2009 Vol. 27, No. 3
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2009, 27(3): 170-173.
Abstract:
Objective :To study the effects of expression of hypoxia inducible 1 alpha(HIF-1α) on U937 cell stimulated by oxidized low density lipoprotein(ox-LDL) and the influence of lovastatin. Methods :Foam cell formation was tested by oil red O-stain analysis,and expression of HIF-1α was measured by the method of Real-time PCR and Western blotting. Results :Foam cell was not formed by U937 cell without ox-LDL stimulating;U937 cell with ox-LDL stimulating for 24 h was transformed to foam cell.After treated with ox-LDL,the expression of HIF-1αwas markedly increased on U937 cells;with the combined treatment of lovastatin ox-LDL,the expression of HIF-1αwas significantly decreased,and this inhibitory effect was dose dependant. Conclusion :Lovasatin could inhibit both the expression of HIF-1αon U937 and the foam cell formation induced by ox-LDL.
Objective :To study the effects of expression of hypoxia inducible 1 alpha(HIF-1α) on U937 cell stimulated by oxidized low density lipoprotein(ox-LDL) and the influence of lovastatin. Methods :Foam cell formation was tested by oil red O-stain analysis,and expression of HIF-1α was measured by the method of Real-time PCR and Western blotting. Results :Foam cell was not formed by U937 cell without ox-LDL stimulating;U937 cell with ox-LDL stimulating for 24 h was transformed to foam cell.After treated with ox-LDL,the expression of HIF-1αwas markedly increased on U937 cells;with the combined treatment of lovastatin ox-LDL,the expression of HIF-1αwas significantly decreased,and this inhibitory effect was dose dependant. Conclusion :Lovasatin could inhibit both the expression of HIF-1αon U937 and the foam cell formation induced by ox-LDL.
2009, 27(3): 174-176.
Abstract:
Objective :To investigate the regulatory effect of germanium(Ge) on PGE2 of the rheumatoid arthritic model. Methods :The rat model of rheumatoid arthritis(RA) induced by Freund's complete adjuvant(FCA) was interfered with different dosages of β-carboxyethylgermanium sesquioxide(Ge-132).The body weight and the paw volume of each rat model were measured at the 3rd,6th,12th,15th,18th and 21st days,and the weight growth rate and paw swelling rate were caculated.After rats was quickly beheaded at the 21st day,the contents of Prostaglandin E2(PGE2) in the tissue were measured. Results :Appetite,energy,weight gains and the paw volume of germanium with middle and high dosages and Indomethacin(IDMT) treated groups were better then those of the model group(P<0.01).Compared with the IDMT treated group,the level of tissue inflammatory mediator PGE2 in germanuium with middle and high dosages and the normal saline treated groups were significantly lower than that of the model group(P<0.01),and the germanuium with high dosage was the lowest one,while the germanuium with middle dosage and the IDMT treated groups were in the second place,and the germanuium with low dosage was the highest one among all the groups. Conclusion :All the dosages of germanuium were able to decrease PGE2 significantly by measuring the content of the inflammatory mediator;the high dosed germanuium gave better anti-inflammatory effects on the experimental RA rat model than IDMT.There was a relationship between the dose and enhancement effect of germanuium.
Objective :To investigate the regulatory effect of germanium(Ge) on PGE2 of the rheumatoid arthritic model. Methods :The rat model of rheumatoid arthritis(RA) induced by Freund's complete adjuvant(FCA) was interfered with different dosages of β-carboxyethylgermanium sesquioxide(Ge-132).The body weight and the paw volume of each rat model were measured at the 3rd,6th,12th,15th,18th and 21st days,and the weight growth rate and paw swelling rate were caculated.After rats was quickly beheaded at the 21st day,the contents of Prostaglandin E2(PGE2) in the tissue were measured. Results :Appetite,energy,weight gains and the paw volume of germanium with middle and high dosages and Indomethacin(IDMT) treated groups were better then those of the model group(P<0.01).Compared with the IDMT treated group,the level of tissue inflammatory mediator PGE2 in germanuium with middle and high dosages and the normal saline treated groups were significantly lower than that of the model group(P<0.01),and the germanuium with high dosage was the lowest one,while the germanuium with middle dosage and the IDMT treated groups were in the second place,and the germanuium with low dosage was the highest one among all the groups. Conclusion :All the dosages of germanuium were able to decrease PGE2 significantly by measuring the content of the inflammatory mediator;the high dosed germanuium gave better anti-inflammatory effects on the experimental RA rat model than IDMT.There was a relationship between the dose and enhancement effect of germanuium.
