OBJECTIVE To identify the current status of pediatric traditional Chinese medicine (TCM) new drug development in China using registration and approval data, and to provide references for improving the pediatric drug regulatory system. METHODS A total of 468 pediatric TCM new drug registration applications accepted by the China National Medical Products Administration from 2002 to 2024 were collected. Registration profiles, review timelines, registration categories, and product distribution characteristics were analyzed in conjunction with policy backgrounds and literature. RESULTS The total number of registration applications initially increased and then decreased, peaking during the implementation of the 2002 and 2005 editions of the Drug Registration Regulation, followed by a sharp decline after the 2007 edition. The review timelines were progressively shortened, with a notable improvement in approval efficiency under the 2020 edition. Modified new drugs consistently dominated registration categories, while the proportion of TCM compound formulations gradually increased. Products were concentrated in respiratory and digestive system therapies, primarily formulated as granules and tablets. Development in other disease areas and pediatric-friendly dosage forms remained insufficient. CONCLUSION Pediatric TCM development in China predominantly focuses on modified new drugs, with issues of product homogeneity and limited innovation momentum. Recommendations include optimizing priority review mechanisms, establishing specialized pediatric TCM research and development guidelines, strengthening clinical demand-driven innovation, and promoting high-quality pediatric TCM formulations.

OBJECTIVE To construct a competency evaluation index system for clinical pharmacists. METHODS Based on previous research, the method of analytic hierarchy process was used to establish the evaluation hierarchy for competency of clinical pharmacists. A total of 20 experts were included, with an average age of (44.9±5.2) years and an average working seniority of (16.2±8.8) years. RESULTS The weight coefficients of 6 first class indictors, 18 secondary class indictors and 54 third class indictors were confirmed. The weight of each indictor was all consistent with the test. CONCLUSION This study preliminarily constructs a competency evaluation index system for clinical pharmacists, providing reference for the selection, evaluation, and training of clinical pharmacists, and further improvements are still needed.

Diabetic peripheral neuropathy is one of the most common complications of diabetes. Aldose reductase is a key enzyme in the pathogenesis of diabetic complications. This review systematically reviews the efficacy and safety of five kinds of aldose reductase inhibitors in the treatment of diabetic peripheral nerves. Epalrestat is the only aldose reductase inhibitor in clinical application so far. A number of clinical trials have shown that epalrestat has a certain therapeutic effect on diabetic peripheral neuropathy and has sufficient safety, but long-term studies have shown that its therapeutic effect is not better than mecobalamine. Torrestat, zoporestat, ponastat, and fedastat were all withheld from the market or withdrawn from the market due to efficacy or safety concerns, which was inferred to be related to the structural characteristics of the drugs. Development of more effective and safer aldose reductase inhibitors from the perspective of drug structure will become one of the future research focuses on diabetic peripheral neuropathy.

OBJECTIVE To investigate the synthesis and characterization of moxifloxacin hydrochloride. METHODS Using ethyl 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylate and (S,S)-2,8-diazabicyclo[4.3.0] nonane as the starting materials, moxifloxacin hydrochloride was prepared through five steps: chelation, condensation, hydrolysis, salt formation, and refinement. RESULTS and CONCLUSION Compared with other routes, this route is of mild conditions, simple postprocessing, less impurities, high process safety, and less environmental pollution.The prominent advantage of this route is that it can effectively remove boric impurities from moxifloxacin. The chemical structures of the target moxifloxacin hydrochloride and its key intermediates were characterized by IR, HR-MS, XRD and NMR spectra, including ¹H-NMR,¹H-¹HCOSY, ¹³C-NMR, DEPT, HSQC, and HMBC spectra.

