One purpose of this study was to develop a paliperidone(PAL)tri-layer ascending release pushepull osmotic pump(TA-PPOP)tablet which could meet the needs of clinical applications.And another purpose was to investigate ...One purpose of this study was to develop a paliperidone(PAL)tri-layer ascending release pushepull osmotic pump(TA-PPOP)tablet which could meet the needs of clinical applications.And another purpose was to investigate whether different coating materials influenced in vivo performance of TA-PPOP.The ascending release mechanism of this trilayer delivery system on theory was elaborated.TA-PPOP was prepared by means of coating with cellulose acetate(CA)or ethyl cellulose(EC).Several important influence factors such as different core tablet compositions and different coating solution ingredients involved in the formulation procedure were investigated.The optimization of formulation and process was conducted by comparing different in vitro release behaviors of PAL.In vitro dissolution studies indicated that both the two formulations of different coating materials were able to deliver PAL at an ascending release rate during the whole 24 h test.The in vivo pharmacokinetics study showed that both self-made PPOP tablets with different coating had a good in vitro-in vivo correlation(IVIVC)and were bioequivalent with the brand product,which demonstrated no significant influence of the coating materials on the in vivo release acceleration of TA-PPOP.展开更多
In order to evaluate the pharmacokinetic profile of paliperidone extended-release tablets in vivo,a simple and rapid ultra-high performance liquid chromatographyetandem mass spectrometry(UHPLCeMS/MS)method was develop...In order to evaluate the pharmacokinetic profile of paliperidone extended-release tablets in vivo,a simple and rapid ultra-high performance liquid chromatographyetandem mass spectrometry(UHPLCeMS/MS)method was developed and validated for the determination of paliperidone in beagle dog plasma.Paliperidone and diazepam(internal standard)were extracted from plasma samples with diethyl ether,and then separated on a C_(18) column(2.1×50 mm,2.6 mm)under gradient elution with methanol-0.1%formic acid at a flow rate of 0.3 ml/min.The compounds were detected using a triple-quadrupole mass spectrometer equipped with an electrospray ionization(ESI)source.The validated method was linear over the concentration range of 1.00-1000.00 ng/ml and the lower limit of quantitation was 1.00 ng/ml.The intra-day and inter-day precision values were not more than 15%(relative standard deviation<20%at low levels),while the accuracy was within±10%of nominal values.The validated UHPLC-MS/MS method was successfully applied to an oral pharmacokinetic study of paliperidone extended-release tablets in a beagle dog.展开更多
To compare pharmacokinetic behaviors of nitrendipine submicron emulsion with nitrendipine solution following intravenous administration in rats.The plasma concentrations were analyzed by ultra-performance liquid chrom...To compare pharmacokinetic behaviors of nitrendipine submicron emulsion with nitrendipine solution following intravenous administration in rats.The plasma concentrations were analyzed by ultra-performance liquid chromatography coupled with tandem mass spectrometry detection(UPLC-MS/MS)through a new validated method.The pharmacokinetic parameters of the nitrendipine submicron emulsion and nitrendipine solution were as follows:AUC_(0-t) 900.76±186.59 versus 687.08±66.24 ng h/ml,C_(max) 854.54±159.48 versus 610.59±235.99 ng/ml,t_(1/2)2.37±1.99 versus 2.80±2.69 h.The relative bioavailability of nitrendipine submicron emulsion to nitrendipine solution was 131.4±11.3%.The developed methods could meet the requirements of bioanalysis.Compared to the solution injection,intravenous submicron emulsion presents higher systematic exposure which can help to improve the therapeutic efficacy.展开更多
