2016 Vol. 34, No. 4
Display Method:
2016, 34(4): 289-291,296.
doi: 10.3969/j.issn.1006-0111.2016.04.001
Abstract:
Erzhiwan includes two components of Chinese herbal medicines-Ligustri Lucidi Fructus and Herba Ecliptae. Ligustri Lucidi Fructus, Herba Ecliptae and their formulation have various hepatoprotective effects. There are many active ingredients in the formulation, such as triterpenes, iridoids, phenethyl alcohol-glucosides, coumarin ethers, etc. They can resist various chemistry-induced hepatic injury, ischemia reperfusion induced hepatic injury, and hepatic fibrosis. The mechanisms of hepatoprotective effect include anti-oxidative stress, anti-inflammatory, inhibition of hyperplasia and activation of liver stellate cell, motivating the apoptosis of liver stellate cell, influencing the metabolic processes of liver cell, ect. We reviewed and summarized the hepatoprotective effects of Erzhiwan and its components Ligustri Lucidi Fructus and Herba Ecliptae and explore the mechanisms of hepatoprotective effect in order to provide information for further research of pharmacodynamic material base.
Erzhiwan includes two components of Chinese herbal medicines-Ligustri Lucidi Fructus and Herba Ecliptae. Ligustri Lucidi Fructus, Herba Ecliptae and their formulation have various hepatoprotective effects. There are many active ingredients in the formulation, such as triterpenes, iridoids, phenethyl alcohol-glucosides, coumarin ethers, etc. They can resist various chemistry-induced hepatic injury, ischemia reperfusion induced hepatic injury, and hepatic fibrosis. The mechanisms of hepatoprotective effect include anti-oxidative stress, anti-inflammatory, inhibition of hyperplasia and activation of liver stellate cell, motivating the apoptosis of liver stellate cell, influencing the metabolic processes of liver cell, ect. We reviewed and summarized the hepatoprotective effects of Erzhiwan and its components Ligustri Lucidi Fructus and Herba Ecliptae and explore the mechanisms of hepatoprotective effect in order to provide information for further research of pharmacodynamic material base.
2016, 34(4): 292-296.
doi: 10.3969/j.issn.1006-0111.2016.04.002
Abstract:
Orphan nuclear receptor NR4A1 from the NR4A subfamily is one of the transcriptional factors that have not identified specific ligands. Previous studies have found that NR4A1 could regulate cell proliferation, apoptosis, differentiation and stress responses by changing gene expression, post-translational modification and interactions between coregulatory proteins. Recently, it has shown that NR4A1 has an abnormal expression in human atherosclerotic lesions and has been identified as a key regulator gene in vascular cells dysfunction. Regulating NR4A1 expression can have an important impact on the proliferation of smooth muscle cell and endothelial cell activation,meanwhile it could reduce inflammation,foam cell formation and lipid deposition,inhibit vascular remodeling,and prevent the development of atherosclerosis. These studies suggest that NR4A1 might be a novel target for drug development in prevention and treatment of atherosclerosis.
Orphan nuclear receptor NR4A1 from the NR4A subfamily is one of the transcriptional factors that have not identified specific ligands. Previous studies have found that NR4A1 could regulate cell proliferation, apoptosis, differentiation and stress responses by changing gene expression, post-translational modification and interactions between coregulatory proteins. Recently, it has shown that NR4A1 has an abnormal expression in human atherosclerotic lesions and has been identified as a key regulator gene in vascular cells dysfunction. Regulating NR4A1 expression can have an important impact on the proliferation of smooth muscle cell and endothelial cell activation,meanwhile it could reduce inflammation,foam cell formation and lipid deposition,inhibit vascular remodeling,and prevent the development of atherosclerosis. These studies suggest that NR4A1 might be a novel target for drug development in prevention and treatment of atherosclerosis.
2016, 34(4): 297-300,376.
doi: 10.3969/j.issn.1006-0111.2016.04.003
Abstract:
Intracerebral hemorrhage (ICH) refers to bleeding within the brain parenchyma due to the rupture of blood vessels, and is a highly lethal stroke subtype, accounting for nearly 10%-15% of all strokes. The morbidity and mortality of ICH are very high and its pathophysiological mechanisms are currently not fully understood. Therefore, based on current clinical evidence-based medicine, there is no definite and effective medical treatment that can improve the prognosis and survival of patients available yet. As an important tool for basic research, the development and application of the ICH animal model promoted the understanding of the pathophysiological mechanisms and molecular mechanisms leading to brain injury by ICH. Recently, the ICH animal model studies contributed to a number of proposed potential therapeutic strategies, such as the inhibition of thrombin and the reduction of pro-inflammatory pathways. In addition, recent research of stem cells suggested that cell transplantation therapy for the treatment of ICH may also have good prospects. In this review, we discuss the development and application of animal models for studies on ICH and the advances regarding the potential therapeutic strategies for ICH.
Intracerebral hemorrhage (ICH) refers to bleeding within the brain parenchyma due to the rupture of blood vessels, and is a highly lethal stroke subtype, accounting for nearly 10%-15% of all strokes. The morbidity and mortality of ICH are very high and its pathophysiological mechanisms are currently not fully understood. Therefore, based on current clinical evidence-based medicine, there is no definite and effective medical treatment that can improve the prognosis and survival of patients available yet. As an important tool for basic research, the development and application of the ICH animal model promoted the understanding of the pathophysiological mechanisms and molecular mechanisms leading to brain injury by ICH. Recently, the ICH animal model studies contributed to a number of proposed potential therapeutic strategies, such as the inhibition of thrombin and the reduction of pro-inflammatory pathways. In addition, recent research of stem cells suggested that cell transplantation therapy for the treatment of ICH may also have good prospects. In this review, we discuss the development and application of animal models for studies on ICH and the advances regarding the potential therapeutic strategies for ICH.
