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2020 Vol. 38, No. 4

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The mechanism study on Chaihudaxiong mixture in the treatment of coronavirus disease 2019 with network pharmacology approach
XIAO Zhijun, LIU Cuicui, LU Saihua, CAI Jian, XU Feng
2020, 38(4): 289-295. doi: 10.12206/j.issn.1006-0111.202004023
Abstract(6878) HTML (2902) PDF (1025KB)(45)
Abstract:
  Objective  To investigate the pharmacological mechanism of Chaihudaxiong mixture in the treatment of coronavirus disease 2019 (COVID-19) based on a network pharmacology approach.  Methods  The effective ingredients and targets of Chaihudaxiong mixture were collected from Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP). The targets’ names were standardized by Uniprot database. Genes associated with coronavirus were obtained from the GeneCards and OMIM, which were intersected with effective therapeutic targets. A "herbs-ingredients-targets" network was compiled and analyzed by Cytoscape 3.7.2. The protein-protein interaction of the targets was analyzed by String. The GO gene annotation and KEGG signaling pathway analysis were performed using related packages of the R software.  Results  A total of 165 active ingredients and 51 targets were collected. Further analysis revealed that the main active ingredients were β-sitosterol and 11 flavonoids. The core targets were CASP3, MAPK3, IL-6, MAPK8, IL-10, CXCL8, MAPK1 and IL-1B. A total of 1722 GO entries were obtained from the GO gene annotation (P<0.05), including 1612 entries for biological processes, 30 entries for cell composition, and 80 entries for molecular functions. 156 signaling pathways (P<0.05) were obtained with KEGG signaling pathway screen. The important signaling pathways were AGE-RAGE signaling pathway in diabetic complication, Influenza A, IL-17 signaling pathway, TNF signaling pathway and hepatitis B.  Conclusion  This study revealed the synergistic features of multi-component, multi-target, and multi-pathway of Chaihudaxiong mixture in the treatment of COVID-19, which provided an important scientific basis for further understanding the mechanism of Chaihudaxiong mixture in the treatment of COVID-19.
Mechanism of leflunomide in regulating pulmonary fibrosis by regulating miR-449a
LIU Dong, LAI Weinan
2020, 38(4): 296-300, 306. doi: 10.12206/j.issn.1006-0111.201910073
Abstract(6336) HTML (1947) PDF (562KB)(13)
Abstract:
  Objective  To investigate the mechanism of leflunomide (LEF) in regulating pulmonary fibrosis by regulating microRNA (miR)-449a.  Methods  Human lung fibroblasts MRC-5 were divided into 6 groups: control group, LEF group, LEF+mimic group, mimic group, LEF+inhibitor group and inhibitor group. MiR-449a was overexpressed or silenced by plasmid transfection with miR-449a mimic or inhibitor and ncubate for 48 h at 5 mg / L LEF. The cell viability, cell proliferation ability and apoptotic rate of each group were measured by CCK-8 method, clone formation experiment and flow cytometry. Immunofluorescent staining was used to detect α smooth muscle actin (α-SMA) and collagen I (col I). The levels of miRNA and protein were detected using qPCR and Western blot, respectively.  Results  The miR-449a level in the mimic group was significantly higher than that in the control group (P<0.05). The level of miR-449a in LEF group and inhibitor group was significantly lower than that in control group (P<0.05). The expression level of miR-449a in LEF+mimic group was significantly higher than that in LEF group, and the level of miR-449a in LEF+inhibitor group was significantly lower than that in LEF group (P<0.05). The cell viability and cell proliferation ability of the LEF group and inhibitor group were significantly higher than those of the control group (P<0.05). The cell viability and cell proliferation ability of the mimic group were significantly lower than those of the control group (P<0.05). The cell viability and cell proliferation ability of the LEF+mimic group were significantly lower than those of the LEF group, while the cell viability of the LEF+inhibitor group was significantly higher than that of the LEF group (P<0.05). The apoptosis rate of LEF group and inhibitor group was lower than that of control group (P<0.05). The apoptosis rate of mimic group was significantly higher than that of control group (P<0.05). The apoptosis rate of LEF+mimic group was significantly higher than that of LEF group, while the apoptosis rate of LEF+inhibitor group was significantly lower than that of LEF group (P<0.05). The fluorescence intensity of α-SMA and Col I proteins in LEF group and inhibitor group were significantly higher than those in control group (P<0.05). The relative fluorescence intensity of mimic group was lower than that of control group (P<0.05). The relative fluorescence intensities of α-SMA and Col I proteins in LEF+mimic group were significantly lower than those in LEF group, while the relative fluorescence intensities of α-SMA and Col I protein in LEF+inhibitor group were significantly higher than those in LEF group (P<0.05). The levels of p-JNK / JNK in LEF group and inhibitor group were higher than those in control group (P<0.05). The p-JNK / JNK level in the mimic group was significantly lower than that in the control group (P<0.05). The level of p-JNK / JNK in LEF+mimic group was significantly lower than that in LEF group, while the level of p-JNK / JNK in LEF+inhibitor group was significantly higher than that in LEF group (P<0.05).  Conclusion  LEF may activate the JNK pathway by inhibiting the expression of miR-449a in lung fibroblasts, thereby inducing fibroblast activation and proliferation, inhibiting apoptosis, and causing pulmonary fibrosis.
