2007 Vol. 25, No. 5
Display Method:
2007, (5): 290-291.
Abstract:
Objective : To determine the dissociation constant and partition coefficient of mesylate delavirdine. Methods :The dissociation constant was determined with acid-base titration method in methanol /water solutions with different ratios,the value to infinite diluted in pure water was extrapolated and the partition coefficient was determined with bottle-shaking method by HPLC. Results : The pKa and 1gP of mesylate delavirdine in n-octyl alcohol were 4.635 and 2.907 respectively. Conclusions : mesylate delavirdine is a weak acid with lipophilic property.
Objective : To determine the dissociation constant and partition coefficient of mesylate delavirdine. Methods :The dissociation constant was determined with acid-base titration method in methanol /water solutions with different ratios,the value to infinite diluted in pure water was extrapolated and the partition coefficient was determined with bottle-shaking method by HPLC. Results : The pKa and 1gP of mesylate delavirdine in n-octyl alcohol were 4.635 and 2.907 respectively. Conclusions : mesylate delavirdine is a weak acid with lipophilic property.
2007, (5): 292-294.
Abstract:
Objective :To modify a patent method concerning determination of synthetic drugs in traditional chinese medicines based on infrared spectroscopy,in order to improve the accuracy of judgment. Methods : The influences of two different derivative methods and random sampling intervals on prediction were observed. Results :Several parameters were optimized. Results :Better results could be obtained by direct finite difference method(DFDM) or curve fitting method(with small window size),coupled with random sampling intervals extending to negative range. Conclusion : The proposed modification improved the accuracy of the previous patent method.
Objective :To modify a patent method concerning determination of synthetic drugs in traditional chinese medicines based on infrared spectroscopy,in order to improve the accuracy of judgment. Methods : The influences of two different derivative methods and random sampling intervals on prediction were observed. Results :Several parameters were optimized. Results :Better results could be obtained by direct finite difference method(DFDM) or curve fitting method(with small window size),coupled with random sampling intervals extending to negative range. Conclusion : The proposed modification improved the accuracy of the previous patent method.
2007, (5): 295-296,302.
Abstract:
Objective :To study the angiogenesis effects of Shexiang Baoxin pill on cancer. Methods :The model of liver metastasis of colorectal cancer was established on 40 BALB/C nude mice which were xenotransplanted through intraspleen injection of LoVo cells,a human colon cancer cell line.These mice were divided into four groups randomly as following: the high-dose-group with Shexiang Baoxin Pill,the medium-dose-group with Shexiang Baoxin Pill,the low-dose-group with Shexiang Baoxin Pill and the model group.The rats of each group were given intragastric administration every day.After 35 days of treatment,vascular endothelial growth factor(VEGF),basic fibroblast growth factor(bFGF) and Ⅷ-R Ag were messured by immunohistochemical staining. Results :The contents of VEGF,bFGF and Ⅷ-R Ag in herb groups were significantly lower than that of the model group(P<0.05). Conclusion : Shexiang Baoxin Pill can obviously inhibit the angiogeneses in cancer tissues.
Objective :To study the angiogenesis effects of Shexiang Baoxin pill on cancer. Methods :The model of liver metastasis of colorectal cancer was established on 40 BALB/C nude mice which were xenotransplanted through intraspleen injection of LoVo cells,a human colon cancer cell line.These mice were divided into four groups randomly as following: the high-dose-group with Shexiang Baoxin Pill,the medium-dose-group with Shexiang Baoxin Pill,the low-dose-group with Shexiang Baoxin Pill and the model group.The rats of each group were given intragastric administration every day.After 35 days of treatment,vascular endothelial growth factor(VEGF),basic fibroblast growth factor(bFGF) and Ⅷ-R Ag were messured by immunohistochemical staining. Results :The contents of VEGF,bFGF and Ⅷ-R Ag in herb groups were significantly lower than that of the model group(P<0.05). Conclusion : Shexiang Baoxin Pill can obviously inhibit the angiogeneses in cancer tissues.
2007, (5): 297-299.
