21, No.18, No.73, No.77, No.90, No.78, No.88, No.72, No.74, No.80, No.79, No.34 and No.14, respectively.Clustering analysis showed that 106 codonopsis germplasm could be classified into five taxa, among which the agronomic traits and quality indexes except syringin at a higher level in taxon Ⅰ. The overall performance was better, and it could be promoted for cultivation. stepwise multiple regression analysis showed that root length, luxia diameter, dry weight, drying rate, total amino acid, tryptophan, tangshenoside Ⅰ and atractylenolide Ⅲ had significant effects on fresh weight. Root length, total amino acid. Codonopsis polysaccharide, tryptophan, syringin, tangshenoside Ⅰ and atractylenolide Ⅲ had significant effects on extractum. Extractum had significant effects on codonopsis polysaccharide. Total amino acids, tryptophan and syringin had significant effects on lobetyolin. CONCLUSION The results of this study can serve as a reference for screening high-quality germplasm resources and cultivating varieties of Codonopsis pilosula.

  • 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.