Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Preparation and Evaluation of Tablets Rapidly Disintegrating in Salive Containing Bitter-Taste-Masked Granules by the Compression Method
Tatsuya ISHIKAWAYoshiteru WATANABENaoki UTOGUCHIMitsuo MATSUMOTO
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1999 Volume 47 Issue 10 Pages 1451-1454

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Abstract

The aim of this study was to prepare, using taste-masked granules, tablets which can rapidly disintegrate in saliva (rapidly disintegrating tablet), of drugs with bitter taste (pirenzepine HCl or oxybutynin HCl). The taste-masked granules were prepared using aminoalkyl methacrylate copolymers (Eudragit E-100[○!R]) by the extrusion method. None of the drugs dissolved from the granules (% of dissolved, <5%) even at 480 min at pH 6.8 in the dissolution test. However, the drugs dissolved rapidly in the medium at pH 1.2 in the dissolution test. Rapidly disintegrating tablets were prepared using the prepared taste-masked granules, and a mixture of excipients consisting of crystalline cellulose (Avicel PH-102[○!R]) and low-substituted hydroxypropylcellulose (L-HPC, LH-11[○!R]). The granules and excipients were mixed well (mixing ratio by weight, crystalline cellulose : L-HPC=8 : 2) with 1% magnesium stearate, and subsequently compressed at 500-1500 kgf in a single-punch tableting machine. The prepared tablets (compressed at 500 kgf) containing the taste-masked granules have sufficient strength (the crusing strength : oxybutynin tablet, 3.5 kg; pirenzepine tablet, 2.2 kg), and a rapid disintegration time (within 20 s) was observed in the saliva of healthy volunteers. None of the volunteers felt any bitter taste after the disintegration of the tablet which contained the taste-masked granules. We confirmed that the rapidly disintegrating tablets can be prepared using these taste-masked granules and excipients which are commonly used in tablet preparation.

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