2017 Vol. 35, No. 4
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2017, 35(4): 289-293.
doi: 10.3969/j.issn.1006-0111.2017.04.001
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The TNF-α signaling pathway is a valuable target in the therapy of autoimmune diseases. TNF-α binds to two different receptors and exerts anti-inflammatory and anti-rheumatic effects. The drugs of anti-TNF-α are widely used in rheumatoid arthritis, such as infliximab, adalimumab etc. These TNF blockers have become invaluable tools to reduce damages induced by inflammation and allow recovery of the affected tissues. Unfortunately, this therapy has some drawbacks, such as increasing the risk of infection, malignancy and the incidence rate of new auto-immune diseases. Some of these effects are caused by the unwanted abrogation of beneficial TNF signaling. Therefore, elective antagonism of TNFR is an important approach to alleviate the side effects of TNF-α antibody. The medications specifically targeting the TNFR might have better applicability and safety. In this article, research progresses of TNF-α and its receptors in the therapy of rheumatoid arthritis were reviewed.
The TNF-α signaling pathway is a valuable target in the therapy of autoimmune diseases. TNF-α binds to two different receptors and exerts anti-inflammatory and anti-rheumatic effects. The drugs of anti-TNF-α are widely used in rheumatoid arthritis, such as infliximab, adalimumab etc. These TNF blockers have become invaluable tools to reduce damages induced by inflammation and allow recovery of the affected tissues. Unfortunately, this therapy has some drawbacks, such as increasing the risk of infection, malignancy and the incidence rate of new auto-immune diseases. Some of these effects are caused by the unwanted abrogation of beneficial TNF signaling. Therefore, elective antagonism of TNFR is an important approach to alleviate the side effects of TNF-α antibody. The medications specifically targeting the TNFR might have better applicability and safety. In this article, research progresses of TNF-α and its receptors in the therapy of rheumatoid arthritis were reviewed.
2017, 35(4): 294-297,345.
doi: 10.3969/j.issn.1006-0111.2017.04.002
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The incident number and death toll of cardio-cerebrovascular diseases increase continuously in China. The impairment of arterial baroreflex (ABR) is closely related to the genesis and development of cardio-cerebrovascular diseases (such as hypertension and chronic heart failure). Barostim neoTM (by American CRVx. Inc) can reduce blood pressure and heart rate by electrically stimulating carotid sinus baroreceptors and activating baroreflex. Therefore, it can be used to treat resistant hypertension, heart failure and end-stage renal disease, etc. The mechanism of baroreflex activation therapy (BAT) includes inhibiting sympathetic nervous system and rennin-angiotensin system, and increasing the activity of vagus nerve. Thus it improves baroreflex sensitivity and heart rate variability, and restores the structure and function of key organs.
The incident number and death toll of cardio-cerebrovascular diseases increase continuously in China. The impairment of arterial baroreflex (ABR) is closely related to the genesis and development of cardio-cerebrovascular diseases (such as hypertension and chronic heart failure). Barostim neoTM (by American CRVx. Inc) can reduce blood pressure and heart rate by electrically stimulating carotid sinus baroreceptors and activating baroreflex. Therefore, it can be used to treat resistant hypertension, heart failure and end-stage renal disease, etc. The mechanism of baroreflex activation therapy (BAT) includes inhibiting sympathetic nervous system and rennin-angiotensin system, and increasing the activity of vagus nerve. Thus it improves baroreflex sensitivity and heart rate variability, and restores the structure and function of key organs.
2017, 35(4): 298-300,314.
doi: 10.3969/j.issn.1006-0111.2017.04.003
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In recent years, with the wide use of antimicrobial agents, the adverse reactions related to antimicrobial agents have attracted more and more attention.Among them, the adverse reactions in hematological system induced by antibacterial agents seriously affect patient's health and doctor's selection for antibiotics.For example, some beta lactam antibiotics can cause dysfunction of coagulation and hemolytic anemia.Chloramphenicol and sulfonamides can cause aplastic anemia.Linezolid can cause thrombocytopenia and anemia.It is important to understand the adverse reactions in hematological system caused by antibiotics.In this paper, the antibiotic induced adverse reactions in hematological system and their mechanism were summarized in order to provide information for the rational use of antimicrobial agents.
In recent years, with the wide use of antimicrobial agents, the adverse reactions related to antimicrobial agents have attracted more and more attention.Among them, the adverse reactions in hematological system induced by antibacterial agents seriously affect patient's health and doctor's selection for antibiotics.For example, some beta lactam antibiotics can cause dysfunction of coagulation and hemolytic anemia.Chloramphenicol and sulfonamides can cause aplastic anemia.Linezolid can cause thrombocytopenia and anemia.It is important to understand the adverse reactions in hematological system caused by antibiotics.In this paper, the antibiotic induced adverse reactions in hematological system and their mechanism were summarized in order to provide information for the rational use of antimicrobial agents.
2017, 35(4): 301-303,333.
doi: 10.3969/j.issn.1006-0111.2017.04.004
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Monoclonal antibodies have become an important part of biotechnology and pharmaceutical industry. Currently chimeric antibody, humanized antibody and fully human antibody are generally prepared by genetic engineering. With constant improvement in the antibody preparation technology, the antibody applications are rapidly increasing, especially in the development of antibody medications. In recent years, there have been many significant antibody drugs (such as PD-1 antibody, IL-17 antibody, IL-5 antibody, PCSK9 antibody) for the treatment of various diseases and solved a number of clinical problems. In modern medicine, monoclonal antibodies have become effective diagnostic and therapeutic tools. This article is a brief review of the recent antibody development process, clinic applications and significant antibody drugs approved by FDA.
