title: Esophageal transit of risedronate cellulose-coated tablet and gelatin capsule formulations.
abstract: Risedronate sodium is an orally active antiresorptive agent and a member of the pyridinyl class of bisphosphonates. It has been approved for the treatment of Paget's disease of the bone and is under development as a chronic therapy for the treatment and prevention of osteoporosis. A novel cellulose film-coated tablet formulation was developed to optimize esophageal transit of this bisphosphonate. The aim of the present study was to compare the esophageal transit of the film-coated tablet formulation of risedronate with its original gelatin capsule dose form. A total of 25 elderly, healthy volunteers (mean 66 years), who were dysphagia-free, participated in this randomized cross-over study. On separate occasions, volunteers swallowed radiolabeled placebo formulations with 50 ml water. Dynamic images with participants in a sitting position were recorded for 10 min using a gamma camera. Scintigraphic imaging showed a delay in esophageal transit (greater than 15 s) in 28% of patients in the capsule group but in none of the tablet group (P<0.05). The mean transit times of the capsules and tablets were 23.8 and 3.3 s, respectively. Esophageal transit of film-coated tablets was faster than gelatin capsules, suggesting that film-coated tablets would be the appropriate formulation for all pivotal trials with risedronate and for subsequent commercialization.
authors.affiliation: Departments of Medical Physics and Therapeutics, Queen's Medical Centre, University Hospital, Nottingham, UK.
authors.forename: A C
authors.initials: AC
authors.lastname: Perkins
authors.forename: C G
authors.initials: CG
authors.lastname: Wilson
authors.forename: M
authors.initials: M
authors.lastname: Frier
authors.forename: R M
authors.initials: RM
authors.lastname: Vincent
authors.forename: P E
authors.initials: PE
authors.lastname: Blackshaw
authors.forename: R J
authors.initials: RJ
authors.lastname: Dansereau
authors.forename: K D
authors.initials: KD
authors.lastname: Juhlin
authors.forename: P J
authors.initials: PJ
authors.lastname: Bekker
authors.forename: R C
authors.initials: RC
authors.lastname: Spiller
mesh_terms: D000368:Aged; D000369:Aged, 80 and over; D002121:Calcium Channel Blockers / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D002214:Capsules; D002482:Cellulose; D004947:Esophagus / Q000378:metabolism*; D012968:Etidronic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D005079:Excipients; D005260:Female; D005780:Gelatin; D006801:Humans; D007091:Image Processing, Computer-Assisted; D008297:Male; D008875:Middle Aged; D000068296:Risedronic Acid; D013607:Tablets
chemical_list: D002121:Calcium Channel Blockers; D002214:Capsules; D005079:Excipients; D013607:Tablets; D005780:Gelatin; D002482:Cellulose; D000068296:Risedronic Acid; D012968:Etidronic Acid