Preparation and formulation optimization of wound dressings with nitrocellu-lose as membrane material
ZHANG Lingna, WANG Tianyu, HONG Wanfeng, TAO Chun, SONG Hongtao
2020, 38(4): 301-306. doi: 10.12206/j.issn.1006-0111.201910082
Abstract(6332) HTML (2542) PDF (1099KB)(49)
Abstract:
  Objective  To prepare a wound dressing using nitrocellulose as a membrane and optimize its formulation.  Methods  Partial analysis was performed on commercial available products. The wound dressings were prepared by using nitrocellulose as a film-forming material, benzyl alcohol as a bacteriostatic agent, castor oil as a plasticizer, isopropyl palmitate as a skin emollient, camphor as a fragrance, and isopropyl alcohol, ethyl acetate and butyl acetate as volatile solvent. The tensile strength, breakpoint elongation percentage, breathability and waterproof performance were tested and evaluated.  Results  The film-forming performance of the prepared liquid wound dressing was good. The final use amount of nitrocellulose was determined to be 6%. The use amount of plasticizer castor oil was determined to be 4%.  Conclusion  The prepared liquid wound dressing has good film-forming property, good mechanical property, good waterproof and certain breathability.
Preparation and in vitro release of tacrolimus-loaded cationic nanoemulsion-based in-situ gel
LIN Xin, ZHANG Jialiang, SONG Hongtao
2020, 38(4): 307-311, 317. doi: 10.12206/j.issn.1006-0111.201911075
Abstract(6669) HTML (2120) PDF (859KB)(43)
Abstract:
  Objective  In order to improve the problems of poor water-solubility and low bioavailability of ocular tacrolimus, a cationic nanoemulsion in-situ gel of tacrolimus was developed and its drug release behavior in vitro was studied to provide a basis for further research.  Methods  Tacrolimus-loaded cationic nanoemulsion was prepared by high pressure homogenization and dispersed in poloxamer 407 and poloxamer 188 to prepare tacrolimus-loaded cationic nanoemulsion-based in-situ gel. The membraneless dissolution model was used to study the in vitro drug release behavior.  Results  The inverse glass bottle method was used to determine the gelation temperature. The optimal formulation of gel matrix was screened out as 26% poloxamer 407 and 12% poloxamer 188. The in vitro release results showed that the rate of gel dissolution determined the in vitro drug release.  Conclusion  Tacrolimus-loaded cationic nanoemulsion-based in-situ gel is successfully prepared. Its in vitro drug release is stable. It meets the requirement of ophthalmic formulation and shows good prospects for ocular application.