Monoclonal antibodies have become an important part of biotechnology and pharmaceutical industry. Currently chimeric antibody, humanized antibody and fully human antibody are generally prepared by genetic engineering. With constant improvement in the antibody preparation technology, the antibody applications are rapidly increasing, especially in the development of antibody medications. In recent years, there have been many significant antibody drugs (such as PD-1 antibody, IL-17 antibody, IL-5 antibody, PCSK9 antibody) for the treatment of various diseases and solved a number of clinical problems. In modern medicine, monoclonal antibodies have become effective diagnostic and therapeutic tools. This article is a brief review of the recent antibody development process, clinic applications and significant antibody drugs approved by FDA.
2017, 35(4): 304-307.
doi: 10.3969/j.issn.1006-0111.2017.04.005
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Objective To screen the active compounds targeting lung cancer stem cells (LCSCs) from the sponge Aaptos aaptos. Methods The A549-Nanog-GFP model of LCSCs was constructed. Western blot and immunofluorescence were used to examine the expression of pluripotency markers in screening model. The established LCSCs model was used to screen 8 fractions of Aaptos aaptos dichloromethane extract. The active fraction was separated by various chromatographic methods. CCK8 assay was used to screen the compounds for anti-LCSCs activity in vitro. Results LCSCs model with high expression of CD44 and ALDH1A1 protein was successfully constructed. The fraction D6 showed significant inhibitory activity in LCSCs(P<0.01). Four aaptamine alkaloids were isolated from this fraction. Compound AP-1 has good activity against LCSCs(P<0.01)with IC50 value(3.84±0.12) μmol/L. Conclusion AP-1 isolated from the sponge Aaptos aaptos exhibited significant activity against LCSCs.
Objective To screen the active compounds targeting lung cancer stem cells (LCSCs) from the sponge Aaptos aaptos. Methods The A549-Nanog-GFP model of LCSCs was constructed. Western blot and immunofluorescence were used to examine the expression of pluripotency markers in screening model. The established LCSCs model was used to screen 8 fractions of Aaptos aaptos dichloromethane extract. The active fraction was separated by various chromatographic methods. CCK8 assay was used to screen the compounds for anti-LCSCs activity in vitro. Results LCSCs model with high expression of CD44 and ALDH1A1 protein was successfully constructed. The fraction D6 showed significant inhibitory activity in LCSCs(P<0.01). Four aaptamine alkaloids were isolated from this fraction. Compound AP-1 has good activity against LCSCs(P<0.01)with IC50 value(3.84±0.12) μmol/L. Conclusion AP-1 isolated from the sponge Aaptos aaptos exhibited significant activity against LCSCs.
2017, 35(4): 308-314.
doi: 10.3969/j.issn.1006-0111.2017.04.006
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Objective To investigate the chemical constituents of marine sponge Mycale sp. collected from the South China Sea. Methods The ethyl acetate extract of the marine sponge Mycale sp. was separated and purified by repeated column chromatography on silica gel, Sephadex LH-20 and reversed-phase high-performance liquid chromatography (RP-HPLC). The structures of these compounds were identified by means of various modern spectroscopic techniques and comparison with their physicochemical properties to reported data. The tumor cell growth inhibitory activities of these compounds against human breast cancer cell lines MCF-7 and human lung cancer cell lines PC9 were tested by Cell Counting Kit-8 (CCK-8) method. Results Ten compounds were isolated and identified as cyclo-(Pro-Ile)( 1 ),cyclo-(Pro-Leu)( 2 ),cyclo-(Ile-Leu)( 3 ),cyclo-(Phe-Pro)( 4 ),cyclo-(Phe-Val)( 5 ),cyclo-(Phe-Leu)( 6 ),cyclo-(Phe-Ile)( 7 ), 2'-deoxythymidine ( 8 ), thymine ( 9 ), 5-hydroxy-3,4-dimethyl-5-pentyl-2(5H)-furanone ( 10 ). These compounds showed weak tumor cell growth inhibitory activities toward cells MCF-7 and PC9 in vitro. Conclusion Compounds 1 , 2 , 4 , 5 , 6 , 7 and 10 were isolated from the sponge Mycale sp. for the first time. It is the first time to report the antitumor activity evaluation for compounds 1 ~ 10 .
Objective To investigate the chemical constituents of marine sponge Mycale sp. collected from the South China Sea. Methods The ethyl acetate extract of the marine sponge Mycale sp. was separated and purified by repeated column chromatography on silica gel, Sephadex LH-20 and reversed-phase high-performance liquid chromatography (RP-HPLC). The structures of these compounds were identified by means of various modern spectroscopic techniques and comparison with their physicochemical properties to reported data. The tumor cell growth inhibitory activities of these compounds against human breast cancer cell lines MCF-7 and human lung cancer cell lines PC9 were tested by Cell Counting Kit-8 (CCK-8) method. Results Ten compounds were isolated and identified as cyclo-(Pro-Ile)( 1 ),cyclo-(Pro-Leu)( 2 ),cyclo-(Ile-Leu)( 3 ),cyclo-(Phe-Pro)( 4 ),cyclo-(Phe-Val)( 5 ),cyclo-(Phe-Leu)( 6 ),cyclo-(Phe-Ile)( 7 ), 2'-deoxythymidine ( 8 ), thymine ( 9 ), 5-hydroxy-3,4-dimethyl-5-pentyl-2(5H)-furanone ( 10 ). These compounds showed weak tumor cell growth inhibitory activities toward cells MCF-7 and PC9 in vitro. Conclusion Compounds 1 , 2 , 4 , 5 , 6 , 7 and 10 were isolated from the sponge Mycale sp. for the first time. It is the first time to report the antitumor activity evaluation for compounds 1 ~ 10 .
