Abstract:
:The aim of the present study was to mask the bitterness of propiverine hydrochloride (P-4) by converting it to propiverine free base. Fine granules comprising the free base, which was converted from P-4 by desalination, were prepared. By using Fourier transform infrared spectroscopy, thermogravimetry-differential thermal analysis, and powder X-ray diffraction spectra, we confirmed that P-4 had been converted into propiverine free base by desalination during the manufacturing process. Furthermore, the conversion into free base appeared to result in decreased solubility, and both the taste testing sensor and tasting volunteers determined that it masked the bitterness of P-4. On using the gustatory sensation test, the bitterness of the P-4 fine granules was confirmed to be weakened. The dissolution rate and bioavailability of fine granules of the free base were compared with tablets of P-4. The dissolution rate and bioavailability of the fine granules and tablets were almost the same. We successfully masked the taste of P-4 by converting it into free base using a manufacturing process that was suitable for commercial manufacturing.
journal_name
Chem Pharm Bull (Tokyo)journal_title
Chemical & pharmaceutical bulletinauthors
Ogata T,Koide A,Kinoshita M,Ozeki Tdoi
10.1248/cpb.c12-00206subject
Has Abstractpub_date
2012-01-01 00:00:00pages
976-84issue
8eissn
0009-2363issn
1347-5223pii
DN/JST.JSTAGE/cpb/c12-00206journal_volume
60pub_type
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