Comparative of pharmacokinetic of moxifloxacin in the plasma and lung tissues of pneumonia rats and normal rats
CHENG Xi, HUANG Yueying, LI Yi
2020, 38(4): 312-317. doi: 10.12206/j.issn.1006-0111.202002007
Abstract(6772) HTML (1955) PDF (777KB)(21)
Abstract:
  Objective  To compare the pharmacokinetics of moxifloxacin (MXF) administered orally in the plasma and lung tissues of rats with pneumonia infected by Streptococcus pneumoniae (S.p) and normal rats.  Methods  To establish a model of Streptococcus pneumoniae pneumonia rats and normal rats. Moxifloxacin was administered by intragastric administration at 42 mg/kg. Microdialysis technique was used to sample the blood and lung tissues of pneumonia rats and normal rats to determine the free drug concentration of moxifloxacin in each sample, calculate the pharmacokinetic parameters, and compare the pharmacokinetics of oral moxifloxacin in pneumonia rats and normal rats.  Results  The t1/2 of moxifloxacin in the blood of normal rats and pneumonia rats were (5.27±4.38) h, (2.15±0.07) h (P>0.05), and Cmax were (4.94±0.98) μg/ml, respectively, (4.83±0.05) μg/ml (P>0.05), Clast_obs/Cmax were 0.02±0.03, 0.27±0.04 (P<0.05), AUC0-t were (22.33±2.02)μg/ml·h, (12.88±1.19)μg /ml·h (P<0.05), CL/F are (1.79±0.11)(mg/kg)/(μg/ml)·h, (2.49±0.26)(mg/kg)/(μg/ml)·h (P<0.05); Cmax of lung tissue of normal rats and pneumonia rats were (1.42±0.05) μg/ml, (4.84±0.02) μg/ml (P<0.05), t1/2 are (1.9±0.63)h, (3.39±0.79)h (P>0.05), AUMC are (11.93±5.14)μg/ml·h2, (107.01±25.39)μg/ml·h2 (P<0.05), AUC0-t are (3.06±1.0) 7μg/ml·h, (13.16±0.53)μg/ml·h (P<0.01).  Conclusions  ① Under the 400 mg/d dose condition, after intragastric administration of moxifloxacin, the concentration of free drugs in the blood and lung tissues is higher, far exceeding the minimum inhibitory concentration (MIC) and anti-drug resistance concentration (MPC), can effectively remove Streptococcus pneumoniae. ②The free concentration of moxifloxacin in the lung tissue of rats infected with Streptococcus pneumoniae is always higher than that of normal rats, and the Cmax is about 3.4 times that of normal rats. The penetration rate of moxifloxacin in lung tissue of pneumonia rats is significantly higher than that of normal rats.
The metabolic analysis of 11C-flumazenil in different specific radioactivity
ZHANG Zongpeng, WANG Zhiguo, SHI Qingxue, ZHANG Guoxu, HUO Hua
2020, 38(4): 318-321. doi: 10.12206/j.issn.1006-0111.202003141
Abstract(5802) HTML (2013) PDF (561KB)(13)
Abstract:
  Objective  To analyze the metabolic differences of 11C-flumazenil (11C-FMZ) with different specific radioactivity by detecting the percentage proportion of the main metabolites in vivo.  Methods  5 male and 5 female volunteers with average age of (41.7±4.7) years and weight of (69.3±6.8) kg were selected from May to October 2019. 11C-FMZ with high and low specific radioactivity (268.3±57.2)×103 and (57.8±11.4)×103 Ci/mol was injected successively. The percentage of injected dose/liter of 11C-FMZ and its metabolites in the plasma at 1, 2, 3, 4, 5, 10, 15, 20, 30, 40 and 60 min after the injection was measured. Paired sample mean t test was used to calculate and compare the percentage of metabolites in the two groups.  Results  The percentage proportion of metabolites increased gradually with time, and reached the stable level after 15 min. The percentage proportion of low specific radioactivity group was higher than that of high specific radioactivity group with a significant statistical difference between 15 min and 60 min (P<0.05).  Conclusion  The metabolic rate of 11C-FMZ with different specific radioactivity was significantly different after injection and the specific radioactivity difference should be avoided if possible in clinical application.
