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环糊精与氢化可的松类皮质类固醇的包合物

Cyclodextrin Inclusion Complexes with Hydrocortisone-Type Corticosteroids.

作者信息

Kowalska Aleksandra, Szeleszczuk Łukasz

机构信息

Department of Organic and Physical Chemistry, Faculty of Pharmacy, Medical University of Warsaw, Banacha 1 Str., 02-093 Warsaw, Poland.

Doctoral School, Medical University of Warsaw, Żwirki i Wigury 81 Str., 02-093 Warsaw, Poland.

出版信息

Pharmaceutics. 2024 Dec 2;16(12):1544. doi: 10.3390/pharmaceutics16121544.

Abstract

The hydrocortisone-type corticosteroid (HTC) group includes valuable active pharmaceutical ingredients (APIs) such as hydrocortisone, hydrocortisone acetate, cortisone acetate, tixocortol pivalate, prednisolone, methylprednisolone, and prednisone. Unfortunately, those APIs are characterized by low solubility, which hampers their application and reduces their therapeutic efficacy. The low polarity of HTC molecules allows them to form inclusion complexes with various cyclodextrins (CDs); however, as shown in this review, the type of applied CDs has a major impact on the final properties of the formed complex. HTC-CD complexes have been routinely used for over 40 years to achieve various aims. Most frequently, CDs have been utilized as HTC solubilizers and absorption enhancers in pharmaceutical formulations, as well as for separation and analysis by chromatographic and electrophoretic methods. This article reviews the studies describing the synthesis as well as the biological, physiochemical, and structural properties of the inclusion complexes formed between HTC and various cyclodextrins.

摘要

氢化可的松类皮质类固醇(HTC)组包括氢化可的松、醋酸氢化可的松、醋酸可的松、特戊酸替可的松、泼尼松龙、甲泼尼龙和泼尼松等有价值的活性药物成分(API)。不幸的是,这些API的特点是溶解度低,这阻碍了它们的应用并降低了它们的治疗效果。HTC分子的低极性使它们能够与各种环糊精(CD)形成包合物;然而,如本综述所示,所应用的CD类型对形成的复合物的最终性质有重大影响。HTC-CD复合物已常规使用了40多年以实现各种目的。最常见的是,CD已被用作药物制剂中HTC的增溶剂和吸收促进剂,以及用于色谱和电泳方法的分离和分析。本文综述了描述HTC与各种环糊精形成的包合物的合成以及生物学、物理化学和结构性质的研究。

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