2016, 34(4): 301-304,333.
doi: 10.3969/j.issn.1006-0111.2016.04.004
Abstract:
Detection of biomarkers benefited many advanced non-small cell lung cancer (NSCLC) patients. In recent years, epidermal growth factor (EGFR) tyrosine kinase inhibitors (TKIs) represented by Gefitinib, Erlotinib, Afatinib and anaplastic lymphoma kinase (ALK) TKIs represented by Crizotinib have remarkable efficacy. However, the efficacy for most first-generation EGFR-TKI and ALK-TKI is weakened due to secondary resistance. Currently, the third-generation EGFR-TKI which successfully against drug resistance is based on research and development of the second-generation. In addition, there are many other targeted inhibitors of mutation sites for advanced NSCLC. Unfortunately, the largest proportion of Kirsten rat sarcoma viral oncogene homolog (K-RAS) mutation is not targetable with small molecule inhibitors currently. Therefore, based on mechanisms exploration of tumor driven gene mutation, its target drug research and development will be greatly addressed in the future.
Detection of biomarkers benefited many advanced non-small cell lung cancer (NSCLC) patients. In recent years, epidermal growth factor (EGFR) tyrosine kinase inhibitors (TKIs) represented by Gefitinib, Erlotinib, Afatinib and anaplastic lymphoma kinase (ALK) TKIs represented by Crizotinib have remarkable efficacy. However, the efficacy for most first-generation EGFR-TKI and ALK-TKI is weakened due to secondary resistance. Currently, the third-generation EGFR-TKI which successfully against drug resistance is based on research and development of the second-generation. In addition, there are many other targeted inhibitors of mutation sites for advanced NSCLC. Unfortunately, the largest proportion of Kirsten rat sarcoma viral oncogene homolog (K-RAS) mutation is not targetable with small molecule inhibitors currently. Therefore, based on mechanisms exploration of tumor driven gene mutation, its target drug research and development will be greatly addressed in the future.
2016, 34(4): 305-308,321.
doi: 10.3969/j.issn.1006-0111.2016.04.005
Abstract:
This review described the post abdominal surgery anti-adhesive products and technology used domestically and internationally. The methods of administration, evaluation of pharmacodynamics and safety, and mechanism of adhesion were also summarized in this article. This review provides a theoretical basis and research ideas for the development of postoperative anti-adhesive products.
This review described the post abdominal surgery anti-adhesive products and technology used domestically and internationally. The methods of administration, evaluation of pharmacodynamics and safety, and mechanism of adhesion were also summarized in this article. This review provides a theoretical basis and research ideas for the development of postoperative anti-adhesive products.
2016, 34(4): 309-312.
doi: 10.3969/j.issn.1006-0111.2016.04.006
Abstract:
Neuropathic pain (NPP) is a chronic pain that caused by a series of infection and nerve damage events. It has high incidence, complex etiology and seriously affects patients' life quality. Although clinic trials gradually increased, the treatment of neuropathic pain is still insufficient. Recent research focuses on reasonably using drugs of different mechanisms and time of duration. The progress of NPP drugs was reviewed in this paper for providing basis for treatment of neuropathic pain.
Neuropathic pain (NPP) is a chronic pain that caused by a series of infection and nerve damage events. It has high incidence, complex etiology and seriously affects patients' life quality. Although clinic trials gradually increased, the treatment of neuropathic pain is still insufficient. Recent research focuses on reasonably using drugs of different mechanisms and time of duration. The progress of NPP drugs was reviewed in this paper for providing basis for treatment of neuropathic pain.
2016, 34(4): 313-317,353.
doi: 10.3969/j.issn.1006-0111.2016.04.007
Abstract:
Objective To establish an HPLC method for the quantitation of nine ginsenosides (Rc,Rb1,Rb2,Re,Rd,Rg1,Rg2,Rg3 and Rh2) in Panax ginseng samples. Methods An HPLC method was developed to determine the quantities of the nine ginsenosides. The determination was performed on a Zorbax SB C18 column (4.6 mm×250 mm,5 μm) with an Extend-C18 guard column (4.6 mm×12.5 mm,5 μm) at 35℃. The mobile phase was a multi-step acetonitrile-water gradient run at a flow rate of 1.0 ml/min. The detection wavelength was 203 nm. Results The nine ginsenosides were baseline separated within 120 min. The method had good linearity, precision, stability and reproducibility with RSDs all less than 2.0%. The sample recoveries were between 98.3% to 102%. The quantity of total saponins in leaves and fibrous roots of Panax ginseng, which were measured as 48.9 mg/g and 23.6 mg/g, respectively, were higher than those in the other plant components. The amounts of total saponins in Panax ginseng hairy roots were similar to those in taproots and fruits of Panax ginseng, which was 7.47 mg/g. Conclusion The established HPLC method is accurate, simple, rapid, precise and reproducible and could be used for the quantitation of these nine ginsenosides in Panax ginseng samples.
Objective To establish an HPLC method for the quantitation of nine ginsenosides (Rc,Rb1,Rb2,Re,Rd,Rg1,Rg2,Rg3 and Rh2) in Panax ginseng samples. Methods An HPLC method was developed to determine the quantities of the nine ginsenosides. The determination was performed on a Zorbax SB C18 column (4.6 mm×250 mm,5 μm) with an Extend-C18 guard column (4.6 mm×12.5 mm,5 μm) at 35℃. The mobile phase was a multi-step acetonitrile-water gradient run at a flow rate of 1.0 ml/min. The detection wavelength was 203 nm. Results The nine ginsenosides were baseline separated within 120 min. The method had good linearity, precision, stability and reproducibility with RSDs all less than 2.0%. The sample recoveries were between 98.3% to 102%. The quantity of total saponins in leaves and fibrous roots of Panax ginseng, which were measured as 48.9 mg/g and 23.6 mg/g, respectively, were higher than those in the other plant components. The amounts of total saponins in Panax ginseng hairy roots were similar to those in taproots and fruits of Panax ginseng, which was 7.47 mg/g. Conclusion The established HPLC method is accurate, simple, rapid, precise and reproducible and could be used for the quantitation of these nine ginsenosides in Panax ginseng samples.
