2009 Vol. 27, No. 4
Display Method:
2009, 27(4): 254-257.
Abstract:
Objective :To prepare human serum albumin(HSA) injectable gel.To optimize the formulations of injectable gel by a central composite design/response surface methodology. Methods : Injectable gel loaded HSA were prepared with poly(lactic-co-glycolic acid)(PLGA) as carrier material and N-methyl-2-pyrrolidone(NMP) and benzyl benzoate(BB)as co-solvent.Independent variables were PLGA content and the content of co-solvent,and in vitro release was dependent variable.Linear or nonlinear mathematic models were used to estimate the relationship between independent and dependent variables.Response surfaces were delineated according to best-fit mathematic models,and optimum formulations were selected thereform.Prediction was carried out through comparing the observed and predicted values. Results :The trinomial fitting equations of indexes were all superior to their multi-linear regression equations,and the predictive values in the established mathematical model were in good conformity with the experimental values. Conclusion :Central composite design/response surface method shows a good predictability in optimizing the formula technology of BDNF-loaded PLGA nanoparticles.
Objective :To prepare human serum albumin(HSA) injectable gel.To optimize the formulations of injectable gel by a central composite design/response surface methodology. Methods : Injectable gel loaded HSA were prepared with poly(lactic-co-glycolic acid)(PLGA) as carrier material and N-methyl-2-pyrrolidone(NMP) and benzyl benzoate(BB)as co-solvent.Independent variables were PLGA content and the content of co-solvent,and in vitro release was dependent variable.Linear or nonlinear mathematic models were used to estimate the relationship between independent and dependent variables.Response surfaces were delineated according to best-fit mathematic models,and optimum formulations were selected thereform.Prediction was carried out through comparing the observed and predicted values. Results :The trinomial fitting equations of indexes were all superior to their multi-linear regression equations,and the predictive values in the established mathematical model were in good conformity with the experimental values. Conclusion :Central composite design/response surface method shows a good predictability in optimizing the formula technology of BDNF-loaded PLGA nanoparticles.
2009, 27(4): 258-260,320.
Abstract:
Objective :To develop a LC-MS-MS assay for the determination of ibuprofen in human serum and to investigate the pharmacokinetics and bioequivalence of two preparation in Chinese healthy volunteers. Methods : A single per rectum dose of 50 mg ibuprofen test suppositories and reference suppositories was given to 20 healthy male volunteers in a randomized double cross-over design.Ibuprofen concentration were determined by LC-MS-MS assay,and pharmacokinetic parameters were calculated with DAS2.0 practical pharmacokinetics program. Results :The calibration curve was linear over the range of 0.05～6.4 mg/L.The main pharmacokinetic parameters of test suppositories and reference suppositories were as follow: t1/2(2.77±0.65) and(3.02±0.99) h,ρmax(2.148±0.643) and(2.013±0.844) mg/L,tmax(3.2±0.7) and(3.1±0.5) h,AUC0-12(11.37±3.56) and(11.30±4.62)mg·h/L. Conclusion :The method applied was convenient,accurate and specific,and the statistical analysis showed that the test and reference preparation bioequivalent.
Objective :To develop a LC-MS-MS assay for the determination of ibuprofen in human serum and to investigate the pharmacokinetics and bioequivalence of two preparation in Chinese healthy volunteers. Methods : A single per rectum dose of 50 mg ibuprofen test suppositories and reference suppositories was given to 20 healthy male volunteers in a randomized double cross-over design.Ibuprofen concentration were determined by LC-MS-MS assay,and pharmacokinetic parameters were calculated with DAS2.0 practical pharmacokinetics program. Results :The calibration curve was linear over the range of 0.05～6.4 mg/L.The main pharmacokinetic parameters of test suppositories and reference suppositories were as follow: t1/2(2.77±0.65) and(3.02±0.99) h,ρmax(2.148±0.643) and(2.013±0.844) mg/L,tmax(3.2±0.7) and(3.1±0.5) h,AUC0-12(11.37±3.56) and(11.30±4.62)mg·h/L. Conclusion :The method applied was convenient,accurate and specific,and the statistical analysis showed that the test and reference preparation bioequivalent.
