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热熔挤出法改善提取物中虎杖苷的理化性质:一种适用于口腔给药的解决方案

Hot Melt Extrusion for Improving the Physicochemical Properties of Polydatin Derived from Extract; A Solution Recommended for Buccal Applications.

作者信息

Paczkowska-Walendowska Magdalena, Tajber Lidia, Miklaszewski Andrzej, Cielecka-Piontek Judyta

机构信息

Department of Pharmacognosy and Biomaterials, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznan, Poland.

School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, University of Dublin, D02 PN40 Dublin, Ireland.

出版信息

Pharmaceuticals (Basel). 2023 Aug 30;16(9):1226. doi: 10.3390/ph16091226.

Abstract

Three different types of solid dispersions based on polyvinyl polymers and related copolymers (Kollidon VA64, Soluplus and Kollicoat IR) comprising polydatin-rich extract were prepared by hot melt extrusion. The systems were characterized using X-ray powder diffraction, infrared spectroscopy as well as by polydatin release and in vitro permeability. Mucoadhesive tablets were prepared from the extrudates based on Kollidon VA64 and Soluplus to obtain a suitable pharmaceutical form, where (hydroxypropyl)methyl cellulose was added as a mucoadhesive agent. The tablets were evaluated in terms of the kinetics of polydatin release as well as their mucoadhesive properties. The best tabletability properties, polydatin release profile and adequate mucoadhesive properties were obtained by the formulation containing the Kollidon VA64-based extrudate, which makes it an excellent prototype for enhancing the release of poorly water-soluble compounds.

摘要

通过热熔挤出法制备了三种基于聚乙烯基聚合物及相关共聚物(聚乙烯吡咯烷酮VA64、固体分散体聚合物和肠溶型丙烯酸树脂IR)且包含富含虎杖苷提取物的不同类型固体分散体。采用X射线粉末衍射、红外光谱以及虎杖苷释放和体外渗透性对这些体系进行了表征。基于聚乙烯吡咯烷酮VA64和固体分散体聚合物的挤出物制备了粘膜粘附片,以获得合适的药物剂型,其中添加了(羟丙基)甲基纤维素作为粘膜粘附剂。对片剂进行了虎杖苷释放动力学及其粘膜粘附性能方面的评估。含有基于聚乙烯吡咯烷酮VA64挤出物的制剂具有最佳的可压性、虎杖苷释放曲线和足够的粘膜粘附性能,这使其成为增强难溶性化合物释放的优良原型。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f817/10535885/dd30b4545aad/pharmaceuticals-16-01226-g001.jpg

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