Esophageal transit of risedronate cellulose-coated tablet and gelatin capsule formulations

Int J Pharm. 1999 Sep 20;186(2):169-75. doi: 10.1016/s0378-5173(99)00172-6.

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.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Aged, 80 and over
  • Calcium Channel Blockers / administration & dosage*
  • Calcium Channel Blockers / pharmacokinetics*
  • Capsules
  • Cellulose
  • Esophagus / metabolism*
  • Etidronic Acid / administration & dosage
  • Etidronic Acid / analogs & derivatives*
  • Etidronic Acid / pharmacokinetics
  • Excipients
  • Female
  • Gelatin
  • Humans
  • Image Processing, Computer-Assisted
  • Male
  • Middle Aged
  • Risedronic Acid
  • Tablets

Substances

  • Calcium Channel Blockers
  • Capsules
  • Excipients
  • Tablets
  • Gelatin
  • Cellulose
  • Risedronic Acid
  • Etidronic Acid