title: Design and evaluation of an economic taste-masked dispersible tablet of pyridostigmine bromide, a highly soluble drug with an extremely bitter taste.
abstract: Pyridostigmine bromide (PTB) is a highly soluble and extremely bitter drug. Here, an economic complexation technology combined with direct tablet compression method has been developed to meet the requirements of a patient friendly dosage known as taste-masked dispersible tablets loaded PTB (TPDPTs): (1) TPDPTs should have optimal disintegration and good physical resistance (hardness); (2) a low-cost, simple but practical preparation method suitable for industrial production is preferred from a cost perspective. Physicochemical properties of the inclusion complex of PTB with beta-cyclodextrin were investigated by Fourier transformed infrared spectroscopy, differential scanning calorimetry and UV spectroscopy. An orthogonal design was chosen to properly formulate TPDPTs. All volunteers regarded acceptable bitterness of TPDPTs. The properties including disintegration time, weight variation, friability, hardness, dispersible uniformity and drug content of TPDPTs were evaluated. The dissolution profile of TPDPTs in distilled water exhibited a fast rate. Pharmacokinetic results demonstrated that TPDPTs and the commercial tablets were bioequivalent.
authors.affiliation: Department of Thoracic Surgery, Institute of Surgery Research, Daping Hospital, Third Military Medical University, 1–1–20 Shinmachi, Nishi-Tokyo 202–8585, Japan. motsuka@musashino-u.ac.jp
authors.forename: Qunyou
authors.initials: Q
authors.lastname: Tan
authors.forename: Li
authors.initials: L
authors.lastname: Zhang
authors.forename: Liangke
authors.initials: L
authors.lastname: Zhang
authors.forename: Yongzhen
authors.initials: Y
authors.lastname: Teng
authors.forename: Jingqing
authors.initials: J
authors.lastname: Zhang
mesh_terms: D015195:Drug Design; D005260:Female; D006801:Humans; D008297:Male; D015394:Molecular Structure; D011729:Pyridostigmine Bromide / Q000008:administration & dosage / Q000737:chemistry / Q000191:economics*; D012016:Reference Values; D012995:Solubility; D013607:Tablets / Q000008:administration & dosage / Q000737:chemistry / Q000191:economics*; D013649:Taste; D055697:Taste Perception; D047392:beta-Cyclodextrins / Q000737:chemistry
chemical_list: D013607:Tablets; D047392:beta-Cyclodextrins; C031215:betadex; D011729:Pyridostigmine Bromide