Study on pharmacodynamics and safety of self-made compound ketoconazole ointment
YAN Jia, WU Bo, TAO Chun, SONG Hongtao
2020, 38(4): 322-327. doi: 10.12206/j.issn.1006-0111.201909078
Abstract(8194) HTML (3009) PDF (870KB)(27)
Abstract:
  Objective  To evaluate the pharmacodynamics and safety of the self-made compound ketoconazole ointment.  Methods  Using the disk diffusion test, 6 kinds of fungi and 2 kinds of bacteria were selected to investigate the effect of the self-made ointment and 3 commercial products on the diameter of the bacteriostatic circle. In addition, the skin irritation and skin allergies of the single and multiple applications were used to evaluate the safety of the self-made ointment.  Results  The self-made ointment was similar to the commercial products containing ketoconazole. They all showed remarkable bacteriostatic circle against the 6 kinds of fungi. For pseudomonas aeruginosa, none of the preparations contributed to visible bacteriostatic circle. For staphylococcus aureus, the bacteriostatic circle of the self-made ointment was similar to that of commercial mupirocin ointment and was significantly larger than other commercial products. After the treatment with the self-made ointment, the score of the skin irritation was below 0.5 and the sensitization rate was 0. There was no difference in tissue structure between treated and normal skin.  Conclusion  The self-made compound ketoconazole ointment has better safety and better antibacterial property than the commercial products. It is expected to be used for the treatment of superficial skin fugle infections.
Optimization of formulation process and in vitro evaluation of copper sulfide nanoparticles
CHEN Zhenzhen, TAO Chun, ZHANG Xueting, ZHOU Guizhi, ZHANG Qian, SONG Hongtao
2020, 38(4): 328-333, 345. doi: 10.12206/j.issn.1006-0111.201912092
Abstract(6825) HTML (2374) PDF (1508KB)(37)
Abstract:
  Objective  To avoid the accumulation of copper sulfide (CuS) nanoparticles, prepare and optimize CuS nanoparticles, analyze the factors affecting the particle size and evaluate their photothermal properties.  Methods  Based on the single factor study, central composite design-response surface methodology was used to optimize the CuS nanoparticle formulation process. The morphology, particle size stability, photothermal conversion efficiency, photothermal stability of optimized CuS nanoparticles were characterized. The toxicity of CuS nanoparticles on 4T1 breast cancer cells and HK2 kidney cells was evaluated by CCK-8 method. In vitro photothermal experiment was used to investigate the ability of CuS nanoparticles on killing 4T1 breast cancer cells.  Results  The average hydration dynamic diameter of optimized CuS nanoparticles was (10.53±1.63)nm, the actual particle size of CuS nanoparticles showed by TEM image was (3.10±0.81)nm. It had good particle size stability, good photothermal conversion efficiency and photothermal stability. Within the concentration range of 100 μg/ml and 150 μg/ml, it showed no significant toxicity on 4T1 breast cancer cells and HK2 kidney cells, indicating the good stability of CuS nanoparticles. In vitro photothermal therapy showed that CuS nanoparticles had good ability to kill 4T1 breast cancer cells by photothermal.  Conclusion  The prepared CuS nanoparticles have a small particle size (less than 6nm) and a good photothermal effect, which is expected to solve the problem of CuS nanoparticles accumulation in vivo and make it better for tumor treatment.