[Objectives]To make a preliminary study on quality analysis of Root of Griffith Streptocaulon.[Methods]The moisture,ash and extract of Root of Griffith Streptocaulon were tested in accordance with the requirements of ...[Objectives]To make a preliminary study on quality analysis of Root of Griffith Streptocaulon.[Methods]The moisture,ash and extract of Root of Griffith Streptocaulon were tested in accordance with the requirements of 2015 Chinese Pharmacopoeia(Volume 4).[Results]The moisture content of Root of Griffith Streptocaulon was not higher than 12.74%,not lower than 6.26%,total ash content was not higher than 15.36%,not lower than 6.17%,acid-insoluble ash content was not higher than 0.55%,not lower than 0.17%,and extract was not higher than 11.83%,not lower than 5.23%.[Conclusions]This experiment made a preliminary study on the quality analysis of the Root of Griffith Streptocaulon,in the hope of providing a scientific basis for its quality control and formulation of the quality standard.展开更多
Organic scintillators that efficiently generate bright triplet excitons are of critical importance for highperformance X-ray-excited luminescence in radiation detection.However,the nature of triplet-singlet spinforbid...Organic scintillators that efficiently generate bright triplet excitons are of critical importance for highperformance X-ray-excited luminescence in radiation detection.However,the nature of triplet-singlet spinforbidden transitions in these materials often result in long-lived phosphorescence,which is undesirable for ultrafast X-ray detection and imaging.Here we demonstrate that the effect of hybridized local and charge-transfer(HLCT)excited states enables organic scintillators to exhibit highly efficient and fast radioluminescence(RL)in response to X-ray irradiation.Our experimental and theoretical investigation shows that the oxidized 1,8-naphthalimide-phenothiazine dyad(OMNI-PTZ 2)with HLCT-excited states has an enhanced overlap integral of the highest occupied molecular orbital(HOMO)and lowest unoccupied molecular orbital(LUMO)on MNIπ-orbitals,and moderate donor–acceptor electron interactions.As a result,the RL of these crystals exhibits a 61-fold increase and its monoexponential decay lifetime is three orders of magnitude faster compared to its corresponding thermally activated delayed fluorescence(TADF)molecule MNI-PTZ 1.We further demonstrate the practical utility of the OMNI-PTZ 2(G)in high-performance X-ray detection and imaging,achieving an X-ray dose sensitivity of 97 nGy s−1 and an exceptional spatial resolution of 20 lp/mm.Our study provides a promising molecular design principle for utilizing triplet excitons to develop high-efficiency and fast X-ray scintillators for the development of next-generation flexible and stretchable X-ray imaging detectors.展开更多
Metal-organic frameworks(MOFs)are a class of fascinating supramolecular crystalline materials that have been widely developed for catalysis,gas storage,illumination,drug delivery/cytoprotection,and so on.Recently,MOFs...Metal-organic frameworks(MOFs)are a class of fascinating supramolecular crystalline materials that have been widely developed for catalysis,gas storage,illumination,drug delivery/cytoprotection,and so on.Recently,MOFs have been found to have potential applications in X-ray detection due to their high sensitivity,fast response time,high absorption coefficient,and radiation stability.In this review,we present an overview on the fundamental mechanism of using MOFs for X-ray scintillation.We further discuss the recent developments in X-ray detection based on indirect X-ray scintillation and direct X-ray conversion.Finally,we provide a summary and a perspective on the future of this promising research field.展开更多
Aggregation-induced emission enhancement and aggregation-induced chirality inversion are two individ-ual phenomena for the enantiomerically pure organic dyes in the aggregates.Herein we reported for the first time tha...Aggregation-induced emission enhancement and aggregation-induced chirality inversion are two individ-ual phenomena for the enantiomerically pure organic dyes in the aggregates.Herein we reported for the first time that these two interesting phenomena could be observed simultaneously in the aggregated states of enantiomerically pure S/R-1,1?-binaphthol annulated perylene diimides,in which two perylene diimides moieties were bridged by S/R-1,1?-binaphthol(BINOL)at the bay positions.Owing to the rotat-able C2 axes between two naphthol annulated perylene diimides moieties,both of them display intrinsic behaviors of aggregation-induced emission enhancements.At the same time,due to the steric hindrances in the imide and methoxy positions,the neighboring twoπ-systems of these two unique polycyclic aro-matic imides in poor solvents are preferable to adopt a cross-stacking mode and thus form helical X-aggregates of opposite chirality(M/P)with chirality inversion characteristics in their circular dichroism and circularly polarized luminescence spectroscopic studies.展开更多
