Meloxicam-β-cyclodextrin （ME-β-CD） inclusion complex was prepared by a fluid-bed coating technique upon solvent removal and simultaneous depositing onto the surface of nonpareil pellets and using PVP K30 as a bind...Meloxicam-β-cyclodextrin （ME-β-CD） inclusion complex was prepared by a fluid-bed coating technique upon solvent removal and simultaneous depositing onto the surface of nonpareil pellets and using PVP K30 as a binding agent to facilitate good coating. The resultant pellets were spherical and intact in shape with good flowability and friability. SEM analysis showed that the pellets were smooth and had a tightly coated inclusion complex layer. In vitro dissolution of the inclusion complex pellets in pH 7.4 phosphate buffer was dramatically enhanced at an ME/CD ratio of 1/1. DSC and powder X-ray diffractometry proved the absence of crystallinity in the ME/CD inclusion complexes. Moreover, Fourier transform-infrared spectrometry together with Raman spectrometry indicated that the thiazole ring of ME was possibly included in the cavity of β-CD.展开更多
In the present study,a simple and rapid method was developed to improve the in vitro dissolution of repaglinide,an oral antidiabetic drug,which was based on addition of meglumine in 50%(v/v)ethanol to dissolve repagli...In the present study,a simple and rapid method was developed to improve the in vitro dissolution of repaglinide,an oral antidiabetic drug,which was based on addition of meglumine in 50%(v/v)ethanol to dissolve repaglinide,and the drug dissolved in meglumine/50%ethanol was used directly with a binder to prepare tablets.The mechanism of solubilization of repaglinide by meglumine was studied by using infrared spectrum(IR),ultraviolet(UV)measurement through dual wavelength,differential scanning calorimetry(DSC)and X-ray powder diffraction methods.Dissolution tests of repaglinide tablets were performed in the media with different pH values and the repaglinide concentrations were analyzed by High Performance Liquid Chromatography(HPLC)method.The solubility data showed that with the meglumine concentration increasing,the solubility of repaglinide was increased.Meanwhile,tablets with the molar ratio of repaglinide and meglumine 1:2(n/n)resulted in a significant increase in dissolution compared to the repaglinide tablets without using meglumine,and nearly equal to the commercial preparations of Novo-Norm^(®),which concluded that meglumine had a great role in promoting the dissolution of repaglinide.The results of IR and UV dual wavelength methods suggested the formation of repaglinideemeglumine(REPeMEG)molecular complex.DSC results showed that the melting peak of repaglinide disappeared in the REPeMEG coprecipitate,which indicated that repaglinide was stable when existing at amorphous or molecular state.The experiment of X-ray powder diffraction showed that with the solubilization of meglumine,the crystal diffraction peak of repaglinide disappeared,which further inferred that repaglinide was formed complexes with meglumine.It was demonstrated that the method of improving repaglinide with meglumine was reliable and could be suitable for repaglinide tablets production in industry.This study also provides a feasible way to enhance the dissolution of drugs with low solubility,which will be leading to improved bioavailability展开更多
This study investigated the characteristics and genesis of reservoirs in the 2^(nd) and 4^(th) members of Sinian Dengying Formation in northern Sichuan and its surrounding areas, on the basis of outcrop, drilling core...This study investigated the characteristics and genesis of reservoirs in the 2^(nd) and 4^(th) members of Sinian Dengying Formation in northern Sichuan and its surrounding areas, on the basis of outcrop, drilling cores and thin section observation and geochemical analysis. The reservoirs of 2^(nd) member are distributed in the middle part of the stratum. The reservoir quality is controlled by supergene karst and the distribution of mound-shoal complex. The bedded elongated isolated algal framework solution-cave and the residual "grape-lace" cave, which are partially filled with multi-stage dolosparite, constituted the main reservoir space of the 2^(nd) member. There is no asphalt distribution in the pores. The pore connectivity is poor, and the porosity and permeability of the reservoir is relatively low. The reservoirs of 4^(th) member were distributed in the upper and top part of the stratum. The reservoir quality is controlled by burial dissolution and the distribution of mound-shoal complex. The bedded algal framework solution-pores or caves, intercrystalline pores and intercrystalline dissolved pores constituted the main reservoir space of the 4^(th) member. It's partially filled with asphalt and quartz, without any dolosparite fillings in the pores and caves. The pore connectivity is good. Most of the 4^(th) member reservoirs had medium-low porosity and low permeability, and, locally, medium-high porosity and medium permeability. Affected by the development of mound-shoal complex and heterogeneous dissolution, the platform margin along Ningqiang, Guangyuan, Jiange and Langzhong is the most favorable region for reservoir development. Deep buried Dengying Formation in the guangyuan and langzhong areas should be the most important hydrocarbon target for the future exploration.展开更多
基金the School of Pharmacy,Fudan University,for financial support
文摘Meloxicam-β-cyclodextrin （ME-β-CD） inclusion complex was prepared by a fluid-bed coating technique upon solvent removal and simultaneous depositing onto the surface of nonpareil pellets and using PVP K30 as a binding agent to facilitate good coating. The resultant pellets were spherical and intact in shape with good flowability and friability. SEM analysis showed that the pellets were smooth and had a tightly coated inclusion complex layer. In vitro dissolution of the inclusion complex pellets in pH 7.4 phosphate buffer was dramatically enhanced at an ME/CD ratio of 1/1. DSC and powder X-ray diffractometry proved the absence of crystallinity in the ME/CD inclusion complexes. Moreover, Fourier transform-infrared spectrometry together with Raman spectrometry indicated that the thiazole ring of ME was possibly included in the cavity of β-CD.