Study on correlation between plasma concentration of cyclosporine injection and gene polymorphism in renal transplant patients
ZHANG Yanxia, CHEN Quanjin, SONG Hongtao
2020, 38(4): 334-339. doi: 10.12206/j.issn.1006-0111.201911107
Abstract(6588) HTML (2160) PDF (455KB)(28)
Abstract:
  Objective  To investigate the clinical efficacy of cyclosporine injection in subclinical or critical treatment of renal transplant patients, and to establish an individualized dosage regimen of cyclosporine injection by studying the effects of nine single nucleotide polymorphisms related to the pharmacokinetics of cyclosporine on the dose-adjusted trough concentration (C0/D′) of cyclosporine injection.  Methods  Blood samples and clinical data of 144 adult renal transplant patients who used cyclosporine injection were collected and recorded, then, their genotypes of CYP3A4*18B, CYP3A5*3, ABCB1 (C1236T, G2677T/A, C3435T), POR*28, PXR (C5705T, C39823T) and NFKB1-94 ins/del ATTG were determined by Sequenom MassARRAY® SNP methods. Then, the discrepancies of cyclosporine injection’s C0/D′ among the patients with different genotypes was compared and an individualized dosage regimen based on gene polymorphism of cyclosporine injection was established by using multivariate regression analysis.  Results  Cyclosporine injection improved serum creatinine level by 68.8% in renal transplant patients with subclinical or critical rejection, and the steady-state plasma concentration was (189.50±38.56) ng/ml. The CYP3A4*18B gene polymorphism was significantly correlated to C0/D' of cyclosporine injection, and the C0/D' of patients with *1/*1 genotype was significantly higher than patients of *18B/*18B genotype; but CYP3A5*3, ABCB1(C1236T, G2677T/A, C3435T), PXR C5705T, PXR C39823T, NFKB1-94 ins/del ATTG and POR*28 gene polymorphisms were not significantly correlated to C0/D' of cyclosporine injection. In the final regression model, hemoglobin and CYP3A4*18B gene polymorphisms were significantly correlated to C0/D' of cyclosporine injection.  Conclusion  Cyclosporine injection can effectively improve the serum creatinine level in patients with subclinical or critical rejection; CYP3A4*18B gene polymorphism is significantly correlated to C0/D' of cyclosporine injection.
Effects of vitamin K on osteoblastic bone formation and osteoclastic bone absorption
JIANG Yizhong, XIA Tianshuang, XIN Hailiang, JIN Yu'e, JIANG Yiping, XUE Liming
2020, 38(4): 340-345. doi: 10.12206/j.issn.1006-0111.202001077
Abstract(7369) HTML (1710) PDF (819KB)(33)
Abstract:
  Objective  To compare the effects of vitamin K1 (VK1), vitamin K2 (MK4), vitamin K2 (MK7) and vitamin K3 (VK3) on bone formation and bone absorption.  Methods  Osteoblasts were isolated from calvaria of newborn rats and osteoclasts were induced by receptor activator of nuclear factor-κ B ligand (RANKL). ALP and TRAP activity were measured by diphenyl phosphate method. Osteoclast metabolic activity was measured by Celltiter kit. The inhibition of cathepsin K (CTSK) was measured by Z-FR-MCA fluorescent substrate and collagen substrate degradation.  Results  MK4 and MK7 at 0.1~1 μmol/L significantly increased the proliferation of osteoblasts (P<0.05) and at 1 μmol/L increased ALP activity and bone nodule formation area. VK3 inhibited bone nodule formation (P<0.05). VK1,VK3,MK4 and MK7 at 1 μmol/L had no effect on osteoclastic bone absorption. MK4 and MK7 significantly inhibited TRAP activity at 0.1~1 μmol/L (P<0.05), while VK1 and VK3 did not show the inhibitory effect. The inhibition of MK4 at 25 μmol/L on CTSK binding to Z-FR-MCA substrate activity is 58.9% and the inhibition of MK4 at 100 μmol/L on collagen degradation of CTSK activity is 73.2%.  Conclusion  Compared with VK1 and VK3, MK7 and MK4 significantly increase osteoblast activity and inhibit osteoclast bone absorption, MK4 inhibits osteoclast CTSK enzyme activity.
Study on extraction process and antioxidant activity of iridoid glycosides in Damnacanthus officinarum Huang
DUAN Jinhui, LIU Yang, HUANG Rongji, HU Yang, RUAN Jinlan
2020, 38(4): 346-349. doi: 10.12206/j.issn.1006-0111.201911013
Abstract(7318) HTML (2092) PDF (598KB)(24)
Abstract:
  Objective  To optimize the extraction process of main iridoid glycosides in Damnacanthus officinarum Huang and evaluate the antioxidant activity of Damnacanthus officinarum Huang in vitro.  Methods  The classical heating-reflux extraction method was selected. The volume fraction of ethanol, the volume of solvent and extraction time were taken as the evaluation factors. The comprehensive score of extraction yield and the monotropein content were used as the evaluation indexes. An orthogonal test was designed to select the best extraction conditions. The total reducing capacity, DPPH clearance rate and hydroxyl radical scavenging rate were measured to determine its antioxidant activity in vitro.  Results  The optimal extraction process was the reflux with 6 times volume of 60% ethanol for 2 hours. Damnacanthus officinarum Huang has certain antioxidant capacity, and the activity of ethyl acetate part had the best effect.  Conclusion  The optimized extraction process is stable and feasible, which can be used for extraction of the iridoid glycosides from Damnacanthus officinarum Huang. This study has proved that Damnacanthus officinarum Huang has certain antioxidant activity.