2009, 27(3): 177-178,188.
Abstract:
Objective :To explore the rule of secretion of IL-10 stimulated sulfur mustard in human fibroblasts. Methods :The ELISA was used to detect the relationship between dose and efficacy,time course and efficacy of which sulfur mustard adjusted the secretion of IL-10. Results :A portion of IL-10 could be secreted by the human fibroblasts.The secretion of IL-10 could be significantly stimulated after the function of sulfur mustard which depended on the time-course and dosage. Conclusion :The therapeutic mechanism of sulfur mustard to Psoriasis might related with the promotion of the secretion of IL-10.
Objective :To explore the rule of secretion of IL-10 stimulated sulfur mustard in human fibroblasts. Methods :The ELISA was used to detect the relationship between dose and efficacy,time course and efficacy of which sulfur mustard adjusted the secretion of IL-10. Results :A portion of IL-10 could be secreted by the human fibroblasts.The secretion of IL-10 could be significantly stimulated after the function of sulfur mustard which depended on the time-course and dosage. Conclusion :The therapeutic mechanism of sulfur mustard to Psoriasis might related with the promotion of the secretion of IL-10.
2009, 27(3): 179-182,217.
Abstract:
Objective :To optimize the formula of caffeine orally disintegrating tablet and to investigate the related indexes. Methods :Taking the contents of L-HPC,MCC(disintegrating agent)as disintegrants and the disintegrating time(td)as evaluation indexes to carry out the orthogonal experiment to optimize the formula.The dissolution curve of the optimized formula was drawn. Results :The optimized formula for caffeine orally disintegrating tablet was as follows:the contents of caffeine,MCC,L-HPC,and mannitol were 100,40,25,and 105 mg,respectively.The prepared orally disintegrating tablets disintegrated completely within 30 s and dissolved basically within 2 min. Conclusion :This preparation method of oralhy disintegranting tablet of caffeine is simple and available.Determination method has high accuracy and recovery.It is a suitable method for the preparation and content determination of caffeine orally disintegranting tablet.
Objective :To optimize the formula of caffeine orally disintegrating tablet and to investigate the related indexes. Methods :Taking the contents of L-HPC,MCC(disintegrating agent)as disintegrants and the disintegrating time(td)as evaluation indexes to carry out the orthogonal experiment to optimize the formula.The dissolution curve of the optimized formula was drawn. Results :The optimized formula for caffeine orally disintegrating tablet was as follows:the contents of caffeine,MCC,L-HPC,and mannitol were 100,40,25,and 105 mg,respectively.The prepared orally disintegrating tablets disintegrated completely within 30 s and dissolved basically within 2 min. Conclusion :This preparation method of oralhy disintegranting tablet of caffeine is simple and available.Determination method has high accuracy and recovery.It is a suitable method for the preparation and content determination of caffeine orally disintegranting tablet.
2009, 27(3): 183-185.
Abstract:
Objective :To investigate the chemical constituents from fruits of Rosa laevigata Michx fruits. Methods :Multi-chromatographic methods including Silica gel column chromatography and Sephadex LH-20 gel permeation were employed for the isolation and purification.The structures were identified on the basis of chemical evidence and spectral data. Results :Five compounds were isolated and identified as:2α,3β,19α-trihydroxyolean-12-en-28-oic acid(Ⅰ),kaempferol(Ⅱ),potengriffioside A(Ⅲ),β-sitosterol(Ⅳ),daucosterol(Ⅴ).Conclusions:Compound Ⅰ was isolated from fruits of Rosa laevigata Michx for the first time.
Objective :To investigate the chemical constituents from fruits of Rosa laevigata Michx fruits. Methods :Multi-chromatographic methods including Silica gel column chromatography and Sephadex LH-20 gel permeation were employed for the isolation and purification.The structures were identified on the basis of chemical evidence and spectral data. Results :Five compounds were isolated and identified as:2α,3β,19α-trihydroxyolean-12-en-28-oic acid(Ⅰ),kaempferol(Ⅱ),potengriffioside A(Ⅲ),β-sitosterol(Ⅳ),daucosterol(Ⅴ).Conclusions:Compound Ⅰ was isolated from fruits of Rosa laevigata Michx for the first time.
