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COMPARATIVE PHARMACOKINETICS OF TEMAZEPAM GELTHIX AND LIQUID‐FILLED SOFT GELATIN CAPSULES
Author(s) -
Drake J.,
Freedman P. S.,
Hawkins B. C.,
Horth C. E.,
Launchbury A. P.,
WhateleySmith C.
Publication year - 1991
Publication title -
journal of clinical pharmacy and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.622
H-Index - 73
eISSN - 1365-2710
pISSN - 0269-4727
DOI - 10.1111/j.1365-2710.1991.tb00324.x
Subject(s) - pharmacokinetics , cmax , temazepam , bioequivalence , bioavailability , hypnotic , absorption (acoustics) , chemistry , pharmacology , chromatography , anesthesia , medicine , materials science , receptor , composite material , benzodiazepine
Summary An open, randomized, cross‐over study involving 24 healthy volunteers, shows that a novel formulation of temazepam (temazepam Gelthix, TG) in soft gelatin capsules designed to resist i.v. abuse has a similar pharmacokinetic (P‐K) profile to that of a liquid‐filled, reference formulation (TL) when administered as a single oral dose of 20 mg. The relative bioavailability of the two formulations assessed in terms of the area under the time versus plasma concentration profile (AUC), although statistically different ( P <0·05), is well within the acceptable 80–120% limits for bioequivalence. Although the mean C max for TG (616·6 ng/ml) is lower than for TL (707·9 ng/ml) and the median time to reach C max ( T max ) is 40 min (TG) vs. 30 min (TL), there is no significant difference between TG and TL either in their absorption constant (K a ) (0·123 vs. 0·138 min ‐1 respectively) or their distribution (α) (29·5 vs. 32·4 min) and elimination (β) (6·3 vs. 6·6 h) half‐lives ( t 1/2 ). Thus the essential P‐K characteristics for the use of temazepam as a hypnotic and premedicant, specifically a rapid rise followed by a prompt fall in blood levels, are conserved by the Gelthix formulation.