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Pharmacy World and Science

, Volume 18, Issue 3, pp 114–119 | Cite as

Pharmacokinetic aspects of rectal formulations of Temazepam

  • L. M. Hanff
  • W. J. Rutten
Articles

Abstract

An in vitro/in vivo study was carried out with different rectal formulations of temazepam. Pharmacokinetic data were determined in a cross-over study in 10 volunteers after rectal administration of 10 mg temazepam as a polyethylene glycol based suppository (selected from in vitro data), a liquid-filled capsule and a micro-enema respectively, using oral administration of a liquid-filled capsule as a reference. Serum levels of temazepam indicate an instantaneous and complete release from the micro-enema (Frel=0.94±0.21, Cmax 205±36.9 μg/l, tmax 0.49±0.31 hour) and a slower but complete release of temazepam from the suppository (Frel=1.01±0.25, Cmax 202±41.3 μg/l, tmax 1.48±0.41 hour). A high interindividual variation in absorption profiles was observed after rectal administration of the liquid-filled capsule (Frel 0.72±0.36, Cmax 182±122 μg/l, tmax 4.08±4.28 hour), which makes it less suitable for rectal use. The micro-enema and suppository appear to be useful as rectal formulations for temazepam.

Keywords

Temazepam Rectal administration Suppository Capsule Enema Pharmacokinetic 

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Copyright information

© Kluwer Academic Publishers 1996

Authors and Affiliations

  • L. M. Hanff
    • 1
  • W. J. Rutten
    • 2
  1. 1.Department of PharmacyUniversity Hospital RotterdamRotterdamthe Netherlands
  2. 2.Department of Clinical PharmacyMedisch Spectrum TwenteEnschedethe Netherlands

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