Abstract:
Objective :To evaluate the clinical efficacy between urapidil and other vasodilators in acute left heart failure. Methods : 80 patients with acute left heart failure were randomly divided into 4 groups: urapidil group(n=19),phentolamine group(n=21),sodium nitroprusside group(n=16),nitroglycerin group(n=24).The change of dyspneic respiration,heart rate,blood preasure,and lung rales were recorded respectively in the process of the treatment. Results :Remission rate of dyspnea were 94.7% and 93.8% in urapidil group and sodium nitroprusside group respectively(P>0.05),nitroglycerin group was 47.7%(P<0.01).Incidence of heart rate acceleration were 66.7% and 5.3% in phentolamine group and urapidil group respectively(P<0.01).Incidence of blood pressure lowering and hypotension were 31.3% and 5.3% in sodium nitroprusside group and urapidil group respectively(P<0.05).Effective rate of reducing lung rales were 94.7% and 95.2% respectively(P>0.05),nitroglycerin group was 58.3%(P<0.05). Conclusion :The result proved that urapidil could be used as first aid for patients with acute left heart failure.
Objective :To evaluate the clinical efficacy between urapidil and other vasodilators in acute left heart failure. Methods : 80 patients with acute left heart failure were randomly divided into 4 groups: urapidil group(n=19),phentolamine group(n=21),sodium nitroprusside group(n=16),nitroglycerin group(n=24).The change of dyspneic respiration,heart rate,blood preasure,and lung rales were recorded respectively in the process of the treatment. Results :Remission rate of dyspnea were 94.7% and 93.8% in urapidil group and sodium nitroprusside group respectively(P>0.05),nitroglycerin group was 47.7%(P<0.01).Incidence of heart rate acceleration were 66.7% and 5.3% in phentolamine group and urapidil group respectively(P<0.01).Incidence of blood pressure lowering and hypotension were 31.3% and 5.3% in sodium nitroprusside group and urapidil group respectively(P<0.05).Effective rate of reducing lung rales were 94.7% and 95.2% respectively(P>0.05),nitroglycerin group was 58.3%(P<0.05). Conclusion :The result proved that urapidil could be used as first aid for patients with acute left heart failure.
2007, (5): 300-302.
Abstract:
Objective :To establish by capillary gas chromatography for the analysis of organic residual in olmesartan medoxomil by direct injection of solution,and compare with the results. Methods :Wide-bore capillary column(30m ×0.53mm) packed with 6% cyanopropylphenyl-94% dimethylpoly-siloxane(deep film 3μm)was used on a programmed column temperature.DMSO was used as solvent,and samples were injected for the analysis. Results :The calibration curves of methanol,ethanol,ether,acetone,acetonitrile,dichloromethane,n-hexane,isopropylether,ethyl acetate,chloroform,dioxane,toluene,dimethylformam-ide and xylene showed good linearity.The average recoveries were good.The detection limits were 0.4 ng,0.4 ng,1.6 ng,1.2 ng,0.7 ng,2.0 ng,0.5 ng,1.5 ng,0.8 ng,3.3 ng,0.6 ng,0.3 ng,2.8 ng和0.8 ng,respectively. Conclusion :The results showed that the method can be used to detect the organic residual in olmesartan medoxomil,the method have high sensitivity and good repetition.
Objective :To establish by capillary gas chromatography for the analysis of organic residual in olmesartan medoxomil by direct injection of solution,and compare with the results. Methods :Wide-bore capillary column(30m ×0.53mm) packed with 6% cyanopropylphenyl-94% dimethylpoly-siloxane(deep film 3μm)was used on a programmed column temperature.DMSO was used as solvent,and samples were injected for the analysis. Results :The calibration curves of methanol,ethanol,ether,acetone,acetonitrile,dichloromethane,n-hexane,isopropylether,ethyl acetate,chloroform,dioxane,toluene,dimethylformam-ide and xylene showed good linearity.The average recoveries were good.The detection limits were 0.4 ng,0.4 ng,1.6 ng,1.2 ng,0.7 ng,2.0 ng,0.5 ng,1.5 ng,0.8 ng,3.3 ng,0.6 ng,0.3 ng,2.8 ng和0.8 ng,respectively. Conclusion :The results showed that the method can be used to detect the organic residual in olmesartan medoxomil,the method have high sensitivity and good repetition.
2007, (5): 303-306.
Abstract:
Objective :To synthesize metallic salts of norfloxacin(NFLO) and evaluate their bacteriaostatic activities in vitro. Methods : The compounds were syntherized from the starting material norfloxacin and metallic salts.The bateriostatic activities of these new compounds were tested. Results : Five new compounds(NFLO-Ag,,NFLO-Zn,NFLO-Ce,NFLO-Co,NFLO-Bi) were produced and their primary quality criteria were established. Conclusions : The bateriostatic tests showed that these new compounds exhibit more potent antimicrobial activities than sliver sulfadiazine against Escherichia coli,Staphylococcus aureus and Pseudomonas aeruginosa.
