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Objective To compare the dissolution curves of metronidazole tablets from 38 national manufactures and original drugs of Britain in four dissolution mediums,and provide the reference for the quality and clinical effect consistency evaluation of metronidazole tablets.Methods Paddle method was adopted at 50 r · min-1 in four dissolution mediums with the volume of 900 mL.The dissolution profiles were determined by ultraviolet spectrophotometry.The cumulative dissolution percentages were calculated and the dissolution curves were drawn.Similarity factor (f2)was used for comparing of the differences between dissolution curves.Results The dissolution profiles of 4 manufactures in pH 1.2 and 9 manufactures in pH 4.5 were similar (f2 ≥ 50)to that of original drugs,only 1 and 3 were similar to original drugs in water and pH 6.8,respectively.There are no companies whose dissolution curve were similar to that of original drugs in 4 dissolution mediums.Conclusion Great difference exists between domestic manufactures and pharmaceutical enterprises of origin in dissolution behaviors of metronidazole tablets.In order to ensure the consistency between the metronidazole tablets generics and original drugs of Britain in quality and clinical effect.It is advisable for the relevant companies to improve their product quality by improving the formulation and preparation.
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Objective To establish HPLC determination method and impurity profile of the related substances in metronidazole.Methods A Welch Ultimate(R)XB-C1s (4.6 mm× 250 mm,5 μm)was used with a mobile phase consisting of methanol-1.36 g· L-1 solution of potassium dihydrogen phosphate (20∶ 80).The detection wavelength was 315 nm and the flow rate was 1 mL· min-1.Its related substances were determined by principal component self-contrast method.Results Good separation of metronidazole and the impurities could be achieved.Twenty batches of samples in the past six years were determined which meet quality standards.The study of impurity profiles could effectively monitor the synthetic process and the change of impurities in metronidazole.Conclusion The method is simple,quick and sensitive,which can be used to control the related substances in metronidazole.Meanwhile,the impurity profiles ensure the quality stability of metronidazole.
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Objective:To investigate research topics and management methods for hospital pharmacy in order to promote the devel -opment of hospital pharmacy researches .Methods:The basic principles , main research fields , strategies and approaches of topic se-lection in hospital pharmacy , as well as the main points of research management were discussed .Results:The main research fields of hospital pharmacy included experimental studies and soft science researches .The principles of selected topics should follow practicabil-ity, scientificity, innovation, feasibility and effectiveness , and the topics should set off from the thinking path of pharmacy , be for the purpose of translational medicine and be based on the practical problems of clinical drug use .The quality evaluation of generic drugs , druggability research and so on could take advantage of close to clinics of hospital pharmacy , which may be the focus aspects .It is nec-essary to establish a continuous improvement of performance inspection system , improve the construction of echelon personnel and drive mechanism, and strengthen the scientific research cooperation inside and outside the team in hospital pharmacy researches .Conclu-sion:The scientific researches on hospital pharmacy are very important to develop pharmacy , which are worthy of further exploration .
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Objective To explore the effects of volatile oil and 2-undecanone from Houttuynia Cordata Thunb. (H. cordata) on LPS-TLR4 / MD-2-TNF-α signaling pathway. Methods TLR4 / MD-2 blocking agent was used to mask the TLR4 /MD-2 site,then protein expression levels of TLR4 in cells treated with volatile oil and 2-undecanone were analyzed by western blot. ELISA was used to detect the secretion of the inflammatory cytokines such as TNF-α,IL-1β and IL-10. Comparison analysis was then performed from the results of cell experiments in vitro and anti-inflammatory effects through xylene-induced ear edema test in vivo. Results In concentrations between 1 to 10 μg · mL-1 ,Houttuynia volatile oil showed better effect than 2-undecanone on inhibition of TLR4 protein in LPS-induced RAW264. 7 cells, and had some differences in the effects on inflammatory factors. Compared with the LPS+TLR4 / MD-2 group,the LPS+TLR4 / MD-2 + volatile oil group had no significant difference in the expression of TLR4 protein (P>0. 05),but the LPS+TLR4 / MD-2 +2-undecanone group reduced the expression of TLR4 protein obviously. It appeared that volatile oil exerts its anti-inflammatory effect through LPS-TLR4 / MD-2-TNF-αpathway,but 2-undecanone may exert its anti-inflammatory effect by other means. Houttuynia volatile oil showed better anti-inflammatory activity than 2-undecanone in vivo at the same dose. Conclusion There are some differences in anti-inflammatory effects and related mechanisms between volatile oil and 2-undecanone, probably owing to the synergistic effects of multi-ingredients in the volatile oil.
