2019 Vol. 37, No. 2
Display Method:
2019, 37(2): 97-102.
doi: 10.3969/j.issn.1006-0111.2019.02.001
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Obesity is closely relative to the increase in diabetes incidence. Most of the current hypoglycemic medicines,such as insulin and its analogues,insulin secretion enhancers,insulin sensitizers and so on,would lead to weight gain,thus aggravating insulin resistance and increasing the dosage of hypoglycemic drugs,which had formed a vicious circle. The development of new drugs targeting both reducing blood sugar and controlling weight had attracted much more attention. the epidemiology of obese type 2 diabetes mellitus and the effect of currently available hypoglycemic drugs on weight development had been reviewed in this article,and the latest targets of hypoglycemic medicines with weight loss effects were highlighted,in order to provide a potential approach for the treatment of obese type 2 diabetes mellitus.
Obesity is closely relative to the increase in diabetes incidence. Most of the current hypoglycemic medicines,such as insulin and its analogues,insulin secretion enhancers,insulin sensitizers and so on,would lead to weight gain,thus aggravating insulin resistance and increasing the dosage of hypoglycemic drugs,which had formed a vicious circle. The development of new drugs targeting both reducing blood sugar and controlling weight had attracted much more attention. the epidemiology of obese type 2 diabetes mellitus and the effect of currently available hypoglycemic drugs on weight development had been reviewed in this article,and the latest targets of hypoglycemic medicines with weight loss effects were highlighted,in order to provide a potential approach for the treatment of obese type 2 diabetes mellitus.
2019, 37(2): 103-108.
doi: 10.3969/j.issn.1006-0111.2019.02.002
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The detection methods for the illegal addition of PDE-5 inhibitors in botanical dietary supplements were reviewed in this article. So far,FTIR,NIR,and TLC-SERS methods were commonly adopted to rapid detection,and confirmed detection by HPLC,LC-MS methods; NMR and GC-MS methods were used as supplementary tests for structural identification and confirmation. In addition,other high-efficiency detection methods such as XRD and ELISA also provided relevant technical methods for the drug supervision and administration department to carry out the detection of the doping of botanical dietary supplements and ensure that the reasonable and safe use of food and drug.
The detection methods for the illegal addition of PDE-5 inhibitors in botanical dietary supplements were reviewed in this article. So far,FTIR,NIR,and TLC-SERS methods were commonly adopted to rapid detection,and confirmed detection by HPLC,LC-MS methods; NMR and GC-MS methods were used as supplementary tests for structural identification and confirmation. In addition,other high-efficiency detection methods such as XRD and ELISA also provided relevant technical methods for the drug supervision and administration department to carry out the detection of the doping of botanical dietary supplements and ensure that the reasonable and safe use of food and drug.
2019, 37(2): 109-114,155.
doi: 10.3969/j.issn.1006-0111.2019.02.003
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Osteoporosis (OP) is a systemic osteopathy with low bone mineral density and bone quality.It seriously endangered human physical and mental health due to its destructive and widespread characteristics.In clinic,drugs for OP,such as bisphosphonates and estrogens,have potential side effects.Contrarily,traditional Chinese medicine (TCM) has less adverse reactions and significant therapeutic effects.It becomes one of the remarkable complementary and alternative OP therapies.According to TCM theory,kidney is in charge of bone.The bone loss is attributed to the deficiencies of kidney.Therefore,herbs tonifying kidney had been used in the treatment of OP.Based on the different effects,herbs tonifying kidney are divided into tonifying kidney-yang and kidney-yin herbs.This paper reviews the effects and mechanisms of the herbs tonifying kidney-yang and kidney-yin in the OP treatment with the intention of exploring the similarities and differences of their treatment characteristics and providing reference for the development of kidney tonifying herbs in OP prevention and therapy.
Osteoporosis (OP) is a systemic osteopathy with low bone mineral density and bone quality.It seriously endangered human physical and mental health due to its destructive and widespread characteristics.In clinic,drugs for OP,such as bisphosphonates and estrogens,have potential side effects.Contrarily,traditional Chinese medicine (TCM) has less adverse reactions and significant therapeutic effects.It becomes one of the remarkable complementary and alternative OP therapies.According to TCM theory,kidney is in charge of bone.The bone loss is attributed to the deficiencies of kidney.Therefore,herbs tonifying kidney had been used in the treatment of OP.Based on the different effects,herbs tonifying kidney are divided into tonifying kidney-yang and kidney-yin herbs.This paper reviews the effects and mechanisms of the herbs tonifying kidney-yang and kidney-yin in the OP treatment with the intention of exploring the similarities and differences of their treatment characteristics and providing reference for the development of kidney tonifying herbs in OP prevention and therapy.