Determination of propylthiouracil in human plasma by UPLC-MS/MS
LI Qunying, LING Lin, LI Chengjian, ZHOU Jin, LI TianTian, ZHAO Liang, LÜ Lei
2020, 38(4): 350-353, 378. doi: 10.12206/j.issn.1006-0111.202001063
Abstract(5469) HTML (1440) PDF (509KB)(31)
Abstract:
  Objective  To establish a method for the determination of propylthiouracil in human plasma by UPLC-MS/MS and provide methodological basis for therapeutic drug monitoring (TDM) and bioequivalence test (BE) in clinical.  Methods  The chromatographic separation was performed on an Agilent SB-C18 column (4.6 mm×150 mm, 5 μm), the mobile phase was methanol and water containing 0.1% formic acid (80∶20, V/V), isocratic elution. MS condition was optimized in the positive ion detection mode by multiple reaction monitoring (MRM), along with the Agilent JetStream electrospray source interface (AJS-ESI). The precursors to the product ion transitions were m/z 171.1→112.1 for propylthiouracil and m/z 176.1→117.0 for the internal standard (IS).  Results  The calibration curve was linear in the range of 10−5 000 ng/ml for propylthiouracil in human plasma, r=0.999 3. The intra-day and inter-day precision and accuracy were good (RSD<10%, RE<±10%). The matrix effect of different concentrations was less than 110% and the coefficient of variation was less than 5%. The average recovery of different concentrations was 101.60%−113.56%, which conformed with the requirement of methodological validation.  Conclusion  The method is rapid, sensitive and accurate, which can be used for the determination of propylthiouracil in human plasma.
Optimization and purification of extraction of polysaccharides from Anoecto-chilus roxburghii
ZHANG Songbai, ZHANG Xun, XU Wen, XU Wei, HUANG Zehao, LIN Yu, CHEN Shuyun
2020, 38(4): 354-358, 382. doi: 10.12206/j.issn.1006-0111.202001025
Abstract(5603) HTML (1763) PDF (1329KB)(22)
Abstract:
  Objective  To optimize the process of ultrasonic extraction of polysaccharide in Anoectochilus roxburghii and to investigate the method of protein removal.  Methods  The extraction rate of polysaccharide was used as the detection index. On the basis of single factor investigation, Box-Behnken experimental design and response surface method were used to optimize the three factors of material-liquid ratio, ultrasonic time and ultrasonic extraction temperature. The five deproteinization methods including Sevage reagent method, TCA method, salt method (NaOH-CaCl2 and NaOH-NaCl) and hydrochloric acid method were investigated with the retention rate of polysaccharide and protein removal rate.  Results  The optimal extraction conditions of polysaccharide from Anoectochilus roxburghii were as follows: liquid-to-solid ratio was 10∶1, extraction temperature was 48 ℃ and extraction time was 36 min with extraction 2 times, ultrasonic power was 300 W, the extraction rate was 13.13%. NaOH-CaCl2 deproteinized methods∶ the loss rate of polysaccharide was 18.74%, and the removal rate of protein was 95.62%.  Conclusion  Ultrasonic extraction is easy to operate, and the optimized extraction method can achieve a high extraction rate. NaOH-CaCl2 deproteinization methods can get high protein removal rate and polysaccharide retention rate. This method is suitable for the research and development of the active components of the polysaccharides from Anoectochilus roxburghii.