Objective :To synthesize metallic salts of norfloxacin(NFLO) and evaluate their bacteriaostatic activities in vitro. Methods : The compounds were syntherized from the starting material norfloxacin and metallic salts.The bateriostatic activities of these new compounds were tested. Results : Five new compounds(NFLO-Ag,,NFLO-Zn,NFLO-Ce,NFLO-Co,NFLO-Bi) were produced and their primary quality criteria were established. Conclusions : The bateriostatic tests showed that these new compounds exhibit more potent antimicrobial activities than sliver sulfadiazine against Escherichia coli,Staphylococcus aureus and Pseudomonas aeruginosa.
2007, (5): 307-309.
Abstract:
Objective : To establish an HPLC method for determination of salvianolic acid B in Danshen leaves and stems,and compare the content of salvianolic acid B in Danshen leaves and stems of different species,different locations and growth stages,so as to supply some evidence for the further exploitation and utilization of Danshen leaves and stems reasonably. Methods : The determination was performed on Phenomenex C18 column(250 mm×4.6 mm 5μm);The mobile phase consisted of acetonitrile-meon-0.25%orthophosphoric acid solution(10∶30∶60) with a flow-rate of 1.0 mL/min.The detecting wavelength was at 286 nm. Results : The calibration curves were good linear regression(r=0.999 9) with measurement ranges(0.488～8.54μg).The recoveries were 98.17%. Conclusions : The method was successfully applied to quantify salvianolic acid B in Danshsen leaves and stems,and salvianolic acid B cotents in Danshsen leaves and stems of different species were not at the same level;Salviae miltiorrhiza Bge contained the higher salvianolic acid B than Salvia miltiorrhiza bge.f.alba.The salvianolic acid B contents in Danshsen leaves and stems from Sishui was the highest in Augest among different locations and growth stages for the same species.
Objective : To establish an HPLC method for determination of salvianolic acid B in Danshen leaves and stems,and compare the content of salvianolic acid B in Danshen leaves and stems of different species,different locations and growth stages,so as to supply some evidence for the further exploitation and utilization of Danshen leaves and stems reasonably. Methods : The determination was performed on Phenomenex C18 column(250 mm×4.6 mm 5μm);The mobile phase consisted of acetonitrile-meon-0.25%orthophosphoric acid solution(10∶30∶60) with a flow-rate of 1.0 mL/min.The detecting wavelength was at 286 nm. Results : The calibration curves were good linear regression(r=0.999 9) with measurement ranges(0.488～8.54μg).The recoveries were 98.17%. Conclusions : The method was successfully applied to quantify salvianolic acid B in Danshsen leaves and stems,and salvianolic acid B cotents in Danshsen leaves and stems of different species were not at the same level;Salviae miltiorrhiza Bge contained the higher salvianolic acid B than Salvia miltiorrhiza bge.f.alba.The salvianolic acid B contents in Danshsen leaves and stems from Sishui was the highest in Augest among different locations and growth stages for the same species.
2007, (5): 310-312.
Abstract:
Objective :To study the synthesis of finasteride. Methods : Finasteride was synthesized from pregnenolone acetic ester,and by hypobromous acid oxidation,methanol esterification to give 3-oxo-4-androstene-17β-carboxylic methyl ester.Then by Oppenauer oxidation,cleavage of △4-double bond by oxidation,ring closure by ammonia,hydrogenation of △5-double bond,dehydrogenation of 1,2-position in A-ring and Bodroux reaction to get product. Results :Overall yield was 36.5%. Conclusion :The material of this synthesis is inexpensive,the process is simple,the cost is low and the yield is good.
Objective :To study the synthesis of finasteride. Methods : Finasteride was synthesized from pregnenolone acetic ester,and by hypobromous acid oxidation,methanol esterification to give 3-oxo-4-androstene-17β-carboxylic methyl ester.Then by Oppenauer oxidation,cleavage of △4-double bond by oxidation,ring closure by ammonia,hydrogenation of △5-double bond,dehydrogenation of 1,2-position in A-ring and Bodroux reaction to get product. Results :Overall yield was 36.5%. Conclusion :The material of this synthesis is inexpensive,the process is simple,the cost is low and the yield is good.
2007, (5): 312-314,345.
Abstract:
Objective : To improve the synthetic process of 7-azaindol-3-carboxylic acid. Methods : The succinonitrile was taken as the original raw material.The isopropyl ether,n-heptane,and chlorobenzene, which were used in original technics,were subsituted by ethyl acetate,petroleun ether,and xylene respectively.The disposition technics was optimized. Results : The technics was successfully improved due to its low cost,small toxicity,convenient disposition and high yield. Conclusions : The higher overall yields was 43.4%.This improved method is more suitable for industrial production for its low cost.