2019, 37(2): 115-120,145.
doi: 10.3969/j.issn.1006-0111.2019.02.004
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Objective To study the effects of positive electret 5-FU patch on the expression of type Ⅰ,Ⅲ collagens and TGF-β in rabbit ear scar tissue. Methods The positive electret 5-fluorouracil (5-FU) patches with surface potential of+5 kV were made by attaching the positive charged polypropylene (PP) electret on the back layer of the 5-FU patch.The positive electrets,5-FU patch and positive electret 5-FU patches were applied to the wound surface on rabbit ear.The scar proliferation index was calculated to study the status of the scar.the HE staining,Masson staining and immunohistochemical methods were used to study the effects of the positive electrets,5-FU patch and the positive electret 5-FU patch on the expression of type Ⅰ,Ⅲ collagen and TGF-β in the rabbit ear scar tissue. Results ① The hypertrophic scar (HS) was formed after 4 weeks natural healing.② The positive electret will not lead to excessive wound repair.③ Both the 5-FU patch and the positive electret 5-FU patch reduced the expression of type Ⅰ collagen,type Ⅲ collagen and TGF-β in scar tissue and inhibited the growth of HS.④ The positive electret 5-FU patch had better inhibiting effect in HS growth than 5-FU patch. Conclusion The combination of positive electret and 5-FU can achieve better results in inhibiting the growth of hypertrophic scar.
Objective To study the effects of positive electret 5-FU patch on the expression of type Ⅰ,Ⅲ collagens and TGF-β in rabbit ear scar tissue. Methods The positive electret 5-fluorouracil (5-FU) patches with surface potential of+5 kV were made by attaching the positive charged polypropylene (PP) electret on the back layer of the 5-FU patch.The positive electrets,5-FU patch and positive electret 5-FU patches were applied to the wound surface on rabbit ear.The scar proliferation index was calculated to study the status of the scar.the HE staining,Masson staining and immunohistochemical methods were used to study the effects of the positive electrets,5-FU patch and the positive electret 5-FU patch on the expression of type Ⅰ,Ⅲ collagen and TGF-β in the rabbit ear scar tissue. Results ① The hypertrophic scar (HS) was formed after 4 weeks natural healing.② The positive electret will not lead to excessive wound repair.③ Both the 5-FU patch and the positive electret 5-FU patch reduced the expression of type Ⅰ collagen,type Ⅲ collagen and TGF-β in scar tissue and inhibited the growth of HS.④ The positive electret 5-FU patch had better inhibiting effect in HS growth than 5-FU patch. Conclusion The combination of positive electret and 5-FU can achieve better results in inhibiting the growth of hypertrophic scar.
2019, 37(2): 121-125.
doi: 10.3969/j.issn.1006-0111.2019.02.005
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Objective To explore the impact of chronic unpredicted mild stress (CUMS)induced depression on mRNA and protein expression of liver organic anion transporting polypeptides (Oatps) in rats. Methods Twenty-four male SD rats were divided into depression group and control group.Rats in depression group were exposed CUMS for 8 weeks consecutively.Weight,open-field test,sucrose preference,plasma concentration of noradrenaline and corticosterone were assayed before and after model establishment to evaluate the depression.The mRNA and protein expression of liver Oatp1a1,Oatp1a4 and Oatp1b2 were measured by RT-qPCR and Western blotting,respectively. Results In CUMS induced depression group,weight,sucrose consumption,vertical score and horizontal score were decreased while levels of corticosterone and norepinephrine were increased compared with control group.The mRNA and protein expression of liver Oatp1a1,Oatp1a4 and Oatp1b2 were reduced compared with control group. Conclusion The mRNA and protein expression of liver Oatps in rats were regulated down by CUMS induced depression.
Objective To explore the impact of chronic unpredicted mild stress (CUMS)induced depression on mRNA and protein expression of liver organic anion transporting polypeptides (Oatps) in rats. Methods Twenty-four male SD rats were divided into depression group and control group.Rats in depression group were exposed CUMS for 8 weeks consecutively.Weight,open-field test,sucrose preference,plasma concentration of noradrenaline and corticosterone were assayed before and after model establishment to evaluate the depression.The mRNA and protein expression of liver Oatp1a1,Oatp1a4 and Oatp1b2 were measured by RT-qPCR and Western blotting,respectively. Results In CUMS induced depression group,weight,sucrose consumption,vertical score and horizontal score were decreased while levels of corticosterone and norepinephrine were increased compared with control group.The mRNA and protein expression of liver Oatp1a1,Oatp1a4 and Oatp1b2 were reduced compared with control group. Conclusion The mRNA and protein expression of liver Oatps in rats were regulated down by CUMS induced depression.
2019, 37(2): 126-134.
doi: 10.3969/j.issn.1006-0111.2019.02.006
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Objective To explore the intrinsic mechanism of kidney injury due to calcium oxalate crystal by the study on the changes of metabolites in the urine of mice. Method UPLC-Q-TOF/MS-based metabolomics method was used to determine the changes of endogenous metabolites in mice urine with glyoxylate-induced mouse calcium oxalate crystal model.The multivariate statistics analysis and metabolite pathway analysis were performed by SIMCA-P and Metabo Analyst software respectively. Result Compared with the control group,the kidney tissue of the model group showed obvious calcium salt deposition and the serum creatinine and urea nitrogen levels increased abnormally.21 differential metabolites,such as uric acid,taurine and phenylalanine,were detected from the urine. Conclusion The differential metabolites mainly involve amino acid metabolism,energy metabolism,taurine metabolism,purine metabolism and VB6 metabolism,which is of great importantce to the mechanism study and the biomaker screening for the early stage stone disease.