2016, 34(4): 318-319,371.
doi: 10.3969/j.issn.1006-0111.2016.04.008
Abstract:
Objective To study the influence of eleutheroside E(ELE)on the learning and memory abilities of mice induced by para-chlorophenylalanine (PCPA) and on hippocampus' monoamine neurotransmitters of serotonin(5-HT),5-hydroxindole acetic acid (5-HIAA), dopamine (DA) and norepinephrine (NA). Methods Balb/c mice were randomized into control group, model group, positive group and three treatment groups (high, moderate and low dose group). The mouse injury model was established by PCPA abdominal injection. The mice's abilities of learning and memory were detected in the Morris water maze test after 14 days of prevention medicine. The contents of 5-HT, 5-HIAA, DA and NA in mice's hippocampus were detected by Elisa kit. Results The behavior results showed that, compared with control group, the times across the platform by model group decreased significantly (P<0.01). The times across the platform by high and moderate dose groups increased significantly (P<0.01) after the administration of ELE. The contents of 5-HT and 5-HIAA of the model group were lower than those of the control group (P<0.01). The contents of NA was lower too (P<0.05). The contents of 5-HT and 5-HIAA of different dose groups were much higher than those of the model group. Conclusion The enhancement of learning and memory ability in the mouse injury model established by PCPA might be related with the improvement of the contents of 5-HT, 5-HIAA, DA, NA in mice's hippocampus by ELE.
Objective To study the influence of eleutheroside E(ELE)on the learning and memory abilities of mice induced by para-chlorophenylalanine (PCPA) and on hippocampus' monoamine neurotransmitters of serotonin(5-HT),5-hydroxindole acetic acid (5-HIAA), dopamine (DA) and norepinephrine (NA). Methods Balb/c mice were randomized into control group, model group, positive group and three treatment groups (high, moderate and low dose group). The mouse injury model was established by PCPA abdominal injection. The mice's abilities of learning and memory were detected in the Morris water maze test after 14 days of prevention medicine. The contents of 5-HT, 5-HIAA, DA and NA in mice's hippocampus were detected by Elisa kit. Results The behavior results showed that, compared with control group, the times across the platform by model group decreased significantly (P<0.01). The times across the platform by high and moderate dose groups increased significantly (P<0.01) after the administration of ELE. The contents of 5-HT and 5-HIAA of the model group were lower than those of the control group (P<0.01). The contents of NA was lower too (P<0.05). The contents of 5-HT and 5-HIAA of different dose groups were much higher than those of the model group. Conclusion The enhancement of learning and memory ability in the mouse injury model established by PCPA might be related with the improvement of the contents of 5-HT, 5-HIAA, DA, NA in mice's hippocampus by ELE.
2016, 34(4): 320-323,342.
doi: 10.3969/j.issn.1006-0111.2016.04.009
Abstract:
Objective To prepare sorafenib (SFN)/mesoporous silica solid dispersion (SD) and investigate characteristics in vitro and in vivo. Methods The SD was prepared by solvent evaporation method; the optimal ratio of SFN to mesoporous silica was determined by examining the dissolution of formula, the drug state and physical stability of SD were examined by DSC and XRD; the surface morphology was characterized by electron microscope; the pharmacokinetics of SD was studied for the solid dispersion which compared with SFN powders in vivo study using rats. Results SFN raw drug was crystalline and its dissolution was <10%; the dissolution of SD increased with an increase in amount of mesoporous silica; when the ratio of SFN to mesoporous silica was 1:5, drug in SD was non-crystalline state and the dissolution was >90%. The physical state and dissolution of SFN in SD were hardly changed during the six months accelerated test. The cmax of SD group was 1.8 times that of powder group, relative bioavailability was 175%. Conclusion The physical stability of self-preparing solid dispersions is good, the dissolution and oral absorption are improved by solid dispersion.
Objective To prepare sorafenib (SFN)/mesoporous silica solid dispersion (SD) and investigate characteristics in vitro and in vivo. Methods The SD was prepared by solvent evaporation method; the optimal ratio of SFN to mesoporous silica was determined by examining the dissolution of formula, the drug state and physical stability of SD were examined by DSC and XRD; the surface morphology was characterized by electron microscope; the pharmacokinetics of SD was studied for the solid dispersion which compared with SFN powders in vivo study using rats. Results SFN raw drug was crystalline and its dissolution was <10%; the dissolution of SD increased with an increase in amount of mesoporous silica; when the ratio of SFN to mesoporous silica was 1:5, drug in SD was non-crystalline state and the dissolution was >90%. The physical state and dissolution of SFN in SD were hardly changed during the six months accelerated test. The cmax of SD group was 1.8 times that of powder group, relative bioavailability was 175%. Conclusion The physical stability of self-preparing solid dispersions is good, the dissolution and oral absorption are improved by solid dispersion.
2016, 34(4): 324-326,347.
doi: 10.3969/j.issn.1006-0111.2016.04.010
Abstract:
Objective Study on skin irritation and allergenicity of indomethacin emulsion, in order to provide theoretical basis for clinical safe medication. Methods New Zealand white rabbits were used to test skin irritation, given 0.5g test substance for 14 days. The skin irritation was observed in the two groups with eight rabbits each during the experiment. Six rabbits in each group were sacrificed 72 hours after the last medication and skin tissues were taken for histopathology examination; and the skin tissues of remaining two rabbits were taken for histopathology examination in 14th day after the last medication. Guinea pigs were used to test skin allergenicity, given 0.5g test substance on day 0, 7, 14 for local induction. On day 28, the animal subjects were given 0.4g test substance on non-administration skin of guinea pigs for local excitation. Results Slight irritation of indomethacin emulsion on normal or damaged skin was observed but it is reversible after withdrawal for rabbits. Sensitization effect on the skin of guinea pig was not found. Conclusion Indomethacin emulsion is not suitable to long-term use clinically, and skin irritation need to pay more attention.
