Aim A new solid SMEDDS (self-microemulsifying drug delivery system) capsule has been developed to increase the solubility and dissolution rate. Methods The solubilities of carvedilol in various bases were investigated...Aim A new solid SMEDDS (self-microemulsifying drug delivery system) capsule has been developed to increase the solubility and dissolution rate. Methods The solubilities of carvedilol in various bases were investigated. Ternary phase diagrams were used to evaluate the self-emulsification and self-microemulsfication domains. The particle size distribution and ζ-potential were determined. The mean diameter of the three formulae decreased with an increase of Lutrol F68. Results The in vitro dissolution rate of ...展开更多
An emulsion-congealing technique is used to prepare solid lipid microparticles (SLM) containing ibuprofen with glyceryl behenate, tripalmitin and beewax as excipients. The difference of the solubility parameters bet...An emulsion-congealing technique is used to prepare solid lipid microparticles (SLM) containing ibuprofen with glyceryl behenate, tripalmitin and beewax as excipients. The difference of the solubility parameters between the excipients and ibuprofen are used to analyze their compatibility. Both the solubility parameter analysis and the experimental results show that glyceryl behenate is the best among the three excipients. The solid particles disperse well in aqueous phase when the drug loading reaches 10% (relative to lipid only). Glycerides exhibit marked polymorphism and their rapid rates of crystallization accelerate the formation of metastable crystal modification. The metastable crystal modification characterizes high drug loading capacity but less stability. Increasing the content of lipophilic drug in a lipid matrix facilitates the transformation of excipients to more stable polymorphic forms.展开更多
A synergistic UV/TiO2/Fenton(PCF)process is investigated for the degradation of ibuprofen(IBP)at circumneutral pH.The IBP decay in the PCF process is much faster than that with the conventional UV,UV/H2O2,Fenton,photo...A synergistic UV/TiO2/Fenton(PCF)process is investigated for the degradation of ibuprofen(IBP)at circumneutral pH.The IBP decay in the PCF process is much faster than that with the conventional UV,UV/H2O2,Fenton,photo‐Fenton,and photocatalysis processes.The kinetics analysis showed that the IBP decay follows a two‐stage pseudo‐first order profile,that is,a fast IBP decay(k1)followed by a slow decay(k2).The effects of various parameters,including initial pH level,dosage of Fenton’s reagent and TiO2,wavelength of UV irradiation,and initial IBP concentration,are evaluated.The optimum pH level,[Fe2+]0,[Fe2+]0/[H2O2]0 molar ratio,and[TiO2]0 are determined to be approximately 4.22,0.20 mmol/L,1/40,and 1.0 g/L,respectively.The IBP decay at circumneutral pH(i.e.,6.0–8.0 for wastewater)shows the same IBP decay efficiency as that at the optimum pH of 4.22 after 30 min,which suggests that the PCF process is applicable for the treatment of wastewater in the circumneutral pH range.The lnk1 and lnk2 are observed to be linearly correlated to 1/pH0,[IBP]0,[H2O2]0,[H2O2]0/[Fe2+]0 and ln[TiO2]0.Mathematical models are therefore derived to predict the IBP decay.展开更多
The separation method using chiral stationary phase (CSP) for the preparation of enantioselective compound was widely used. In this work, supercritical fluid chromatography(SFC) was proposed to resolve the chiral ...The separation method using chiral stationary phase (CSP) for the preparation of enantioselective compound was widely used. In this work, supercritical fluid chromatography(SFC) was proposed to resolve the chiral mixtures. To determine the optimum operating conditions for the chiral separation of the racemic ibuprofen, the retention factors and resolutions with the change in pressure, temperature and the content of IPA (%, by volume) in supercritical CO2 were investigated. Experiments showed that the retention factor decreased with the increase of pressure and decrease in temperature. The retention factor was also influenced by the content of IPA in mobile phase, as the content of IPA in the supercritical fluid increased, the retention factor decreased. The resolution of the enantiomers became worse with the increase of IPA in the supercritical fluid. Through optimizing the experimental conditions, a SFC procedure with 13MPa, 311.15K and 4% IPA in CO2 was obtained. The peak shape of the enantiomers was symmetric with supercritical fluid chromatography when compared to the asymmetric peak shape obtained by the conventional liquid chromatography. This work demonstrated that the developed supercritical fluid chromatography procedure was suitable for the chiral separation of ibuprofen enantiomers.展开更多
