title: Bitterness evaluation of intact and crushed Vesicare orally disintegrating tablets using taste sensors.
abstract: OBJECTIVE
  Vesicare tablets, whose main component is solifenacin succinate, are known to be extremely bitter. The purpose of this study was to evaluate the effect of crushing on the bitterness of the Vesicare orally disintegrating tablets (ODTs).
  
  
  METHODS
  Vesicare ODTs and conventional Vesicare tablets (CTs) were crushed either heavily or lightly. The bitterness scores and release rates of sample solutions obtained 5, 10, 30, 60, 90 or 120 s after placing a crushed CT or ODT containing 5 mg solifenacin in 40 ml of water were predicted using two taste sensors (SA402B and a-ASTREE) and HPLC, respectively. The particle size and the surfaces of the crushed tablets were observed microscopically.
  
  
  RESULTS
  The predicted bitterness scores and the drug release rates of CTs were high, irrespective of the degree of crushing. The lightly crushed ODT was predicted to be less bitter than the heavily crushed ODT. In lightly crushed ODTs, spherical particles were observed, about 200 mm in diameter.
  
  
  CONCLUSIONS
  The degree of crushing was a critical factor in determining the expression of bitterness by crushed ODTs. When intact tablets of Vesicare must be crushed to adjust the dosage, it is strongly recommended that ODTs be crushed gently.
authors.affiliation: Department of Clinical Pharmaceutics, Mukogawa Women's University, Nishinomiya, Japan.
authors.forename: Tamami
authors.initials: T
authors.lastname: Haraguchi
authors.forename: Airi
authors.initials: A
authors.lastname: Miyazaki
authors.forename: Miyako
authors.initials: M
authors.lastname: Yoshida
authors.forename: Takahiro
authors.initials: T
authors.lastname: Uchida
mesh_terms: D000284:Administration, Oral; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D010316:Particle Size; D011812:Quinuclidines / Q000008:administration & dosage / Q000737:chemistry*; D000069464:Solifenacin Succinate; D013607:Tablets; D013649:Taste; D044005:Tetrahydroisoquinolines / Q000008:administration & dosage / Q000737:chemistry*; D013997:Time Factors; D064804:Urological Agents / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D011812:Quinuclidines; D013607:Tablets; D044005:Tetrahydroisoquinolines; D064804:Urological Agents; D000069464:Solifenacin Succinate