Objective : To improve the synthetic process of 7-azaindol-3-carboxylic acid. Methods : The succinonitrile was taken as the original raw material.The isopropyl ether,n-heptane,and chlorobenzene, which were used in original technics,were subsituted by ethyl acetate,petroleun ether,and xylene respectively.The disposition technics was optimized. Results : The technics was successfully improved due to its low cost,small toxicity,convenient disposition and high yield. Conclusions : The higher overall yields was 43.4%.This improved method is more suitable for industrial production for its low cost.
2007, (5): 325-327.
Abstract:
Objective :To discuss the feasibility of determining the contents of trace element in Fructus cnidii by spectrophotometry,and to expound the potential relationship between the sorts and contents of the elements in crude drugs and the pharmacological function of Fructus cnidii. Methods :Different metal ions can be colored with specific color reagent,engendering visible light absorption,so spectrophotometry was adopted to determine the contents both of the Fructus cnidii and the standard substance of human hair. Results :The results showed that the Fructus cnidii was rich in trace element,the content of Fe was especially higher.Fe in Fructus cnidii is highest to 136.69mg/kg,Zn is highest to 51.72mg/kg,Cu is highest to 33.49mg/kg. Conclusion :Spectrophotometry was simple,high-speed and accurate,which could be popularized widely.The relationship between the sorts and contents of the elements in Fructus cnidii and the pharmacological function of them is so consanguineous that the further research is needed to ascertain.
Objective :To discuss the feasibility of determining the contents of trace element in Fructus cnidii by spectrophotometry,and to expound the potential relationship between the sorts and contents of the elements in crude drugs and the pharmacological function of Fructus cnidii. Methods :Different metal ions can be colored with specific color reagent,engendering visible light absorption,so spectrophotometry was adopted to determine the contents both of the Fructus cnidii and the standard substance of human hair. Results :The results showed that the Fructus cnidii was rich in trace element,the content of Fe was especially higher.Fe in Fructus cnidii is highest to 136.69mg/kg,Zn is highest to 51.72mg/kg,Cu is highest to 33.49mg/kg. Conclusion :Spectrophotometry was simple,high-speed and accurate,which could be popularized widely.The relationship between the sorts and contents of the elements in Fructus cnidii and the pharmacological function of them is so consanguineous that the further research is needed to ascertain.
2007, (5): 328-330.
Abstract:
Objective :To establish a method for the determination of the content of procaine hydrochloride in cradiac standstill solution. Method:Ultraviolet spectrophotometric method was used to directly determine the content of procaine hydrochloride.The wavelength of detection was 290nm. Results :The liner range was 0.5～8μg/mL(r=0.999 9).The relative recovery of the method was 98.59% with RSD of 0.033%. Conclusions : This method is simple,rapid,accurate and can be used to determine the content of procaine hydrochloride in the preparation.
Objective :To establish a method for the determination of the content of procaine hydrochloride in cradiac standstill solution. Method:Ultraviolet spectrophotometric method was used to directly determine the content of procaine hydrochloride.The wavelength of detection was 290nm. Results :The liner range was 0.5～8μg/mL(r=0.999 9).The relative recovery of the method was 98.59% with RSD of 0.033%. Conclusions : This method is simple,rapid,accurate and can be used to determine the content of procaine hydrochloride in the preparation.
2007, (5): 330-331,333.
Abstract:
Objective :To establish a method of HPLC for determination of paecniflorin in Rupixiao tablets. Methods :A Diamonsil C18 column was used.The mobile phase was acetonitrile-water(20∶80).The flow rate was 1.0 mL/min.The detection wavelength was set as 230 nm. Results :The linear range of paecniflorin was 4.0～16.0 μg/mL,and the average recovery rate was 99.75%,RSD was 1.07%. Conclusion :The method is simple,reliable,and accurate and can be applied to the quality control of preparation.
Objective :To establish a method of HPLC for determination of paecniflorin in Rupixiao tablets. Methods :A Diamonsil C18 column was used.The mobile phase was acetonitrile-water(20∶80).The flow rate was 1.0 mL/min.The detection wavelength was set as 230 nm. Results :The linear range of paecniflorin was 4.0～16.0 μg/mL,and the average recovery rate was 99.75%,RSD was 1.07%. Conclusion :The method is simple,reliable,and accurate and can be applied to the quality control of preparation.
2007, (5): 332-333.
