Aim To establish a sensitive HPLC method for determination of piperazine ferulate and to study its pharmacokinetics in healthy volunteers. Methods Piperazine ferulate was separated on a Shimadzu C_ 18 column with acet...Aim To establish a sensitive HPLC method for determination of piperazine ferulate and to study its pharmacokinetics in healthy volunteers. Methods Piperazine ferulate was separated on a Shimadzu C_ 18 column with acetic acid (0.1%)-methanol (60 ∶ 40, V/V) as mobile phase after liquid-liquid extraction, and detection was performed at 310 nm. Piperazine ferulate pharmacokinetic parameters after a single oral dose of 200 mg of piperazine ferulate dispersible tablets in 20 healthy male volunteers were calculate...展开更多
The objective of this study was to prepare and characterize paclitaxel-polyvinylpyrrolidone （PTX-PVP） solid dispersions with the intention of improving its solubility and dissolution properties. The PTX-PVP solid di...The objective of this study was to prepare and characterize paclitaxel-polyvinylpyrrolidone （PTX-PVP） solid dispersions with the intention of improving its solubility and dissolution properties. The PTX-PVP solid dispersion systems were prepared by solvent method. The release rate ofpaclitaxel was determined from dissolution studies and the physicochemical properties of solid dispersion were investigated by differential scanning calorimetry （DSC）, powder X-ray diffraction （PXRD） and scanning electron microscopy （SEM）. The cytotoxicities ofpaclitaxel in solid dispersion to the SKOV-3 cells were assayed by a SRB staining method. The results showed that the solubility and dissolution rate of paclitaxel were significantly improved in solid dispersion system compared with that of the pure drug and physical mixture. The results of DSC and PXRD showed that the paclitaxel in solid dispersion was amorphous form. No paclitaxel crystals in the solid dispersions was found during SEM analysis. Cytotoxicity study suggested that the inhibitory rates of PTX-PVP solid dispersion to SKOV-3 cells were higher than that of pure paclitaxel. The solubility and dissolution of paclitaxel were improved by solid dispersion technique. In vitro cytotoxicity of paclitaxel in solid dispersion was higher than that of pure drug.展开更多
To prepare a solid dispersion of cisapride with hydroxypropylmethyl cellulose(HPMC E5 LV) as carrier for the purpose of accelerating the in vitro drug release by means ofimproving the solubility of the model drug. Met...To prepare a solid dispersion of cisapride with hydroxypropylmethyl cellulose(HPMC E5 LV) as carrier for the purpose of accelerating the in vitro drug release by means ofimproving the solubility of the model drug. Methods Alcohol and simulated gastric fluid (SGF) wereused to dissolve cisapride and HPMC in order to make the model drug dispersed homogeneously in thecarrier. The HPMC-cisapride solid dispersion was then obtained by conventional solvent evaporationmethod. Powder X-ray diffraction (XRD) was used to measure the diffraction peaks of pure carrier,pure cisapride, physical mixture of HPMC with cisapride (4:1), and HPMC-cisapride solid dispersion(4:1) to confirm the crystal existence. The solubility of pure drug and HPMC-cisapride soliddispersion was measured with water, SGF and simulated intestinal fluid (SIF) . The in vitro drugreleases of the sustained release tablet prepared with pure cisapride or HPMC-cisapride soliddispersion were investigated with water and SGF as media, respectively. Results No diffraction peakswere found by X-ray diffraction in the HPMC-cisapride solid dispersion (4:1), indicating that thedrug existed in an amorphous form at that drug-carrier ratio. Compared with the pure drug, thesolubilities of HPMC-cisapride solid dispersion are increased by 239.4% in SGF, 132.6% in water, and117.9% in SIF. According to the in vitro drug release, the sustained release tablet prepared withHPMC-cisapride solid dispersion had a faster drug release than did that prepared with pure drug. Thein vitro drug release profiles were found to comply with Higuchi's rule. Conclusion The in vitrodrug release of the sustained release tablet made by HPMC-cisapride solid dispersion is improvedowing to the increased drug solubility.展开更多
The effect of a modified ester collector named as BL on the flotation of chalcopyrite at low temperatures was investigated by micro-flotation tests,contact angle measurements,adsorption experiments,laser particle size...The effect of a modified ester collector named as BL on the flotation of chalcopyrite at low temperatures was investigated by micro-flotation tests,contact angle measurements,adsorption experiments,laser particle size analysis,cryogenic transmission electron microscopy(Cryo-TEM)and Fourier transform infrared(FTIR)analyses.Micro-flotation tests proved that the collecting ability of BL for chalcopyrite was significantly better than that of N,N-diethyl dithiocarbamate propiononitrile ester(ester-105)at low temperatures.Combined with laser particle size,Cryo-TEM and FTIR analyses,it was found that the particle size of BL in water was smaller than that of ester-105,and the distributed density of BL was higher than that of ester-105 at low temperatures,indicating that BL dispersed well at low temperatures.Therefore,BL was more easily adsorbed on the chalcopyrite surface and improved the surface hydrophobic degree of chalcopyrite,which were also confirmed by the contact angle measurements and adsorption experiments.展开更多