2009, 27(4): 261-263.
Abstract:
Objective :To investigate the effects of Zhixiao Tongmaining granules on diabetic nephropathy. Methods : The blood stasis of rats were detected by blood rheometer to investigate the effects of activating blood circulation to dissipate blood stasis of Zhixiao Tongmaining granules.The yin deficiency model of mice were made by intragastric administration of thyroxin(3 mg) and reserpine(0.01 mg/10 g) for investigating the effects of body weight of rats and endurance test.Mice qi-deficiency model of were made by limiting mice food-intake for one week for investigating the effects of body weight of rats and lymphocyte percentage of peripheral blood. Results :Compared with model group,Zhixiao Tongmaining granules can improve condition of blood stasis on rats,extend survival time of mice on staying power experiment,increase body weight of rats,index number of thymus,index number of spleen. Conclusion :Zhixiao Tongmaining granules can decrease whole blood specific viscosity of blood stasis rats,effectively improve condition of blood stasis.Zhixiao Tongmaining granules have the effect of improving the condition of yin deficency mice,also have part of therapeutic action on mice with qi deficiency.
Objective :To investigate the effects of Zhixiao Tongmaining granules on diabetic nephropathy. Methods : The blood stasis of rats were detected by blood rheometer to investigate the effects of activating blood circulation to dissipate blood stasis of Zhixiao Tongmaining granules.The yin deficiency model of mice were made by intragastric administration of thyroxin(3 mg) and reserpine(0.01 mg/10 g) for investigating the effects of body weight of rats and endurance test.Mice qi-deficiency model of were made by limiting mice food-intake for one week for investigating the effects of body weight of rats and lymphocyte percentage of peripheral blood. Results :Compared with model group,Zhixiao Tongmaining granules can improve condition of blood stasis on rats,extend survival time of mice on staying power experiment,increase body weight of rats,index number of thymus,index number of spleen. Conclusion :Zhixiao Tongmaining granules can decrease whole blood specific viscosity of blood stasis rats,effectively improve condition of blood stasis.Zhixiao Tongmaining granules have the effect of improving the condition of yin deficency mice,also have part of therapeutic action on mice with qi deficiency.
2009, 27(4): 264-265,269.
Abstract:
Objective :To study the effect and revelation of Joint Medical Asset Repository on enhancing the effectiveness of U.S.military medical supply system. Methods : Analyzing relevant literature and reports on the development and application of the U.S.army's Joint Medical Asset Repository. Results :Joint Medical Asset Repository constituted the U.S.military information platform on medical supply,improved the medicine supply chain,and enhanced the U.S.army's ability to provide emergency medical supply.
Objective :To study the effect and revelation of Joint Medical Asset Repository on enhancing the effectiveness of U.S.military medical supply system. Methods : Analyzing relevant literature and reports on the development and application of the U.S.army's Joint Medical Asset Repository. Results :Joint Medical Asset Repository constituted the U.S.military information platform on medical supply,improved the medicine supply chain,and enhanced the U.S.army's ability to provide emergency medical supply.
2009, 27(4): 266-269.
Abstract:
Objective :Design and synthesis of novel triazole antifungal derivatives based on the structure of fluconazole. Methods : A cyclohexyl group introduced and a series title compounds synthesized All of them were confirmed by MS,1H-NMR,et al.The antifungal activities were also evaluated against the eight common pathogenic fungi. Results :Eleven title compounds were synthesized.Some of the title compounds exhibited activity against fungi tested to some extent. Conclusion :A cyclohexyl group introduced to the side chain affected the antifungal activity.
Objective :Design and synthesis of novel triazole antifungal derivatives based on the structure of fluconazole. Methods : A cyclohexyl group introduced and a series title compounds synthesized All of them were confirmed by MS,1H-NMR,et al.The antifungal activities were also evaluated against the eight common pathogenic fungi. Results :Eleven title compounds were synthesized.Some of the title compounds exhibited activity against fungi tested to some extent. Conclusion :A cyclohexyl group introduced to the side chain affected the antifungal activity.
2009, 27(4): 270-273,278.