文摘One purpose of this study was to develop a paliperidone(PAL)tri-layer ascending release pushepull osmotic pump(TA-PPOP)tablet which could meet the needs of clinical applications.And another purpose was to investigate whether different coating materials influenced in vivo performance of TA-PPOP.The ascending release mechanism of this trilayer delivery system on theory was elaborated.TA-PPOP was prepared by means of coating with cellulose acetate(CA)or ethyl cellulose(EC).Several important influence factors such as different core tablet compositions and different coating solution ingredients involved in the formulation procedure were investigated.The optimization of formulation and process was conducted by comparing different in vitro release behaviors of PAL.In vitro dissolution studies indicated that both the two formulations of different coating materials were able to deliver PAL at an ascending release rate during the whole 24 h test.The in vivo pharmacokinetics study showed that both self-made PPOP tablets with different coating had a good in vitro-in vivo correlation(IVIVC)and were bioequivalent with the brand product,which demonstrated no significant influence of the coating materials on the in vivo release acceleration of TA-PPOP.
文摘In order to evaluate the pharmacokinetic profile of paliperidone extended-release tablets in vivo,a simple and rapid ultra-high performance liquid chromatographyetandem mass spectrometry(UHPLCeMS/MS)method was developed and validated for the determination of paliperidone in beagle dog plasma.Paliperidone and diazepam(internal standard)were extracted from plasma samples with diethyl ether,and then separated on a C_(18) column(2.1×50 mm,2.6 mm)under gradient elution with methanol-0.1%formic acid at a flow rate of 0.3 ml/min.The compounds were detected using a triple-quadrupole mass spectrometer equipped with an electrospray ionization(ESI)source.The validated method was linear over the concentration range of 1.00-1000.00 ng/ml and the lower limit of quantitation was 1.00 ng/ml.The intra-day and inter-day precision values were not more than 15%(relative standard deviation<20%at low levels),while the accuracy was within±10%of nominal values.The validated UHPLC-MS/MS method was successfully applied to an oral pharmacokinetic study of paliperidone extended-release tablets in a beagle dog.
文摘To compare pharmacokinetic behaviors of nitrendipine submicron emulsion with nitrendipine solution following intravenous administration in rats.The plasma concentrations were analyzed by ultra-performance liquid chromatography coupled with tandem mass spectrometry detection(UPLC-MS/MS)through a new validated method.The pharmacokinetic parameters of the nitrendipine submicron emulsion and nitrendipine solution were as follows:AUC_(0-t) 900.76±186.59 versus 687.08±66.24 ng h/ml,C_(max) 854.54±159.48 versus 610.59±235.99 ng/ml,t_(1/2)2.37±1.99 versus 2.80±2.69 h.The relative bioavailability of nitrendipine submicron emulsion to nitrendipine solution was 131.4±11.3%.The developed methods could meet the requirements of bioanalysis.Compared to the solution injection,intravenous submicron emulsion presents higher systematic exposure which can help to improve the therapeutic efficacy.
基金The First Batch High-level Talent Scientific Research Project of The Affiliated Hospital of Youjiang Medical University for Nationalities in 2019。
文摘[Objectives]To make a preliminary study on quality analysis of Root of Griffith Streptocaulon.[Methods]The moisture,ash and extract of Root of Griffith Streptocaulon were tested in accordance with the requirements of 2015 Chinese Pharmacopoeia(Volume 4).[Results]The moisture content of Root of Griffith Streptocaulon was not higher than 12.74%,not lower than 6.26%,total ash content was not higher than 15.36%,not lower than 6.17%,acid-insoluble ash content was not higher than 0.55%,not lower than 0.17%,and extract was not higher than 11.83%,not lower than 5.23%.[Conclusions]This experiment made a preliminary study on the quality analysis of the Root of Griffith Streptocaulon,in the hope of providing a scientific basis for its quality control and formulation of the quality standard.