Objective Study on skin irritation and allergenicity of indomethacin emulsion, in order to provide theoretical basis for clinical safe medication. Methods New Zealand white rabbits were used to test skin irritation, given 0.5g test substance for 14 days. The skin irritation was observed in the two groups with eight rabbits each during the experiment. Six rabbits in each group were sacrificed 72 hours after the last medication and skin tissues were taken for histopathology examination; and the skin tissues of remaining two rabbits were taken for histopathology examination in 14th day after the last medication. Guinea pigs were used to test skin allergenicity, given 0.5g test substance on day 0, 7, 14 for local induction. On day 28, the animal subjects were given 0.4g test substance on non-administration skin of guinea pigs for local excitation. Results Slight irritation of indomethacin emulsion on normal or damaged skin was observed but it is reversible after withdrawal for rabbits. Sensitization effect on the skin of guinea pig was not found. Conclusion Indomethacin emulsion is not suitable to long-term use clinically, and skin irritation need to pay more attention.
2016, 34(4): 327-329.
doi: 10.3969/j.issn.1006-0111.2016.04.011
Abstract:
Objective To evaluate the physical dependence of total Ervatamia yunnansis alkaloid. Methods The physical dependence of total Ervatamia yunnansis alkaloid was observed by jump test in mice and spontaneous withdrawal test in rats. Results In the jump test, after injecting total Ervatamia yunnansis alkaloid (total dosage of 140 and 430 mg/kg) for 7 days continuously, the mice didn't show any withdrawal symptom and the loss of body weight. In the spontaneous withdrawal test, two dosages of total Ervatamia yunnansis alkaloid (total dosage of 210 and 775 mg/kg) were continuously given for 30 days. The withdrawal response and the loss of body weight were not found in rats after drug withdrawal. Conclusion Total Ervatamia yunnansis alkaloid showed no obvious withdrawal symptoms in mice and rats, which suggests that it has no physical dependence.
Objective To evaluate the physical dependence of total Ervatamia yunnansis alkaloid. Methods The physical dependence of total Ervatamia yunnansis alkaloid was observed by jump test in mice and spontaneous withdrawal test in rats. Results In the jump test, after injecting total Ervatamia yunnansis alkaloid (total dosage of 140 and 430 mg/kg) for 7 days continuously, the mice didn't show any withdrawal symptom and the loss of body weight. In the spontaneous withdrawal test, two dosages of total Ervatamia yunnansis alkaloid (total dosage of 210 and 775 mg/kg) were continuously given for 30 days. The withdrawal response and the loss of body weight were not found in rats after drug withdrawal. Conclusion Total Ervatamia yunnansis alkaloid showed no obvious withdrawal symptoms in mice and rats, which suggests that it has no physical dependence.
2016, 34(4): 330-333.
doi: 10.3969/j.issn.1006-0111.2016.04.012
Abstract:
Objective The research is about optimization of preparation procedure of self-microemulsifying dropping pills of paclitaxel (PTX-SM-DP). The drug release in vitro of PTX-SM-DP was investigated. Methods The ratio of SMEDDS and bases, dropping distance, temperature and speed of dripping were investigated by using the orthogonal test. The weight difference of dropping pill, hardness and roundness were evaluated to optimize the preparation conditions of PTX-SM-DP. Dissolution of vitro was determined. Results The optimal preparation conditions were as follows:the ratio of SMEDDS and bases was 1:3, dropping distance was 15 cm, temperature of dripping preparation was 80℃ and dripping speed was 30 drops/min. Conclusion The optimized technical condition is stable and feasible. PTX-SM-DP can improve paclitaxel dissolution.
Objective The research is about optimization of preparation procedure of self-microemulsifying dropping pills of paclitaxel (PTX-SM-DP). The drug release in vitro of PTX-SM-DP was investigated. Methods The ratio of SMEDDS and bases, dropping distance, temperature and speed of dripping were investigated by using the orthogonal test. The weight difference of dropping pill, hardness and roundness were evaluated to optimize the preparation conditions of PTX-SM-DP. Dissolution of vitro was determined. Results The optimal preparation conditions were as follows:the ratio of SMEDDS and bases was 1:3, dropping distance was 15 cm, temperature of dripping preparation was 80℃ and dripping speed was 30 drops/min. Conclusion The optimized technical condition is stable and feasible. PTX-SM-DP can improve paclitaxel dissolution.
2016, 34(4): 334-337.
doi: 10.3969/j.issn.1006-0111.2016.04.013
Abstract:
Objective To design and synthesis novel triazole antifungal derivatives with dithiocarbamates side chain and study the antifungal activities. Methods Nine title compounds were synthesized and characterized by 1H NMR, MS spectra. The in vitro antifungal activities of all the compounds were evaluated against eight human pathogenic fungi. Results The title compounds exhibited strong antifungal activities. Some compounds showed excellent activities against Candida albicans with the MIC80 values less than 0.125 g/ml, 6d was 64 times higher than that of Itraconazole. Conclusion The introduction of the propyl, sulphur and benzyl moiety to the side chain could affect the antifungal activities.
Objective To design and synthesis novel triazole antifungal derivatives with dithiocarbamates side chain and study the antifungal activities. Methods Nine title compounds were synthesized and characterized by 1H NMR, MS spectra. The in vitro antifungal activities of all the compounds were evaluated against eight human pathogenic fungi. Results The title compounds exhibited strong antifungal activities. Some compounds showed excellent activities against Candida albicans with the MIC80 values less than 0.125 g/ml, 6d was 64 times higher than that of Itraconazole. Conclusion The introduction of the propyl, sulphur and benzyl moiety to the side chain could affect the antifungal activities.