OBJECTIVE To study the relationship between the spectral effect and the antibacterial effect of Rhizoma macrophylla L. based on grey correlation degree method and partial least square method. METHODS HPLC was used to establish the fingerprint of 13 batches of Moghania macrophylla (Willd.) Kuntze. The antibacterial activity of Moghania macrophylla (Willd.) Kuntze against 4 common pathogenic bacteria (Staphylococcus epidermidis, Escherichia coli, Staphylococcus aureus and Bacillus subtilis) was determined by microdilution method. Using the Similarity Evaluation System of Fingerprint of Traditional Chinese Medicine (TCM), the characteristic maps of 13 batches of Moghania macrophylla (Willd.) Kuntze were established, and the similarity evaluation and characteristic peak identification were carried out. The relative inhibition rate was used as the index of antibacterial activity, and the spectral effect relationship was established by using grey correlation analysis and partial least square method. RESULTS There were 29 common peaks in the fingerprints of 13 batches of samples, and the similarity was no less than 0.906. Peaks 12, 16, 17, 19 and 20 were identified as genistein, ononin, daidzein, genistein and chickpeas A. Staphylococcus epidermidis, Escherichia coli and Staphylococcus aureus had good bacteriostatic effect on 4 kinds of pathogenic bacteria. The results of spectral effect relationship analysis showed that peak 16 (ononin), peak 20 (chickpea A), peak 21 and peak 25 were the main active components of the antibacterial activity. CONCLUSION Through the study of the spectrum effect relationship, it is confirmed that the antibacterial effect of Moghania macrophylla (Willd.) Kuntze is the result of the combined action of many components, which could provide reference for the basic research and quality control of pharmacodynamic substances of Moghania macrophylla (Willd.) Kuntze.

OBJECTIVE To establish the UPLC fingerprint of wild Qingqiao from Hebei province, analyze the correlation between fingerprint and antioxidant effect, and preliminarily determine its antioxidant active substances, so as to provide a basis for controlling the quality of wild Qingqiao from Hebei province. METHODS The fingerprints of 29 batches of wild Qingqiao from Hebei province were established by UPLC, and the common peaks were identified by UPLC-Q-TOF-MS. The free radical scavenging rate of 1,1-diphenyl-2-picrylhydrazyl (DPPH) method and 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) method was used as the antioxidant index to evaluate the antioxidant activity of wild Qingqiao from Hebei province. The spectrum-effect relationship between common peaks and antioxidant activity of wild Qingqiao from Hebei province was analyzed by grey correlation method and partial least squares regression. RESULTS The UPLC fingerprints of 29 batches of wild Qingqiao from Hebei province were established, and the similarity was between 0.950 and 0.999. A total of 20 common peaks were identified. The common peaks were identified by comparison of standards and UPLC-Q-TOF-MS analysis as citric acid, rengynic acid-1'-O-β-D-glucoside, rengynic acid, rengyol, forsythoside D, adoxosidic acid, forsythide, forsythenside B, 4-hydroxybenzaldehyde, (+)-epipinoresinol-4'-O-β-D-glucoside, forsythoside J, forsythoside A, calcelarioside A, rutin, isoquercetin, rhamnetin, ferulic acid, forsythin, pinoresinol and forsythigenin. By scavenging DPPH and ABTS free radicals, it was found that 29 batches of wild Qingqiao from Hebei province had antioxidant capacity. The results of spectrum-effect analysis showed that 9 components such as citric acid, rengynic acid-1'-O-β-D-glucoside and rengynic acid were positively correlated with antioxidant capacity. Based on the two statistical models, it can be inferred that forsythoside A, rhamnetin and ferulic acid are the main components of the antioxidant activity of wild Qingqiao from Hebei province. CONCLUSION In this study, a quality evaluation model based on chemical composition and antioxidant activity was established, which could provide reference for the antioxidant active ingredients and quality control of wild Forsythiae Fructus from Hebei.