Abstract:
Objective :To establish a method for determining the content of hydroquinone in compound hydroquinone cream. Methods :The dual wavelength UV-spectrophotometric method was used for hydroquinone analysis. Results :The linear range of hydroquinone was 4.06 μg/mL-24.36 μg/mL(r=0.999 8,n=6),the average recovery was 95.87 %,RSD was 0.51%. Conclusion :This method is simple,rapid and accurate.
Objective :To establish a method for determining the content of hydroquinone in compound hydroquinone cream. Methods :The dual wavelength UV-spectrophotometric method was used for hydroquinone analysis. Results :The linear range of hydroquinone was 4.06 μg/mL-24.36 μg/mL(r=0.999 8,n=6),the average recovery was 95.87 %,RSD was 0.51%. Conclusion :This method is simple,rapid and accurate.
2007, (5): 334-336.
Abstract:
Objective :To establish the determination method of the content of psoralen and isopsoralen in compound Buguzhi granule. Methods :A HPLC method was adopted.This analysis was carried on a column of Waters RP-C18 with a mobile phase of water-methanol at the ratio of 5050.The detection wavelength was 246nm. Results :Within the range of 1.88～30.10 μg/mL,psoralen assumed fine linear relation between sample size and response,the average recovery was 98.56%,and RSD was 1.83%;within the range of 1.52～24.30 μg/mL,isopsoralen assumed fine linear relation between sample size and response,the average recovery was 97.82%,and RSD was 2.01%. Conclusion :This Method is simple,reliable and accurate and can be used in the quality control of Compound Buguzhi granule.
Objective :To establish the determination method of the content of psoralen and isopsoralen in compound Buguzhi granule. Methods :A HPLC method was adopted.This analysis was carried on a column of Waters RP-C18 with a mobile phase of water-methanol at the ratio of 5050.The detection wavelength was 246nm. Results :Within the range of 1.88～30.10 μg/mL,psoralen assumed fine linear relation between sample size and response,the average recovery was 98.56%,and RSD was 1.83%;within the range of 1.52～24.30 μg/mL,isopsoralen assumed fine linear relation between sample size and response,the average recovery was 97.82%,and RSD was 2.01%. Conclusion :This Method is simple,reliable and accurate and can be used in the quality control of Compound Buguzhi granule.
2007, (5): 340-342,345.
Abstract:
Objective : To discuss the current status and the developing direction of Chinese traditional drug pharmacovigilance. Methods : Comparing with the advanced work of the pharmacovigilance in the world.The instruction books,the expression of Chinese traditional medicine pharmacovigilance and some problems of the injections for Chinese traditional drug were analyzed.. Results : The obvious insufficiency in Chinese traditional drug pharmacovigilance existed. Conclusion : The pre-marking evaluation of Chinese traditional drug should be paid attention.Pharmaceutical enterprise should be the main force in the pharmacovigilance work.The Chinese traditional drug pharmacovigilance should be the medical workers'duty.
Objective : To discuss the current status and the developing direction of Chinese traditional drug pharmacovigilance. Methods : Comparing with the advanced work of the pharmacovigilance in the world.The instruction books,the expression of Chinese traditional medicine pharmacovigilance and some problems of the injections for Chinese traditional drug were analyzed.. Results : The obvious insufficiency in Chinese traditional drug pharmacovigilance existed. Conclusion : The pre-marking evaluation of Chinese traditional drug should be paid attention.Pharmaceutical enterprise should be the main force in the pharmacovigilance work.The Chinese traditional drug pharmacovigilance should be the medical workers'duty.
2007, (5): 346-347,352.
Abstract:
Objective :To provide references for the rational use of dl-lysine acetylsalicylate in clinical practice. Methods :Adverse reactions resulted from dl-lysine acetylsalicylate reported in recent years in domestic literatures were statistically classified and analyzed. Results :The general rules and characteristics of occurrence of adverse reactions resulting from dl-lysine acetylsalicylate were summarized. Conclusion :While using dl-lysine acetylsalicylate in clinical practice, high attention must be paid to consequences of its adverse reactions.
Objective :To provide references for the rational use of dl-lysine acetylsalicylate in clinical practice. Methods :Adverse reactions resulted from dl-lysine acetylsalicylate reported in recent years in domestic literatures were statistically classified and analyzed. Results :The general rules and characteristics of occurrence of adverse reactions resulting from dl-lysine acetylsalicylate were summarized. Conclusion :While using dl-lysine acetylsalicylate in clinical practice, high attention must be paid to consequences of its adverse reactions.
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