基金supported by the National Key R&D Program of China(grant no.2020YFA0709900)the National Natural Science Foundation of China(grant nos.21971041,22201042,22027805,62134003,and 22104016)+2 种基金the Natural Science Foundation of Fujian Province(grant nos.2020J01447,2022J06008,and 2022J0121)the Research Foundation of Education Bureau of Fujian Province(grant no.JAT210001)the Fuzhou University Testing Fund of Precious Apparatus(grant no.2022T001).
文摘Organic scintillators that efficiently generate bright triplet excitons are of critical importance for highperformance X-ray-excited luminescence in radiation detection.However,the nature of triplet-singlet spinforbidden transitions in these materials often result in long-lived phosphorescence,which is undesirable for ultrafast X-ray detection and imaging.Here we demonstrate that the effect of hybridized local and charge-transfer(HLCT)excited states enables organic scintillators to exhibit highly efficient and fast radioluminescence(RL)in response to X-ray irradiation.Our experimental and theoretical investigation shows that the oxidized 1,8-naphthalimide-phenothiazine dyad(OMNI-PTZ 2)with HLCT-excited states has an enhanced overlap integral of the highest occupied molecular orbital(HOMO)and lowest unoccupied molecular orbital(LUMO)on MNIπ-orbitals,and moderate donor–acceptor electron interactions.As a result,the RL of these crystals exhibits a 61-fold increase and its monoexponential decay lifetime is three orders of magnitude faster compared to its corresponding thermally activated delayed fluorescence(TADF)molecule MNI-PTZ 1.We further demonstrate the practical utility of the OMNI-PTZ 2(G)in high-performance X-ray detection and imaging,achieving an X-ray dose sensitivity of 97 nGy s−1 and an exceptional spatial resolution of 20 lp/mm.Our study provides a promising molecular design principle for utilizing triplet excitons to develop high-efficiency and fast X-ray scintillators for the development of next-generation flexible and stretchable X-ray imaging detectors.
基金supported by the National Natural Science Foundation of China(21971041,22001039)the Natural Science Foundation of Fujian Province(2020J01447)the Research Foundation of Education Bureau of Fujian Province(JAT210001)。
文摘Metal-organic frameworks(MOFs)are a class of fascinating supramolecular crystalline materials that have been widely developed for catalysis,gas storage,illumination,drug delivery/cytoprotection,and so on.Recently,MOFs have been found to have potential applications in X-ray detection due to their high sensitivity,fast response time,high absorption coefficient,and radiation stability.In this review,we present an overview on the fundamental mechanism of using MOFs for X-ray scintillation.We further discuss the recent developments in X-ray detection based on indirect X-ray scintillation and direct X-ray conversion.Finally,we provide a summary and a perspective on the future of this promising research field.
基金supported by the National Natural Sci-ence Foundation of China(No.21971041)Natural Science Foundation of Fujian Province(No.2020J01447).
文摘Aggregation-induced emission enhancement and aggregation-induced chirality inversion are two individ-ual phenomena for the enantiomerically pure organic dyes in the aggregates.Herein we reported for the first time that these two interesting phenomena could be observed simultaneously in the aggregated states of enantiomerically pure S/R-1,1?-binaphthol annulated perylene diimides,in which two perylene diimides moieties were bridged by S/R-1,1?-binaphthol(BINOL)at the bay positions.Owing to the rotat-able C2 axes between two naphthol annulated perylene diimides moieties,both of them display intrinsic behaviors of aggregation-induced emission enhancements.At the same time,due to the steric hindrances in the imide and methoxy positions,the neighboring twoπ-systems of these two unique polycyclic aro-matic imides in poor solvents are preferable to adopt a cross-stacking mode and thus form helical X-aggregates of opposite chirality(M/P)with chirality inversion characteristics in their circular dichroism and circularly polarized luminescence spectroscopic studies.