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This study examined the anti-viral effect of ursolic acid on guinea pig cytomegalovirus (GPCMV) and explored the steps of viral replication targeted by ursolic acid. Cytopathic effect assay and MTT method were employed to determine the 50% cellular cytotoxicity (CC(50)), 50% effective concentration (EC(50)) and therapeutic index (TI) with GPCMV. To investigate the specific anti-viral effect of ursolic acid at different temperatures and time points, two other medicines, ganciclovir and Jinyebaidu (JYBD), serving as controls, were studied for comparison. Our results showed that the CC50 of ganciclovir, JYBD and ursolic acid were 333.8, 3015.6, 86.7 μg/mL, respectively; EC(50) of ganciclovir, JYBD and ursolic acid was 48.1, 325.5 and 6.8 μg/mL, respectively; TI of ganciclovir, JYBD and ursolic acid was 7, 9, 13, respectively. Similar with ganciclovir, ursolic acid could inhibit the viral synthesis, but did not affect the viral adsorption onto and penetration into cells. We are led to conclude that the anti-cytomegalovirus effect of ursolic acid is significantly stronger than ganciclovir or JYBD, and the cytotoxic effect of ursolic acid lies in its ability to inhibit viral synthesis.
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Animals , Antiviral Agents , Pharmacology , Cells, Cultured , Guinea Pigs , Roseolovirus , Triterpenes , PharmacologyABSTRACT
This study examined the anti-viral effect of ursolic acid on guinea pig cytomegalovirus (GPCMV) and explored the steps of viral replication targeted by ursolic acid. Cytopathic effect assay and MTT method were employed to determine the 50% cellular cytotoxicity (CC(50)), 50% effective concentration (EC(50)) and therapeutic index (TI) with GPCMV. To investigate the specific anti-viral effect of ursolic acid at different temperatures and time points, two other medicines, ganciclovir and Jinyebaidu (JYBD), serving as controls, were studied for comparison. Our results showed that the CC50 of ganciclovir, JYBD and ursolic acid were 333.8, 3015.6, 86.7 μg/mL, respectively; EC(50) of ganciclovir, JYBD and ursolic acid was 48.1, 325.5 and 6.8 μg/mL, respectively; TI of ganciclovir, JYBD and ursolic acid was 7, 9, 13, respectively. Similar with ganciclovir, ursolic acid could inhibit the viral synthesis, but did not affect the viral adsorption onto and penetration into cells. We are led to conclude that the anti-cytomegalovirus effect of ursolic acid is significantly stronger than ganciclovir or JYBD, and the cytotoxic effect of ursolic acid lies in its ability to inhibit viral synthesis.
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<p><b>OBJECTIVE</b>To study the in vitro anti-human cytomegalovirus effect and the cytotoxicity of Forsythia suspensa and its main active ingredient quercetin.</p><p><b>METHOD</b>The 0% toxic dose (TD0), minimum effective concentration (MEC) and therapeutic index (TI) of anti-human cytomegalovirus activity by F. suspensa and quercetin were detected with the cytopathic assay and MTT method. Ganciclovir was used as the control drug for comparison.</p><p><b>RESULT</b>The TD0 of ganciclovir, F. suspensa and quercetin were 10, 30, 30 mg L(-1), the MEC were 10, 30, 0.3 mg x L(-1), TI were 1, 1 and 100, respectively.</p><p><b>CONCLUSION</b>The anti-human cytomegalovirus effect of quercetin is much higher than ganciclovir and F. suspensa, and the cytotoxicity is equivalent to F. suspensa but lower than ganciclovir. Therefore, quercetin has the potential advantages of anti-human cytomegalovirus effect.</p>
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Humans , Antiviral Agents , Pharmacology , Toxicity , Cell Line , Cytomegalovirus , Drugs, Chinese Herbal , Pharmacology , Toxicity , Forsythia , Chemistry , Quercetin , Pharmacology , ToxicityABSTRACT
Radix Isatidis (Banlangen in Chinese), used to clearing away heat and toxic material, is a traditional Chinese medicinal (TCM) herb. It is frequently used for preventing and treating infectious diseases caused by viruses. To provide scientific basis for the effect of Radix Isatidis on infectious diseases, the traditional effect and new research development on pharmacological activities are summarized in the review. According to the existed problems in the clinical application, the weak links and shortages of quality research and industrialized production of Radix Isatidis are discussed. It could present the new ideas for improving the technology of Radix Isatidis preparation, and promoting the rational use of the preparation in the clinical treatment.