2009, 27(3): 186-188.
Abstract:
Objective :To prepare kaempferol-3-O-rutinoside phospholipid complex and study its physic chemical properties. Methods :Solubility and water oil distribution coefficient of the complex were studied,and compared with kaempferol-3-O-rutinoside. Results :There were a great improvements in the solubility of kaempferol-3-O-rutinoside phospholipid complex both in water and in n-octanol.Some differences of apparent oil/water distribution coefficients in the systems consisted of different pH water and n-octanol were found between the complex and kaempferol-3-O-rutinoside. Conclusion :The drug-phospholipid complexes may show some superior chemico-physical properties and enhance the absorption of the drugs.
Objective :To prepare kaempferol-3-O-rutinoside phospholipid complex and study its physic chemical properties. Methods :Solubility and water oil distribution coefficient of the complex were studied,and compared with kaempferol-3-O-rutinoside. Results :There were a great improvements in the solubility of kaempferol-3-O-rutinoside phospholipid complex both in water and in n-octanol.Some differences of apparent oil/water distribution coefficients in the systems consisted of different pH water and n-octanol were found between the complex and kaempferol-3-O-rutinoside. Conclusion :The drug-phospholipid complexes may show some superior chemico-physical properties and enhance the absorption of the drugs.
2009, 27(3): 189-192.
Abstract:
Objective :To investigate the efficacy and safety of irinotecan(CPT-11) plus fluorouracil(5-FU) and leucovorin(LV) in patients with advanced gastric carcinoma,in reference to those of paclitaxel(TAX) and cisplatin(DDP) combined with 5-FU and LV. Methods :63 Patients with untreated advanced gastric carcinoma were randomly enrolled into treatment group and control group.The treatment group were treated with CTP-11 200 mg on day 1,LV 200 mg and 5-FU 500 mg on day 1～5 while the control group were given TAX 180 mg on day 1,DDP 60mg on day 3,LV 200 mg and 5-FU 500 mg on day 1～5.Both regimens were repeated every 3 weeks.All the patients received at least two treatments and were evaluable for response rate,survival time,and adverse effect. Results :In 31 evaluable patients in treatment group,CR 0 case,PR 8 cases(25.8 %),SD 12 cases(38.7 %),and PD 11 cases(35.5 %).The response rate was 25.8 %(8/31).In 29 evaluable patients in control group,CR 0 case,PR 8 cases(27.6 %),SD 12 cases(41.4 %),and PD 9 cases(31.0 %).The response rate was 25.8 %(8/31).No significant difference was found in terms of response rate between two groups.The median survival and 1-year survival rates were 7.7 and 8.3 months,and 34.4 % and 41.4 % for both groups,respectively.There was no significant difference between two groups.The most common drug-related adverse effects,mainly grade Ⅰ and Ⅱ,included neutropenia,hepatic toxicity,neurotoxicity,diarrhea,nausea,and vomiting.The incidence rate of diarrhea in treatment group was significantly higher than that in control group.Adverse effects of grade Ⅲ and Ⅳ rested on neutropenia and neurotoxicity,and the incidence rate in treatment group was significantly lower than that in control group.No treatment-related death occurred. Conclusion :Intravenous drip of CPT-11/5-FU/LV seems an active approach for untreated advanced gastric carcinoma with tolerated side effects.Further extensive investigations concerning the dose and course of treatment are demand.