Abstract:
Objective :To analyze chemical constituents of Sini decoction by rapid-resolution liquid chromatography-time of flight mass spectrometry(RRLC-TOF/MS). Methods : IThe separation was performed on a SHISEIDO CAPCELL PAK C18 reverse phase column(50 mm×2.0 mm,2 μm).The mobile phase consisted of water containing 0.1% formic acid and acetonitrile was used as gradient elute.The flow rate was 0.25 mL/min.Time-of-flight mass spectrometer(TOF/MS) was applied for qualitative analysis under positive ion mode. Results :Under optimized LC/MS condition,thirty-four of the major chemical constituents of Sini decoction were identified by RRLC-TOF/MS.All of the constituents were surveyed and classified according to their medicinal materials derivation. Conclusion :A rapid and efficient method for studying the chemical constituents of Sini decoction by RRLC-TOF/MS was established.
Objective :To analyze chemical constituents of Sini decoction by rapid-resolution liquid chromatography-time of flight mass spectrometry(RRLC-TOF/MS). Methods : IThe separation was performed on a SHISEIDO CAPCELL PAK C18 reverse phase column(50 mm×2.0 mm,2 μm).The mobile phase consisted of water containing 0.1% formic acid and acetonitrile was used as gradient elute.The flow rate was 0.25 mL/min.Time-of-flight mass spectrometer(TOF/MS) was applied for qualitative analysis under positive ion mode. Results :Under optimized LC/MS condition,thirty-four of the major chemical constituents of Sini decoction were identified by RRLC-TOF/MS.All of the constituents were surveyed and classified according to their medicinal materials derivation. Conclusion :A rapid and efficient method for studying the chemical constituents of Sini decoction by RRLC-TOF/MS was established.
2009, 27(4): 274-275,304.
Abstract:
Objective : To study the effect of ZTC1+1 natural clarifying agents on the purification of Qingkailing oral liquid. Methods :The nitrogen content of Qingkailing oral liquid was taken as index.The optimum conditions were obtained by orthogonal experimentations. Results : The result showed that ZTC1+1 natural clarifying agents can effectively improve the content of Qingkailing oral liquid.The purifying effect was relative to the addition order of ZTC1+1 natural clarifying agents and the flocculation temperature. Conclusion :ZTC1+1 natural clarifying agents can be used for production of Qingkailing oral liquid.
Objective : To study the effect of ZTC1+1 natural clarifying agents on the purification of Qingkailing oral liquid. Methods :The nitrogen content of Qingkailing oral liquid was taken as index.The optimum conditions were obtained by orthogonal experimentations. Results : The result showed that ZTC1+1 natural clarifying agents can effectively improve the content of Qingkailing oral liquid.The purifying effect was relative to the addition order of ZTC1+1 natural clarifying agents and the flocculation temperature. Conclusion :ZTC1+1 natural clarifying agents can be used for production of Qingkailing oral liquid.
2009, 27(4): 276-278.
Abstract:
Objective : To study the pharmacokinetics of self-emulsifying drug delivery systems of adefovir dipivoxil in rats. Methods : Six SD rats were randomly divided into two groups for oral administration of the self-emulsifying adefovir dipivoxil and adefovir dipivoxil tablets at a single dose of 100 mg/kg.HPLC method was applied to determine the plasma concentration of these two groups.The calculations of pharmacokinetic parameters were performed with 3P87 program. Results :For the self-emulsifying adefovir dipivoxil,Cmax and AUC were 2.509 4 μg/mL and 277.291 1 μg·min/mL,respectively;while for adefovir sipivoxil tablet,Cmax and AUC were 1.725 8 μg/mL and 215.919 6 μg·min/mL,respectively. Conclusions :The oral bioavailability of the self-emulsifying adefovir dipivoxil was better than tadefovir dipivoxil tablet.