2017, 35(4): 315-320,382.
doi: 10.3969/j.issn.1006-0111.2017.04.007
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Objective To investigate the chemical constituents in the marine sponge, Spongia sp., collected from the Xisha Islands. Methods The pure chemical components from the petroleum ether extract of Spongia sp.were obtained by repeated column chromatography on silica gel,ODS,Sephadex LH-20 and semi-preparative HPLC.Their structures were determined by spectroscopic analysis and comparison with the reported data.The antifungal activity of those compounds was evaluated by dilution method. Results 9 compounds were isolated and identified,including smenodiol( 1 ),smenospongorine( 2 ),5-epi-smenospongorine( 3 ),dictyoceratin C( 4 ),epi-smenospongidine( 5 ),dictyoceratin A( 6 ),stigmasta-4,6,8(14),22-tetraen-3-one( 7 ),3-oxo-4,6,8(14)-triunsaturated steroids( 8 ),ergosta-4,6,8(14),22-tetraen-3-one( 9 ). Conclusion Compounds 1 ~ 9 were isolated from the sponge of genus spongia for the first time.Compound 2 、 3 、 5 and 9 exhibited antifungal activities against Candida albicans,Trichophyton mentaqrophytes and Trichophyton rubrum with the MIC values of 12.5~25 μg/ml.
Objective To investigate the chemical constituents in the marine sponge, Spongia sp., collected from the Xisha Islands. Methods The pure chemical components from the petroleum ether extract of Spongia sp.were obtained by repeated column chromatography on silica gel,ODS,Sephadex LH-20 and semi-preparative HPLC.Their structures were determined by spectroscopic analysis and comparison with the reported data.The antifungal activity of those compounds was evaluated by dilution method. Results 9 compounds were isolated and identified,including smenodiol( 1 ),smenospongorine( 2 ),5-epi-smenospongorine( 3 ),dictyoceratin C( 4 ),epi-smenospongidine( 5 ),dictyoceratin A( 6 ),stigmasta-4,6,8(14),22-tetraen-3-one( 7 ),3-oxo-4,6,8(14)-triunsaturated steroids( 8 ),ergosta-4,6,8(14),22-tetraen-3-one( 9 ). Conclusion Compounds 1 ~ 9 were isolated from the sponge of genus spongia for the first time.Compound 2 、 3 、 5 and 9 exhibited antifungal activities against Candida albicans,Trichophyton mentaqrophytes and Trichophyton rubrum with the MIC values of 12.5~25 μg/ml.
2017, 35(4): 321-324,366.
doi: 10.3969/j.issn.1006-0111.2017.04.008
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Objective To prepare an in situ gel system for nasal delivery of menthol and to evaluate the safety of this formulation. Methods Menthol in situ gel was prepared with deacetylatedgellan gum. The nasal mucocilia toxicities of this formulation was evaluated using in situ toad palate model.Guinea pig skin sensitization test and the rabbit skin irritation test were conducted. Skin allergy and irritation reaction were monitored and scored. Results No significant effect on nasal mucosa ciliary movement and the morphology of rat nasal mucosa were observed.The formulation did not induce any dermal irritation in rabbits. Skin allergic reaction was not found in guinea pigs. Conclusion The preparation of menthol in situ nasal gel with low ciliary toxicity was easily achieved. This gel has good physiological flexibility.The further investigation was warranted for this formulation as an intranasal drug delivery system.
Objective To prepare an in situ gel system for nasal delivery of menthol and to evaluate the safety of this formulation. Methods Menthol in situ gel was prepared with deacetylatedgellan gum. The nasal mucocilia toxicities of this formulation was evaluated using in situ toad palate model.Guinea pig skin sensitization test and the rabbit skin irritation test were conducted. Skin allergy and irritation reaction were monitored and scored. Results No significant effect on nasal mucosa ciliary movement and the morphology of rat nasal mucosa were observed.The formulation did not induce any dermal irritation in rabbits. Skin allergic reaction was not found in guinea pigs. Conclusion The preparation of menthol in situ nasal gel with low ciliary toxicity was easily achieved. This gel has good physiological flexibility.The further investigation was warranted for this formulation as an intranasal drug delivery system.
2017, 35(4): 325-327,349.
doi: 10.3969/j.issn.1006-0111.2017.04.009
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Objective To prepare diosmin suppository and establish a method for its quality control. Methods Diosmin was used as active ingredient. Polyethylene glycol 6000, polyethylene glycol 400 and glycerol were chosen as substrates. Fusion method was applied to prepare the diosmin suppository. The appearance, content uniformity, weight variation and melting time of suppository were evaluated. Results The diosmin suppository has brown color with good hardness at room temperature. The content uniformity, weight variation, melting time and dissolution rate meet the requirements of quality control. Conclusion The diosmin suppository prepared by this method was satisfied the quality requirements of suppository and serves as a new formulation of diosmin.
Objective To prepare diosmin suppository and establish a method for its quality control. Methods Diosmin was used as active ingredient. Polyethylene glycol 6000, polyethylene glycol 400 and glycerol were chosen as substrates. Fusion method was applied to prepare the diosmin suppository. The appearance, content uniformity, weight variation and melting time of suppository were evaluated. Results The diosmin suppository has brown color with good hardness at room temperature. The content uniformity, weight variation, melting time and dissolution rate meet the requirements of quality control. Conclusion The diosmin suppository prepared by this method was satisfied the quality requirements of suppository and serves as a new formulation of diosmin.