Objective :To investigate the efficacy and safety of irinotecan(CPT-11) plus fluorouracil(5-FU) and leucovorin(LV) in patients with advanced gastric carcinoma,in reference to those of paclitaxel(TAX) and cisplatin(DDP) combined with 5-FU and LV. Methods :63 Patients with untreated advanced gastric carcinoma were randomly enrolled into treatment group and control group.The treatment group were treated with CTP-11 200 mg on day 1,LV 200 mg and 5-FU 500 mg on day 1～5 while the control group were given TAX 180 mg on day 1,DDP 60mg on day 3,LV 200 mg and 5-FU 500 mg on day 1～5.Both regimens were repeated every 3 weeks.All the patients received at least two treatments and were evaluable for response rate,survival time,and adverse effect. Results :In 31 evaluable patients in treatment group,CR 0 case,PR 8 cases(25.8 %),SD 12 cases(38.7 %),and PD 11 cases(35.5 %).The response rate was 25.8 %(8/31).In 29 evaluable patients in control group,CR 0 case,PR 8 cases(27.6 %),SD 12 cases(41.4 %),and PD 9 cases(31.0 %).The response rate was 25.8 %(8/31).No significant difference was found in terms of response rate between two groups.The median survival and 1-year survival rates were 7.7 and 8.3 months,and 34.4 % and 41.4 % for both groups,respectively.There was no significant difference between two groups.The most common drug-related adverse effects,mainly grade Ⅰ and Ⅱ,included neutropenia,hepatic toxicity,neurotoxicity,diarrhea,nausea,and vomiting.The incidence rate of diarrhea in treatment group was significantly higher than that in control group.Adverse effects of grade Ⅲ and Ⅳ rested on neutropenia and neurotoxicity,and the incidence rate in treatment group was significantly lower than that in control group.No treatment-related death occurred. Conclusion :Intravenous drip of CPT-11/5-FU/LV seems an active approach for untreated advanced gastric carcinoma with tolerated side effects.Further extensive investigations concerning the dose and course of treatment are demand.
2009, 27(3): 193-194,200.
Abstract:
Objective :To study the pharmacokinetics of minocycline hydrochloride in 10 Chinese healthy volunteers after a single intravenous administration of 200mg minocycline. Methods :Minocycline hydrochloride concentration in plasma was measured by an improved HPLC method,and the pharmacokinetic parameters were calculated. Results :After single dose administration of 200 mg minocycline,the main pharmacokinetic parameters t1/2,Cmax,tmax,AUC0→72h,AUC0→∞were(18.1±4.07) h,(4.744±0.887) mg/L,2.0 h,(75.71 ±10.68) mg·h/L,(79.90±12.81) mg·h/L,respectively. Conclusion :The main pharmacokinetic parameters of minocycline are consistent with those reported previously.
Objective :To study the pharmacokinetics of minocycline hydrochloride in 10 Chinese healthy volunteers after a single intravenous administration of 200mg minocycline. Methods :Minocycline hydrochloride concentration in plasma was measured by an improved HPLC method,and the pharmacokinetic parameters were calculated. Results :After single dose administration of 200 mg minocycline,the main pharmacokinetic parameters t1/2,Cmax,tmax,AUC0→72h,AUC0→∞were(18.1±4.07) h,(4.744±0.887) mg/L,2.0 h,(75.71 ±10.68) mg·h/L,(79.90±12.81) mg·h/L,respectively. Conclusion :The main pharmacokinetic parameters of minocycline are consistent with those reported previously.
2009, 27(3): 195-197,204.
Abstract:
Objective :To compare the dissolution in vitro of felodipine tablets of four pharmaceutical factories so as to make a reference to clinical application of felodipine tablets. Methods :The dissolubility of felodipine tablets of four pharmaceutical factories was inspected in the following 5 mediums:water,pH 1.2 artificial gastric juice,pH 4.0 acetate buffer solution,pH 6.8 phosphate buffer solution(the above 4 mediums were used according to the project of drug quality's re-evaluation in Japan)and the mediums that used in ChP 2005.The dissolution tests were proceeded using paddle method at 50 r/min. Results :The cumulative dissolution of all felodipine tablets in 30 min was over 80% when the mediums regulated in ChP 2005 was used.However,when the mediums that regulated in the project of drug quality's re-evaluation in Japan were used,only the products of one manufacture could dissolved over 90% in 6h. Conclusion :The dissolution of the same batch of felodipine tablets in different mediums verifies obviously.There are significant difference among the quality of the felodipine tablets of different pharmaceutical factories,which should be given attention to in clinical application.