2016, 34(4): 338-342.
doi: 10.3969/j.issn.1006-0111.2016.04.014
Abstract:
Objective To establish quality control of Xinnaoling granules. Methods Thin layer chromatography (TLC) methods were used to identify Rhizoma Corydalis, Radix Angelicae dahuricae, Cortex Magnoliae officinalis, Radix Glycyrrhizae, Rhizoma Ligusticum, Ligusticum wallichii, Schisandra Chinensis, Dendranthema morifolium. The concentration of salvianolic acid B was determined by high performance liquid chromatography (HPLC). The method employed a column of Agilent Eclipse XDB-C18 (4.6 mm×250 mm,5 μm) with a mobile phase of 0.5% formic acid (A)-acetonitrile (B) at a temperature 25℃. The gradient elution program was as follow:0~5 min 24% B, 5~6 min 24%~19% B, 6~25 min 19~20% B. The flow rate was 1.0 ml/min, and the injection volume was 10 μl and the detection wavelength was 286 nm. Results The spots in TLC plates were clear and specific. As for salvianolic acid B, the linear range was 20-1280 μg/ml and the equation of linear regression of salvianolic acid B was Y=13.304 X-117.50 (r=0.9999, n=7). The average recovery rate was 96.17% (RSD=1.10%). Conclusion The method was proved to be simple, reliable, reproducible, and could be used in the quality control of Xinnaoling granules.
Objective To establish quality control of Xinnaoling granules. Methods Thin layer chromatography (TLC) methods were used to identify Rhizoma Corydalis, Radix Angelicae dahuricae, Cortex Magnoliae officinalis, Radix Glycyrrhizae, Rhizoma Ligusticum, Ligusticum wallichii, Schisandra Chinensis, Dendranthema morifolium. The concentration of salvianolic acid B was determined by high performance liquid chromatography (HPLC). The method employed a column of Agilent Eclipse XDB-C18 (4.6 mm×250 mm,5 μm) with a mobile phase of 0.5% formic acid (A)-acetonitrile (B) at a temperature 25℃. The gradient elution program was as follow:0~5 min 24% B, 5~6 min 24%~19% B, 6~25 min 19~20% B. The flow rate was 1.0 ml/min, and the injection volume was 10 μl and the detection wavelength was 286 nm. Results The spots in TLC plates were clear and specific. As for salvianolic acid B, the linear range was 20-1280 μg/ml and the equation of linear regression of salvianolic acid B was Y=13.304 X-117.50 (r=0.9999, n=7). The average recovery rate was 96.17% (RSD=1.10%). Conclusion The method was proved to be simple, reliable, reproducible, and could be used in the quality control of Xinnaoling granules.
2016, 34(4): 343-347.
doi: 10.3969/j.issn.1006-0111.2016.04.015
Abstract:
Objective To improve the quality standard of Minuo Hair Solution and to ensure product quality. Methods Thin layer chromatography (TLC) and UV-visible spectroscopy (UV-Vis) method was used for the qualitative identification of Angelica sinensis, Paeoniae Radix Rubra, Dictamni Cortex and minoxidil respectively. The Quantitive determination of minoxidil was completed by first order derivative spectroscopy. Results The spots in TLC were clear without inference. And the same color spots appeared in the corresponding position of references and reference drugs. The UV-Vis spectral absorption of minoxidil were in (230±3), (262±3),(286±3) nm. The linear range of minoxidil was obtained between 6.2 and 18.6 μg/ml (r=0.9997). The average recovery was 99.4% (RSD=0.22%). Conclusion The method is simple,accurate and reproducible,and can be effectively used to control the quality of Minuo Hair Solution.
Objective To improve the quality standard of Minuo Hair Solution and to ensure product quality. Methods Thin layer chromatography (TLC) and UV-visible spectroscopy (UV-Vis) method was used for the qualitative identification of Angelica sinensis, Paeoniae Radix Rubra, Dictamni Cortex and minoxidil respectively. The Quantitive determination of minoxidil was completed by first order derivative spectroscopy. Results The spots in TLC were clear without inference. And the same color spots appeared in the corresponding position of references and reference drugs. The UV-Vis spectral absorption of minoxidil were in (230±3), (262±3),(286±3) nm. The linear range of minoxidil was obtained between 6.2 and 18.6 μg/ml (r=0.9997). The average recovery was 99.4% (RSD=0.22%). Conclusion The method is simple,accurate and reproducible,and can be effectively used to control the quality of Minuo Hair Solution.
2016, 34(4): 348-350,356.
doi: 10.3969/j.issn.1006-0111.2016.04.016
Abstract:
Objective To study the rat pulmonary irritant of aerosol inhaled Tanreqing and Reduning injection. Methods Rats were devided into two groups for each medicine (low concentration group and high concentration group), nebulized drug administration for seven days, with the control group irrigated with saline, and were sacrificed. Through bronchoalveolar lavage, excurrent bronchoalveolar lavage fluid (BALF) was used for total protein determination and LDH vitality test to evaluate pulmonary toxicity of two medicines. Results The protein concentrations of two groups in low and high concentrations of Tanreqing and Reduning respectively are (193.78±27.74),(235.33±50.41) μg/ml;(174.02±17.82),(227.27±66.03) μg/ml;LDH vitalities respectively are 1065.21±181.76,1467.33±101.87;307.97±47.56,1377.29±566.48. By t-test, compared with normal saline, there was no significant effect among these five groups on protein concentration, but these two medicine were able to improve LDH activity (P<0.05) which was more obvious in high concentration group. When two medicines were in low concentration, LDH activity was higher in Tanreqing group with statistical significance (P<0.05). Conclusion Aerosol inhaled Tanreqing and Reduning injection in rats have some pulmonary irritation and potential safety hazard in this delivery way.
Objective To study the rat pulmonary irritant of aerosol inhaled Tanreqing and Reduning injection. Methods Rats were devided into two groups for each medicine (low concentration group and high concentration group), nebulized drug administration for seven days, with the control group irrigated with saline, and were sacrificed. Through bronchoalveolar lavage, excurrent bronchoalveolar lavage fluid (BALF) was used for total protein determination and LDH vitality test to evaluate pulmonary toxicity of two medicines. Results The protein concentrations of two groups in low and high concentrations of Tanreqing and Reduning respectively are (193.78±27.74),(235.33±50.41) μg/ml;(174.02±17.82),(227.27±66.03) μg/ml;LDH vitalities respectively are 1065.21±181.76,1467.33±101.87;307.97±47.56,1377.29±566.48. By t-test, compared with normal saline, there was no significant effect among these five groups on protein concentration, but these two medicine were able to improve LDH activity (P<0.05) which was more obvious in high concentration group. When two medicines were in low concentration, LDH activity was higher in Tanreqing group with statistical significance (P<0.05). Conclusion Aerosol inhaled Tanreqing and Reduning injection in rats have some pulmonary irritation and potential safety hazard in this delivery way.