2017, 35(4): 328-333.
doi: 10.3969/j.issn.1006-0111.2017.04.010
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Objective To develop a method for determination of iridoid glycosides in Morinda of ficinalis How. and optimize the extraction methods for iridoid glycosides in Morinda of ficinalis How. Methods The iridoid glycosides, including monotropein, deacetyl asperulosidic acid,asperulosidic acid and asperuloside as standards, HPLC method was developed to determine the content of iridoid glycosides in Morinda of ficinalis How. The separation was performed on Venusil MP C18 (250 mm×4.6 mm, 5 μm) column. The mobile phase was acetonitrile (A)-0.2% phosphoric acid and 0.01 disodium hydrogen phosphate buffer salt (B) with gradient elution (0-12 min, 1%-2% A; 12-30 min, 2%-25% A). The detection wavelength was 235 nm. The flow rate was set at 1.0 ml/min and the column temperature at 25 ℃. The injection volume was 20 μl. Single factor analysis and orthogonal test were used to optimize extraction method of iridoid glycosides in Morinda of ficinalis How. Results Monotropein, deacetyl asperulosidic acid, asperulosidic acid and asperuloside showed good linearity (r>0.999 5) in the ranges of 0.375-12 μg, 0.13-4.16 μg, 0.016-0.516 μg and 0.012-0.384 μg, respectively. This validated method has good repeatability, precision, recovery and stability. It was conformed to meet the requirements and regulation. The optimal extraction method included soaking the raw materials with 16 times of 10% ethanol for 9 h, and then extraction by percolation with the flow rate of 0.8 BV/h. Conclusion The HPLC method sensitively and precisely determined the content of iridoid glycosides in Morinda of ficinalis How. The optimized extraction method extracted these constituents effectively.
Objective To develop a method for determination of iridoid glycosides in Morinda of ficinalis How. and optimize the extraction methods for iridoid glycosides in Morinda of ficinalis How. Methods The iridoid glycosides, including monotropein, deacetyl asperulosidic acid,asperulosidic acid and asperuloside as standards, HPLC method was developed to determine the content of iridoid glycosides in Morinda of ficinalis How. The separation was performed on Venusil MP C18 (250 mm×4.6 mm, 5 μm) column. The mobile phase was acetonitrile (A)-0.2% phosphoric acid and 0.01 disodium hydrogen phosphate buffer salt (B) with gradient elution (0-12 min, 1%-2% A; 12-30 min, 2%-25% A). The detection wavelength was 235 nm. The flow rate was set at 1.0 ml/min and the column temperature at 25 ℃. The injection volume was 20 μl. Single factor analysis and orthogonal test were used to optimize extraction method of iridoid glycosides in Morinda of ficinalis How. Results Monotropein, deacetyl asperulosidic acid, asperulosidic acid and asperuloside showed good linearity (r>0.999 5) in the ranges of 0.375-12 μg, 0.13-4.16 μg, 0.016-0.516 μg and 0.012-0.384 μg, respectively. This validated method has good repeatability, precision, recovery and stability. It was conformed to meet the requirements and regulation. The optimal extraction method included soaking the raw materials with 16 times of 10% ethanol for 9 h, and then extraction by percolation with the flow rate of 0.8 BV/h. Conclusion The HPLC method sensitively and precisely determined the content of iridoid glycosides in Morinda of ficinalis How. The optimized extraction method extracted these constituents effectively.
2017, 35(4): 334-336,370.
doi: 10.3969/j.issn.1006-0111.2017.04.011
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Objective To test the acute toxicity and determine the safe dose range of Moringa oleifera leaves and seeds. Methods Acute toxicity tests were performed based on the documented experimental designs in Research Methods of Pharmacology of Chinese Traditional Medicine. Results The maximum tolerated dose of the superfine powder and alcoholic-aqueous extract of Moringa oleifera leaves were 0.4 g/20 g and 0.8 g/20 g for mice. The safe dose for human is under or equal to 10 g/50 kg and 20 g/50 kg. Conclusion Moringa oleifera leaves were safe for medical and food use. The further research and development is warranted for this plant.
Objective To test the acute toxicity and determine the safe dose range of Moringa oleifera leaves and seeds. Methods Acute toxicity tests were performed based on the documented experimental designs in Research Methods of Pharmacology of Chinese Traditional Medicine. Results The maximum tolerated dose of the superfine powder and alcoholic-aqueous extract of Moringa oleifera leaves were 0.4 g/20 g and 0.8 g/20 g for mice. The safe dose for human is under or equal to 10 g/50 kg and 20 g/50 kg. Conclusion Moringa oleifera leaves were safe for medical and food use. The further research and development is warranted for this plant.
2017, 35(4): 337-340,358.
doi: 10.3969/j.issn.1006-0111.2017.04.012
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Objective To investigate the effect of Euphorbia helioscopia on MDA-MB-231 cells and its mechanism. Methods The cell viability was detected by MTT assay. The production of ROS in MDA-MB-231 cells was measured by fluorescence microscopy. The apoptotic rate was detected by flow cytometry. Apoptosis DNA fragments were detected by TUNEL assay. Western blot was used to assess the expression of caspase-9, caspase-3 and PARP. Results MTT assay showed that the extract significantly inhibited the viability of MDA-MB-231 cells, which can be diminished by the ROS inhibitor NAC and the caspase inhibitor Z-VAD-FMK. The marked increase in the production of ROS induced by the extract was observed with fluorescence microscopy. Flow cytometry showed that the PI positive staining cells increased significantly after the treatment of the extract, but was diminished by NAC. Caspase-9 and caspase-3 were activated after the treatment of the extract while the PARP was cleaved. TUNEL showed that a significant increase in apoptotic DNA fragmentation induced by the extract, which can be diminished by NAC and Z-VAD-FMK. Conclusion Ethyl acetate extract inhibited the MDA-MB-231 cells and induced apoptosis. The mechanism may involve with the mitochondrial damage due to the excessive ROS.