OBJECTIVE To screen the effective components and potent substances of Bletilla striata and to preliminarily predict its mechanism of action. METHODS Oxford cup and microdilution methods were used to evaluate the inhibition of Propionibacterium acnes, Staphylococcus epidermidis and Staphylococcus aureus in different extracted parts of Bletilla striata. Subsequently, a mouse model of acne vulgaris was established to assess the effects of the different extracted components of Bletilla striata on auricular tissue lesions, histopathology, and inflammatory factors. Furthermore, the chemical compositions of the three extracts were analyzed using ultra high performance liquid chromatography-tandem quadrupole mass spectrometry (UPLC-Q-TOF-MS). Network pharmacology was utilized to predict the relevant targets, pharmacodynamic components, and related pathways of Bletilla Striata in the treatment of acne. Additionally, molecular docking was performed on the key pharmacodynamic components and targets to further validate these pharmacodynamic substances. RESULTS The ethyl acetate extract of Bletilla striata could effectively inhibit three kinds of acne-causing bacteria, and its MIC was 2.34, 2.34, 4.59 mg·mL^-1, respectively, the ethyl acetate extract of Bletilla striata significantly improved the auricular tissue lesions in mice, while the remaining two extracts exhibited no anti-acne effect. A total of 51 components of Bletilla striata were identified, including 48 components in the ethyl acetate extract, 13 components in the butanol extract, and 15 components in the water extract, stilbenes were most enriched in the ethyl acetate extract. The results of network pharmacology and molecular docking validation indicated that constituents such as batatasin Ⅲ, 3-(4-hydroxybenzyl)-4-methoxy-2, 7-dihydroxy-9, 10-dihydrophenanthreneand, 3-O-methylbatatasin Ⅲ may serve as key active constituents of Bletilla striata in the treatment of acne. Additionally, MAPK1 and TNF among others may represent potential targets of Bletilla striata in anti-acne therapy. CONCLUSION This study shows that the ethyl acetate extracted parts of Bletilla striata have good anti-acne effects, in which the Stilbenes represented by batatasin Ⅲ may be the main medicinal components, which may provide important references for the in-depth study of the mechanism of Bletilla striata in treating acne.

OBJECTIVE To explore the effect and molecular mechanism of nalmefene on postoperative cognitive dysfunction (POCD) in aged rats. METHODS Seventeen-month-old SD rats were randomly divided into control group (Control), model group (Model), model + nalmefene group (Model+Nal), model+nalmefene+EX527 group (Model+Nal+EX527) with 8 rats in each group after one week of acclimatization. The POCD animal models (excluding the Control group) were established by sevoflurane anesthesia and exploratory laparotomy. The rats in Model+Nal group were subcutaneously injected with 0.1 mg·kg^-1 nalmefene hydrochloride 30 min before anesthesia induction. The rats in Model+Nal+EX527 group were injected subcutaneously with 0.1 mg·kg^-1 nalmefene hydrochloride and intraperitoneally with 10 mg·kg^-1 EX527 (Sirt1 inhibitor) 30 min before anesthesia induction. Morris water maze experiment was conducted to analyze the cognitive abilities of rats. Hippocampal tissues were collected 3 d after surgery. The pathological changes of the hippocampus were observed by HE staining. Neuron apoptosis was analyzed by Tunel staining. ELISA method was used to detect the contents of TNF-α and IL-6. The protein expression levels of Bax, Bcl-2, Sirt1, TLR4 and NF-κB p65 were determined by Western blot. RESULTS Compared with the Control group, the cognitive dysfunction was seen, neuronal damage and the proportion of apoptotic neurons in hippocampal DG region were increased, TNF-α and IL-6 contents as well as the expression of Bax, TLR4 and NF-κB p65 were elevated, while the expression of Bcl-2 and Sirt1 was decreased in the Model group (P<0.001). Compared with the Model group, the cognitive ability was enhanced, neuronal damage and the proportion of apoptotic neurons in hippocampal DG region were decreased, TNF-α and IL-6 contents as well as the expression of Bax, TLR4 and NF-κB p65 were reduced, whereas the expression of Bcl-2 and Sirt1 was elevated in the Model+Nal group (P<0.001). Compared with the Model+Nal group, the cognitive ability was suppressed, neuronal damage and the proportion of apoptotic neurons in hippocampal DG region were increased, TNF-α and IL-6 contents as well as the expression of Bax, TLR4 and NF-κB p65 were elevated, while the expression of Bcl-2 and Sirt1 was decreased in the Model+Nal+EX527 group (P<0.001). CONCLUSION Nalmefene can reduce neuroinflammation and neuronal damage, and improve cognitive dysfunction in aged POCD rats through regulating Sirt1/TLR4/NF-κB pathway.