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Animals , Humans , Communicable Disease Control , Methods , Communicable Diseases , Drug Therapy , Virology , Drugs, Chinese Herbal , Therapeutic Uses , Medicine, Chinese Traditional , Methods , Viruses , VirulenceABSTRACT
To investigate the effect of the anti-endotoxic part of Radix Isatidis on the expression of moesin mRNA in murine tissues induced by lipopolysaccharide (LPS), the sample solution of F(022) part from Radix Isatidis was intraperitoneally administered to experimental mice, and the lipopoly-saccharide (LPS) were injected into the tail vein, and then the tissues of liver, kidney and spleen were colleted and cut into slices. The mRNA was detected by moesin mRNA hybridization in situ. The staining results were observed under microscope. It was found that moesin mRNA expression was increased in the tissues of liver, kidndy and spleen in mice treated with LPS, while in the mice pre-treated with F(022) part from Radix Isatidis, the LPS-induced moesin mRNA expressions in these tissues were inhibited in a dose-dependant manner. Our study showed that F(022) part from Radix Isatidis can inhibit the LPS-induced expression of moesin mRNA in the tissues of liver, kidney and spleen in mice.
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To investigate the effect of the anti-endotoxic part of Radix lsatidis on the expression of moesin mRNA in murine tissues induced by lipopolysaccharide (LPS), the sample solution of F022 part from Radix lsatidis was intraperitoneally administered to experimental mice, and the lipopolysaccharide (LPS) were injected into the tail vein, and then the tissues of liver, kidney and spleen were colleted and cut into slices. The mRNA was detected by moesin mRNA hybridization in situ. The staining results were observed under microscope. It was found that moesin mRNA expression was increased in the tissues of liver, kidndy and spleen in mice treated with LPS, while in the mice pre-treated with F022 part from Radix Isatidis, the LPS-induced moesin mRNA expressions in these tissues were inhibited in a dose-dependant manner. Our study showed that F022 part from Radix Isatidis can inhibit the LPS-induced expression of moesin mRNA in the tissues of liver, kidney and spleen in mice.
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To find a component with the strongest anti-endotoxin effect from the four components (F021, F022, F023, and F024) of chloroform extract (F02) of Radix Isatidis, the protective effects of the five components on endotoxin-challenged mice and their effects on the production of TNFalpha and IL-6 by macrophages from the endotoxin-challenged mice were compared. It was found that the five components all had protective effects on endotoxin-challenged mice in terms of mortality. The mortalities of the mice challenged by 2.42 mg/kg endotoxin were 30 %, 50 %, 20 %, 50 % and 60 % after treatment with F02, F021, F022, F023, and F024. The 5 components all had inhibitory effects on the production of TNFalpha and IL-6 by macrophages from the mice. At a concentration of LPS of 50 ng/mL, the inhibitory rates of F02 , F021 1, F022, F023, and F024 for the production of TNFalpha and IL-6 were 76.54 %, 30.86 %, 78.60 %, 36.63 %, 2.06 % and 75.85 %, 18.45 %, 77.68 %, 24.41 %, 3.64% and at the dose of 100 ng/mL, the inhibitory rates were 49.65 Y, 16.86 %, 66.97 %, 13.39 %, 7.16 % and 59.78 %, 1.28 %, 61.86 %, 2.08 %, 1.44 %, respectively. It is concluded that the component F022 of Radix Isatidis has the strongest anti-endotoxin effect.