2016, 34(4): 351-353.
doi: 10.3969/j.issn.1006-0111.2016.04.017
Abstract:
Objective To develop a new high performance liquid chromatography (HPLC) coupled with Evaporative Light Scattering Detector (ELSD) method for simultaneous determination of two indicative components (peimine and peiminine) in Xiaoer Baotaikang granules. Methods The analysis was performed on a Thermo C18 column (250 mm×4.6 mm, 5 μm) by using a mobile phase consisted of acetonitrile-water and diethylamine(65:35:0.03), and the flow rate was 1.0 ml/min; ELSD parameters:the temperature of drift tube was 85℃ and the carrier gas flow rate was 2.2 L/min. Results The linear ranges of peimine and peiminine were 0.586~5.860 μg (r=0.9996) and 0.564~5.640 μg (r=0.9999), respectively. The average recovery rate for peimine and peiminine was 99.44% (RSD was 0.7%) and 98.56% (RSD was 1.0%),respectively. Conclusion s The method is sample,accurate and reproducible, which could be used for the quality control of Xiaoer Baotaikang granules.
Objective To develop a new high performance liquid chromatography (HPLC) coupled with Evaporative Light Scattering Detector (ELSD) method for simultaneous determination of two indicative components (peimine and peiminine) in Xiaoer Baotaikang granules. Methods The analysis was performed on a Thermo C18 column (250 mm×4.6 mm, 5 μm) by using a mobile phase consisted of acetonitrile-water and diethylamine(65:35:0.03), and the flow rate was 1.0 ml/min; ELSD parameters:the temperature of drift tube was 85℃ and the carrier gas flow rate was 2.2 L/min. Results The linear ranges of peimine and peiminine were 0.586~5.860 μg (r=0.9996) and 0.564~5.640 μg (r=0.9999), respectively. The average recovery rate for peimine and peiminine was 99.44% (RSD was 0.7%) and 98.56% (RSD was 1.0%),respectively. Conclusion s The method is sample,accurate and reproducible, which could be used for the quality control of Xiaoer Baotaikang granules.
2016, 34(4): 354-356.
doi: 10.3969/j.issn.1006-0111.2016.04.018
Abstract:
Objective To investigate the mechanism of anti-epileptic effect of the curcumin. Methods The SD rats were injected intraperitoneally with pentylenetetrazol kindling 25.0 mg/kg to induce a rat epilepsy model. All of the treatments were performed once a day continuously for 28 days. The rats in blank group and model group received 5 ml of normal saline. The rats in the high and low curcumin group were given 200 mg/kg and 100 mg/kg of curcumin once a day, respectively. The rats in the sodium valproate (VPA) group were given 400 mg/kg of VPA once a day by gavage. After treatment, the seizures level was recorded by using the Racine's six point grading scale, and the expression of IL-2 and IL-6 of hippocampus were detected by the enzyme linked immunoassay (ELISA). Results The seizures level was reduced by curcumin in epileptic rats. The expressions of IL-2 and IL-6 of the model group were significantly higher than those of the blank group (P<0.05), while those rats of the anti-epileptic groups, including high dose group and low dose group, were lower than those rats of the model group (P<0.05). When compared with the curcumin low dose group, the expression of IL-2 and IL-6 of curcumin high dose group is lower (P<0.05). There was no significant difference between the high dose curcumin group and VPA group (P>0.05). Conclusion The curcumin can reduce the seizure level in rats, it shows some anti-epileptic effets and dose-dependently, which may be through down-regulating the expression of IL-2 and IL-6 in hippocampus.
Objective To investigate the mechanism of anti-epileptic effect of the curcumin. Methods The SD rats were injected intraperitoneally with pentylenetetrazol kindling 25.0 mg/kg to induce a rat epilepsy model. All of the treatments were performed once a day continuously for 28 days. The rats in blank group and model group received 5 ml of normal saline. The rats in the high and low curcumin group were given 200 mg/kg and 100 mg/kg of curcumin once a day, respectively. The rats in the sodium valproate (VPA) group were given 400 mg/kg of VPA once a day by gavage. After treatment, the seizures level was recorded by using the Racine's six point grading scale, and the expression of IL-2 and IL-6 of hippocampus were detected by the enzyme linked immunoassay (ELISA). Results The seizures level was reduced by curcumin in epileptic rats. The expressions of IL-2 and IL-6 of the model group were significantly higher than those of the blank group (P<0.05), while those rats of the anti-epileptic groups, including high dose group and low dose group, were lower than those rats of the model group (P<0.05). When compared with the curcumin low dose group, the expression of IL-2 and IL-6 of curcumin high dose group is lower (P<0.05). There was no significant difference between the high dose curcumin group and VPA group (P>0.05). Conclusion The curcumin can reduce the seizure level in rats, it shows some anti-epileptic effets and dose-dependently, which may be through down-regulating the expression of IL-2 and IL-6 in hippocampus.
2016, 34(4): 357-358,384.
doi: 10.3969/j.issn.1006-0111.2016.04.019
Abstract:
Objective To investigate the stability of torasemide injection and predict its expiration date in room temperatue. Methods The contents of torasemide were determined by HPLC. The expiration date was predicted by classical constant-temperature experiment. Results The contents of torasemide degradation with time according to a first order reaction at room temperature (25℃). The disintegration rate constant K was K25℃=5.1869×10-6 h-1 and the expiration date of torasemide injection was t0.9=2.32 years. Conclusion The torasemide injection expiration date was tentatively scheduled for two years.