Objective :To compare the dissolution in vitro of felodipine tablets of four pharmaceutical factories so as to make a reference to clinical application of felodipine tablets. Methods :The dissolubility of felodipine tablets of four pharmaceutical factories was inspected in the following 5 mediums:water,pH 1.2 artificial gastric juice,pH 4.0 acetate buffer solution,pH 6.8 phosphate buffer solution(the above 4 mediums were used according to the project of drug quality's re-evaluation in Japan)and the mediums that used in ChP 2005.The dissolution tests were proceeded using paddle method at 50 r/min. Results :The cumulative dissolution of all felodipine tablets in 30 min was over 80% when the mediums regulated in ChP 2005 was used.However,when the mediums that regulated in the project of drug quality's re-evaluation in Japan were used,only the products of one manufacture could dissolved over 90% in 6h. Conclusion :The dissolution of the same batch of felodipine tablets in different mediums verifies obviously.There are significant difference among the quality of the felodipine tablets of different pharmaceutical factories,which should be given attention to in clinical application.
2009, 27(3): 198-200.
Abstract:
Objective :To set up a method for determination of arginine and leucine in human fibrin sealant kit. Methods :A Shim-pack CLC-ODS column was used after pre-column derivatization with 2,4-dinitrobenzene fluoride,with the mobile phase of 50% acetonitrile and 0.05mol/L acetate buffer,and the UV detection wavelength was 362 nm.The content was analyzed by external standard method. Results :These two amino acid derivatives can be well separated under the chromatographic conditions.The average recovery was 102.8%(RSD=0.83%) for Arg,and 103.8%(RSD=0.92%) for Leu. Conclusion :The method is accurate,convenient,low-cost and suitable for determination of the two amino-acids in human fibrin sealant kit.
Objective :To set up a method for determination of arginine and leucine in human fibrin sealant kit. Methods :A Shim-pack CLC-ODS column was used after pre-column derivatization with 2,4-dinitrobenzene fluoride,with the mobile phase of 50% acetonitrile and 0.05mol/L acetate buffer,and the UV detection wavelength was 362 nm.The content was analyzed by external standard method. Results :These two amino acid derivatives can be well separated under the chromatographic conditions.The average recovery was 102.8%(RSD=0.83%) for Arg,and 103.8%(RSD=0.92%) for Leu. Conclusion :The method is accurate,convenient,low-cost and suitable for determination of the two amino-acids in human fibrin sealant kit.
2009, 27(3): 201-204.
Abstract:
Objective :To establish a simultaneous determination method of steroidal saponin Ⅰ、Ⅱ、Ⅵ、Ⅶ in Paris ployphylla by RP-HPLC. Methods :The column was Agilent SB C18(4.6 mm×150 mm,5 μm).The mobile phase was acetonitrile-water with gradient elution at a flow rate of 0.8 mL/min.The UV detection was performed at 210 nm. Results :The calibration curves showed good linearity(r>0.999 8,n=5).The recoveries of the four steroidal saponins were from 98.12% to 104.3%.The limits of detection(LOD) ranged from 11.8 to 21.0 ng and limits of quantification(LOQ) ranged from 38.4 to 75.0 ng for all the reference standards,respectively.The results showed that the contents of the four steroidal saponins in Paris polyphylla very from different producing area. Conclusion :The method is accurate,convenient,and suitable for the quantitative analysis of four saponins from Paris ployphylla.
Objective :To establish a simultaneous determination method of steroidal saponin Ⅰ、Ⅱ、Ⅵ、Ⅶ in Paris ployphylla by RP-HPLC. Methods :The column was Agilent SB C18(4.6 mm×150 mm,5 μm).The mobile phase was acetonitrile-water with gradient elution at a flow rate of 0.8 mL/min.The UV detection was performed at 210 nm. Results :The calibration curves showed good linearity(r>0.999 8,n=5).The recoveries of the four steroidal saponins were from 98.12% to 104.3%.The limits of detection(LOD) ranged from 11.8 to 21.0 ng and limits of quantification(LOQ) ranged from 38.4 to 75.0 ng for all the reference standards,respectively.The results showed that the contents of the four steroidal saponins in Paris polyphylla very from different producing area. Conclusion :The method is accurate,convenient,and suitable for the quantitative analysis of four saponins from Paris ployphylla.
2009, 27(3): 205-208.