Objective To explore the intrinsic mechanism of kidney injury due to calcium oxalate crystal by the study on the changes of metabolites in the urine of mice. Method UPLC-Q-TOF/MS-based metabolomics method was used to determine the changes of endogenous metabolites in mice urine with glyoxylate-induced mouse calcium oxalate crystal model.The multivariate statistics analysis and metabolite pathway analysis were performed by SIMCA-P and Metabo Analyst software respectively. Result Compared with the control group,the kidney tissue of the model group showed obvious calcium salt deposition and the serum creatinine and urea nitrogen levels increased abnormally.21 differential metabolites,such as uric acid,taurine and phenylalanine,were detected from the urine. Conclusion The differential metabolites mainly involve amino acid metabolism,energy metabolism,taurine metabolism,purine metabolism and VB6 metabolism,which is of great importantce to the mechanism study and the biomaker screening for the early stage stone disease.
2019, 37(2): 135-140,150.
doi: 10.3969/j.issn.1006-0111.2019.02.007
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Objective To develop a multi-purpose protective cream with waterproof,sunscreen and jellyfish sting protection and optimize the formulation to provide good water resistance,high SPF,suitable viscosity and good stability. Methods The mass fraction of the film former VP/Hexadecene copolymer (Antaron V-216) in the formulation was optimized through the measurement of SPF value,critical wavelength and water resistance.Based on viscosity,centrifugal stability and freeze-thaw stability,the central composite design-response surface method was used to optimize the mass fraction of two emulsifiers and CaCl2 aqueous solution in the cream. Results When the film former Antaron V-216 has a mass fraction of 3%,the SPF value of the cream is significantly increased.When the mass fraction of emulsifier lauryl PEG/PPG-18/18 methicone (DC5200) is 0.76%,the mass fraction of emulsifier cetyl PEG/PPG-10/1 dimethicone (EM180) is 2.32% and the mass fraction of CaCl2 aqueous solution is 44.86%,the cream has suitable viscosity and good stability. Conclusion The optimized formulation has high water resistance and SPF value,suitable viscosity and good stability.
Objective To develop a multi-purpose protective cream with waterproof,sunscreen and jellyfish sting protection and optimize the formulation to provide good water resistance,high SPF,suitable viscosity and good stability. Methods The mass fraction of the film former VP/Hexadecene copolymer (Antaron V-216) in the formulation was optimized through the measurement of SPF value,critical wavelength and water resistance.Based on viscosity,centrifugal stability and freeze-thaw stability,the central composite design-response surface method was used to optimize the mass fraction of two emulsifiers and CaCl2 aqueous solution in the cream. Results When the film former Antaron V-216 has a mass fraction of 3%,the SPF value of the cream is significantly increased.When the mass fraction of emulsifier lauryl PEG/PPG-18/18 methicone (DC5200) is 0.76%,the mass fraction of emulsifier cetyl PEG/PPG-10/1 dimethicone (EM180) is 2.32% and the mass fraction of CaCl2 aqueous solution is 44.86%,the cream has suitable viscosity and good stability. Conclusion The optimized formulation has high water resistance and SPF value,suitable viscosity and good stability.
2019, 37(2): 141-145.
doi: 10.3969/j.issn.1006-0111.2019.02.008
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Objective To explore the possible mechanism of synergistic effect of synbiotic preparations by regulating intestinal flora to achieve antihypertensive effect by the metabolomics-related techniques. Methods Fourteen spontaneously hypertensive rats were randomly divided into two groups,7 rats in each of the model group and the treatment group,and another 7 Wistar Kyoto rats were used as the control group.Ileum metabolic profiling among the control group,Spontaneous hypertension model group and symbiotic treatment group were analyzed by ultra-high performance liquid chromatography coupled with tandem quadrupole time of flight mass spectrometry (UHPLC-Q-TOF MS).The potential biomarkers for the treatment of spontaneous hypertension were selected. Results In additional,27 metabolites with significant differences between the control and model group were identified by analysis of metabonomics.Among these metabolites,LysoPE and PC could be significantly re-regulated in the treatment group,compared with the model group. Conclusion Synbiotics could improve the status of spontaneous hypertension by changing the structure of the intestinal microbiota,regulating LysoPE and PC-related signaling pathways.Metabolomics could help to understand the pathogenesis of essential hypertension and the hypotensive mechanism of synbiotics at the molecular level.