Objective To predict the main active ingredients,potential targets and molecular mechanisms of Yuan Zhi powder in treatment of dementia by using network pharmacology.Methods A database of chemical constituents of Yuan...Objective To predict the main active ingredients,potential targets and molecular mechanisms of Yuan Zhi powder in treatment of dementia by using network pharmacology.Methods A database of chemical constituents of Yuan Zhi powder was constructed by using databases and literatures.Potential targets were predicted by reverse molecular docking,and then a component-target network was constructed.The target network of Alzheimer's disease(AD)was mapped and analyzed to obtain the“active ingredient-AD target”network.The key targets were screened through network analysis.Finally,the rationality of the prediction was analyzed by comparing with the target reported in the literatures.Results There were180chemical constituents acting on the AD target,and the targets included three key targets(cyclooxygenase-2,muscarinic acetylcholine receptor M1,and muscarinic acetylcholine receptor M2)and an important target(acetylcholine esterase).Alzheimer's disease may be treated by regulating the activity of acetylcholine receptors and the binding toβ-amyloid protein,and its biological process may be concentrated in the acetylcholine receptor signal pathway,negative regulation of synaptic transmission and so on.Conclusion The fact that Yuan Zhi powder can treat AD is consistent with the characteristics of multi-components-multitargets-multiple pathways of traditional Chinese medicine.The important targets obtained from network analysis have a large proportion in literature research,so network analysis have some rationality.展开更多
During the process of unsealing an old ammunition box in order to destroy it, a 42-year-old ammunition technician was fatally injured due to an anti-personnel ARGES EM01-type rifle grenade detonation. The explosion to...During the process of unsealing an old ammunition box in order to destroy it, a 42-year-old ammunition technician was fatally injured due to an anti-personnel ARGES EM01-type rifle grenade detonation. The explosion took place in the victim＇s hands, in point-blank range. This report aimed to show the anatomical position, the severity and the dispersion extent of the multiple injuries in the human body due to the detonation, and draw firm conclusions regarding the position of the human body and the circumstances prevailing at the moment of the explosion.展开更多
文摘Aim To establish a sensitive HPLC method for determination of piperazine ferulate and to study its pharmacokinetics in healthy volunteers. Methods Piperazine ferulate was separated on a Shimadzu C_ 18 column with acetic acid (0.1%)-methanol (60 ∶ 40, V/V) as mobile phase after liquid-liquid extraction, and detection was performed at 310 nm. Piperazine ferulate pharmacokinetic parameters after a single oral dose of 200 mg of piperazine ferulate dispersible tablets in 20 healthy male volunteers were calculate...
文摘The objective of this study was to prepare and characterize paclitaxel-polyvinylpyrrolidone （PTX-PVP） solid dispersions with the intention of improving its solubility and dissolution properties. The PTX-PVP solid dispersion systems were prepared by solvent method. The release rate ofpaclitaxel was determined from dissolution studies and the physicochemical properties of solid dispersion were investigated by differential scanning calorimetry （DSC）, powder X-ray diffraction （PXRD） and scanning electron microscopy （SEM）. The cytotoxicities ofpaclitaxel in solid dispersion to the SKOV-3 cells were assayed by a SRB staining method. The results showed that the solubility and dissolution rate of paclitaxel were significantly improved in solid dispersion system compared with that of the pure drug and physical mixture. The results of DSC and PXRD showed that the paclitaxel in solid dispersion was amorphous form. No paclitaxel crystals in the solid dispersions was found during SEM analysis. Cytotoxicity study suggested that the inhibitory rates of PTX-PVP solid dispersion to SKOV-3 cells were higher than that of pure paclitaxel. The solubility and dissolution of paclitaxel were improved by solid dispersion technique. In vitro cytotoxicity of paclitaxel in solid dispersion was higher than that of pure drug.