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To find a component with the strongest anti-endotoxin effect from the four components (F021 , F022, F023, and F024 ) of chloroform extract (F02) of Radix Isatidis, the protective effects of the five components on endotoxin-challenged mice and their effects on the production of TNFα and IL-6 by macrophages from the endotoxin-challenged mice were compared. It was found that the five components all had protective effects on endotoxin-challenged mice in terms of mortality. The mortalities of the mice challenged by 2.42 mg/kg endotoxin were 30 %, 50 %, 20 %, 50 % and 60 %after treatment with F02, E021 , F022, F023, and F024. The 5 components all had inhibitory effects on the production of TNFα and IL-6 by macrophages from the mice. At a concentration of LPS of 50 ng/mL, the inhibitory rates of F02 , F021 1, F022 , F023 , and F024 for the production of TNFα and IL-6were 76.54 %, 30.86 %, 78. 60 %, 36.63 %, 2.06 % and 75.85 %, 18. 45 %, 77.68 %, 24.41%, 3.64% and at the dose of 100 ng/mL, the inhibitory rates were 49.65 %, 16.86 %, 66.97 %, 13.39 %, 7.16 % and 59.78 %, 1.28 %, 61.86 %, 2.08 %, 1.44 %, respectively. It is concluded that the component F022 of Radix Isatidis has the strongest anti-endotoxin effect.
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The effects of active antiendotoxin chemical fraction isolated from Radix Isatidis (fraction D) on TNF-α and IL-8 secretion in HL-60 cells induced by lipopolysaccharide (LPS) were studied. The appropriate densities of cell suspension and fraction D solution were determined by MTT colorimetric method. Fraction D and LPS were added to HL-60 cell suspension with three different methods respectively. The contents of TNF-α and IL-8 in the cultured supernatant induced by LPS were detected by using ELISA method. The results showed that the absorbance (A) was directly proportional to the number of cells and the linearity was good in the range from 0.25 × 105 to 2 ×105 cell/mL cell suspension. The fraction D significantly inhibited the oversecretion of TNF-α and IL-8 in HL-60 cells induced by LPS at the concentration of 7. 812 mg/mL which had no cytotoxicity. It was indicated that the antiendotoxin mechanism of the active fraction from Radix Isatidis was contributed to the inhibition of the oversecretion of cytokines induced by LPS.
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OBJECTIVE:To extract and purify organic acids with macroporous resins from Folium Isatidis.METHODS:Folium Isatidis was extracted with 70% aqueous ethanol(pH=2)by Soxhlet extraction.The process was optimized by employing orthogonal test design with the content of anthranilic acid as the index.RESULTS:The resin HPD100 had much better adsorption capacity and desorption ratio by using 3 BV 60% aqueous ethanol to extract organic acids in Folium Isatidis than other resins.The results showed that HPD100 possessed the better ecomic under the concentration of sample 0.18mg?mL-1,the condition of pH 3.5,and flowing rate of 2BV?h-1.CONCLUSION:Macroporous resin HPD100 may be value of isolating and purifying the organic acids from Folium Isatidis.
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In order to investigate the immunoactivity of Lycium Barbarum glycopeptide (LBG), the routinely prepared murine splenic lymphocyte suspension was separately added into the samples with different concentrations (500, 100, 10, 1 microg/ml) of LBG as LBG groups. Blank control group in the absence of Lycium Barbarum glycopeptide or ConA and positive control group in the presence of 0.5 ml ConA but in the absence of LBG were created. 0.5 ml LBG samples with different concentrations in combination with 0. 5 ml ConA (10 microg/ml) into each well to observe the synergic effects of LBG and ConA as LBG+ConA groups. After incubation for 72 h at 37 degrees C, the samples were analyzed by CFSE-labeled cells combined with flow cytometry, and MTT. Flow cytometry revealed that both LBG could enhance the murine splenic lymphocyte proliferative reaction. Combined use of LBG and ConA had synergic effects. MTT demonstrated that sample A could obviously promote the murine splenic lymphocyte proliferative reaction as compared with control group (P<0. 01), while sample B could also enhance the lymphocyte proliferation at a high dose. In combination with ConA, sample A had synergic effects at high dose, while sample B showed obviously synergic effects (P<0.05). It was concluded that both samples (A and B) had strong immunocompetence.