Objective To explore the possible mechanism of synergistic effect of synbiotic preparations by regulating intestinal flora to achieve antihypertensive effect by the metabolomics-related techniques. Methods Fourteen spontaneously hypertensive rats were randomly divided into two groups,7 rats in each of the model group and the treatment group,and another 7 Wistar Kyoto rats were used as the control group.Ileum metabolic profiling among the control group,Spontaneous hypertension model group and symbiotic treatment group were analyzed by ultra-high performance liquid chromatography coupled with tandem quadrupole time of flight mass spectrometry (UHPLC-Q-TOF MS).The potential biomarkers for the treatment of spontaneous hypertension were selected. Results In additional,27 metabolites with significant differences between the control and model group were identified by analysis of metabonomics.Among these metabolites,LysoPE and PC could be significantly re-regulated in the treatment group,compared with the model group. Conclusion Synbiotics could improve the status of spontaneous hypertension by changing the structure of the intestinal microbiota,regulating LysoPE and PC-related signaling pathways.Metabolomics could help to understand the pathogenesis of essential hypertension and the hypotensive mechanism of synbiotics at the molecular level.
2019, 37(2): 146-150.
doi: 10.3969/j.issn.1006-0111.2019.02.009
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Objective To study the protective effect and mechanism of dichloroacetate (DCA) on BV2 microglia in oxygen glucose deprivation (OGD) injury model. Methods BV2 cells were divided into 3 groups:CON group,OGD group and DCA intervention group.The injury model was established by OGD 4 h.CCK-8 and flow cytometry was used to detect apoptosis and expression of ROS and NO in cells.Western blot was used to detect the expression of proteins related to NF-κB pathway. Results CCK-8 and flow cytometry showed that the apoptosis of BV2 cells induced by OGD and the expression of ROS and NO in OGD cells were decreased significantly by DCA (P<0.05).Western blot analysis showed that the expression of I-κB,JNK and NF-κB protein in BV2 cells mediated by OGD injury were influenced significantly by DCA (P<0.05). Conclusion DCA had a protective effect on OGD-injured BV2 cells through anti-oxidation and anti-apoptosis.
Objective To study the protective effect and mechanism of dichloroacetate (DCA) on BV2 microglia in oxygen glucose deprivation (OGD) injury model. Methods BV2 cells were divided into 3 groups:CON group,OGD group and DCA intervention group.The injury model was established by OGD 4 h.CCK-8 and flow cytometry was used to detect apoptosis and expression of ROS and NO in cells.Western blot was used to detect the expression of proteins related to NF-κB pathway. Results CCK-8 and flow cytometry showed that the apoptosis of BV2 cells induced by OGD and the expression of ROS and NO in OGD cells were decreased significantly by DCA (P<0.05).Western blot analysis showed that the expression of I-κB,JNK and NF-κB protein in BV2 cells mediated by OGD injury were influenced significantly by DCA (P<0.05). Conclusion DCA had a protective effect on OGD-injured BV2 cells through anti-oxidation and anti-apoptosis.
2019, 37(2): 151-155.
doi: 10.3969/j.issn.1006-0111.2019.02.010
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Objective To investigate the active secondary metabolites of coral derived fungi Aspergillus flavipes. Methods Compounds were isolated and purified by means of various chromatographic techniques,including Silica gel column chromatography,Sephadex LH-20 chromatography and HPLC.The structure of the compounds was identified by NMR combined with the data reported.The nuclear factor kappa B receptor activating factor ligand (RANKL) was used to induce bone marrow macrophage cells (BMMs) differentiate into mature osteoclasts.The tartrate-resistant acid phosphatase (TRAP) specific staining was used to test the inhibitory activity of compounds on osteoclast differentiation. Results Four cytochalasins were isolated from the fungus and their structures were identified as trichalasins H,aspergilluchalasin,aspochalasin I and aspochalasin D.Compounds 3 and 4 showed inhibitory activity on osteoclast differentiation. Conclusion This was the first report of inhibiting osteoclast differentiation activity of compounds 3 and 4.These two compounds might have great significance in the study of new anti-osteoporosis drugs.
Objective To investigate the active secondary metabolites of coral derived fungi Aspergillus flavipes. Methods Compounds were isolated and purified by means of various chromatographic techniques,including Silica gel column chromatography,Sephadex LH-20 chromatography and HPLC.The structure of the compounds was identified by NMR combined with the data reported.The nuclear factor kappa B receptor activating factor ligand (RANKL) was used to induce bone marrow macrophage cells (BMMs) differentiate into mature osteoclasts.The tartrate-resistant acid phosphatase (TRAP) specific staining was used to test the inhibitory activity of compounds on osteoclast differentiation. Results Four cytochalasins were isolated from the fungus and their structures were identified as trichalasins H,aspergilluchalasin,aspochalasin I and aspochalasin D.Compounds 3 and 4 showed inhibitory activity on osteoclast differentiation. Conclusion This was the first report of inhibiting osteoclast differentiation activity of compounds 3 and 4.These two compounds might have great significance in the study of new anti-osteoporosis drugs.
