title: Taste masking of propiverine hydrochloride by conversion to its free base.
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.
authors.affiliation: Formulation Research Laboratory, Tokushima Research Center, Taiho Pharmaceutical Co., Ltd., 224-2 Hiraishi-ebisuno, Kawauchi-cho, Tokushima 771-0194, Japan. tetsu-ogata@taiho.co.jp
authors.forename: Tetsuo
authors.initials: T
authors.lastname: Ogata
authors.forename: Atsuo
authors.initials: A
authors.lastname: Koide
authors.forename: Masahiro
authors.initials: M
authors.lastname: Kinoshita
authors.forename: Tetsuya
authors.initials: T
authors.lastname: Ozeki
mesh_terms: D000818:Animals; D001561:Benzilates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D001682:Biological Availability; D018680:Cholinergic Antagonists / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D004285:Dogs; D008855:Microscopy, Electron, Scanning; D033362:Powder Diffraction; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013649:Taste / Q000187:drug effects*; D013818:Thermogravimetry
chemical_list: D001561:Benzilates; D018680:Cholinergic Antagonists; C015586:propiverine