Butriptyline: Human pharmacokinetics and comparative bioavailability of conventional and sustained release formulations

✍ Scribed by Jean Bourgouin; Marc-Andre Gagnon; Robert Elie; Dushan Dvornik; Ramona Gonzalez; Michael Kraml

• Publisher: John Wiley and Sons
• Year: 1981
• Tongue: English
• Weight: 367 KB
• Volume: 2
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bdd.2510020204

✦ Synopsis

Abstract

The pharmacokinetics and relative bioavailability of butriptyline from conventional and a sustained release (SR) formulation have been studied in a panel of 14 volunteers. A single oral dose of 75 mg butriptyline hydrochloride was administered and a 2 × 2 latin square design was followed. Pharmacokinetic modelling has shown that the plasma butriptyline concentration/time profile is adequately described by a two‐compartment open model; good agreement was obtained for the model‐fitted and measured parameters. The SR formulation was shown to possess sustained release characteristics as evidenced by the increase in T~max~ for 2.6 to 7.5 h, the decrease in C~max~ from 46.5 to 20.3 ng ml^−1^, and a three‐fold increase in ‘half‐value duration’ (HVD). The changes have been achieved without any significant decrease in the relative bioavailability of the SR formulation. The half‐life of butriptyline in plasma was about 20 h and was not formulation dependant.