The process of resolution of racemic ketoprofen using n-octyl-d-glucamine as an optical resolution agent was investigated. The process consists of preparation of the diastereomer salt of ketoprofen with n-octyl-d-gluc...The process of resolution of racemic ketoprofen using n-octyl-d-glucamine as an optical resolution agent was investigated. The process consists of preparation of the diastereomer salt of ketoprofen with n-octyl-d-glucamine, liberation of S-(+)-ketoprofen from its diastereomer salt and recovery of the remaining ketoprofen and n-octyl-d- glucamine. The suitable conditions for preparation of the diastereomer salt were methanol and ethyl acetate (1.1 by volume) as the solvent, the ratio of solvent volume to ketoprofen mass at 8ml:1g, and the molar ratio of ketoprofen to n-octyl-d-glucamine at 1:1. The preferred approach to liberate S-(+)-ketoprofen from its diastereomer salt was alkali dissolution, acid adjustment and ethyl acetate extraction. Racemization of the recovered ketoprofen could be achieved by reacting the recovered ketoprofen with 10% NaOH at 507 kPa for 6h. The recovered n-octyl-d- glucamine could be refined by acid dissolution and alkali adjustment. S-(+)-ketoprofen can be obtained with high optical purity and yield, showing that the present process is a practical and efficient one which can be used in industrial scale for preparation of S-(+)-ketoprofen.展开更多
Objectives To evaluate the plasma atherosclerotic biomarkers in patients with type 2 diabetes mellitus (T2DM) and arteriosclerosis obliteran (ASO) when treated with Probucol plus Cilostazol in combination and indi...Objectives To evaluate the plasma atherosclerotic biomarkers in patients with type 2 diabetes mellitus (T2DM) and arteriosclerosis obliteran (ASO) when treated with Probucol plus Cilostazol in combination and individually. Methods In this open-label study, patients aged 40-75 years were randomized to receive conventional therapy alone, or with Cilostazol 100 mg bid, or with Probucol 250 mg bid, or with both in combination. Endpoints included changes in plasma biomarker and safety at 12 weeks. Results Of the 200 randomized pati- ents, 165 for per-protocol and 160 for the safety (QTc intervals) were set, respectively. Probucol significantly reduced total cholesterol (P 〈 0.001), low-density lipoprotein cholesterol (LDL-C), (P = 0.01), and high-density lipoprotein cholesterol (HDL-C) (P 〈 0.001) compared with conventional therapy. Cilostazol was effective in increasing HDL-C (P = 0.002) and reducing triglycerides levels (P 〈 0.01) compared with conventional therapy. A trend towards significance was observed for the difference between conventional therapy alone and Probucol plus Cilostazol group for the change in oxidized low-density lipoprotein (Ox-LDL, P = 0.065). No significant effects on the majority of the remaining biomarkers were found across the treatment groups. Conclusions We have confirmed that Ox-LDL could be a possible plasma atherosclerotic biomarker among the evaluated biomarkers, which reflected the synergetic effect of Cilostazol plus Probucol in patients with T2DM and ASO shown previously in preclinical studies.展开更多
We extend the exciton population equations of a two-level quantum dot system with weak excitation to the ones with strong excitations, in which, the phonon-induced intensity-dependent dephasing time and decay rate are...We extend the exciton population equations of a two-level quantum dot system with weak excitation to the ones with strong excitations, in which, the phonon-induced intensity-dependent dephasing time and decay rate are involved. The straightforward calculated populations from the modified population equations demonstrate the damping behavior of Rabi oscillation as the external field increasing. The effect of the intensity-dependent dephasing time and the intensity-dependent decay rate are also discussed.展开更多
The Darboux transformations from arbitrary solutions of reduced Maxwell-Bloch equations is constructed in this article. Hence, in principle, we can find multi-soliton solutions by algebric algorithm, and the formula w...The Darboux transformations from arbitrary solutions of reduced Maxwell-Bloch equations is constructed in this article. Hence, in principle, we can find multi-soliton solutions by algebric algorithm, and the formula will be given explicitly.展开更多
Ibuprofen is widely used as a non-steroidal anti-inflammatory drug and produced as racemic mixture. Its pharmacological activity resides only in S-(+)-enantiomer, and R-()-enantiomer is not only inactive but also has ...Ibuprofen is widely used as a non-steroidal anti-inflammatory drug and produced as racemic mixture. Its pharmacological activity resides only in S-(+)-enantiomer, and R-()-enantiomer is not only inactive but also has many side effects. Thus it is necessary to separate R-enantiomer from racemic ibuprofen. We studied optical separation of racemic Ibuprofen with chiral high performance liquid chromatography (HPLC). Out of three different chiral stationary phases, which were selected on the basis of structure and availability, two were found to be ef-fective. There was optimum eluent composition for each stationary phase for good resolution in optical separation. Resolution decreased with increase of eluent flow rate, but effect of injection volume on resolution was insignificant at high eluent flow rate.展开更多