2019, 37(2): 156-161,169.
doi: 10.3969/j.issn.1006-0111.2019.02.011
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Objective To develop a rapid method to characterize the inhibitory effect of amphotericin B(AMB) against Candida albicans by dynamic surface enhanced Raman spectroscopy(D-SERS). Methods D-SERS were applied to analyze the effect of AMB on the Raman spectra of C.albicans by examining the relationship between the peak intensity ratio and the concentration of drug at Raman shift at 656 cm-1 and 729 cm-1 under different interaction time by a sensitive C.albicans and different AMB concentrations. Results The peak intensity ratio was negatively correlated with the concentration of AMB,which could be used to describe the inhibitory effect of AMB on C.albicans in a certain concentration and action time. Conclusion This method could characterize the inhibitory effect of AMB against C.albicans rapidly,which provided a simpler and faster detection method for characterizing more drug-pathogen interactions.
Objective To develop a rapid method to characterize the inhibitory effect of amphotericin B(AMB) against Candida albicans by dynamic surface enhanced Raman spectroscopy(D-SERS). Methods D-SERS were applied to analyze the effect of AMB on the Raman spectra of C.albicans by examining the relationship between the peak intensity ratio and the concentration of drug at Raman shift at 656 cm-1 and 729 cm-1 under different interaction time by a sensitive C.albicans and different AMB concentrations. Results The peak intensity ratio was negatively correlated with the concentration of AMB,which could be used to describe the inhibitory effect of AMB on C.albicans in a certain concentration and action time. Conclusion This method could characterize the inhibitory effect of AMB against C.albicans rapidly,which provided a simpler and faster detection method for characterizing more drug-pathogen interactions.
2019, 37(2): 162-165.
doi: 10.3969/j.issn.1006-0111.2019.02.012
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Objective To establish a HPLC method for the determination of the voriconazole concentration in human plasma,which can be used for voriconazole monitoring clinically. Methods High performance liquid chromatography (HPLC-UV) detection method was used with papaverine as internal standard.Acetonitrile protein precipitation method was employed to treat plasma samples.The chromatographic column was ACE5C18-AR150 mm×4.6 mm with the mobile phase 0.025 mol/L sodium dihydrogen phosphate (containing triethylamine 400 μl/L,pH=7.0 adjusted by 0.25 mol/L sodium hydroxide) - acetonitrile (67∶33).The flow rate was l ml/min,the column temperature at 40 ℃,the detection wavelength at 255,276 nm (double wavelength detection) and sampling amount 20 μl. Results The retention time of voriconazole nitrogen oxide,voriconazole and papaverine were 4.5,11.3 and 13.7 min respectively.The linear ranges of voriconazole and voriconazole nitrogen oxides in plasma were 0.5-20.0 μg/ml (r=0.999 5).The quantitative lower limits were 0.5 μg/ml with RSD< 11%.The recovery rates of extraction were between 90.3% and 109.9%. Conclusion This simple and accurate method is suitable for clinical monitoring of voriconazole.
Objective To establish a HPLC method for the determination of the voriconazole concentration in human plasma,which can be used for voriconazole monitoring clinically. Methods High performance liquid chromatography (HPLC-UV) detection method was used with papaverine as internal standard.Acetonitrile protein precipitation method was employed to treat plasma samples.The chromatographic column was ACE5C18-AR150 mm×4.6 mm with the mobile phase 0.025 mol/L sodium dihydrogen phosphate (containing triethylamine 400 μl/L,pH=7.0 adjusted by 0.25 mol/L sodium hydroxide) - acetonitrile (67∶33).The flow rate was l ml/min,the column temperature at 40 ℃,the detection wavelength at 255,276 nm (double wavelength detection) and sampling amount 20 μl. Results The retention time of voriconazole nitrogen oxide,voriconazole and papaverine were 4.5,11.3 and 13.7 min respectively.The linear ranges of voriconazole and voriconazole nitrogen oxides in plasma were 0.5-20.0 μg/ml (r=0.999 5).The quantitative lower limits were 0.5 μg/ml with RSD< 11%.The recovery rates of extraction were between 90.3% and 109.9%. Conclusion This simple and accurate method is suitable for clinical monitoring of voriconazole.
2019, 37(2): 166-169.
doi: 10.3969/j.issn.1006-0111.2019.02.013
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Objective To study the preparation process of bromhexine hydrochloride nasal drop,develop the assay method for the main component in the drop and evaluate its transdermal penetration in vitro. Methods The bromhexine hydrochloride was prepared with dispersion method. HPLC was used for the assay. The flow phase is methanol-acetic acid solution (55∶45). The flow rate was 1.0 ml/min. The detection wavelength was 247 nm. The column temperature was 30 ℃. The in vitro transdermal test was carried out on KM mice. Results Bromhexine hydrochloride nasal drop was a suspension preparation. Bromhexine hydrochloride presented good linearity in the range of 37.44-187.2 μg/ml with the regression equation Y=11.996X+124.6 (r=0.9999). The average recoveries of low,medium and high concentrations were 104.00%,101.59%,98.51% respectively with RSD of 0.89%,1.35%,0.35%(n=9). The cumulative penetration rate of bromhexine hydrochloride in 24 h was 60.29%. Conclusion This nasal drop formulation was acceptable. The preparation process was feasible and assay method was accurate and reliable.
