Abstract
The effect of mechanical grinding on the physicochemical properties of acetaminophen in the presence of three additives,α- orβ-cyclodextrin and microcrystalline cellulose, was studied by using TLC, powder X-ray diffraction analysis, infrared spectroscopy and differential scanning calorimetry. The results indicate that the crystallinity of physical mixtures of acetaminophen and the described additives decreased with increased grinding time and formed an amorphous state when mixtures containingα- orβ-cyclodextrin were ground with acetaminophen. We also found that the acetaminophen molecules could be included step-by-step into the cavity ofβ-cyclodextrin molecules and formed an amorphous inclusion complex.α-Cyclodextrin and microcrystalline cellulose did not form an inclusion complex with acetaminophen, but acted only to decrease the crystallinity of the ground mixtures. The mechanical grinding efficiency for acetaminophen was improved in the order ofβ-cyclodextrin ≫α-cyclodextrin > microcrystalline cellulose.
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This paper is part XI of ‘Drug Interaction in Pharmaceutical Formulations.
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Lin, SY., Lee, CS. The effect of mechanical grinding on the formation and crystallinity changes of the inclusion complex of acetaminophen andβ-cyclodextrin. J Incl Phenom Macrocycl Chem 7, 477–485 (1989). https://doi.org/10.1007/BF01080458
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DOI: https://doi.org/10.1007/BF01080458