The interaction between ibuprofen and maltodextrins with different dextrose equivalent was studied in solution and solid state in order to investigate the effect on the solubility of ibuprofen and to determine their u...The interaction between ibuprofen and maltodextrins with different dextrose equivalent was studied in solution and solid state in order to investigate the effect on the solubility of ibuprofen and to determine their usefulness in terms of chiral recognition. Apparent binding constants were calculated using nuclear magnetic resonance spectroscopy experiments and solubility studies. The results showed an increase in the apparent solubility of ibuprofen in the presence of maltodextrins that depended on their ionization state. The freeze-drying method was used to prepare solid complexes, while physical mixtures were obtained by simple blending. These solid systems were characterized in the solid state using differential scanning calorimetry, thermogravimetric analysis, Fourier Transform-Infrared spectroscopy, scanning electron microscopy and X-ray diffractometry. Detailed nuclear magnetic resonance studies provided evidence of the influence of the type and concentration of the maltodextrin host on the chiral recognition of racemic ibuprofen, indicating that these linear ligands act as chiral selectors.展开更多
The aim of this study was to characterize the provesicle formulation of nateglinide(NTG)to facilitate the development of a novel controlled release system of NTG with improved efficacy and oral bioavailability compare...The aim of this study was to characterize the provesicle formulation of nateglinide(NTG)to facilitate the development of a novel controlled release system of NTG with improved efficacy and oral bioavailability compared to the currently marketed NTG formulation(Glinate^(™)60).NTG provesicles were prepared by a slurry method using the non-ionic surfactant,Span 60(SP),and cholesterol(CH)as vesicle forming agents and maltodextrin as a coated carrier.Multilamellar niosomes with narrow size distribution were shown to be successfully prepared by means of dynamic laser scattering(DLS)and field emission scanning electron microscopy(FESEM).The absence of drug-excipient interactions was confirmed by Fourier transform infrared spectroscopy(FT-IR),differential scanning calorimetry(DSC)and X-ray diffraction(XRD)studies.In vitro release of NTG in different dissolution media was improved compared to pure drug.A goat intestinal permeation study revealed that the provesicular formulation(F4)with an SP:CH ratio of 5:5 gave higher cumulative amount of drug permeated at 48 h compared to Glinate^(™)60 and control.A pharmacodynamic study in streptozotocin-induced diabetic rats confirmed that formulation F4 significantly(P<0.05)reduced blood glucose levels in comparison to Glinate 60.Overall the results show that controlled release NTG provesicles offer a useful and promising oral delivery system for the treatment of type Ⅱ diabetes.展开更多
该文以文冠果种仁油为芯材,以阿拉伯胶-麦芽糊精(acacia senegal-maltodextrin,AS-MD)或大豆分离蛋白-麦芽糊精(soy protein isolate-maltodextrin,SPI-MD)为壁材,制备了5组不同壁材构成的文冠果油微胶囊粉末。通过对文冠果油微胶囊的...该文以文冠果种仁油为芯材,以阿拉伯胶-麦芽糊精(acacia senegal-maltodextrin,AS-MD)或大豆分离蛋白-麦芽糊精(soy protein isolate-maltodextrin,SPI-MD)为壁材,制备了5组不同壁材构成的文冠果油微胶囊粉末。通过对文冠果油微胶囊的包埋率、理化指标、微观形态、体相结构和热稳定性进行比较研究,确定最优壁材配比。结果表明,由质量比为3∶2的SPI-MD壁材组成制备的微胶囊包埋率高达77.09%,湿润性和溶解性等理化性质均优于其他组;该组微胶囊的质量保留率和结晶度最高,氧化稳定性明显提升,表面结构呈完整球形、结构致密。总之,SPI和MD作为壁材对文冠果油具有较好的包埋和保护作用,最优壁材配比为3∶2。该研究结果为优化文冠果油微胶囊的制备工艺提供了理论依据。展开更多
文摘The interaction between ibuprofen and maltodextrins with different dextrose equivalent was studied in solution and solid state in order to investigate the effect on the solubility of ibuprofen and to determine their usefulness in terms of chiral recognition. Apparent binding constants were calculated using nuclear magnetic resonance spectroscopy experiments and solubility studies. The results showed an increase in the apparent solubility of ibuprofen in the presence of maltodextrins that depended on their ionization state. The freeze-drying method was used to prepare solid complexes, while physical mixtures were obtained by simple blending. These solid systems were characterized in the solid state using differential scanning calorimetry, thermogravimetric analysis, Fourier Transform-Infrared spectroscopy, scanning electron microscopy and X-ray diffractometry. Detailed nuclear magnetic resonance studies provided evidence of the influence of the type and concentration of the maltodextrin host on the chiral recognition of racemic ibuprofen, indicating that these linear ligands act as chiral selectors.
基金This work was financially supported by the All India Council of Technical Education(AICTE)India(Grant No.KLECOP/QIP/2010).
文摘The aim of this study was to characterize the provesicle formulation of nateglinide(NTG)to facilitate the development of a novel controlled release system of NTG with improved efficacy and oral bioavailability compared to the currently marketed NTG formulation(Glinate^(™)60).NTG provesicles were prepared by a slurry method using the non-ionic surfactant,Span 60(SP),and cholesterol(CH)as vesicle forming agents and maltodextrin as a coated carrier.Multilamellar niosomes with narrow size distribution were shown to be successfully prepared by means of dynamic laser scattering(DLS)and field emission scanning electron microscopy(FESEM).The absence of drug-excipient interactions was confirmed by Fourier transform infrared spectroscopy(FT-IR),differential scanning calorimetry(DSC)and X-ray diffraction(XRD)studies.In vitro release of NTG in different dissolution media was improved compared to pure drug.A goat intestinal permeation study revealed that the provesicular formulation(F4)with an SP:CH ratio of 5:5 gave higher cumulative amount of drug permeated at 48 h compared to Glinate^(™)60 and control.A pharmacodynamic study in streptozotocin-induced diabetic rats confirmed that formulation F4 significantly(P<0.05)reduced blood glucose levels in comparison to Glinate 60.Overall the results show that controlled release NTG provesicles offer a useful and promising oral delivery system for the treatment of type Ⅱ diabetes.
文摘该文以文冠果种仁油为芯材,以阿拉伯胶-麦芽糊精(acacia senegal-maltodextrin,AS-MD)或大豆分离蛋白-麦芽糊精(soy protein isolate-maltodextrin,SPI-MD)为壁材,制备了5组不同壁材构成的文冠果油微胶囊粉末。通过对文冠果油微胶囊的包埋率、理化指标、微观形态、体相结构和热稳定性进行比较研究,确定最优壁材配比。结果表明,由质量比为3∶2的SPI-MD壁材组成制备的微胶囊包埋率高达77.09%,湿润性和溶解性等理化性质均优于其他组;该组微胶囊的质量保留率和结晶度最高,氧化稳定性明显提升,表面结构呈完整球形、结构致密。总之,SPI和MD作为壁材对文冠果油具有较好的包埋和保护作用,最优壁材配比为3∶2。该研究结果为优化文冠果油微胶囊的制备工艺提供了理论依据。