Objective To study the preparation process of bromhexine hydrochloride nasal drop,develop the assay method for the main component in the drop and evaluate its transdermal penetration in vitro. Methods The bromhexine hydrochloride was prepared with dispersion method. HPLC was used for the assay. The flow phase is methanol-acetic acid solution (55∶45). The flow rate was 1.0 ml/min. The detection wavelength was 247 nm. The column temperature was 30 ℃. The in vitro transdermal test was carried out on KM mice. Results Bromhexine hydrochloride nasal drop was a suspension preparation. Bromhexine hydrochloride presented good linearity in the range of 37.44-187.2 μg/ml with the regression equation Y=11.996X+124.6 (r=0.9999). The average recoveries of low,medium and high concentrations were 104.00%,101.59%,98.51% respectively with RSD of 0.89%,1.35%,0.35%(n=9). The cumulative penetration rate of bromhexine hydrochloride in 24 h was 60.29%. Conclusion This nasal drop formulation was acceptable. The preparation process was feasible and assay method was accurate and reliable.
2019, 37(2): 170-172,187.
doi: 10.3969/j.issn.1006-0111.2019.02.014
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Objective To develop a method for the determination of the dissolution of Zhibitai capsules. Methods The chromatographic analysis was carried out on a ZABAX-C18column(250 mm×4.6 mm,5 μm)with methanol-0.05% phosphate solution(60∶40) as mobile phase.The flow rate was 1.0 ml/min and the detection wavelength was 238 nm.According to the third dissolution method (small glass-method) described in the Pharmacopoeia of the People's Republic of China (2015Edition,Volume 4),the dissolution determination conditions were established using SOTAX AT7 intelligent drug dissolution instrument,and dissolution medium,rotational speed and sampling time were selected. Results The method showed perfect specificity under the established chromatographic conditions.The linear ranges of lovastatin was 1.63-122.2 μg/ml(r=1.000 0).The dissolution rates of the samples were consistent.The 1.0% sodium dodecyl sulfate in phosphate solution (pH 7.0) was selected as release media,rotational speed was 100 r/min,the sampling time point was 45 min.The dissolution limit was not less than 80% of the labeled amount. Conclusion The established method could be used for the dissolution determination and the quality control,and provide reference for the improvement of quality standards of Zhibitai capsules.
Objective To develop a method for the determination of the dissolution of Zhibitai capsules. Methods The chromatographic analysis was carried out on a ZABAX-C18column(250 mm×4.6 mm,5 μm)with methanol-0.05% phosphate solution(60∶40) as mobile phase.The flow rate was 1.0 ml/min and the detection wavelength was 238 nm.According to the third dissolution method (small glass-method) described in the Pharmacopoeia of the People's Republic of China (2015Edition,Volume 4),the dissolution determination conditions were established using SOTAX AT7 intelligent drug dissolution instrument,and dissolution medium,rotational speed and sampling time were selected. Results The method showed perfect specificity under the established chromatographic conditions.The linear ranges of lovastatin was 1.63-122.2 μg/ml(r=1.000 0).The dissolution rates of the samples were consistent.The 1.0% sodium dodecyl sulfate in phosphate solution (pH 7.0) was selected as release media,rotational speed was 100 r/min,the sampling time point was 45 min.The dissolution limit was not less than 80% of the labeled amount. Conclusion The established method could be used for the dissolution determination and the quality control,and provide reference for the improvement of quality standards of Zhibitai capsules.
2019, 37(2): 173-176.
doi: 10.3969/j.issn.1006-0111.2019.02.015
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Objective To establish a method for the assay of six active ingredients in Kuhuang injection and study the infusion stability prepared with three different solvents. Methods ①UPLC-MS/MS was used to determine the contents of matrine,dioscin,emodin,rhein,aloe emodin,and saikosaponin A from Sophora flavescens,Rhubarb Artemisia oleracea,and Radix Bupleuri in Kuhuang injection. ②36 hour stability study at room temperature was conducted on the infusions prepared with 5% glucose solution,10% glucose solution and fructose injection. Results ①6 active ingredients in Kuhuang injection were completely separated in 15 minutes and the peak area was linear with the concentration for each component. The stability of the solution was good within 24 hours and the average recovery rate was between 99.86% and 99.92%. ②All three infusion was clear after 36 hours,no turbidity,sedimentation or color change. The pH value of 10% glucose infusion in the minimal dose group with indoor illumination was significantly increased after 8 h. The stability for shading group was better than illumination group. In the maximum dose group,the infusion made with fructose had micro particles after 24 hours and did not meet the requirements. All the rests met the requirements after 36 hours. Conclusion UPLC-MS/MS method is simple,accurate and reliable. It can be used for the determination of active ingredients in Kuhuang injection. Specifically,fructose injection is not a suitable solvent for Kuhuang injection. The infusion should be kept shaded to improve the stability.