Objective : To study the pharmacokinetics of self-emulsifying drug delivery systems of adefovir dipivoxil in rats. Methods : Six SD rats were randomly divided into two groups for oral administration of the self-emulsifying adefovir dipivoxil and adefovir dipivoxil tablets at a single dose of 100 mg/kg.HPLC method was applied to determine the plasma concentration of these two groups.The calculations of pharmacokinetic parameters were performed with 3P87 program. Results :For the self-emulsifying adefovir dipivoxil,Cmax and AUC were 2.509 4 μg/mL and 277.291 1 μg·min/mL,respectively;while for adefovir sipivoxil tablet,Cmax and AUC were 1.725 8 μg/mL and 215.919 6 μg·min/mL,respectively. Conclusions :The oral bioavailability of the self-emulsifying adefovir dipivoxil was better than tadefovir dipivoxil tablet.
2009, 27(4): 279-281.
Abstract:
Objective :To investigate the physico-chemical properties of scopolamine hydrobromide micromulsion and its transdermal delivery effect in vitro. Methods : The O/W microemulsion was prepared with the system contained of Cremophor RH-40-ethanol-Labrafil-water according to the pseudo-ternary phase diagrams.The values of droplet diameter and viscosity were investigated and the permeation flux of scopolamine hydrobromide was determined in vitro using Franz difusion cel1 with nude rats skin.The content of scopolamine hydrobromide was determined by HPLC. Results :The results indicated that the values of droplet diameter and viscosity and the permeation rate were influenced by the Km value and the contents of oil and water. Conclusion : The highest percutaneous scopolamine hydrobromide absorption microemulsion system with suitable diameter and viscosity contains 30%Cremophor RH-40+ethanol、10%Labrafil M 1944 CS 、1.5% scopolamine hydrobromide and 58.5% water,Km=21.
Objective :To investigate the physico-chemical properties of scopolamine hydrobromide micromulsion and its transdermal delivery effect in vitro. Methods : The O/W microemulsion was prepared with the system contained of Cremophor RH-40-ethanol-Labrafil-water according to the pseudo-ternary phase diagrams.The values of droplet diameter and viscosity were investigated and the permeation flux of scopolamine hydrobromide was determined in vitro using Franz difusion cel1 with nude rats skin.The content of scopolamine hydrobromide was determined by HPLC. Results :The results indicated that the values of droplet diameter and viscosity and the permeation rate were influenced by the Km value and the contents of oil and water. Conclusion : The highest percutaneous scopolamine hydrobromide absorption microemulsion system with suitable diameter and viscosity contains 30%Cremophor RH-40+ethanol、10%Labrafil M 1944 CS 、1.5% scopolamine hydrobromide and 58.5% water,Km=21.
2009, 27(4): 282-283,293.
Abstract:
Objective :To establish a carbazole method for the simultaneous determination of sodium hyaluronate(SH) and chondroitin sulfate(CS). Methods : By regulating acidity or alkalinity and ionic strength with sodium acetate,CS was selectively precipitated with cetylpyridinium chloride(CPC),whereas SH was not.So SH and CS were separated. Results :The sample pretreatment conditions were as follows:Measuring 10 mL mixture of SH and CS accurately,adding 1.6 g sodium acetate and 10 mL CPC of 12.5 mmol/L,standing for 1 h after stirring thoroughly,then,the solution was filtered with 20 μm filter membrane and the filtrate was used to determine the content of SH;the precipitates on the filter membrane were resolved with 1.4 mol/L NaCl solution by ultrasonic treatment for the determination of CS.The average recoveries of SH and CS were 101.2% and 99.4% with RSD of 1.05% and 0.96%,respectively. Conclusion :This method can be used for the simultaneous determination of SH and CS without interference with each other.
Objective :To establish a carbazole method for the simultaneous determination of sodium hyaluronate(SH) and chondroitin sulfate(CS). Methods : By regulating acidity or alkalinity and ionic strength with sodium acetate,CS was selectively precipitated with cetylpyridinium chloride(CPC),whereas SH was not.So SH and CS were separated. Results :The sample pretreatment conditions were as follows:Measuring 10 mL mixture of SH and CS accurately,adding 1.6 g sodium acetate and 10 mL CPC of 12.5 mmol/L,standing for 1 h after stirring thoroughly,then,the solution was filtered with 20 μm filter membrane and the filtrate was used to determine the content of SH;the precipitates on the filter membrane were resolved with 1.4 mol/L NaCl solution by ultrasonic treatment for the determination of CS.The average recoveries of SH and CS were 101.2% and 99.4% with RSD of 1.05% and 0.96%,respectively. Conclusion :This method can be used for the simultaneous determination of SH and CS without interference with each other.