Objective To investigate the effect of Euphorbia helioscopia on MDA-MB-231 cells and its mechanism. Methods The cell viability was detected by MTT assay. The production of ROS in MDA-MB-231 cells was measured by fluorescence microscopy. The apoptotic rate was detected by flow cytometry. Apoptosis DNA fragments were detected by TUNEL assay. Western blot was used to assess the expression of caspase-9, caspase-3 and PARP. Results MTT assay showed that the extract significantly inhibited the viability of MDA-MB-231 cells, which can be diminished by the ROS inhibitor NAC and the caspase inhibitor Z-VAD-FMK. The marked increase in the production of ROS induced by the extract was observed with fluorescence microscopy. Flow cytometry showed that the PI positive staining cells increased significantly after the treatment of the extract, but was diminished by NAC. Caspase-9 and caspase-3 were activated after the treatment of the extract while the PARP was cleaved. TUNEL showed that a significant increase in apoptotic DNA fragmentation induced by the extract, which can be diminished by NAC and Z-VAD-FMK. Conclusion Ethyl acetate extract inhibited the MDA-MB-231 cells and induced apoptosis. The mechanism may involve with the mitochondrial damage due to the excessive ROS.
2017, 35(4): 341-345.
doi: 10.3969/j.issn.1006-0111.2017.04.013
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Objective To simplify the calculation of T>MIC and evaluate meropenem regimens based on the simple mathematical model of T>MIC reported in literature for two-compartment model. Methods Six meropenem regimens were designed according to the recommended dose with the infusion duration of 0.5 h and 3 h. Four different MIC susceptibility breakpoint of meropenem against clinical microbiologic flora were used to formulate different T>MIC.Each T>MIC was calculated by both the simple and two-compartment model of T>MIC.Meropenem regimens were evaluated for different bacterial infections based on the simple model of T>MIC with 40%~100% of the T>MIC% as the target. The t-test suggested no significant difference between the pairs of T>MIC calculated by the two models. Results and Conclusion Simple model of T>MIC can replace the two-compartment model.Meropenem regimens can be optimized based on this simple model of T>MIC conveniently and quickly.
Objective To simplify the calculation of T>MIC and evaluate meropenem regimens based on the simple mathematical model of T>MIC reported in literature for two-compartment model. Methods Six meropenem regimens were designed according to the recommended dose with the infusion duration of 0.5 h and 3 h. Four different MIC susceptibility breakpoint of meropenem against clinical microbiologic flora were used to formulate different T>MIC.Each T>MIC was calculated by both the simple and two-compartment model of T>MIC.Meropenem regimens were evaluated for different bacterial infections based on the simple model of T>MIC with 40%~100% of the T>MIC% as the target. The t-test suggested no significant difference between the pairs of T>MIC calculated by the two models. Results and Conclusion Simple model of T>MIC can replace the two-compartment model.Meropenem regimens can be optimized based on this simple model of T>MIC conveniently and quickly.
2017, 35(4): 346-349.
doi: 10.3969/j.issn.1006-0111.2017.04.014
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Objective To develop a UPLC-MS method for the determination of pazopanib in rat plasma, and study the pharmacokinetics of pazopanib in rats. Methods The effective UPLC MS/MS separation of the examined compounds was applied on an Acquity BEH C18 column with a gradient mobile phase system. AB Sciex QTRAP 5500 triple quadruple mass spectrometer equipped with an electrospray ionization (ESI) interface was used for mass spectrometric detection. The MRM transitions of m/z 438.3→357.2 and m/z 285.2→193.1 were used to quantify for pazopanib and ISTD, respectively; 6 rats were given 80 mg/kg pazopanib intragastric administration. Blood samples were collected from the tail vein at different point after administration. The concentration of pazopanib in plasma was detected by the UPLC-MS methods. The pharmacokinetics parameters were analyzed by DAS program. Results Pazopanib and ISTD were eluted at 1.10 and 1.37 min respectively. Excellent liner relationship was obtained from the range of 0.25 μg/ml to 40.00 μg/ml (r=0.999 2). The intra-day RSD were 6.17%, 2.73% and 2.54% and inter-day RSD were 7.56%, 5.98% and 2.84% respectively at three concentrations (0.50, 10.00, 30.00 μg/ml), the recoveries were (78.4±4.8)%, (85.9±3.5)% and (81.1±4.2)% respectively, the Matrix effect were (106.7±5.3) %, (101.3±6.7) % and (97.6±4.4) % respectively at three concentrations (0.50, 10.00, 30.00 μg/ml); 6 rats were given 80 mg/kg pazopanib intra-gastric administration. The main pharmacokinetics parameters of pazopanib were as following: cmax (20.22±1.95) μg/ml,tmax (1.75±0.76) h,t1/2 (7.35±2.31) h,AUC0-t (213.16±39.92) μg·h/L,AUC0-∞ (215.79±39.84) μg·h/L,Vd (4.10±1.78) L/kg,CL (0.38±0.07) L/h. Conclusion The method was simple, rapid, accurately,which could be used to determine the pazopanib concentration in rat plasma and study on its pharmacokinetics. Pazopanib was fitted to the first-order elimination kinetics in rats.
