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
目的探究非淀粉多糖对酶法制备高分支麦芽糊精黏弹特性的影响。方法利用α-葡萄糖基转移酶(α-glucanotransferase,α-GT)和马铃薯淀粉制备高分支麦芽糊精,并对其分子量、分支度和消化性进行测定。采用动态流变仪分别测试黄原胶、桃胶...目的探究非淀粉多糖对酶法制备高分支麦芽糊精黏弹特性的影响。方法利用α-葡萄糖基转移酶(α-glucanotransferase,α-GT)和马铃薯淀粉制备高分支麦芽糊精,并对其分子量、分支度和消化性进行测定。采用动态流变仪分别测试黄原胶、桃胶、香豆胶、刺槐豆胶和魔芋胶5种非淀粉多糖对高分支麦芽糊精的增稠效果。选取增稠效果适中、稳定性高的香豆胶按不同质量比与高分支麦芽糊精混合,进行振荡流变测试。通过傅里叶红外光谱对混合体系的结构进行表征。结果所得高分支麦芽糊精重均分子量为2.78×106 g/mol,聚合度(degree of polymerization,DP)≤5的超短链含量为52.09%,消化率显著降低。测得的剪切流变曲线均符合Herschel-Bulkley模型(决定系数R2>0.99),增稠效果魔芋胶>刺槐豆胶>香豆胶>黄原胶>桃胶,体系稳定性香豆胶>桃胶>刺槐豆胶>魔芋胶>黄原胶。振荡流变测定结果表明,随着香豆胶含量的增加,储能模量、损耗模量和损耗角正切tanδ均逐渐减小,混合体系由黏性液体逐渐偏向于弹性固体。傅里叶红外光谱结果表明,随着香豆胶在体系中的含量增加,指纹区峰值强度下降。结论α-GT改性马铃薯淀粉,可以制备出一种分支度高、分子量低且具有缓慢消化特性的高分支糊精。5种非淀粉多糖均可增加高分支麦芽糊精的黏弹特性,且当高分支糊精与香豆胶的质量比例为5:1时,黏度最大,弹性最小,混合体系具有更好的协同增稠效果。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.
文摘目的探究非淀粉多糖对酶法制备高分支麦芽糊精黏弹特性的影响。方法利用α-葡萄糖基转移酶(α-glucanotransferase,α-GT)和马铃薯淀粉制备高分支麦芽糊精,并对其分子量、分支度和消化性进行测定。采用动态流变仪分别测试黄原胶、桃胶、香豆胶、刺槐豆胶和魔芋胶5种非淀粉多糖对高分支麦芽糊精的增稠效果。选取增稠效果适中、稳定性高的香豆胶按不同质量比与高分支麦芽糊精混合,进行振荡流变测试。通过傅里叶红外光谱对混合体系的结构进行表征。结果所得高分支麦芽糊精重均分子量为2.78×106 g/mol,聚合度(degree of polymerization,DP)≤5的超短链含量为52.09%,消化率显著降低。测得的剪切流变曲线均符合Herschel-Bulkley模型(决定系数R2>0.99),增稠效果魔芋胶>刺槐豆胶>香豆胶>黄原胶>桃胶,体系稳定性香豆胶>桃胶>刺槐豆胶>魔芋胶>黄原胶。振荡流变测定结果表明,随着香豆胶含量的增加,储能模量、损耗模量和损耗角正切tanδ均逐渐减小,混合体系由黏性液体逐渐偏向于弹性固体。傅里叶红外光谱结果表明,随着香豆胶在体系中的含量增加,指纹区峰值强度下降。结论α-GT改性马铃薯淀粉,可以制备出一种分支度高、分子量低且具有缓慢消化特性的高分支糊精。5种非淀粉多糖均可增加高分支麦芽糊精的黏弹特性,且当高分支糊精与香豆胶的质量比例为5:1时,黏度最大,弹性最小,混合体系具有更好的协同增稠效果。