Objective To establish a method for the assay of six active ingredients in Kuhuang injection and study the infusion stability prepared with three different solvents. Methods ①UPLC-MS/MS was used to determine the contents of matrine,dioscin,emodin,rhein,aloe emodin,and saikosaponin A from Sophora flavescens,Rhubarb Artemisia oleracea,and Radix Bupleuri in Kuhuang injection. ②36 hour stability study at room temperature was conducted on the infusions prepared with 5% glucose solution,10% glucose solution and fructose injection. Results ①6 active ingredients in Kuhuang injection were completely separated in 15 minutes and the peak area was linear with the concentration for each component. The stability of the solution was good within 24 hours and the average recovery rate was between 99.86% and 99.92%. ②All three infusion was clear after 36 hours,no turbidity,sedimentation or color change. The pH value of 10% glucose infusion in the minimal dose group with indoor illumination was significantly increased after 8 h. The stability for shading group was better than illumination group. In the maximum dose group,the infusion made with fructose had micro particles after 24 hours and did not meet the requirements. All the rests met the requirements after 36 hours. Conclusion UPLC-MS/MS method is simple,accurate and reliable. It can be used for the determination of active ingredients in Kuhuang injection. Specifically,fructose injection is not a suitable solvent for Kuhuang injection. The infusion should be kept shaded to improve the stability.
2019, 37(2): 177-182.
doi: 10.3969/j.issn.1006-0111.2019.02.016
Abstract:
Objective To establish an one step assay method for 10 active components (neochlorogenic acid,chlorogenic acid,cryptochlorogenic acid,caffeic acid,forsythoside B,forsythoside A,baicalin,wogonoside,baicalein,wogonin)in compound Jinyinhua granules. Methods The Kromasil C18 column (250 mm×4.6 mm，5 μm) was used with the column temperature at 35 ℃ and PDA detection wavelength at 320 nm.A gradient elution with acetonitri-0.1% phosphoric acid was adopted at the flow rate of 0.8 ml/min.The injection volume was 10 μl. Results The good resolution was achieved for the 10 active components.The linear ranges of neochlorogenic acid,chlorogenic acid,cryptochlorogenic acid,caffeic acid,forsythoside B,forsythoside A,baicalin,wogonoside,baicalein,wogonin were 10.20-340.06,7.19-239.81,6.12-203.84,15.00-500.00,20.16-671.85,25.19-839.67,14.61-487.14,10.52-350.66,7.32-244.01,7.61-253.82 μg/ml respectively.The average recoveries (n=6) were between 97.67% and 99.00% and RSDs between 0.94% and 1.37%.The average contents of neochlorogenic acid,chlorogenic acid,cryptochlorogenic acid,caffeic acid,forsythoside B,forsythoside A,baicalin,wogonoside,baicalein,wogonin from 10 batches of preparations were 0.579 0,1.523 5,1.080 9,0.083 1,0.468 0,0.739 6,1.977 9,0.351 5,0.246 8 and 0.256 6 mg/g. Conclusion This simple and accurate method can be used as one of quality control methods for the compound Jinyinhua granules.
Objective To establish an one step assay method for 10 active components (neochlorogenic acid,chlorogenic acid,cryptochlorogenic acid,caffeic acid,forsythoside B,forsythoside A,baicalin,wogonoside,baicalein,wogonin)in compound Jinyinhua granules. Methods The Kromasil C18 column (250 mm×4.6 mm，5 μm) was used with the column temperature at 35 ℃ and PDA detection wavelength at 320 nm.A gradient elution with acetonitri-0.1% phosphoric acid was adopted at the flow rate of 0.8 ml/min.The injection volume was 10 μl. Results The good resolution was achieved for the 10 active components.The linear ranges of neochlorogenic acid,chlorogenic acid,cryptochlorogenic acid,caffeic acid,forsythoside B,forsythoside A,baicalin,wogonoside,baicalein,wogonin were 10.20-340.06,7.19-239.81,6.12-203.84,15.00-500.00,20.16-671.85,25.19-839.67,14.61-487.14,10.52-350.66,7.32-244.01,7.61-253.82 μg/ml respectively.The average recoveries (n=6) were between 97.67% and 99.00% and RSDs between 0.94% and 1.37%.The average contents of neochlorogenic acid,chlorogenic acid,cryptochlorogenic acid,caffeic acid,forsythoside B,forsythoside A,baicalin,wogonoside,baicalein,wogonin from 10 batches of preparations were 0.579 0,1.523 5,1.080 9,0.083 1,0.468 0,0.739 6,1.977 9,0.351 5,0.246 8 and 0.256 6 mg/g. Conclusion This simple and accurate method can be used as one of quality control methods for the compound Jinyinhua granules.
2019, 37(2): 183-187.
doi: 10.3969/j.issn.1006-0111.2019.02.017
Abstract:
Objective To participate in the clinical treatment and pharmaceutical care for a patient with subacute stent thrombosis complicated with liver-function abnormalities after percutaneous coronary intervention(PCI)and to explore the role of clinical pharmacists in the treatment group. Methods Clinical pharmacists took an active part in the treatment process by analyzing the causes of subacute stent thrombosis and abnormal liver function after PCI.Pharmaceutical professional knowledge was used according to the patient's condition,genotype,combined medication,interaction,and adverse reaction and so on.The patient's antiplatelet therapy was timely adjusted to ticagrelor 90 mg po bid,and the dose of rosuvastatin was 10 mg po qn.Pharmaceutical care and medication education were also provided. Results The suggestions of clinical pharmacists were adopted by physicians and the patient was recovered. Conclusion Clinical pharmacists should use professional skill to assist physician to adjust the drug treatment program for patients,so as to guarantee the safe and effective of medicines use.
Objective To participate in the clinical treatment and pharmaceutical care for a patient with subacute stent thrombosis complicated with liver-function abnormalities after percutaneous coronary intervention(PCI)and to explore the role of clinical pharmacists in the treatment group. Methods Clinical pharmacists took an active part in the treatment process by analyzing the causes of subacute stent thrombosis and abnormal liver function after PCI.Pharmaceutical professional knowledge was used according to the patient's condition,genotype,combined medication,interaction,and adverse reaction and so on.The patient's antiplatelet therapy was timely adjusted to ticagrelor 90 mg po bid,and the dose of rosuvastatin was 10 mg po qn.Pharmaceutical care and medication education were also provided. Results The suggestions of clinical pharmacists were adopted by physicians and the patient was recovered. Conclusion Clinical pharmacists should use professional skill to assist physician to adjust the drug treatment program for patients,so as to guarantee the safe and effective of medicines use.
2019, 37(2): 188-192.
doi: 10.3969/j.issn.1006-0111.2019.02.018
Abstract:
Objective To systematically evaluate the adverse drug reactions(ADR) and the Adverse drug events(ADE) of children using different aminopyrine in order to know the distribution of ADR and ADE, including the organ distribution, severity distribution, composition and influential factors of ADR and ADE. Methods Literature was retrieved in electronic databases covering CNKI,VIP, WANFANG data,CBM, Embase and PubMed, aminopyrine, analgin, medicine with the components of aminopyrine, and adverse drug reactions, adverse drug events, allergies etc. were taken as free words for comprehensive search. According to the criteria of inclusion and exclusion, the data were selected and collected. The total number and composition ratio of aminopyrine's ADR and ADE were calculated and the differences between the analgin, compound aminopyrine and the components of aminopyrine were analyzed according to different categories (age, drug allergy history, organ system involved, combination therapy, etc.). Results ① A total of 484 Chinese literatures were included, including 555 cases，there were 205 cases of children;② A total of 70 English literatures were included, including 73 cases, there were 34 cases of children;③ The ADR/ADE reported in Chinese and English literatures mainly involving the hematopoietic system, mucocutaneous system, urinary system, circulatory system which led to systemic reactions such as shock. The prognosis varies, with 174 cases recovered(72.80%), 30 cases death (12.55%)and 14 cases (5.86%) of the outcome were bone marrow transplantation, finger and toe amputation, subtotal gastrectomy and other serious adverse reactions. ④ most of the adverse reactions of the dose for the regular dose, but there were also over-dose medical staff caused by adverse events. Conclusion The use of aminopyrine might cause serious damage to children's hematopoietic system and urinary system, with serious adverse reactions and even deaths reported annually. It was suggested that aminopyrine as a potentially lethal drug should be withdrawal quickly.
Objective To systematically evaluate the adverse drug reactions(ADR) and the Adverse drug events(ADE) of children using different aminopyrine in order to know the distribution of ADR and ADE, including the organ distribution, severity distribution, composition and influential factors of ADR and ADE. Methods Literature was retrieved in electronic databases covering CNKI,VIP, WANFANG data,CBM, Embase and PubMed, aminopyrine, analgin, medicine with the components of aminopyrine, and adverse drug reactions, adverse drug events, allergies etc. were taken as free words for comprehensive search. According to the criteria of inclusion and exclusion, the data were selected and collected. The total number and composition ratio of aminopyrine's ADR and ADE were calculated and the differences between the analgin, compound aminopyrine and the components of aminopyrine were analyzed according to different categories (age, drug allergy history, organ system involved, combination therapy, etc.). Results ① A total of 484 Chinese literatures were included, including 555 cases，there were 205 cases of children;② A total of 70 English literatures were included, including 73 cases, there were 34 cases of children;③ The ADR/ADE reported in Chinese and English literatures mainly involving the hematopoietic system, mucocutaneous system, urinary system, circulatory system which led to systemic reactions such as shock. The prognosis varies, with 174 cases recovered(72.80%), 30 cases death (12.55%)and 14 cases (5.86%) of the outcome were bone marrow transplantation, finger and toe amputation, subtotal gastrectomy and other serious adverse reactions. ④ most of the adverse reactions of the dose for the regular dose, but there were also over-dose medical staff caused by adverse events. Conclusion The use of aminopyrine might cause serious damage to children's hematopoietic system and urinary system, with serious adverse reactions and even deaths reported annually. It was suggested that aminopyrine as a potentially lethal drug should be withdrawal quickly.
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