Objective To develop a UPLC-MS method for the determination of pazopanib in rat plasma, and study the pharmacokinetics of pazopanib in rats. Methods The effective UPLC MS/MS separation of the examined compounds was applied on an Acquity BEH C18 column with a gradient mobile phase system. AB Sciex QTRAP 5500 triple quadruple mass spectrometer equipped with an electrospray ionization (ESI) interface was used for mass spectrometric detection. The MRM transitions of m/z 438.3→357.2 and m/z 285.2→193.1 were used to quantify for pazopanib and ISTD, respectively; 6 rats were given 80 mg/kg pazopanib intragastric administration. Blood samples were collected from the tail vein at different point after administration. The concentration of pazopanib in plasma was detected by the UPLC-MS methods. The pharmacokinetics parameters were analyzed by DAS program. Results Pazopanib and ISTD were eluted at 1.10 and 1.37 min respectively. Excellent liner relationship was obtained from the range of 0.25 μg/ml to 40.00 μg/ml (r=0.999 2). The intra-day RSD were 6.17%, 2.73% and 2.54% and inter-day RSD were 7.56%, 5.98% and 2.84% respectively at three concentrations (0.50, 10.00, 30.00 μg/ml), the recoveries were (78.4±4.8)%, (85.9±3.5)% and (81.1±4.2)% respectively, the Matrix effect were (106.7±5.3) %, (101.3±6.7) % and (97.6±4.4) % respectively at three concentrations (0.50, 10.00, 30.00 μg/ml); 6 rats were given 80 mg/kg pazopanib intra-gastric administration. The main pharmacokinetics parameters of pazopanib were as following: cmax (20.22±1.95) μg/ml,tmax (1.75±0.76) h,t1/2 (7.35±2.31) h,AUC0-t (213.16±39.92) μg·h/L,AUC0-∞ (215.79±39.84) μg·h/L,Vd (4.10±1.78) L/kg,CL (0.38±0.07) L/h. Conclusion The method was simple, rapid, accurately,which could be used to determine the pazopanib concentration in rat plasma and study on its pharmacokinetics. Pazopanib was fitted to the first-order elimination kinetics in rats.
2017, 35(4): 350-352,384.
doi: 10.3969/j.issn.1006-0111.2017.04.015
Abstract:
Objective To establish the quality standard of Santeng oral solution. Method Sargentodoxa Caulis and Spatholobi Caulis were identified by thin layer chromatography. Chlorogenic acid was assayed by high performance liquid chromatography. The chromatographic column is Agilent Zorbax SB C18 (4.6 mm×250 mm, 5 μm) with a stable temperature of 35 ℃. The mobile phase in isocratic elution consists of acetonitrile and 0.1% folic acid aqueous solution with a preliminary volume ratio of 9∶91. The flow rate is 1.0 ml/min with an injection volume of 20 μl. Results Thin layer chromatography showed distinct spots of Sargentodoxa Caulis and Spatholobi Caulis with a great specificity. A regression formula Y=60.14X－6.37(r>0.999 9) was obtained with a good linearity in concentration range of 2.70~202.50 μg/ml. Conclusion A simple, stable and repeatable method was established for the quality control of Santeng oral solution.
Objective To establish the quality standard of Santeng oral solution. Method Sargentodoxa Caulis and Spatholobi Caulis were identified by thin layer chromatography. Chlorogenic acid was assayed by high performance liquid chromatography. The chromatographic column is Agilent Zorbax SB C18 (4.6 mm×250 mm, 5 μm) with a stable temperature of 35 ℃. The mobile phase in isocratic elution consists of acetonitrile and 0.1% folic acid aqueous solution with a preliminary volume ratio of 9∶91. The flow rate is 1.0 ml/min with an injection volume of 20 μl. Results Thin layer chromatography showed distinct spots of Sargentodoxa Caulis and Spatholobi Caulis with a great specificity. A regression formula Y=60.14X－6.37(r>0.999 9) was obtained with a good linearity in concentration range of 2.70~202.50 μg/ml. Conclusion A simple, stable and repeatable method was established for the quality control of Santeng oral solution.
2017, 35(4): 353-354,378.
doi: 10.3969/j.issn.1006-0111.2017.04.016
Abstract:
Objective To establish a HPLC method for determination of berberine hydrochloride in Dongbai Tonglin Heji. Methods The separation column of Kromasil C18(150 mm×4.6 mm,5 μm) was used. The mobile phase was acetonitrile and 0.05 mol/L NaH2PO4 solution(pH was adjusted to about 3 with phosphoric acid). The flow rate was 1.0 ml/min with the column at room temperature and the detection wavelengths at 345 nm for berberine hydrochloride. Results The linear range of berberine hydrochloride was 1.00~50.00 μg/ml(r=0.999 6). The average recoveries of berberine hydrochloride were 104.70%(RSD 1.60%, n=5). Conclusion This method is accurate, sensitive, selective and reproducible. It provides an alternative method to improve the quality control of Dongbai Tonglin Heji.
Objective To establish a HPLC method for determination of berberine hydrochloride in Dongbai Tonglin Heji. Methods The separation column of Kromasil C18(150 mm×4.6 mm,5 μm) was used. The mobile phase was acetonitrile and 0.05 mol/L NaH2PO4 solution(pH was adjusted to about 3 with phosphoric acid). The flow rate was 1.0 ml/min with the column at room temperature and the detection wavelengths at 345 nm for berberine hydrochloride. Results The linear range of berberine hydrochloride was 1.00~50.00 μg/ml(r=0.999 6). The average recoveries of berberine hydrochloride were 104.70%(RSD 1.60%, n=5). Conclusion This method is accurate, sensitive, selective and reproducible. It provides an alternative method to improve the quality control of Dongbai Tonglin Heji.
2017, 35(4): 355-358.
doi: 10.3969/j.issn.1006-0111.2017.04.017
Abstract:
Objective To establish the quality standard for YI SHI MINGMU granules. Methods TLC method was used to identify Lycium barbarum L and Salvia miltiorrhiza. HPLC method was used to quantitatively analyze the concentration of Tanshinol sodium. The analysis was carried out on a column of Kromasil C18(4.6 mm×150 mm,5 μm)with a mobile phase of methanol and 0.5 % acetic acid at the flow rate of 0.4 ml/min. Column temperature was 30 ℃. The detection wavelength was 280 nm. Results The linearity range of Tanshinol sodium was 2.00~60.00 μg/ml,r2=0.999 7(n=6),with the average recoveries of 105.62%, RSD=1.60%. Conclusion This method is accurate, simple, reliable and reproducible. It can be used for the quality control of YI SHI MINGMU granules.