文摘To prepare a solid dispersion of cisapride with hydroxypropylmethyl cellulose(HPMC E5 LV) as carrier for the purpose of accelerating the in vitro drug release by means ofimproving the solubility of the model drug. Methods Alcohol and simulated gastric fluid (SGF) wereused to dissolve cisapride and HPMC in order to make the model drug dispersed homogeneously in thecarrier. The HPMC-cisapride solid dispersion was then obtained by conventional solvent evaporationmethod. Powder X-ray diffraction (XRD) was used to measure the diffraction peaks of pure carrier,pure cisapride, physical mixture of HPMC with cisapride (4:1), and HPMC-cisapride solid dispersion(4:1) to confirm the crystal existence. The solubility of pure drug and HPMC-cisapride soliddispersion was measured with water, SGF and simulated intestinal fluid (SIF) . The in vitro drugreleases of the sustained release tablet prepared with pure cisapride or HPMC-cisapride soliddispersion were investigated with water and SGF as media, respectively. Results No diffraction peakswere found by X-ray diffraction in the HPMC-cisapride solid dispersion (4:1), indicating that thedrug existed in an amorphous form at that drug-carrier ratio. Compared with the pure drug, thesolubilities of HPMC-cisapride solid dispersion are increased by 239.4% in SGF, 132.6% in water, and117.9% in SIF. According to the in vitro drug release, the sustained release tablet prepared withHPMC-cisapride solid dispersion had a faster drug release than did that prepared with pure drug. Thein vitro drug release profiles were found to comply with Higuchi's rule. Conclusion The in vitrodrug release of the sustained release tablet made by HPMC-cisapride solid dispersion is improvedowing to the increased drug solubility.
基金financial supports from the National Natural Science Foundation of China(No.52074206)the Talent Science and Technology Fund of Xi’an University of Architecture and Technology,China(No.ZR19062)+4 种基金the Open Foundation of State Key Laboratory of Mineral Processing,China(No.BGRIMM-KJSKL-2021-19)the Natural Science Basic Research Plan in Shaanxi Province of China(No.2021JQ-507)the Special Research Project of Shaanxi Education Department,China(No.21JK0731)the Key Program for International S&T Cooperation Projects of Shaanxi Province,China(No.2021KWZ-16)the Natural Science Foundation of Qinghai Province,China(No.2021-ZJ-975Q)。
文摘The effect of a modified ester collector named as BL on the flotation of chalcopyrite at low temperatures was investigated by micro-flotation tests,contact angle measurements,adsorption experiments,laser particle size analysis,cryogenic transmission electron microscopy(Cryo-TEM)and Fourier transform infrared(FTIR)analyses.Micro-flotation tests proved that the collecting ability of BL for chalcopyrite was significantly better than that of N,N-diethyl dithiocarbamate propiononitrile ester(ester-105)at low temperatures.Combined with laser particle size,Cryo-TEM and FTIR analyses,it was found that the particle size of BL in water was smaller than that of ester-105,and the distributed density of BL was higher than that of ester-105 at low temperatures,indicating that BL dispersed well at low temperatures.Therefore,BL was more easily adsorbed on the chalcopyrite surface and improved the surface hydrophobic degree of chalcopyrite,which were also confirmed by the contact angle measurements and adsorption experiments.
基金funding support from the Major new drug creation project (2017ZX09101002-002-008)National Natural Science Foundation of China (81403171)Autonomous Program of China Academy of Chinese Medical Sciences (QZPT001 and 2014065)
文摘Objective To predict the main active ingredients,potential targets and molecular mechanisms of Yuan Zhi powder in treatment of dementia by using network pharmacology.Methods A database of chemical constituents of Yuan Zhi powder was constructed by using databases and literatures.Potential targets were predicted by reverse molecular docking,and then a component-target network was constructed.The target network of Alzheimer's disease(AD)was mapped and analyzed to obtain the“active ingredient-AD target”network.The key targets were screened through network analysis.Finally,the rationality of the prediction was analyzed by comparing with the target reported in the literatures.Results There were180chemical constituents acting on the AD target,and the targets included three key targets(cyclooxygenase-2,muscarinic acetylcholine receptor M1,and muscarinic acetylcholine receptor M2)and an important target(acetylcholine esterase).Alzheimer's disease may be treated by regulating the activity of acetylcholine receptors and the binding toβ-amyloid protein,and its biological process may be concentrated in the acetylcholine receptor signal pathway,negative regulation of synaptic transmission and so on.Conclusion The fact that Yuan Zhi powder can treat AD is consistent with the characteristics of multi-components-multitargets-multiple pathways of traditional Chinese medicine.The important targets obtained from network analysis have a large proportion in literature research,so network analysis have some rationality.
文摘During the process of unsealing an old ammunition box in order to destroy it, a 42-year-old ammunition technician was fatally injured due to an anti-personnel ARGES EM01-type rifle grenade detonation. The explosion took place in the victim＇s hands, in point-blank range. This report aimed to show the anatomical position, the severity and the dispersion extent of the multiple injuries in the human body due to the detonation, and draw firm conclusions regarding the position of the human body and the circumstances prevailing at the moment of the explosion.