2009, 27(4): 284-285,288.
Abstract:
Objective : To establish a HPLC method for simultaneous determination of five flavone constituents in Epimedium Brevicornum. Methods :The determination was performed on Diamonsil-C18 column(4.6mm×250mm,5μm,Dikma).The mobile phase was consisted of acetonitrile-formic acid aqueous solution with a flow rate of 0.9 mL/min.The detection wavelength was set at 270 nm. Results :A method has been established for determination of epimedin A1,epimedin B,icariin,sagittatoside A,baohuoside I in one run by HPLC. Conclusion :The established method is simple,convenient,accurate and reliable,and suitable for the quality control of Epimedium Brevicornum.
Objective : To establish a HPLC method for simultaneous determination of five flavone constituents in Epimedium Brevicornum. Methods :The determination was performed on Diamonsil-C18 column(4.6mm×250mm,5μm,Dikma).The mobile phase was consisted of acetonitrile-formic acid aqueous solution with a flow rate of 0.9 mL/min.The detection wavelength was set at 270 nm. Results :A method has been established for determination of epimedin A1,epimedin B,icariin,sagittatoside A,baohuoside I in one run by HPLC. Conclusion :The established method is simple,convenient,accurate and reliable,and suitable for the quality control of Epimedium Brevicornum.
2009, 27(4): 286-288.
Abstract:
Objective :To establish a method for determination of hyperoside in Shanzha Maiqu granule. Methods :HPLC was adopted with Agilent ZORBAX SB-C18 column(4.6 mm×250 mm,5 μm),methanol-tetrahydrofuran-0.5% H3PO4(0.917.681.5) as mobile phase at flow rate of 1.0 mL/min and 360 nm as detecting wavelength.Column temperature was room temperature and sample size was 20 μL. Results :The linear range of hyperoside was 0.018 624～0.465 6 μg(r=0.999 9).The average recovery rate of hyperoside was 96.09% and RSD was 0.82%(n=5).The contents of hyperoside in ten batches of Shanzha Maiqu granule were deteminted between 49～65 μg. Conclusion :This method is simple,accurate and reproducible,suitable for quality control of the drug.
Objective :To establish a method for determination of hyperoside in Shanzha Maiqu granule. Methods :HPLC was adopted with Agilent ZORBAX SB-C18 column(4.6 mm×250 mm,5 μm),methanol-tetrahydrofuran-0.5% H3PO4(0.917.681.5) as mobile phase at flow rate of 1.0 mL/min and 360 nm as detecting wavelength.Column temperature was room temperature and sample size was 20 μL. Results :The linear range of hyperoside was 0.018 624～0.465 6 μg(r=0.999 9).The average recovery rate of hyperoside was 96.09% and RSD was 0.82%(n=5).The contents of hyperoside in ten batches of Shanzha Maiqu granule were deteminted between 49～65 μg. Conclusion :This method is simple,accurate and reproducible,suitable for quality control of the drug.
2009, 27(4): 289-290,293.
Abstract:
Objective :To determine the content of luteolin in three kinds of Chrysanthemum morifolium that are often seen in market by HPLC. Methods : The luteolin was quantified by reverse-HPLC on Diamosil C18 column(250 mm×4.6 mm,5 μm)using methanol-water(changed from 50∶50 to 80∶20 in 30 min at pace) as mobile phase with a flow rate of 1 mL/min.The detecting wavelength was 350 nm. Results :The linear range of luteolin was 0.224 ～2.24 μg(r=0.999 9).The average recovery was 99.40%,and RSD was 2.67%(n=9).The average content of luteolin in Hangju,Gongju and Haoju was 0.34,0.41,0.69 mg/g,and RSD was 0.8%,1.2%,1.3%,respectively.(n=6). Conclusion :The content of luteolin in Haoju was the highest.The established method is delicate,simple,convenient,accurate,reproducible,and suitable for the quality control of luteolin in defferent kinds of Chrysanthemum morifolium that are often seen in market.