Objective To establish the quality standard for YI SHI MINGMU granules. Methods TLC method was used to identify Lycium barbarum L and Salvia miltiorrhiza. HPLC method was used to quantitatively analyze the concentration of Tanshinol sodium. The analysis was carried out on a column of Kromasil C18(4.6 mm×150 mm,5 μm)with a mobile phase of methanol and 0.5 % acetic acid at the flow rate of 0.4 ml/min. Column temperature was 30 ℃. The detection wavelength was 280 nm. Results The linearity range of Tanshinol sodium was 2.00~60.00 μg/ml,r2=0.999 7(n=6),with the average recoveries of 105.62%, RSD=1.60%. Conclusion This method is accurate, simple, reliable and reproducible. It can be used for the quality control of YI SHI MINGMU granules.
Determination of madecassoside and asiaticoside in Centella asiatica formula granules by HPLC method
2017, 35(4): 359-361.
doi: 10.3969/j.issn.1006-0111.2017.04.018
Abstract:
Objective To establish a HPLC method for determination of madecassoside and asiaticoside in Centella asiatica formula granules. Methods Chromatographic separation was performed on Ultimate AQ-C18 column(4.6 mm×250 mm,5 μm) with mobile phase of acetonitrile(A)-2 mmol/L β-cyclodextrin(0~30 min:21% A→23% A; 30~60 min:23% A→25% A).The flow rate was set at 1.0 ml/min, the column temperature at 30 ℃ and detection wavelength at 205 nm. Results Madecassoside and asiaticoside showed good linearity (r>0.9995) in the ranges of 0.187 7~3.754 μg and 0.184 3~3.686 μg respectively. The specificity, repeatability, precision,recovery and stability were satisfied to the method validation requirements of China Pharmacopoeia. Conclusion The method can determine madecassoside and asiaticoside in Centella asiatica formula granules.
Objective To establish a HPLC method for determination of madecassoside and asiaticoside in Centella asiatica formula granules. Methods Chromatographic separation was performed on Ultimate AQ-C18 column(4.6 mm×250 mm,5 μm) with mobile phase of acetonitrile(A)-2 mmol/L β-cyclodextrin(0~30 min:21% A→23% A; 30~60 min:23% A→25% A).The flow rate was set at 1.0 ml/min, the column temperature at 30 ℃ and detection wavelength at 205 nm. Results Madecassoside and asiaticoside showed good linearity (r>0.9995) in the ranges of 0.187 7~3.754 μg and 0.184 3~3.686 μg respectively. The specificity, repeatability, precision,recovery and stability were satisfied to the method validation requirements of China Pharmacopoeia. Conclusion The method can determine madecassoside and asiaticoside in Centella asiatica formula granules.
2017, 35(4): 362-366.
doi: 10.3969/j.issn.1006-0111.2017.04.019
Abstract:
Hepatocellular carcinoma is a malignant tumor with high morbidity and mortality globally. The therapeutic results on hepatocellular carcinoma with surgery and other classical treatments are not satisfactory. Tumor immunotherapies, such as dendritic cells and cytokine-induced killer cells (DC-CIK), tumor-infiltrating lymphocytes (TIL), chimeric antigen receptor T cells (CAR-T), immune checkpoint blockade (such as PD-1 blockade,CTL4 blockade) etc., are very promising new therapeutic approaches. In this paper, the progresses in the immunotherapy, mainly on PD-1, DC-CIK, TIL, are reviewed. Also pluripotent immune killer cells (PIK) which was developed in our lab was briefly introduced.
Hepatocellular carcinoma is a malignant tumor with high morbidity and mortality globally. The therapeutic results on hepatocellular carcinoma with surgery and other classical treatments are not satisfactory. Tumor immunotherapies, such as dendritic cells and cytokine-induced killer cells (DC-CIK), tumor-infiltrating lymphocytes (TIL), chimeric antigen receptor T cells (CAR-T), immune checkpoint blockade (such as PD-1 blockade,CTL4 blockade) etc., are very promising new therapeutic approaches. In this paper, the progresses in the immunotherapy, mainly on PD-1, DC-CIK, TIL, are reviewed. Also pluripotent immune killer cells (PIK) which was developed in our lab was briefly introduced.
2017, 35(4): 367-370.
doi: 10.3969/j.issn.1006-0111.2017.04.020
Abstract:
Objective To optimize the treatment plan for dermatitis medicamentosa in a patient with abnormal liver function associated with infection. Methods The culprit medication for drug eruption was identified by reviewing the patient's liver and kidney function, routine blood count, therapeutic drugs, allergic history, by analyzing the characteristics of the compounding medication, combined with literature search on drug eruption diagnosis and treatments. Following the antihistamines and glucocorticoid use guidelines, the treatment plan was optimized by selecting appropriate antihistamines and glucocorticoids based on their metabolism and excretion pathway. Results The rash was poorly controlled after clinical pharmacist's initial recommendation to use chlorpheniramine (intramuscular injection) and cetirizine (oral). The clinical pharmacist further suggested dexamethasone intravenous drip. The patient recovered well with the combination therapy of antihistamines and glucocorticoid. Conclusion When drug eruption occurred, clinical pharmacists should evaluate patient's disease and medications comprehensively, provide timely and accurate pharmaceutical care to patients.