Detectione of the contents of ginsenoside Rb1 and astragaloside IV in Weikang granules by HPLC-ELSD
LIU Lu, YU Shuangyu, LIU Yanhua
2020, 38(4): 359-363. doi: 10.12206/j.issn.1006-0111.202001083
Abstract(5768) HTML (2280) PDF (508KB)(21)
Abstract:
  Objective  To optimize the extraction method and develop the detection method of ginsenoside Rb1 and astragaloside Ⅳ in Weikang granules.  Methods  The extraction process of ginsenoside Rb1 and astragaloside Ⅳ in Weikang granules were optimized by single factor investigation, with the contents of ginsenoside Rb1 and astragaloside Ⅳ as optimization indicators. The HPLC-ELSD method was developed for the detection of ginsenoside Rb1 and astragaloside Ⅳ in Weikang granules. Separation was carried out on an XBridge®Shield RP18 column (4.6 mm×250 mm, 5 μm) with a mobile phase consisting of acetonitrile-water(32:68)at the flow rate of 1 ml/min. The column temperature was maintained at 30 ℃. The drift tube temperature was set at 60 ℃, and the carrier gas flow rate was 1.7 SLM.  Results  The optimized extraction methods of ginsenoside Rb1 and astragaloside Ⅳ in Weikang granules were as the following: methanol reflux extraction for 1.5 h, and n-butanol extraction and ammonia washed for 5 and 2 times, respectively. The HPLC-ELSD method was established to detect the contents of ginsenoside Rb1 and astragaloside Ⅳ. The linear relationship was good (r > 0.9997). The intra-day and inter-day precision was less than 1%. The recovery rates were 95.65% and 100.57%. The stability and repeatability RSD were less than 3%. The contents were 2.8630 mg/g and 0.2576 mg/g. The RSDs were 0.62% and 1.51%, respectively.  Conclusion  The extraction method of ginsenoside Rb1 and astragaloside Ⅳ in Weikang granules is optimized, and a reliable, accurate and reproducible HPLC-ELSD method for the detection of the contents of ginsenoside Rb1 and astragaloside Ⅳ in Weikang granules is established.
Application of near infrared spectroscopy analysis method in rapid detection of sodium aescinate
WANG Boyang, BAO Yi, LI Jie, GENG Zheng
2020, 38(4): 364-367. doi: 10.12206/j.issn.1006-0111.202002011
Abstract(5055) HTML (1895) PDF (668KB)(14)
Abstract:
  Objective  To establish a fast detection method of sodium aescinate by using near infrared (NIR) spectroscopy analysis method for the determination of the content of sodium aescinate for injection.  Methods  OPUS software was used to optimize the collected spectrum. PLS algorithm and factorization algorithm were used to establish quantitative model and qualitative model.  Results  The correlation coefficient of the quantitative model reached 0.9926, the RMSECV deviation was 0.253. The deviation between the predicted value of the sample and the true measured value was less than 5%, which could accurately predict the content of sodium aescinate.  Conclution  The qualitative model can effectively distinguish the samples of other varieties that have not participated in the modeling, and provide a reference for the rapid screening of the drug.
The clinical effect of Yaotongning capsule combined with etoricoxib in the treatment of lumbar pain and inflammatory status in elderly patients with lumbar osteoarthritis
LI Pengfei, JIAN Qiang, QIAO Meina, SUN Changgui, GAO Junfeng
2020, 38(4): 368-372. doi: 10.12206/j.issn.1006-0111.201912170
Abstract(8078) HTML (2174) PDF (473KB)(21)
Abstract:
  Objective  To study the clinical effect of Yaotongning capsule combined with etoricoxib for the pain and inflammation of lumbar vertebrae in elderly patients with lumbar osteoarthritis.  Methods  120 elderly patients with lumbar osteoarthritis admitted to our hospital from January 2016 to June 2018 were randomly divided into the control group and the observation group, with 60 patients in each group. Patients in the control group were treated with etoricoxib, while patients in the observation group were treated with etoricoxib plus Yaotongning capsule orally. Both groups received medications for 2 weeks. Spinal pain and quality of life score changes were recorded. The inflammatory cytokines in serum TNF-α, GM-CSF, COX-2 and BMP-2 levels were monitored. The clinical efficacy was compared and drug safety profile was evaluated for two groups.  Results  The effective rates of the control group and the observation group were 78.33% and 91.67% respectively. The effective rate in the observation group weas significantly higher (P<0.05). After treatment, the VAS score for the patients in the observation group was significantly lower than that in the control group (P<0.05). The SF-36 score in the observation group was significantly increased (P<0.05), and the levels of TNF-α,GM-CSF and COX-2 in the serum were significantly lower than those in the control group (P<0.05), and the levels of BMP-2 were significantly increased (P<0.05).  Conclusion  Yaotongning capsule combined with etoricoxib in the treatment of senile lumbar osteoarthritis has definite curative effect. It significantly reduced lumbar pain, improved quality of life, inhibited inflammatory reaction, and had a better drug safety profile. The further clinical investigation for the combination therapy is warranted.
