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
Constructing bismuth oxyhalide solid solutions with a single homogeneous phase have intrigued the research community;however,a deeper understanding of the intrinsic origin for improved bulk-charge separation is still ...Constructing bismuth oxyhalide solid solutions with a single homogeneous phase have intrigued the research community;however,a deeper understanding of the intrinsic origin for improved bulk-charge separation is still unclear.Herein,a series of Bi_(24)O_(31)Cl_(x)Br_(10-x) solid solutions with the same structural characteristics were synthesized by crystal structure regulation.Combining density functional theory calculation,Kelvin probe force microscopy,and zeta potential testing results,an enhanced internal electric field(IEF)intensity between[Bi_(24)O_(31)]and[X]layers was achieved by changing halogen types and ratios.This greatly facilitated bulk-charge separation and transfer efficiency,which is significant for the degradation of phenolic organic pollutants.Owing to the enhanced IEF intensity,the charge carrier density of Bi_(24)O_(31)Cl_(4)Br_(6) was 33.1 and 4.7 times stronger than that of Bi_(24)O_(31)Cl_(10) and Bi_(24)O_(31)Br_(10),respectively.Therefore,Bi24O31Cl4Br6 had an optimal photoactivity for the degradation of bisphenol A,which was 6.21 and 2.71 times higher than those of Bi_(24)O_(31)Cl_(10) and Bi_(24)O_(31)Br_(10),respectively.Thus,this study revealed the intrinsic mechanism of the solid solution strategy for photocatalytic performance enhancement with respect to an IEF.展开更多
Abstract: The objective was to obtain solid dispersion to improve the dissolution rate, solubility and oral absorption of MB (mebendazole), poor water-soluble drugs. The new formulation was characterized by DSC (d...Abstract: The objective was to obtain solid dispersion to improve the dissolution rate, solubility and oral absorption of MB (mebendazole), poor water-soluble drugs. The new formulation was characterized by DSC (differential scanning calorimetry), PXRD (powder X-ray diffraction), FT-1R (fourier transform infrared spectroscopy) and STEM (scanning transmission electron microscopy) methods. Solid dispersions of MB with polyvinylpyrrolidone K-30 (PVP K30) were prepared by solvent evaporation method. The solubility of MB (original powder) and that of the solid dispersions was measured at 25℃ in ethanol-water. The aqueous solubility of MB was favoured by the presence of the polymer in solvent mixtures. Combination of solid dispersions with co-solvents increased the water solubility of MB in a larger extent that each method separately. Solubility parameter (o) was used to relate to solubility profiles. MB and the solid dispersions show a solubility curve with a single peak at 51 = 30.78 MPav2. Solid state characterizations indicated that the solid dispersion exist an amorphous material entrapped in polymer matrix getting highest improvement in wettability and solubility.展开更多
In the present research, we selected Sylysia as a porous material and febuxostat(FBT) as model drug to prepare the FBT SiO2 solid dispersions using a solvent evaporation method. We firstly established an HPLC method...In the present research, we selected Sylysia as a porous material and febuxostat(FBT) as model drug to prepare the FBT SiO2 solid dispersions using a solvent evaporation method. We firstly established an HPLC method for determining FBT in our prepared FBT SiO2 solid dispersions. And then, the characteristics of FBT SiO2 solid dispersions were investigated, including differential scanning calorimetry(DSC), powder X-ray diffraction(PXRD), scanning electron microscope(SEM), particle size and distribution. The solubility and dissolution of FBT SiO2 solid dispersion were also evaluated. The results of DSC and PXRD showed that the FBT existed in an amorphous state in FBT SiO2 solid dispersions. The SEM and particle size results indicated that the shape and average particle size of FBT SiO2 solid dispersions was similar to the Sylysia. The solubility and dissolution of FBT in FBT SiO2 solid dispersions were significantly enhanced compared with the pure FBT. In conclusion, we successfully prepared FBT SiO2 solid dispersions to increase the solubility and dissolution rate of the poorly water-soluble FBT.展开更多
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Constructing bismuth oxyhalide solid solutions with a single homogeneous phase have intrigued the research community;however,a deeper understanding of the intrinsic origin for improved bulk-charge separation is still unclear.Herein,a series of Bi_(24)O_(31)Cl_(x)Br_(10-x) solid solutions with the same structural characteristics were synthesized by crystal structure regulation.Combining density functional theory calculation,Kelvin probe force microscopy,and zeta potential testing results,an enhanced internal electric field(IEF)intensity between[Bi_(24)O_(31)]and[X]layers was achieved by changing halogen types and ratios.This greatly facilitated bulk-charge separation and transfer efficiency,which is significant for the degradation of phenolic organic pollutants.Owing to the enhanced IEF intensity,the charge carrier density of Bi_(24)O_(31)Cl_(4)Br_(6) was 33.1 and 4.7 times stronger than that of Bi_(24)O_(31)Cl_(10) and Bi_(24)O_(31)Br_(10),respectively.Therefore,Bi24O31Cl4Br6 had an optimal photoactivity for the degradation of bisphenol A,which was 6.21 and 2.71 times higher than those of Bi_(24)O_(31)Cl_(10) and Bi_(24)O_(31)Br_(10),respectively.Thus,this study revealed the intrinsic mechanism of the solid solution strategy for photocatalytic performance enhancement with respect to an IEF.
文摘Abstract: The objective was to obtain solid dispersion to improve the dissolution rate, solubility and oral absorption of MB (mebendazole), poor water-soluble drugs. The new formulation was characterized by DSC (differential scanning calorimetry), PXRD (powder X-ray diffraction), FT-1R (fourier transform infrared spectroscopy) and STEM (scanning transmission electron microscopy) methods. Solid dispersions of MB with polyvinylpyrrolidone K-30 (PVP K30) were prepared by solvent evaporation method. The solubility of MB (original powder) and that of the solid dispersions was measured at 25℃ in ethanol-water. The aqueous solubility of MB was favoured by the presence of the polymer in solvent mixtures. Combination of solid dispersions with co-solvents increased the water solubility of MB in a larger extent that each method separately. Solubility parameter (o) was used to relate to solubility profiles. MB and the solid dispersions show a solubility curve with a single peak at 51 = 30.78 MPav2. Solid state characterizations indicated that the solid dispersion exist an amorphous material entrapped in polymer matrix getting highest improvement in wettability and solubility.
基金National Natural Science Foundation of China(Grant No.81172992)the National Basic Research Program of China(Grant No.973 Program 2009CB930300)Innovation Team of Ministry of Education(Grant No.BMU20110263)
文摘In the present research, we selected Sylysia as a porous material and febuxostat(FBT) as model drug to prepare the FBT SiO2 solid dispersions using a solvent evaporation method. We firstly established an HPLC method for determining FBT in our prepared FBT SiO2 solid dispersions. And then, the characteristics of FBT SiO2 solid dispersions were investigated, including differential scanning calorimetry(DSC), powder X-ray diffraction(PXRD), scanning electron microscope(SEM), particle size and distribution. The solubility and dissolution of FBT SiO2 solid dispersion were also evaluated. The results of DSC and PXRD showed that the FBT existed in an amorphous state in FBT SiO2 solid dispersions. The SEM and particle size results indicated that the shape and average particle size of FBT SiO2 solid dispersions was similar to the Sylysia. The solubility and dissolution of FBT in FBT SiO2 solid dispersions were significantly enhanced compared with the pure FBT. In conclusion, we successfully prepared FBT SiO2 solid dispersions to increase the solubility and dissolution rate of the poorly water-soluble FBT.