Covering a wide range of bulk densities, density profiles for hard-sphere chain fluids (HSCFs) with chain length of 3,4,8,20,32 and 64 confined between two surfaces were obtained by Monte Carlo simulations using exten...Covering a wide range of bulk densities, density profiles for hard-sphere chain fluids (HSCFs) with chain length of 3,4,8,20,32 and 64 confined between two surfaces were obtained by Monte Carlo simulations using extended continuum configurational-bias (ECCB) method. It is shown that the enrichment of beads near surfaces is happened at high densities due to the bulk packing effect, on the contrary, the depletion is revealed at low densities owing to the configurational entropic contribution. Comparisons with those calculated by density functional theory presented by Cai et al. indicate that the agreement between simulations and predictions is good. Compressibility factors of bulk HSCFs calculated using volume fractions at surfaces were also used to test the reliability of various equations of state of HSCFs by different authors.展开更多
By numerically solving the Maxwell-Bloch equations using an iterative predictor-corrector finite-difference time-domain technique, we investigate propagating properties of a few-cycle laser pulse in a 4,4'-bis(di-n-...By numerically solving the Maxwell-Bloch equations using an iterative predictor-corrector finite-difference time-domain technique, we investigate propagating properties of a few-cycle laser pulse in a 4,4'-bis(di-n-butylamino) stilbene (BDBAS) molecular medium when a static electric field exists. Dynamical two-photon absorption (TPA) cross sections are obtained and optical limiting (OL) behavior is displayed. The results show that when the static electric field intensity increases, the dynamical TPA cross section is enhanced and the OL behavior is improved. Moreover, both even- and odd-order harmonic spectral components are generated with existence of the static electric field because it breaks the inversion symmetry of the BDBAS molecule. This work provides a method to modulate the nonlinear optical properties of the BDBAS compounds.展开更多
An entomological survey of Phlebotomine sand flies (Diptera: Psychodidae) was carried out in three sectors of Foum Jamgta region (province of Azilal, Morocco) during the year 2010. Morphological identification wa...An entomological survey of Phlebotomine sand flies (Diptera: Psychodidae) was carried out in three sectors of Foum Jamgta region (province of Azilal, Morocco) during the year 2010. Morphological identification was performed on a total of 1,152 sand flies (23% females and 77% males) collected by sticky paper traps. 80% of the total collected flies were identified as Phlebotomus (Paraphlebotomus) sergenti (Parrot) (57%) and Phlebotomus (Larroussius) longicuspis (Nitzulescu) (23%). In addition to these dominant species, four other species were found, Phlebotomus (Phlebotomus) papatasi (Scopoli), Sergentomyia (Sergentomyia) minuta (Rondani), Phlebotomus (Larroussius) perniciosus (Newstead) and Phlebotomus (Paraphlebotomus) chabaudi (Croset). Overall, the population dynamics show a yearly bimodal pattern related to rainfall and temperature, and with high density around human dwellings. The spatiotemporal distribution of sand fly species was helpful to discuss strategies that might be useful in controlling cutaneous leishmaniasis transmission in this endemic focus.展开更多
文摘Aim A new solid SMEDDS (self-microemulsifying drug delivery system) capsule has been developed to increase the solubility and dissolution rate. Methods The solubilities of carvedilol in various bases were investigated. Ternary phase diagrams were used to evaluate the self-emulsification and self-microemulsfication domains. The particle size distribution and ζ-potential were determined. The mean diameter of the three formulae decreased with an increase of Lutrol F68. Results The in vitro dissolution rate of ...
基金Supported by the National Natural Science Foundation of China (No.20536020, No.20476033), the China Distinguished Young Scientist Fund (No.20225620) and Guangdong Province Science Fund (No.04020121).
文摘An emulsion-congealing technique is used to prepare solid lipid microparticles (SLM) containing ibuprofen with glyceryl behenate, tripalmitin and beewax as excipients. The difference of the solubility parameters between the excipients and ibuprofen are used to analyze their compatibility. Both the solubility parameter analysis and the experimental results show that glyceryl behenate is the best among the three excipients. The solid particles disperse well in aqueous phase when the drug loading reaches 10% (relative to lipid only). Glycerides exhibit marked polymorphism and their rapid rates of crystallization accelerate the formation of metastable crystal modification. The metastable crystal modification characterizes high drug loading capacity but less stability. Increasing the content of lipophilic drug in a lipid matrix facilitates the transformation of excipients to more stable polymorphic forms.
