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研究辊压茶碱及其二元混合物的可压缩性和可压实性参数。

Investigation of compressibility and compactibility parameters of roller compacted Theophylline and its binary mixtures.

机构信息

Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland.

出版信息

Int J Pharm. 2011 Sep 15;416(1):97-103. doi: 10.1016/j.ijpharm.2011.06.012. Epub 2011 Jun 15.

Abstract

Roller compaction is a dry granulation method which results in tablets with inferior tensile strength comparing to direct compaction. The effect of roller compaction on compressibility and compactibility of tablets prepared from Theophylline anhydrate powder, Theophylline anhydrate fine powder and Theophylline monohydrate was investigated by measuring tensile strength of tablets as well as calculating compressibility and compactibility parameters by Leuenberger equation. The tablets under the same conditions were prepared by direct compaction and roller compaction. The binary mixtures of Theophylline anhydrate powder, Theophylline anhydrate fine powder, Theophylline monohydrate and microcrystalline cellulose were prepared in order to determine the optimal ratio of active material and excipients which delivers a sufficient mechanical strength of tablets. Tensile strength of MCC tablets and compactibility parameters calculated by Leuenberger equation after roller compaction was significantly decreased, while THAP, THAFP and THMO tablets showed only a minor reduction in compactibility and compressibility. Adding MCC to a mixture with Theophylline showed that the right choice and ratio of excipients can enable a sufficient mechanical strength of the tablets after roller compaction.

摘要

辊压是一种干法造粒方法,其制成的片剂的拉伸强度比直接压片差。通过测量片剂的拉伸强度,并通过 Leuenberger 方程计算可压缩性和可压实性参数,研究了辊压对茶碱无水物粉末、茶碱细粉和一水茶碱片剂的可压缩性和可压实性的影响。在相同条件下,通过直接压片和辊压制备片剂。制备了茶碱无水物粉末、茶碱细粉、一水茶碱和微晶纤维素的二元混合物,以确定提供片剂足够机械强度的活性物质和赋形剂的最佳比例。辊压后 MCC 片剂的拉伸强度和 Leuenberger 方程计算的可压实性参数显著降低,而 THAP、THAFP 和 THMO 片剂的可压实性和可压缩性仅略有降低。向茶碱混合物中添加 MCC 表明,正确选择和赋形剂比例可以使辊压后片剂具有足够的机械强度。

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