Abstract:
Objective :To study optimum technology of extracting the active components of Panax notoginseng. Methods :Extracting the components by hot water,ethanol reflux and ultrasonic extraction method,then separating with ultrafiltration and macroporous adsorption resin.The total saponins yield,and ginsenoside Rb1,Rg1 contents extracted from of Panax notoginseng were determined. Results :The optimum extraction for Panax notoginseng is ultrasound extraction three times per day and two hours for each time. Conclusion :The best extraction process could get the largest amount of active components,and the simple process is simple.
Objective :To study optimum technology of extracting the active components of Panax notoginseng. Methods :Extracting the components by hot water,ethanol reflux and ultrasonic extraction method,then separating with ultrafiltration and macroporous adsorption resin.The total saponins yield,and ginsenoside Rb1,Rg1 contents extracted from of Panax notoginseng were determined. Results :The optimum extraction for Panax notoginseng is ultrasound extraction three times per day and two hours for each time. Conclusion :The best extraction process could get the largest amount of active components,and the simple process is simple.
2009, 27(3): 209-210,213.
Abstract:
Objective :To study the chemical constituents of the seeds of Zizyphus jujuba Mill. Methods :Multi-chromatographic methods including silica gel column chromatography and Sephadex LH-20 gel permeation were employed for the isolation and purification.The structures were identified on the basis of chemical reaction and spectral analisis. Results :Seven compounds were isolated and identified as stigmast-4-en-3-one,phenylalanine,glycerol,isoswertis,hexacosanoic acid,quercetin and nolic acid. Conclusion :Compound 5,6 and 7 were isolated from the seeds of Zizyphus jujuba Mil1for the first time.
Objective :To study the chemical constituents of the seeds of Zizyphus jujuba Mill. Methods :Multi-chromatographic methods including silica gel column chromatography and Sephadex LH-20 gel permeation were employed for the isolation and purification.The structures were identified on the basis of chemical reaction and spectral analisis. Results :Seven compounds were isolated and identified as stigmast-4-en-3-one,phenylalanine,glycerol,isoswertis,hexacosanoic acid,quercetin and nolic acid. Conclusion :Compound 5,6 and 7 were isolated from the seeds of Zizyphus jujuba Mil1for the first time.
2009, 27(3): 228-230,235.
Abstract:
Objective :To investigate the characteristics of antibiotic drug use in the respiratory department of a large general hospital for the clinical therapy. Methods :A retrospective cohort study was conducted on the infection patients from Jan.2003 to Dec.2007 in the respiratory department of Chinese PLA general hospital.The change of the infectious disease distribution,the antibiotics consumption,and the relation between disease and drug consumption were analyzed. Results :(1) The lower respiratory tract infection was the major disease in the patients of the respiratory department.(2) The antibiotics of the consumption in respiratory department were Cephalosporin/β-lactamase inhibitors,Pennicllins /β-lactamase inhibitors in sequence,and the Carbapenem and polypeptide antibiotics remained at a relatively low level.(3) The defined daily doses of antibiotics were different between the lower and upper respiratory tract infection.(4)The drug utilization index of amoxicillin group antibiotics was increased year by year and no significant change was found in other kinds of antibiotics. Conclusion :Significant changes were found in the antibiotics use among the patients within respirator department of this large general hospital,and that should be paid more attention in the clinical work.
Objective :To investigate the characteristics of antibiotic drug use in the respiratory department of a large general hospital for the clinical therapy. Methods :A retrospective cohort study was conducted on the infection patients from Jan.2003 to Dec.2007 in the respiratory department of Chinese PLA general hospital.The change of the infectious disease distribution,the antibiotics consumption,and the relation between disease and drug consumption were analyzed. Results :(1) The lower respiratory tract infection was the major disease in the patients of the respiratory department.(2) The antibiotics of the consumption in respiratory department were Cephalosporin/β-lactamase inhibitors,Pennicllins /β-lactamase inhibitors in sequence,and the Carbapenem and polypeptide antibiotics remained at a relatively low level.(3) The defined daily doses of antibiotics were different between the lower and upper respiratory tract infection.(4)The drug utilization index of amoxicillin group antibiotics was increased year by year and no significant change was found in other kinds of antibiotics. Conclusion :Significant changes were found in the antibiotics use among the patients within respirator department of this large general hospital,and that should be paid more attention in the clinical work.
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