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以冻干法与相转化法制备的细菌纤维素为稀释剂,采用湿法制粒制备对乙酰氨基酚片的性质比较

Comparison of Properties of Acetaminophen Tablets Prepared by Wet Granulation Using Freeze-Dried Versus Phase-Inversion Bacterial Cellulose as Diluent.

作者信息

Kaewpradit Sirikanya, Chingunpitak Jiraporn, Samhadthai Wannaphorn, Suppawattana Thanyanit, Jantarat Chutima

机构信息

Drug and Cosmetics Excellence Center, Walailak University, Thasala, Nakhon Si Thammarat, 80160, Thailand.

School of Pharmacy, Walailak University, Thasala, Nakhon Si Thammarat, 80160, Thailand.

出版信息

AAPS PharmSciTech. 2024 Feb 8;25(2):32. doi: 10.1208/s12249-024-02752-7.

Abstract

Bacterial cellulose (BC) is an interesting material for drug delivery applications due to its high purity. This study aimed to compare the properties of tablets prepared by the wet granulation method using bacterial cellulose prepared by different methods as a diluent, using acetaminophen as a model drug. BC used as diluents were prepared using two different methods: freeze-drying (BC-FD) and phase-inversion (BC-PI), and their characteristics were analyzed and compared with that of commercial microcrystalline cellulose PH 101 (Comprecel® M101). Acetaminophen tablets were prepared by wet granulation using BC-FD, BC-PI, or Comprecel® M101 as diluents, and their tablet properties were examined. The result showed that the morphology, polymorph, and crystallinity of BC-PI and Comprecel® M101 were similar but they were different compared with that of BC-FD. Tablets could be successfully formed using BC-PI and Comprecel® M101 as diluents without any physical defects but the tablet prepared using BC-FD as diluent appeared chipped edge. The characteristics (thickness, weight variation, hardness, friability, disintegration, drug content, and dissolution) of the tablets prepared using BC-PI diluent were also similar to those prepared using Comprecel® M101 diluent, but those of BC-FD diluent were inferior. This indicates that BC prepared in BC-PI can potentially be used as a diluent for tablets prepared by wet granulation.

摘要

细菌纤维素(BC)因其高纯度而成为药物递送应用中一种有趣的材料。本研究旨在比较以不同方法制备的细菌纤维素作为稀释剂,采用湿法制粒工艺制备的片剂的性能,以对乙酰氨基酚作为模型药物。用作稀释剂的BC采用两种不同方法制备:冷冻干燥(BC-FD)和相转化(BC-PI),并对其特性进行分析,与市售微晶纤维素PH 101(Comprecel® M101)进行比较。以BC-FD、BC-PI或Comprecel® M101作为稀释剂,通过湿法制粒制备对乙酰氨基酚片剂,并对其片剂性能进行考察。结果表明,BC-PI和Comprecel® M101的形态、多晶型和结晶度相似,但与BC-FD相比有所不同。以BC-PI和Comprecel® M101作为稀释剂可成功制得片剂,无任何物理缺陷,但以BC-FD作为稀释剂制备的片剂出现边缘破损。以BC-PI作为稀释剂制备的片剂的特性(厚度、重量差异、硬度、脆碎度、崩解度、药物含量和溶出度)也与以Comprecel® M101作为稀释剂制备的片剂相似,但以BC-FD作为稀释剂的片剂性能较差。这表明通过BC-PI制备的BC有潜力用作湿法制粒制备片剂的稀释剂。

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