文摘A synergistic UV/TiO2/Fenton(PCF)process is investigated for the degradation of ibuprofen(IBP)at circumneutral pH.The IBP decay in the PCF process is much faster than that with the conventional UV,UV/H2O2,Fenton,photo‐Fenton,and photocatalysis processes.The kinetics analysis showed that the IBP decay follows a two‐stage pseudo‐first order profile,that is,a fast IBP decay(k1)followed by a slow decay(k2).The effects of various parameters,including initial pH level,dosage of Fenton’s reagent and TiO2,wavelength of UV irradiation,and initial IBP concentration,are evaluated.The optimum pH level,[Fe2+]0,[Fe2+]0/[H2O2]0 molar ratio,and[TiO2]0 are determined to be approximately 4.22,0.20 mmol/L,1/40,and 1.0 g/L,respectively.The IBP decay at circumneutral pH(i.e.,6.0–8.0 for wastewater)shows the same IBP decay efficiency as that at the optimum pH of 4.22 after 30 min,which suggests that the PCF process is applicable for the treatment of wastewater in the circumneutral pH range.The lnk1 and lnk2 are observed to be linearly correlated to 1/pH0,[IBP]0,[H2O2]0,[H2O2]0/[Fe2+]0 and ln[TiO2]0.Mathematical models are therefore derived to predict the IBP decay.
文摘The separation method using chiral stationary phase (CSP) for the preparation of enantioselective compound was widely used. In this work, supercritical fluid chromatography(SFC) was proposed to resolve the chiral mixtures. To determine the optimum operating conditions for the chiral separation of the racemic ibuprofen, the retention factors and resolutions with the change in pressure, temperature and the content of IPA (%, by volume) in supercritical CO2 were investigated. Experiments showed that the retention factor decreased with the increase of pressure and decrease in temperature. The retention factor was also influenced by the content of IPA in mobile phase, as the content of IPA in the supercritical fluid increased, the retention factor decreased. The resolution of the enantiomers became worse with the increase of IPA in the supercritical fluid. Through optimizing the experimental conditions, a SFC procedure with 13MPa, 311.15K and 4% IPA in CO2 was obtained. The peak shape of the enantiomers was symmetric with supercritical fluid chromatography when compared to the asymmetric peak shape obtained by the conventional liquid chromatography. This work demonstrated that the developed supercritical fluid chromatography procedure was suitable for the chiral separation of ibuprofen enantiomers.
文摘The process of resolution of racemic ketoprofen using n-octyl-d-glucamine as an optical resolution agent was investigated. The process consists of preparation of the diastereomer salt of ketoprofen with n-octyl-d-glucamine, liberation of S-(+)-ketoprofen from its diastereomer salt and recovery of the remaining ketoprofen and n-octyl-d- glucamine. The suitable conditions for preparation of the diastereomer salt were methanol and ethyl acetate (1.1 by volume) as the solvent, the ratio of solvent volume to ketoprofen mass at 8ml:1g, and the molar ratio of ketoprofen to n-octyl-d-glucamine at 1:1. The preferred approach to liberate S-(+)-ketoprofen from its diastereomer salt was alkali dissolution, acid adjustment and ethyl acetate extraction. Racemization of the recovered ketoprofen could be achieved by reacting the recovered ketoprofen with 10% NaOH at 507 kPa for 6h. The recovered n-octyl-d- glucamine could be refined by acid dissolution and alkali adjustment. S-(+)-ketoprofen can be obtained with high optical purity and yield, showing that the present process is a practical and efficient one which can be used in industrial scale for preparation of S-(+)-ketoprofen.
文摘Objectives To evaluate the plasma atherosclerotic biomarkers in patients with type 2 diabetes mellitus (T2DM) and arteriosclerosis obliteran (ASO) when treated with Probucol plus Cilostazol in combination and individually. Methods In this open-label study, patients aged 40-75 years were randomized to receive conventional therapy alone, or with Cilostazol 100 mg bid, or with Probucol 250 mg bid, or with both in combination. Endpoints included changes in plasma biomarker and safety at 12 weeks. Results Of the 200 randomized pati- ents, 165 for per-protocol and 160 for the safety (QTc intervals) were set, respectively. Probucol significantly reduced total cholesterol (P 〈 0.001), low-density lipoprotein cholesterol (LDL-C), (P = 0.01), and high-density lipoprotein cholesterol (HDL-C) (P 〈 0.001) compared with conventional therapy. Cilostazol was effective in increasing HDL-C (P = 0.002) and reducing triglycerides levels (P 〈 0.01) compared with conventional therapy. A trend towards significance was observed for the difference between conventional therapy alone and Probucol plus Cilostazol group for the change in oxidized low-density lipoprotein (Ox-LDL, P = 0.065). No significant effects on the majority of the remaining biomarkers were found across the treatment groups. Conclusions We have confirmed that Ox-LDL could be a possible plasma atherosclerotic biomarker among the evaluated biomarkers, which reflected the synergetic effect of Cilostazol plus Probucol in patients with T2DM and ASO shown previously in preclinical studies.
