Mosig Johanna, Kleinebudde Peter
Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University, Duesseldorf, 40225, Germany.
J Pharm Sci. 2015 Mar;104(3):1108-18. doi: 10.1002/jps.24321. Epub 2015 Jan 5.
The influence of lubrication and particle size on the reduced compactability after dry granulation was investigated. Powder cellulose, lactose, magnesium carbonate, and two types of microcrystalline cellulose were roll compacted, granulated, and sieved into particle fractions. Particle fractions were compressed into tablets using internal and external lubrication. Internal lubrication resulted in an overlubrication of the granule material compared with the powder material. This resulted in extraordinary high reduction of compactability after dry granulation for lubricant-sensitive materials. The granule size can cause differences in strength, whereby the degree of this effect was material dependent. The loss in strength with increasing compaction force was comparable for different particles sizes of one material, suggesting a change in material properties independently of the size. Granule hardening could be one reason as for higher compaction forces the integrity of the granule structure survived the compression step. The results demonstrated that granule lubrication mainly influence the degree of the reduced compactability after dry granulation and must be considered for the evaluation of mechanism for this phenomenon. Hardening of the material as well as size enlargement will cause the loss in strength after recompression, but the influence of both depends strongly on the material.
研究了润滑和粒径对干法制粒后可压性降低的影响。将粉末状纤维素、乳糖、碳酸镁和两种微晶纤维素进行滚压、制粒，并筛分成不同的颗粒级分。使用内加和外加润滑剂将颗粒级分压制成片剂。与粉末物料相比，内加润滑剂导致颗粒物料过度润滑。这使得对润滑剂敏感的物料在干法制粒后可压性大幅降低。颗粒大小会导致强度差异，且这种影响的程度取决于物料。对于一种物料的不同粒径，随着压制力增加强度的损失相当，这表明物料性质的变化与粒径无关。颗粒硬化可能是一个原因，因为对于较高的压制力，颗粒结构的完整性在压缩步骤中得以保留。结果表明，颗粒润滑主要影响干法制粒后可压性降低的程度，在评估此现象的机制时必须予以考虑。物料硬化以及粒径增大都会导致再次压制后强度损失，但两者的影响都强烈取决于物料。