Objective :To determine the content of luteolin in three kinds of Chrysanthemum morifolium that are often seen in market by HPLC. Methods : The luteolin was quantified by reverse-HPLC on Diamosil C18 column(250 mm×4.6 mm,5 μm)using methanol-water(changed from 50∶50 to 80∶20 in 30 min at pace) as mobile phase with a flow rate of 1 mL/min.The detecting wavelength was 350 nm. Results :The linear range of luteolin was 0.224 ～2.24 μg(r=0.999 9).The average recovery was 99.40%,and RSD was 2.67%(n=9).The average content of luteolin in Hangju,Gongju and Haoju was 0.34,0.41,0.69 mg/g,and RSD was 0.8%,1.2%,1.3%,respectively.(n=6). Conclusion :The content of luteolin in Haoju was the highest.The established method is delicate,simple,convenient,accurate,reproducible,and suitable for the quality control of luteolin in defferent kinds of Chrysanthemum morifolium that are often seen in market.
2009, 27(4): 291-293.
Abstract:
Objective : To determine quantitatively ginsenoside Re in total ginsenoside from stalk and leaf of Panax ginseng,and to provide experimental evident for total ginsenoside quality control of Panax ginseng. Methods :The method was developed with the condition as follows:Diamonsil C18(4.6 mm×25 mm,5 μm) and DIKMA EasyGuard C18(10 mm×4.6 mm) was used as chromatographic column and guard column respectively.Gradient elution was employed with the mobile phase of acetonitrile-0.5% acetic acid/water at a flow rate of 1.25 mL/min.ELSD:temperature of the drift tube 40 ℃;gas pressure: 3.4 bar;gain: 7. Results :The standard curve: C=1.191×10-7A-0.187 6;the linear range: 0.038～1.14 mg/mL,r=0.999 3;the limits of detection: 20 ng(S/N>3);recovery rate of the added sample: 96.84%～104.21%. Conclusion :With its accuracy,sensitivity,reproducibility as well as the simplicity of sample preparation,this method is feasible for quality control of total ginsenoside from stalk and leaf of Panax ginseng.
Objective : To determine quantitatively ginsenoside Re in total ginsenoside from stalk and leaf of Panax ginseng,and to provide experimental evident for total ginsenoside quality control of Panax ginseng. Methods :The method was developed with the condition as follows:Diamonsil C18(4.6 mm×25 mm,5 μm) and DIKMA EasyGuard C18(10 mm×4.6 mm) was used as chromatographic column and guard column respectively.Gradient elution was employed with the mobile phase of acetonitrile-0.5% acetic acid/water at a flow rate of 1.25 mL/min.ELSD:temperature of the drift tube 40 ℃;gas pressure: 3.4 bar;gain: 7. Results :The standard curve: C=1.191×10-7A-0.187 6;the linear range: 0.038～1.14 mg/mL,r=0.999 3;the limits of detection: 20 ng(S/N>3);recovery rate of the added sample: 96.84%～104.21%. Conclusion :With its accuracy,sensitivity,reproducibility as well as the simplicity of sample preparation,this method is feasible for quality control of total ginsenoside from stalk and leaf of Panax ginseng.
2009, 27(4): 294-296.
Abstract:
Objective :The study was aimed at the quality management which the department of drug R&D wanted to build. Methods : The method of project breakdown was used.The key-point emphasis and the target in different stage were put forward according to the《Drug Administration Law》,《Provision for Drug Registration》 and 《Good Manufacture Practice》(GMP). Results & Conclusions :The product quality was designed firstly.The quality of the termination product was determined by the level of management in R&D stage.The idea of canonical management and Client-Centered were the guarantee of high quality product.
Objective :The study was aimed at the quality management which the department of drug R&D wanted to build. Methods : The method of project breakdown was used.The key-point emphasis and the target in different stage were put forward according to the《Drug Administration Law》,《Provision for Drug Registration》 and 《Good Manufacture Practice》(GMP). Results & Conclusions :The product quality was designed firstly.The quality of the termination product was determined by the level of management in R&D stage.The idea of canonical management and Client-Centered were the guarantee of high quality product.
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