Objective To investigate the stability of torasemide injection and predict its expiration date in room temperatue. Methods The contents of torasemide were determined by HPLC. The expiration date was predicted by classical constant-temperature experiment. Results The contents of torasemide degradation with time according to a first order reaction at room temperature (25℃). The disintegration rate constant K was K25℃=5.1869×10-6 h-1 and the expiration date of torasemide injection was t0.9=2.32 years. Conclusion The torasemide injection expiration date was tentatively scheduled for two years.
Effect of preoperative compound matrine injection combined with chemotherapy on lung cancer patients
2016, 34(4): 359-362.
doi: 10.3969/j.issn.1006-0111.2016.04.020
Abstract:
Objective To study the effect of preoperative compound matrine injection combined with chemotherapy on serum index apoptotic molecules and signaling molecules expression in tumor tissues of lung cancer patients. Methods Patients with diagnosed lung cancer and planed for surgery in our hospital were selected and divided into combined marine with chemotherapy group and chemotherapy group. Then lung cancer marker molecule contents in serum and mRNA contents of apoptosis regulatory molecules, signaling molecules in tumor tissue were assayed. Results 1Serum lung cancer marker molecules:compared with chemotherapy group, lung cancer marker molecules in serum of combined therapy group SCC, Cyfra21-1, VEGF, TGF-β1, TSGF contents in serum were lower; 2mRNA contents of apoptosis regulation molecules in tumor tissues:compared with chemotherapy group, apoptosis regulation molecules mRNA contents of Caspase-3/7, Fas/FasL, Bim in tumor tissues of combined therapy group were higher, mRNA content of Pim-1 was lower; 3mRNA contents of signal molecules in tumor tissues:compared with signal molecules in tumor tissues of chemotherapy group, mRNA contents of Wnt1, β-catenin, Wnt5a, NFAT, JAK2 and STAT3 in tumor tissues of combined treatment group were lower. Conclusion Preoperative compound matrine injection combined with chemotherapy can be more effective in killing lung cancer cells, reducing serum marker levels, inducing cancer cell apoptosis, inhibiting signaling function; it's an ideal pre-surgery chemotherapy method for patients with non-small cell lung cancer.
Objective To study the effect of preoperative compound matrine injection combined with chemotherapy on serum index apoptotic molecules and signaling molecules expression in tumor tissues of lung cancer patients. Methods Patients with diagnosed lung cancer and planed for surgery in our hospital were selected and divided into combined marine with chemotherapy group and chemotherapy group. Then lung cancer marker molecule contents in serum and mRNA contents of apoptosis regulatory molecules, signaling molecules in tumor tissue were assayed. Results 1Serum lung cancer marker molecules:compared with chemotherapy group, lung cancer marker molecules in serum of combined therapy group SCC, Cyfra21-1, VEGF, TGF-β1, TSGF contents in serum were lower; 2mRNA contents of apoptosis regulation molecules in tumor tissues:compared with chemotherapy group, apoptosis regulation molecules mRNA contents of Caspase-3/7, Fas/FasL, Bim in tumor tissues of combined therapy group were higher, mRNA content of Pim-1 was lower; 3mRNA contents of signal molecules in tumor tissues:compared with signal molecules in tumor tissues of chemotherapy group, mRNA contents of Wnt1, β-catenin, Wnt5a, NFAT, JAK2 and STAT3 in tumor tissues of combined treatment group were lower. Conclusion Preoperative compound matrine injection combined with chemotherapy can be more effective in killing lung cancer cells, reducing serum marker levels, inducing cancer cell apoptosis, inhibiting signaling function; it's an ideal pre-surgery chemotherapy method for patients with non-small cell lung cancer.
2016, 34(4): 363-365.
doi: 10.3969/j.issn.1006-0111.2016.04.021
Abstract:
Objective To discuss the pharmaceutical care experience of the clinical pharmacist in anti-infectious treatment of one patient with febrile neutropenia. Methods The clinical pharmacists participated in the treatment of the patient with febrile neutropenia. According to the patient's laboratory indices and vital signs, the pharmacist assisted clinicians to formulate the anti-infection regimen, recommend for rational use of drugs, carried out drug education to the patient, and track drug efficacy and adverse drug reactions (ADR). Results The patient's infection was well controlled and effectively avoid the occurrence of ADR. Conclusion With pharmaceutical care through clinical pharmacists, infection in the patient with febrile neutropenia would be controlled, the patient's life quality could be improved.
Objective To discuss the pharmaceutical care experience of the clinical pharmacist in anti-infectious treatment of one patient with febrile neutropenia. Methods The clinical pharmacists participated in the treatment of the patient with febrile neutropenia. According to the patient's laboratory indices and vital signs, the pharmacist assisted clinicians to formulate the anti-infection regimen, recommend for rational use of drugs, carried out drug education to the patient, and track drug efficacy and adverse drug reactions (ADR). Results The patient's infection was well controlled and effectively avoid the occurrence of ADR. Conclusion With pharmaceutical care through clinical pharmacists, infection in the patient with febrile neutropenia would be controlled, the patient's life quality could be improved.
2016, 34(4): 366-371.
doi: 10.3969/j.issn.1006-0111.2016.04.022
Abstract:
Objective To discuss dendritic cell-cytokine-induced killer (DC-CIK) cell therapy effects and clinical outcomes in patients with colorectal cancer in order to have better clinical treatment. Methods A retrospective analysis of the data of 66 patients with colorectal cancer from the Biological Therapy Department of the Eastern Hepatobiliary Surgery Hospital was performed from January 2012 to January 2014, and then was followed up. Taking gender, age, degree of pathological differentiation, TNM staging, surgical methods, and targeted therapy as the research basis, by the Kaplan-Meier single factor and Cox multiple factors analysis we mainly discuss the DC-CIK cell treatment's effect on the prognoses of patients. Results Kaplan-Meier single factor analysis results indicate:to a certain extent, DC-CIK cell therapy can improve the prognoses of patients; Cox multi-factor analysis results indicate whether accepting DC-CIK cell therapy is an independent factor influencing the prognoses of patients. Conclusion DC-CIK cells therapy can improve the prognoses of patients with colorectal cancer.
