Acute pharmacokinetic and pharmacodynamic comparison of two different formulations of temazepam. 1985

M J Mattila, and M Mattila, and P Tuomainen

Twelve healthy subjects ingested temazepam 20 mg in two different formulations (soft gelatine capsule or uncoated tablet) and matched placebo at one-week intervals in double-blind and cross-over conditions. Venous blood was sampled before the drug intake and 0.5, 1, 2, 3, 8, 12, and 24 hours after it, and plasma temazepam concentrations were assayed by gas chromatography. Psychomotor performance was measured objectively (digit symbol substitution, letter cancellation, Maddox wing) and subjectively (visual analogue scales) before the drug intake and 1, 2, and 3 hours after it. Peak concentrations of plasma temazepam were reached at about one hour, and they were higher after the capsule than after the tablet (mean values 750 vs. 587 ng/ml), while the computed AUCs and elimination half-lives (6-22 hours) proved to be similar after either formulation. Impaired performance was measured in objective tests over the first three hours, the capsule being somewhat more effective than the tablet. Self-assessments indicating subjective sedation returned to the placebo level within 3 hours after the capsule but not after the tablet. This rapid subjective recovery after the capsule might result from an acute tolerance developed after the high peak, and it tallies with the lack of residual sedation previously reported in trials with temazepam 20 mg given in soft gelatine capsules.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D002214 Capsules Hard or soft soluble containers used for the oral administration of medicine. Capsule,Microcapsule,Microcapsules
D004311 Double-Blind Method A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment. Double-Masked Study,Double-Blind Study,Double-Masked Method,Double Blind Method,Double Blind Study,Double Masked Method,Double Masked Study,Double-Blind Methods,Double-Blind Studies,Double-Masked Methods,Double-Masked Studies,Method, Double-Blind,Method, Double-Masked,Methods, Double-Blind,Methods, Double-Masked,Studies, Double-Blind,Studies, Double-Masked,Study, Double-Blind,Study, Double-Masked
D005260 Female Females
D005780 Gelatin A product formed from skin, white connective tissue, or bone COLLAGEN. It is used as a protein food adjuvant, plasma substitute, hemostatic, suspending agent in pharmaceutical preparations, and in the manufacturing of capsules and suppositories. Gelafusal
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D013607 Tablets Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed) Tablet

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