OBJECTIVE To establish an LC-MS/MS method for determining the concentration of acteoside(the main component of Rehmannia glutinosa leaf total glycosides capsules) in the plasma of young rats and investigate the exposure levels and toxicokinetic characteristics of acteoside following repeated oral gavage administration of different doses of Rehmannia glutinosa leaf total glycosides capsules. METHODS Plasma samples were processed using protein precipitation with methanol-acetonitrile (1∶1). Chromatographic separation was performed on a Waters ACQUITY UPLC HSS T3 column (2.1 mm×100 mm, 1.7 μm), with mobile phase consisting of 0.1% formic acid in water and 0.1% formic acid in acetonitrile, at a flow rate of 0.5 mL·min^-1. The injection volume was 2 μL. Mass spectrometry detection was carried out using electrospray ionization in negative mode (ESI^-1) and multiple reaction monitoring (MRM). The ion transitions monitored were 623.1/160.9 for acteoside and 269.0/158.9 for genistein which served as the internal standard. The established LC-MS/MS method was applied to analyze the plasma concentrations of acteoside in young Wistar rats after the first and last administrations of Rehmannia glutinosa leaf total glycosides capsules during a toxicity study. Pharmacokinetic profiles were constructed and kinetic parameters were calculated. RESULTS An LC-MS/MS method was developed and validated for the accurate determination of acteoside in rat plasma within a concentration range of 2-500 ng·mL^-1. Young Wistar rats were repeatedly gavaged with suspensions of Rehmannia glutinosa leaf total glycosides capsules for 8 weeks at dose levels ranging from 30 to 750 mg·kg^-1. No accumulation of acteoside exposure was observed within this dose range, and the exposure did not exhibit linear kinetics with increasing dose. CONCLUSION The developed LC-MS/MS method is applicable for measuring the concentration of acteoside from Rehmannia glutinosa leaf total glycosides capsules in rat plasma and supports toxicokinetic studies in young rats.

OBJECTIVE To prepare polymyxin B sulfate multivesicular liposomes (PMB-MVLs), optimize their formulation, and their quality, stability, release and investigate their antibacterial activity in vitro. METHODS The PMB-MVLs were prepared by the double-emulsion method. The response surface method of Box-Behnken design was used to optimize the initial prescription. High performance liquid chromatography method was established to quantitatively analyze PMB in PMB-MVLs. The physicochemical properties, the in vitro drug release behavior, in vitro antimicrobial activity and formulation safety of PMB-MVLs were investigated. RESULTS The appearance of PMB-MVLs prepared by optimal prescription were non-concentric spherical vesicles with uniform size. The encapsulation efficiency of PMB-MVLs were (69.521±1.531)%. The average particle size was (5.84±1.42) μm, and the average Zeta potential was (-26.77±0.55)mV. The PMB-MVLs showed good stability when stored at 4 ℃ for one month. The results showed that PMB-MVLs were released continuously for 72 h in vitro, and there was no sudden release effect. The in vitro antibacterial activities of PMB-MVLs on E.coli and P.aeruginosa were significantly stronger than those of the free PMB. And PMB-MVLs has no risk of hemolysis within its range of antimicrobial activity. CONCLUSION The slow-release PMB-MVLs are successfully prepared with uniform particle size, high encapsulation efficiency, and enhanced antibacterial activity.