Objective To discuss dendritic cell-cytokine-induced killer (DC-CIK) cell therapy effects and clinical outcomes in patients with colorectal cancer in order to have better clinical treatment. Methods A retrospective analysis of the data of 66 patients with colorectal cancer from the Biological Therapy Department of the Eastern Hepatobiliary Surgery Hospital was performed from January 2012 to January 2014, and then was followed up. Taking gender, age, degree of pathological differentiation, TNM staging, surgical methods, and targeted therapy as the research basis, by the Kaplan-Meier single factor and Cox multiple factors analysis we mainly discuss the DC-CIK cell treatment's effect on the prognoses of patients. Results Kaplan-Meier single factor analysis results indicate:to a certain extent, DC-CIK cell therapy can improve the prognoses of patients; Cox multi-factor analysis results indicate whether accepting DC-CIK cell therapy is an independent factor influencing the prognoses of patients. Conclusion DC-CIK cells therapy can improve the prognoses of patients with colorectal cancer.
2016, 34(4): 372-376.
doi: 10.3969/j.issn.1006-0111.2016.04.023
Abstract:
The great potential of cell therapy based on chimeric antigen receptor (CAR) has been demonstrated in the treatment of malignant tumors through 25 years of research.A large number of experimental and clinical data have been reported in recent years.This review compares and analyzes these data to discuss how to enhance the efficacy of CAR-T cell therapy in the treatment of unresectable malignant tumors and to summarize the safety issues and solution strategies of CAR-T cell technology in the treatment of malignant tumors.
The great potential of cell therapy based on chimeric antigen receptor (CAR) has been demonstrated in the treatment of malignant tumors through 25 years of research.A large number of experimental and clinical data have been reported in recent years.This review compares and analyzes these data to discuss how to enhance the efficacy of CAR-T cell therapy in the treatment of unresectable malignant tumors and to summarize the safety issues and solution strategies of CAR-T cell technology in the treatment of malignant tumors.
2016, 34(4): 377-379.
doi: 10.3969/j.issn.1006-0111.2016.04.024
Abstract:
Objective To analyze the use of hypoglycemic agents of diabetic adult patients who were managed in the Community Health Service Center of Huazhong University of Science and Technology in Wuhan. Methods By analyzing of follow-up record of 647 adults with diabetes of the Community Health Service Center outpatient in 2014 to understand about their drug use. Results The ages of prevalence of adult diabetes were 50 to 79 years old (79.29%), of which the majority of patients aged 60 or older (73.11%), men are more than women; the using of antidiabetic monotherapy accounted for 61.36%, the two drugs together accounted for 34.93%, and three or more drugs accounted for 3.71%; α-glucosidase inhibitors, metformin, insulin secretagogues are the highest frequency of use; outpatient diabetics administered orally based. Conclusion The medication use of diabetes in this community was consisted with the requirement of China Guideline for Type 2 Diabetes (2013 edition).
Objective To analyze the use of hypoglycemic agents of diabetic adult patients who were managed in the Community Health Service Center of Huazhong University of Science and Technology in Wuhan. Methods By analyzing of follow-up record of 647 adults with diabetes of the Community Health Service Center outpatient in 2014 to understand about their drug use. Results The ages of prevalence of adult diabetes were 50 to 79 years old (79.29%), of which the majority of patients aged 60 or older (73.11%), men are more than women; the using of antidiabetic monotherapy accounted for 61.36%, the two drugs together accounted for 34.93%, and three or more drugs accounted for 3.71%; α-glucosidase inhibitors, metformin, insulin secretagogues are the highest frequency of use; outpatient diabetics administered orally based. Conclusion The medication use of diabetes in this community was consisted with the requirement of China Guideline for Type 2 Diabetes (2013 edition).
2016, 34(4): 380-384.
doi: 10.3969/j.issn.1006-0111.2016.04.025
Abstract:
Objective To evaluate the effecacy of Bifidobacterium viable triple capsule on anti-Helicobacter pylori (Hp) treatment and its adverse reactions during eradication therapy. Methods Trials on the effect of Bifidobacterium viable triple capsule on Hp eradication were analyzed by Meta-analysis with the software Stata 12.0 for comprehensive quantitative analysis of its clinical efficacy and adverse reactions during treatment. Results Eight randomly controlled trials (n=1144) were included. Pooled Hp eradication rates were 85.91% and 69.21% for patients with and without Bifidobacterium viable triple capsule respectively, with the odds ratio (OR) being 3.07 (95% CI=2.25~4.19, test for overall effect Z=7.08, P<0.01); the occurrences of total adverse reactions were 7.58% and 20.87% respectively, with the summary OR being 0.42 (95% CI=0.29~0.61, test for overall effect Z=4.48, P<0.01). The difference of the two groups was statistically significant. Conclusion Current evidence shows that Bifidobacterium viable triple capsule could increase eradication rate of anti-Hp treatment and improve adverse reactions during therapy.
Objective To evaluate the effecacy of Bifidobacterium viable triple capsule on anti-Helicobacter pylori (Hp) treatment and its adverse reactions during eradication therapy. Methods Trials on the effect of Bifidobacterium viable triple capsule on Hp eradication were analyzed by Meta-analysis with the software Stata 12.0 for comprehensive quantitative analysis of its clinical efficacy and adverse reactions during treatment. Results Eight randomly controlled trials (n=1144) were included. Pooled Hp eradication rates were 85.91% and 69.21% for patients with and without Bifidobacterium viable triple capsule respectively, with the odds ratio (OR) being 3.07 (95% CI=2.25~4.19, test for overall effect Z=7.08, P<0.01); the occurrences of total adverse reactions were 7.58% and 20.87% respectively, with the summary OR being 0.42 (95% CI=0.29~0.61, test for overall effect Z=4.48, P<0.01). The difference of the two groups was statistically significant. Conclusion Current evidence shows that Bifidobacterium viable triple capsule could increase eradication rate of anti-Hp treatment and improve adverse reactions during therapy.
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