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Animals , Male , Mice , Cell Proliferation , Cells, Cultured , Drugs, Chinese Herbal , Pharmacology , Glycopeptides , Pharmacology , Interleukin-2 , Lycium , Chemistry , Lymphocyte Activation , Lymphocytes , Cell Biology , Allergy and Immunology , Mice, Inbred BALB C , Spleen , Cell BiologyABSTRACT
The anti-endotoxic effect of syringic acid (SA) isolated from Radix Isatidis (Banlangen, BLG) was studied. SA was extracted and isolated from BLG and diluted into 1% solution. The content of SA-pretreated endotoxin (ET) was quantitatively determined using Limulus test. The ability of fever induction of ET pretreated with SA was measured using endotoxin-induced fever test in rabbits. The LPS-induced death in mice pretreated with and without SA was compared. Results showed that after pretreatment with SA, 83.16% of ET was destroyed, the ET-induced fever in rabbits relieved markedly and the LPS-induced death rate in mice dropped from 68% to 20%. It was concluded that SA isolated from BLG had anti-endotoxic effects.
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Animals , Female , Male , Mice , Rabbits , Drugs, Chinese Herbal , Pharmacology , Endotoxemia , Blood , Endotoxins , Escherichia coli , Gallic Acid , Pharmacology , Isatis , Chemistry , Limulus Test , Plant Roots , ChemistryABSTRACT
The anti-endotoxic effect of syringic acid (SA) isolated from Radix Isatidis (Banlangen, BLG) was studied. SA was extracted and isolated from BLG and diluted into 1% solution. The content of SA-pretreated endotoxin (ET) was quantitatively determined using Limulus test. The ability of fever induction of ET pretreated with SA was measured using endotoxin-induced fever test in rabbits. The LPS-induced death in mice pretreated with and without SA was compared. Results showed that after pretreatment with SA, 83.16% of ET was destroyed, the ET-induced fever in rabbits relieved markedly and the LPS-induced death rate in mice dropped from 68% to 20%. It was concluded that SA isolated from BLG had anti-endotoxic effects.
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Drugs, Chinese Herbal/pharmacology , Endotoxemia/blood , Endotoxins/antagonists & inhibitors , Escherichia coli , Gallic Acid/analogs & derivatives , Gallic Acid/pharmacology , Isatis/chemistry , Limulus Test , Plant Roots/chemistryABSTRACT
OBJECTIVE:To apply the kinetic turbidimetric Limulus test to the endotoxin assay of Levocarnitine sodium chloride injection.METHODS:The16-fold dilution of Levocarnitine sodium chloride injection was prepared.The content of bacterial endotoxin in Levocarnitine sodium chloride injection was determined with kinetic turbidimetric Limulus test after screen test and validation test.RESULTS:The16-fold dilution of Levocarnitine sodium chloride injection was effective to e?liminate the interference in Limulus test.The average recovery was in the range of50%～200%.CONCLUSION:The kinetic turbidimetric Limulus test provides a new and quick method for the quantitative determination of bacterial endotoxin in Levo?carnitine sodium chloride injection.
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OBJECTIVE:To explore the way out for the continuing development of hospital preparations.METHODS:We analyzed the current situation of hospital preparations and the existing problems in pharmaceutical research related to hospital preparations and discussed the feasible developmental direction of hospital preparations.RESULTS:To achieve a continuing development for hospital preparations,hospitals have to improve their current technology for preparations,closely combine the characteristics of hospitals to prepare preparations targeted to the needs of the clinic,shift to the development of new drugs on the basis of the existing preparations and carry out pharmaceutical work and basic study closely related to clinical pharmacy.CONCLUSION:Transformation from a simple supply type to a technology-based supply type and exploitation research type will be a feasible trend for the development of hospital preparations.