基金The work was supported by Shenyang Pharmaceutical University(10163),including the financial support.
文摘In the present study,a simple and rapid method was developed to improve the in vitro dissolution of repaglinide,an oral antidiabetic drug,which was based on addition of meglumine in 50%(v/v)ethanol to dissolve repaglinide,and the drug dissolved in meglumine/50%ethanol was used directly with a binder to prepare tablets.The mechanism of solubilization of repaglinide by meglumine was studied by using infrared spectrum(IR),ultraviolet(UV)measurement through dual wavelength,differential scanning calorimetry(DSC)and X-ray powder diffraction methods.Dissolution tests of repaglinide tablets were performed in the media with different pH values and the repaglinide concentrations were analyzed by High Performance Liquid Chromatography(HPLC)method.The solubility data showed that with the meglumine concentration increasing,the solubility of repaglinide was increased.Meanwhile,tablets with the molar ratio of repaglinide and meglumine 1:2(n/n)resulted in a significant increase in dissolution compared to the repaglinide tablets without using meglumine,and nearly equal to the commercial preparations of Novo-Norm^(®),which concluded that meglumine had a great role in promoting the dissolution of repaglinide.The results of IR and UV dual wavelength methods suggested the formation of repaglinideemeglumine(REPeMEG)molecular complex.DSC results showed that the melting peak of repaglinide disappeared in the REPeMEG coprecipitate,which indicated that repaglinide was stable when existing at amorphous or molecular state.The experiment of X-ray powder diffraction showed that with the solubilization of meglumine,the crystal diffraction peak of repaglinide disappeared,which further inferred that repaglinide was formed complexes with meglumine.It was demonstrated that the method of improving repaglinide with meglumine was reliable and could be suitable for repaglinide tablets production in industry.This study also provides a feasible way to enhance the dissolution of drugs with low solubility,which will be leading to improved bioavailability
基金Supported by the China National Science and Technology Major Project(2017ZX05001001-002)
文摘This study investigated the characteristics and genesis of reservoirs in the 2^(nd) and 4^(th) members of Sinian Dengying Formation in northern Sichuan and its surrounding areas, on the basis of outcrop, drilling cores and thin section observation and geochemical analysis. The reservoirs of 2^(nd) member are distributed in the middle part of the stratum. The reservoir quality is controlled by supergene karst and the distribution of mound-shoal complex. The bedded elongated isolated algal framework solution-cave and the residual "grape-lace" cave, which are partially filled with multi-stage dolosparite, constituted the main reservoir space of the 2^(nd) member. There is no asphalt distribution in the pores. The pore connectivity is poor, and the porosity and permeability of the reservoir is relatively low. The reservoirs of 4^(th) member were distributed in the upper and top part of the stratum. The reservoir quality is controlled by burial dissolution and the distribution of mound-shoal complex. The bedded algal framework solution-pores or caves, intercrystalline pores and intercrystalline dissolved pores constituted the main reservoir space of the 4^(th) member. It's partially filled with asphalt and quartz, without any dolosparite fillings in the pores and caves. The pore connectivity is good. Most of the 4^(th) member reservoirs had medium-low porosity and low permeability, and, locally, medium-high porosity and medium permeability. Affected by the development of mound-shoal complex and heterogeneous dissolution, the platform margin along Ningqiang, Guangyuan, Jiange and Langzhong is the most favorable region for reservoir development. Deep buried Dengying Formation in the guangyuan and langzhong areas should be the most important hydrocarbon target for the future exploration.
