生物利用度更高的β-环糊精新多聚物

Chemistry Pub Date : 2023-12-23 DOI:10.3390/chemistry6010003
A. K. Gatiatulin, Ilya S. Balakhontsev, Sofia M. Talashmanova, M. Ziganshin, V. Gorbatchuk
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引用次数: 0

摘要

通过粉末 X 射线衍射、红外光谱和热分析,首次获得了无水 β-环糊精的一种新的多晶体(多晶体 III),并对其进行了表征。利用溶液热量计测定了这种多晶体在水中的溶解焓和溶解时间,并将其与β-环糊精的干燥商品形式(多晶体 I)、其无定形形式以及 2-羟丙基-β-环糊精的溶解焓和溶解时间进行了比较。利用差示扫描量热法测定了多晶体 I 和 III 在较大温度范围内的比热容,从而得出了 298 K 时多晶体转变的焓和吉布斯能值。由于能量丰富,新发现的 β-环糊精多晶体与干燥的商用 β-环糊精相比,溶解速率明显更高,对水的亲和力也更强。这些特性使得这种新的多晶体在水溶液和糊剂中的客体工业应用中大有可为,并可能成为水溶性 β-环糊精衍生物的理想替代品。
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New Polymorph of β-Cyclodextrin with a Higher Bioavailability
A new polymorph of anhydrous β-cyclodextrin (polymorph III) was obtained and characterized for the first time using powder X-ray diffraction, infrared spectroscopy, and thermal analysis. The solution enthalpy and time of dissolution in water were determined using solution calorimetry for this polymorph and compared with those of the dried commercial form of β-cyclodextrin (polymorph I), its amorphous form, and 2-hydroxypropyl-β-cyclodextrin. The specific heat capacities of polymorphs I and III were determined using differential scanning calorimetry across a wide range of temperatures, providing enthalpy and Gibbs energy values for the polymorphic transition at 298 K. The affinities of polymorph III and 2-hydroxypropyl-β-cyclodextrin for water were characterized by determining their hydration isotherms, which provided values of hydration Gibbs energy. Being energy-rich, the new-found polymorph of β-cyclodextrin has a significantly higher dissolution rate and an increased affinity for water compared with the dried commercial form of β-cyclodextrin. These properties render the new polymorph promising in industrial applications for guest inclusion in aqueous solutions and pastes, and may be a desirable alternative for water-soluble β-cyclodextrin derivatives.
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