基金The project supported by National Natural Science Foundation of China under Grant Nos. 10534030 and 10474075
文摘We extend the exciton population equations of a two-level quantum dot system with weak excitation to the ones with strong excitations, in which, the phonon-induced intensity-dependent dephasing time and decay rate are involved. The straightforward calculated populations from the modified population equations demonstrate the damping behavior of Rabi oscillation as the external field increasing. The effect of the intensity-dependent dephasing time and the intensity-dependent decay rate are also discussed.
基金the Foundation of Fudan University for Young Teachers
文摘The Darboux transformations from arbitrary solutions of reduced Maxwell-Bloch equations is constructed in this article. Hence, in principle, we can find multi-soliton solutions by algebric algorithm, and the formula will be given explicitly.
文摘Ibuprofen is widely used as a non-steroidal anti-inflammatory drug and produced as racemic mixture. Its pharmacological activity resides only in S-(+)-enantiomer, and R-()-enantiomer is not only inactive but also has many side effects. Thus it is necessary to separate R-enantiomer from racemic ibuprofen. We studied optical separation of racemic Ibuprofen with chiral high performance liquid chromatography (HPLC). Out of three different chiral stationary phases, which were selected on the basis of structure and availability, two were found to be ef-fective. There was optimum eluent composition for each stationary phase for good resolution in optical separation. Resolution decreased with increase of eluent flow rate, but effect of injection volume on resolution was insignificant at high eluent flow rate.
基金Supported by the National Science Foundation of China (No. 29736170, No. 20025618) and the Doctoral Research Foundation by Ministry of Education of China (No. 1999025103). Additional support provided by the Visiting Researcher Foundation of University La
文摘Covering a wide range of bulk densities, density profiles for hard-sphere chain fluids (HSCFs) with chain length of 3,4,8,20,32 and 64 confined between two surfaces were obtained by Monte Carlo simulations using extended continuum configurational-bias (ECCB) method. It is shown that the enrichment of beads near surfaces is happened at high densities due to the bulk packing effect, on the contrary, the depletion is revealed at low densities owing to the configurational entropic contribution. Comparisons with those calculated by density functional theory presented by Cai et al. indicate that the agreement between simulations and predictions is good. Compressibility factors of bulk HSCFs calculated using volume fractions at surfaces were also used to test the reliability of various equations of state of HSCFs by different authors.
文摘By numerically solving the Maxwell-Bloch equations using an iterative predictor-corrector finite-difference time-domain technique, we investigate propagating properties of a few-cycle laser pulse in a 4,4'-bis(di-n-butylamino) stilbene (BDBAS) molecular medium when a static electric field exists. Dynamical two-photon absorption (TPA) cross sections are obtained and optical limiting (OL) behavior is displayed. The results show that when the static electric field intensity increases, the dynamical TPA cross section is enhanced and the OL behavior is improved. Moreover, both even- and odd-order harmonic spectral components are generated with existence of the static electric field because it breaks the inversion symmetry of the BDBAS molecule. This work provides a method to modulate the nonlinear optical properties of the BDBAS compounds.
文摘An entomological survey of Phlebotomine sand flies (Diptera: Psychodidae) was carried out in three sectors of Foum Jamgta region (province of Azilal, Morocco) during the year 2010. Morphological identification was performed on a total of 1,152 sand flies (23% females and 77% males) collected by sticky paper traps. 80% of the total collected flies were identified as Phlebotomus (Paraphlebotomus) sergenti (Parrot) (57%) and Phlebotomus (Larroussius) longicuspis (Nitzulescu) (23%). In addition to these dominant species, four other species were found, Phlebotomus (Phlebotomus) papatasi (Scopoli), Sergentomyia (Sergentomyia) minuta (Rondani), Phlebotomus (Larroussius) perniciosus (Newstead) and Phlebotomus (Paraphlebotomus) chabaudi (Croset). Overall, the population dynamics show a yearly bimodal pattern related to rainfall and temperature, and with high density around human dwellings. The spatiotemporal distribution of sand fly species was helpful to discuss strategies that might be useful in controlling cutaneous leishmaniasis transmission in this endemic focus.