Impact of “4+7” City Drug Centralized Procurement Program on the utilization of original and generic cardiovascular drugs in a tertiary hospital
WANG Hui, LI Xin, CHEN Jing
2020, 38(4): 373-378. doi: 10.12206/j.issn.1006-0111.202001054
Abstract(6023) HTML (1974) PDF (509KB)(66)
Abstract:
  Objective  To analyze the impact of “4+7” City Drug Centralized Procurement Program on the utilization of cardiovascular medicines, and to provide a reference for optimizing the policy of generic medicines as substitutes for original medicines.  Methods  Eleven drugs, both generic and original were selected for treatment of cardiovascular diseases in an outpatient clinic of a tertiary hospital in Shanghai. The proportion of use of generic drugs and original drug, ratio of used amount, daily cost ratio, and potential cost savings rate of replacement of original drug by generic drug were analyzed before the “4+7” (2018.04.01-2018.09.30) and after the “4+7” (2019.04.01-2019.09.30).  Results  After the “4+7”, the proportion of the original research drug used decreased from 84.32% to 58.12%, and the ratio of amount of used money decreased from 86.02% to 78.16%; the proportion of generic medicines used increased from 15.68% to 41.88%, and the ratio of amount used increased from 13.98% to 21.84%; the daily cost ratio of generic medicine to original medicine decreased from 0.87 to 0.39. Under the same condition, the potential cost savings of replacing the original drug with generic drugs before and after the “4+7” were RMB 3.703 million and RMB 3.399 million, respectively, and the cost saving rate was 35% and 61%, respectively.  Conclusion  The “4+7” City Drug Centralized Procurement Program significantly increase the use of cardiovascular generic drugs and significantly reduce the cost of drugs; however, it has a small impact on the quantity and amount of generic drugs used. There is still a significant potential for cost saving. It is recommended to further increase the publicity of the policy on the substitution of original drug by generic, expedite the consistency evaluation process of generic drugs and take measures to avoid the widening of the price gap between original drugs and generics.
Analysis on the use of narcotic drugs for inpatients
HAN Baichen, ZHANG Meiling, ZHANG Ying, YANG Yang
2020, 38(4): 379-382. doi: 10.12206/j.issn.1006-0111.202004095
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Abstract:
  Objective  To investigate and analyze the inpatient use of narcotic drugs, provide reference for clinical norms and rational use of narcotic drugs.  Methods  The narcotic prescription number, usage and cost were analyzed statistically. The inpatient narcotic use was analyzed by screening the dose form, indication, and dosage.  Results  The injections topped the list of narcotic prescriptions from year 2016 to 2019 with 15 820 (61.4%), 15 813 (61.5%), 16 682 (64.7%) and 17 293 (71.5%) prescriptions respectively. The oral and topical narcotic drugs were less prescribed. Although pethidine hydrochloride injection prescriptions decreased year by year, it still topped in the narcotic use with 8 009 (31.1%), 7 707 (30.0%), 7 151 (27.7%) and 6 844 (28.3%) prescriptions each year. Pethidine hydrochloride injection was mostly used for patients with cancer and chronic pancreatitis.  Conclusion  Doctors preferred to use injectable narcotics for patients with moderate to severe pain. Improper use of narcotic drugs was noticed, such as unsuitable choice of dose form, inappropriate use of pethidine hydrochloride injection, etc. Pharmacists should keep vigilant in prescription review and medication intervention for narcotic drugs to improve the standardization and rational use of narcotics.
2020, 38(4): 383-384. doi: 10.12206/j.issn.1006-0111.201912069
Abstract(5170) HTML (990) PDF (356KB)(26)
Abstract: