2007 Vol. 25, No. 6
Display Method:
2007, (6): 353-357.
Abstract:
The rutaecarpine is an effective component from Evodia rutaecarpa(Juss.) Benth.Current advances in the study of rutaecarpine is reviewed,including synthesize,effects on metabolizing enzyme,metabolic mechanism, pharmacological activity,etc.
The rutaecarpine is an effective component from Evodia rutaecarpa(Juss.) Benth.Current advances in the study of rutaecarpine is reviewed,including synthesize,effects on metabolizing enzyme,metabolic mechanism, pharmacological activity,etc.
2007, (6): 369-371.
Abstract:
Objective :To compare the effect of simvastatin in the hyperlipemia model of the golden hamster and the Wistar rat,discuss the reasonable application of the two animal hyperlipemia models. Methods :Thirty male golden hamsters weighing 100-130 g and thirty male Wistar rat weighing 200-300 g were respectively randomized into 3 groups with 10 in each,named as the normal group,model group and simvastatin group.After the models of hyperlipemia were established,the simvastatin groups were treated with the dosage of 10mg/（kg·d） simvastatin.Observe the effect of simvastatin on lipid level in the 14th and 28th day.Analysed the effect of simvastatin in the two hyperlipemia models. Results :Simvastatin decreased the lipid level of the two hyperlipemia model.The effect in Wistar rat is better than in golden hamster. Conclusion : Wistar rat is more susceptible to simvastatin than golden hamster.The hyperlipemia model of Wistar rat is adapt to the application of the selection of cholesterol-lowering drugs.The hyperlipemia model of golden hamster is suit to the before clinical research of the novel cholesterol-lowering drugs.
Objective :To compare the effect of simvastatin in the hyperlipemia model of the golden hamster and the Wistar rat,discuss the reasonable application of the two animal hyperlipemia models. Methods :Thirty male golden hamsters weighing 100-130 g and thirty male Wistar rat weighing 200-300 g were respectively randomized into 3 groups with 10 in each,named as the normal group,model group and simvastatin group.After the models of hyperlipemia were established,the simvastatin groups were treated with the dosage of 10mg/（kg·d） simvastatin.Observe the effect of simvastatin on lipid level in the 14th and 28th day.Analysed the effect of simvastatin in the two hyperlipemia models. Results :Simvastatin decreased the lipid level of the two hyperlipemia model.The effect in Wistar rat is better than in golden hamster. Conclusion : Wistar rat is more susceptible to simvastatin than golden hamster.The hyperlipemia model of Wistar rat is adapt to the application of the selection of cholesterol-lowering drugs.The hyperlipemia model of golden hamster is suit to the before clinical research of the novel cholesterol-lowering drugs.
2007, (6): 372-375.
Abstract:
Objective :To determine the structural features of a set of diverse colchicines-site inhibitors. Methods :The features were revealed by matching the binding conformations generated from docking studies of eight inhibitors,and combined with the available SAR results. Results : The feature is represented as two hydrophobic groups（A and B） and a bridge linked between them,but A and B should be in the same side of the bridge.The volume size and the existence of hydrogen-bond acceptor of group A may have some influence on binding.Group B should be a hydrophobic planar ring,and polar functional group is advantageous.The bridge part could accept 1-4 atoms,but the Sp2 hybrid is welcome. Conclusion :this result may provide useful insights for the design of novel Colchicine-site inhibitors.
Objective :To determine the structural features of a set of diverse colchicines-site inhibitors. Methods :The features were revealed by matching the binding conformations generated from docking studies of eight inhibitors,and combined with the available SAR results. Results : The feature is represented as two hydrophobic groups（A and B） and a bridge linked between them,but A and B should be in the same side of the bridge.The volume size and the existence of hydrogen-bond acceptor of group A may have some influence on binding.Group B should be a hydrophobic planar ring,and polar functional group is advantageous.The bridge part could accept 1-4 atoms,but the Sp2 hybrid is welcome. Conclusion :this result may provide useful insights for the design of novel Colchicine-site inhibitors.
2007, (6): 376-378.
Abstract:
Objective :To observe the stability of cefotaxime(CTX) to broad-and extended-spectrum β-lactamase,and to compare inhibiting-βlactamase activities of tazobactam and sulbactam. Methods : 60 strains of Gram-negative bacilli from Affiliated Hospital of North Sichuan Medical College were dealed with ultrasonic wave and their β-lactamases were extracted and these enzymes were detected by three-dimensional test.β-lactamase activitiy and hydrolysis of CTX were quantitated spectrophotometrically and calculated. Results :In these β-lactamases of 60 strains of Gram-negitive bacilli,the number of extended-spectrum β-lactamases and broad-spectrum β-lactamases were 31 and 29,respectively,and their medians of enzyme activities were 3 094 U and 528 U(P<0.05).The medians of β-lactamases activities of Escherichia coli,Enterobacter cloacae and Pseudomonas aeruginosa were 2 656 U,1 185 U and 165.5 U,respectively.The median of hydrolysis rates(HR) of CTX by ESBLs and BSBLs were 20.10% and 3.15%,respectively(P<0.05).The combination of CTX/TAZ and CTX/SBT(the ratio=2-1) could make the HR drop significantly(P<0.05),but the effects of TAZ and SBT were of no differences(P>0.05). Conclusion :The hydrolysis activities of ESBLs on CTX was higher than that of BSBLs.TAZ and SBT could effectively inhibit hydrolysis of CTX by β-lactamases,but these two inhibitors had little difference in their potency.
Objective :To observe the stability of cefotaxime(CTX) to broad-and extended-spectrum β-lactamase,and to compare inhibiting-βlactamase activities of tazobactam and sulbactam. Methods : 60 strains of Gram-negative bacilli from Affiliated Hospital of North Sichuan Medical College were dealed with ultrasonic wave and their β-lactamases were extracted and these enzymes were detected by three-dimensional test.β-lactamase activitiy and hydrolysis of CTX were quantitated spectrophotometrically and calculated. Results :In these β-lactamases of 60 strains of Gram-negitive bacilli,the number of extended-spectrum β-lactamases and broad-spectrum β-lactamases were 31 and 29,respectively,and their medians of enzyme activities were 3 094 U and 528 U(P<0.05).The medians of β-lactamases activities of Escherichia coli,Enterobacter cloacae and Pseudomonas aeruginosa were 2 656 U,1 185 U and 165.5 U,respectively.The median of hydrolysis rates(HR) of CTX by ESBLs and BSBLs were 20.10% and 3.15%,respectively(P<0.05).The combination of CTX/TAZ and CTX/SBT(the ratio=2-1) could make the HR drop significantly(P<0.05),but the effects of TAZ and SBT were of no differences(P>0.05). Conclusion :The hydrolysis activities of ESBLs on CTX was higher than that of BSBLs.TAZ and SBT could effectively inhibit hydrolysis of CTX by β-lactamases,but these two inhibitors had little difference in their potency.
2007, (6): 379-381.
Abstract:
Objective :To establish a simple,rapid,sensitive column-switching HPLC method for the analysis of the 10-hydroxycamptothecin（HCPT） in human serum. Methods : A precolumn containing restricted access media（RAM） was used for the sample clean-up and trace enrichment and was combined with a C18 column for the final separation.The HCPT was monitored with fluorescence detector,excitation and emission wavelengths being 385 and 539 nm,respectively. Results : The analytical time was 8 minutes.There was a linear response range of 1-1 000 ng/mL with correlation coefficient of 0.998 while the limit of detection was 0.1 ng/mL.The intraday and interday variations were less than 5%. Conclusion : This analytic procedure has been applied to a pharmacokinetic study of HCPT in clinical patients and the pharmacokinetic parameters of one-compartment model were calculated.
Objective :To establish a simple,rapid,sensitive column-switching HPLC method for the analysis of the 10-hydroxycamptothecin（HCPT） in human serum. Methods : A precolumn containing restricted access media（RAM） was used for the sample clean-up and trace enrichment and was combined with a C18 column for the final separation.The HCPT was monitored with fluorescence detector,excitation and emission wavelengths being 385 and 539 nm,respectively. Results : The analytical time was 8 minutes.There was a linear response range of 1-1 000 ng/mL with correlation coefficient of 0.998 while the limit of detection was 0.1 ng/mL.The intraday and interday variations were less than 5%. Conclusion : This analytic procedure has been applied to a pharmacokinetic study of HCPT in clinical patients and the pharmacokinetic parameters of one-compartment model were calculated.
2007, (6): 382-385.
Abstract:
Objective :To establish a method to determine the active components of lignans(schisandrin,schisandtherin A,deoxyschizandrin and schisandrin B) in decoction granule of Schisandra chinensis.To find and anylyse the difference of components of different factories. Methods :RP-HPLC method was used.The column was Hypersil ODS C18(4.6 mm×250 mm,10 μm) with the mobile phase of acetonititrile(A) and H2O(B),the flow rate was 1.0 mL/min,the column temperature was set at 25 ℃ and the detection wavelength was set at 254 nm. Results : The content of schisandrin was from 0 to 1.292 3mg/package,schisandtherin A was from 0 to 0.560 8 mg/package,deoxyschizandrin was from 0 to 0.168 8mg/package.Schisandrin B was not detected. Conclusion : The content of schisandrin,schisandtherin A and deoxyschizandrin were obviously different in decoction granule of Schisandra chinensis produced by different factories.
Objective :To establish a method to determine the active components of lignans(schisandrin,schisandtherin A,deoxyschizandrin and schisandrin B) in decoction granule of Schisandra chinensis.To find and anylyse the difference of components of different factories. Methods :RP-HPLC method was used.The column was Hypersil ODS C18(4.6 mm×250 mm,10 μm) with the mobile phase of acetonititrile(A) and H2O(B),the flow rate was 1.0 mL/min,the column temperature was set at 25 ℃ and the detection wavelength was set at 254 nm. Results : The content of schisandrin was from 0 to 1.292 3mg/package,schisandtherin A was from 0 to 0.560 8 mg/package,deoxyschizandrin was from 0 to 0.168 8mg/package.Schisandrin B was not detected. Conclusion : The content of schisandrin,schisandtherin A and deoxyschizandrin were obviously different in decoction granule of Schisandra chinensis produced by different factories.
2007, (6): 386-387,390.
Abstract:
Objective :To compare the effect between the membrane separation technique and the traditional method being used to concentrate polysaccharides from Liuwei Dihuang formula. Methods : The extract liquid of Liuwei Dihuang formula was divided into several levels and segments using nanofiltration and ultrafiltration of 10 000Mr.The polysaccharides in every level's extracted liquid were quantitate by sulfuric acid-anthrone colorimetric method at detecting wavelength 625 nm. Results : The polysaccharides in the production made by membrane separation technique were 6.5 times as much as that in the production made by the traditional method. Conclusion : The membrane separation technique was superior in concentration polysaccharides compared with the traditional method.
Objective :To compare the effect between the membrane separation technique and the traditional method being used to concentrate polysaccharides from Liuwei Dihuang formula. Methods : The extract liquid of Liuwei Dihuang formula was divided into several levels and segments using nanofiltration and ultrafiltration of 10 000Mr.The polysaccharides in every level's extracted liquid were quantitate by sulfuric acid-anthrone colorimetric method at detecting wavelength 625 nm. Results : The polysaccharides in the production made by membrane separation technique were 6.5 times as much as that in the production made by the traditional method. Conclusion : The membrane separation technique was superior in concentration polysaccharides compared with the traditional method.
2007, (6): 388-390.
Abstract:
Objective :To establish a liquid chromatography-electrospray ionization tandem mass spectrometry(LC-ESI-MS-MS) for the identification of glibenclamide and phenformin illegally added in Jiangtang Capsule. Methods :The detection was performed on Altima C18 column with a mobile phase of acetonitrile-formic acid solution(65-35).The above compounds were identified by LC-MS-MS. Results :Glibenclamide and phenformin were detected illegally added in one sample of Jiangtang capsule. Conclusion :This is an effective method with characteristic and sensitivity for analysis of chemical drugs added in TCM.