Objective To optimize the treatment plan for dermatitis medicamentosa in a patient with abnormal liver function associated with infection. Methods The culprit medication for drug eruption was identified by reviewing the patient's liver and kidney function, routine blood count, therapeutic drugs, allergic history, by analyzing the characteristics of the compounding medication, combined with literature search on drug eruption diagnosis and treatments. Following the antihistamines and glucocorticoid use guidelines, the treatment plan was optimized by selecting appropriate antihistamines and glucocorticoids based on their metabolism and excretion pathway. Results The rash was poorly controlled after clinical pharmacist's initial recommendation to use chlorpheniramine (intramuscular injection) and cetirizine (oral). The clinical pharmacist further suggested dexamethasone intravenous drip. The patient recovered well with the combination therapy of antihistamines and glucocorticoid. Conclusion When drug eruption occurred, clinical pharmacists should evaluate patient's disease and medications comprehensively, provide timely and accurate pharmaceutical care to patients.
2017, 35(4): 371-374.
doi: 10.3969/j.issn.1006-0111.2017.04.021
Abstract:
Objective To discuss the knowledge and skills that clinical pharmacist should master to successfully perform the work in Department of Critical Care Medicine. Methods To illustrate the problem solving process with case studies in critical care setting. Results Clinical pharmacists communicate with the healthcare workers actively to provide professional pharmaceutical knowledge with evidence-based pharmacy in taking care of critical patients. Conclusion Clinical pharmacists in Department of Critical Care Medicine should possess extensive clinical and pharmaceutical knowledge, actively apply evidence-based pharmacy, and pay attention to every details in drug administration and therapy.
Objective To discuss the knowledge and skills that clinical pharmacist should master to successfully perform the work in Department of Critical Care Medicine. Methods To illustrate the problem solving process with case studies in critical care setting. Results Clinical pharmacists communicate with the healthcare workers actively to provide professional pharmaceutical knowledge with evidence-based pharmacy in taking care of critical patients. Conclusion Clinical pharmacists in Department of Critical Care Medicine should possess extensive clinical and pharmaceutical knowledge, actively apply evidence-based pharmacy, and pay attention to every details in drug administration and therapy.
2017, 35(4): 375-378.
doi: 10.3969/j.issn.1006-0111.2017.04.022
Abstract:
Objective To evaluate the cost and effectiveness for five combination therapy of β-lactam antibiotic with azithromycin in the treatment of mycoplasma pneumonia (MP) complicated with bacterial infection. Methods A retrospective study was conducted to compare the cost and effectiveness of the five regimens. Results The effective rates of group A, B, C, D and E were 97.29%, 100%, 96.55%, 95.65% and 97.36% respectively. The costs were (2 831.13±910.16) yuan,(2 816.31±127.11) yuan,(3 453.29±645.89) yuan,(4 382.42±1484.26) yuan,(3 703.39±124.86) yuan respectively. The cost-effectiveness ratios were (29.10±9.36), (28.16±5.24), (35.77±6.69), (38.04±7.90)and (35.26±10.10)respectively. Conclusion In terms of pharmacoeconomics, the combination of cefpiramide with azithromycin in group B has the lowest cost and cost-effectiveness ratio. This regimen is the most effective and economically favored combination. It is the treatment of first choice for pediatric MP patients complicated with bacterial infection.
Objective To evaluate the cost and effectiveness for five combination therapy of β-lactam antibiotic with azithromycin in the treatment of mycoplasma pneumonia (MP) complicated with bacterial infection. Methods A retrospective study was conducted to compare the cost and effectiveness of the five regimens. Results The effective rates of group A, B, C, D and E were 97.29%, 100%, 96.55%, 95.65% and 97.36% respectively. The costs were (2 831.13±910.16) yuan,(2 816.31±127.11) yuan,(3 453.29±645.89) yuan,(4 382.42±1484.26) yuan,(3 703.39±124.86) yuan respectively. The cost-effectiveness ratios were (29.10±9.36), (28.16±5.24), (35.77±6.69), (38.04±7.90)and (35.26±10.10)respectively. Conclusion In terms of pharmacoeconomics, the combination of cefpiramide with azithromycin in group B has the lowest cost and cost-effectiveness ratio. This regimen is the most effective and economically favored combination. It is the treatment of first choice for pediatric MP patients complicated with bacterial infection.
2017, 35(4): 379-382.
doi: 10.3969/j.issn.1006-0111.2017.04.023
Abstract:
Objective To promote the rational antibacterial drug use for common digestive system (DS) diseases by reviewing the clinical application of antibacterial drugs for hospitalized patients, formulating the hospital clinical specification of antibacterial drugs for common DS diseases and establishing the clinical application of antibacterial drug differentiation index for DS department. Methods 300 cases were selected from 2 060 hospitalized DS patients in the year 2014 based on the given disease ratio. The usage rate and intensity of antibiotics were calculated with survey and medical statistical analysis. The differentiation index for the clinical application of antibacterial drugs were established. Results Theoretical values of usage rate and use intensity of antibiotics in DS department were 29.0%, 41.5 DDDs according to analysis. However, the practical values were 40.3%, 50.3 DDDs. Conclusion It is necessary to improve the level of clinical antibacterial drug use. One effective way to achieve such goal is to establish the differentiation index of antibacterial drug clinical application for the department.
Objective To promote the rational antibacterial drug use for common digestive system (DS) diseases by reviewing the clinical application of antibacterial drugs for hospitalized patients, formulating the hospital clinical specification of antibacterial drugs for common DS diseases and establishing the clinical application of antibacterial drug differentiation index for DS department. Methods 300 cases were selected from 2 060 hospitalized DS patients in the year 2014 based on the given disease ratio. The usage rate and intensity of antibiotics were calculated with survey and medical statistical analysis. The differentiation index for the clinical application of antibacterial drugs were established. Results Theoretical values of usage rate and use intensity of antibiotics in DS department were 29.0%, 41.5 DDDs according to analysis. However, the practical values were 40.3%, 50.3 DDDs. Conclusion It is necessary to improve the level of clinical antibacterial drug use. One effective way to achieve such goal is to establish the differentiation index of antibacterial drug clinical application for the department.
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