Objective :To establish a liquid chromatography-electrospray ionization tandem mass spectrometry(LC-ESI-MS-MS) for the identification of glibenclamide and phenformin illegally added in Jiangtang Capsule. Methods :The detection was performed on Altima C18 column with a mobile phase of acetonitrile-formic acid solution(65-35).The above compounds were identified by LC-MS-MS. Results :Glibenclamide and phenformin were detected illegally added in one sample of Jiangtang capsule. Conclusion :This is an effective method with characteristic and sensitivity for analysis of chemical drugs added in TCM.
2007, (6): 391-391.
Abstract:
Objective :To set up an HPLC method for the content determination of aconitine in shangke liniment. Methods :Chromatography was performed on a MN-Nucleosil 7C6H5 stainless steel column（25 cm×4.0 mm）.The mobile phase was a mixture of methanol-water-chloroform-triethylamine（70-30-1-0.2）,with a flow rate of 1.5 mL/min.The detection wavelength was 235 nm. Results :The calibration curve was linear over the range of 0.050-0.225 μg,the average rate of recovery was 95.42 %,RSD=1.62 %（n=5）. Conclusion :The method proved to be simple,rapid,reliable and well reproducible in the content determination of aconitine in shangke liniment.It may be used as a method of quality control of the preparation.
Objective :To set up an HPLC method for the content determination of aconitine in shangke liniment. Methods :Chromatography was performed on a MN-Nucleosil 7C6H5 stainless steel column（25 cm×4.0 mm）.The mobile phase was a mixture of methanol-water-chloroform-triethylamine（70-30-1-0.2）,with a flow rate of 1.5 mL/min.The detection wavelength was 235 nm. Results :The calibration curve was linear over the range of 0.050-0.225 μg,the average rate of recovery was 95.42 %,RSD=1.62 %（n=5）. Conclusion :The method proved to be simple,rapid,reliable and well reproducible in the content determination of aconitine in shangke liniment.It may be used as a method of quality control of the preparation.
2007, (6): 393-395.
Abstract:
Objective :To assess the drug utilization and tendency of progress of oral hypoglycemic agents in our hospital and to provide references for rational administration clinically. Methods :DDDs,sales quantities,sales expenses and the ratio of sales expenses sequencing to that of DDDs in our hospital during the period of 2003-2005 were analyzed statistically with the method of DDDs analysis. Results :The top two antidiabetic drugs according to DDDs were melbine （dimethyl diguanide） and gliclazide three successive years.The DDDs of acarbose increased dramatically.Which blood glucose regulatsry drugs ranked lower,the ratio of sales expenses sequencing to that of DDDs of glipizide and gliclazide controlled release pellets was equal or about,whereas that of rosiglitazone,acarbose （glucobay） and glimepiride was less than 1. Conclusion :The study shows that the drug utilization of oral hypoglycemic agents in our hospital is basically rational and is in accordance with the trend of advancement and drug therapeutic strategies of diabetes mellitus.
Objective :To assess the drug utilization and tendency of progress of oral hypoglycemic agents in our hospital and to provide references for rational administration clinically. Methods :DDDs,sales quantities,sales expenses and the ratio of sales expenses sequencing to that of DDDs in our hospital during the period of 2003-2005 were analyzed statistically with the method of DDDs analysis. Results :The top two antidiabetic drugs according to DDDs were melbine （dimethyl diguanide） and gliclazide three successive years.The DDDs of acarbose increased dramatically.Which blood glucose regulatsry drugs ranked lower,the ratio of sales expenses sequencing to that of DDDs of glipizide and gliclazide controlled release pellets was equal or about,whereas that of rosiglitazone,acarbose （glucobay） and glimepiride was less than 1. Conclusion :The study shows that the drug utilization of oral hypoglycemic agents in our hospital is basically rational and is in accordance with the trend of advancement and drug therapeutic strategies of diabetes mellitus.
2007, (6): 396-397.
Abstract:
Objective :To investigated the effects of Qishenfukang capsule improving the physical and intellective function in rats,in order to provide laboratory evidence for clinical usage. Methods :The rats were divided into four groups.Qishenfukang capsule(0.3 g,0.6 g,1.2 g/kg)and placebo groups,respectively.Then their body weight,swimming ability and memory were tested. Results :Qishenfukang capsule could increase those rats' weight,prolong their swimming time and improve their memory obviously. Conclusion :Qishenfukang capsule could promote rats' strength and intellectual function.
Objective :To investigated the effects of Qishenfukang capsule improving the physical and intellective function in rats,in order to provide laboratory evidence for clinical usage. Methods :The rats were divided into four groups.Qishenfukang capsule(0.3 g,0.6 g,1.2 g/kg)and placebo groups,respectively.Then their body weight,swimming ability and memory were tested. Results :Qishenfukang capsule could increase those rats' weight,prolong their swimming time and improve their memory obviously. Conclusion :Qishenfukang capsule could promote rats' strength and intellectual function.
2007, (6): 399-400.
Abstract:
Objective :To analyze clinical curative effect of Gefitinib to treat NSCLC(non-small cell lung cancer). Methods :40 cases in-patient with NSCLC in Hospital of PLA General Hospital during Juan 2005 to Dec 2006,were administrated Gefitinib 250 mg daily orally,and investigated for it's curative effect. Results :The total effective rate was 35.0%,CR(complete remission)1 case,PR(partial remission) 13 cases,the disease control rate was 82.5%(CR was 1 case,PR was 13 cases,basio-stabilization was 19 cases).There were 29 male patients and 11 females,and effective rate were 55.2% and 36.4% respectively(P<0.05).The main adverse reaction were nausea and vomiting(37%),anorexy(25%),and exanthem(18%). Conclusion : Gefitinib has a better curative effect to treat NSCLC,and the adverse effect is gently,it can improve majority patient quality of life and survival.
Objective :To analyze clinical curative effect of Gefitinib to treat NSCLC(non-small cell lung cancer). Methods :40 cases in-patient with NSCLC in Hospital of PLA General Hospital during Juan 2005 to Dec 2006,were administrated Gefitinib 250 mg daily orally,and investigated for it's curative effect. Results :The total effective rate was 35.0%,CR(complete remission)1 case,PR(partial remission) 13 cases,the disease control rate was 82.5%(CR was 1 case,PR was 13 cases,basio-stabilization was 19 cases).There were 29 male patients and 11 females,and effective rate were 55.2% and 36.4% respectively(P<0.05).The main adverse reaction were nausea and vomiting(37%),anorexy(25%),and exanthem(18%). Conclusion : Gefitinib has a better curative effect to treat NSCLC,and the adverse effect is gently,it can improve majority patient quality of life and survival.
2007, (6): 403-404.
Abstract:
Objective :To obtain the pharmacokinetics parameters of caffeine in the elderly,presenile,pastadolescenal and young male. Methods :Saliva caffeine(CAF) concentration in 16 old male(aged 67～81 years),20 presenile male(aged 51～60 years),46 pastadolescenal male(aged 35～50 years) and 95 young male(aged 18～34 years) was determined by RP-HPLC method,and according to the saliva concentration time curves,the pharmacokinetic parameters were calculated. Results : The saliva CAF1/2 in the elderly group was significantly increased to those in the other group(P<0.000 5,P<0.000 1,P<0.01),the saliva CAF clearanc was significantly decreased(P<0.000 2,P<0.002,P<0.01) and apparent volume of distribution(Vd) was not different significantly(P>0.05). Conclusion : The saliva CAF1/2 and clearanc in the elderly male were significantly increased and decreased respectively,Vd was not different significantly.
Objective :To obtain the pharmacokinetics parameters of caffeine in the elderly,presenile,pastadolescenal and young male. Methods :Saliva caffeine(CAF) concentration in 16 old male(aged 67～81 years),20 presenile male(aged 51～60 years),46 pastadolescenal male(aged 35～50 years) and 95 young male(aged 18～34 years) was determined by RP-HPLC method,and according to the saliva concentration time curves,the pharmacokinetic parameters were calculated. Results : The saliva CAF1/2 in the elderly group was significantly increased to those in the other group(P<0.000 5,P<0.000 1,P<0.01),the saliva CAF clearanc was significantly decreased(P<0.000 2,P<0.002,P<0.01) and apparent volume of distribution(Vd) was not different significantly(P>0.05). Conclusion : The saliva CAF1/2 and clearanc in the elderly male were significantly increased and decreased respectively,Vd was not different significantly.
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