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Human pharmacokinetics and bioavailability of temazepam administered in soft gelatin capsules

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Summary

Plasma levels of temazepam were determined in healthy subjects after single oral administration of soft and hard gelatin capsules, and after 7 consecutive night-time doses in soft capsules. Absorption from soft gelatin capsules was significantly faster and produced earlier and higher peak plasma levels. The two pharmaceutical forms did not show any significant difference in relative availability. The apparent half-life of temazepam after night-time administration was significantly shorter than after morning administration, but no change in half-life was observed between the first and seventh night-time doses.

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References

  1. Belvedere, G., Tognoni, G., Frigerio, A., Morselli, P.: A specific rapid and sensitive method for gas chromatographic determination of methyl-oxazepam in small samples of blood. Analyt. Lett.5, 531–541 (1972)

    Google Scholar 

  2. Borland, R. G., Nicholson, A. N.: Comparison of the residual effects of two benzodiazepines (nitrazepam and flurazepam hydrochloride) and pentobarbitone sodium on human performance. Brit. J. clin. Pharmacol.2, 9–17 (1975)

    Google Scholar 

  3. Capaccio, A., Ambrosini, G., Veneri, F.: Valutazione controllata dell'attività di una nuova benzodiazepina, il temazepam, nelle sindromi ansiose ed ansioso-depressive di riscontro nella pratica tisiologica. Pneumologia9, 475–486 (1968)

    Google Scholar 

  4. Fargus, P. C. G., Hindmarch, I.: A 1,4 benzodiazepine, temazepam (ER 115): effect on reaction time during psychomotor behaviour related to car driving. IRCS Med. Sci.2, 1173 (1974)

    Google Scholar 

  5. Fuccella, L. M., Tosolini, G., Moro, E., Tamassia, V.: Study of physiological availability of temazepam in man. Int. J. clin. Pharmacol.64, 303–309 (1972)

    Google Scholar 

  6. Hindmarch, I.: Investigations of the behavioural effects of the benzodiazepines. Unpublished Research Seminar, Leeds (1974)

  7. Hindmarch, I.: A 1,4-benzodiazepine, temazepam (K 3917), its effect on some psychological parameters of sleep and behaviour. Arzneim. Forsch. (Drug Res.)25, 1836–1839 (1975)

    Google Scholar 

  8. Hindmarch, I.: A sub-chronic study of the subjective quality of sleep and psychological measures of performance on the morning following night time medication with temazepam. Arzneim. Forsch.26, 2113–2116 (1976)

    Google Scholar 

  9. Kaplan, S. A., de Silva, J. A. F., Jack, M. F., Alexander, K., Strojny, N., Weinfeld, R. E., Puglisi, C. V., Weissman, L.: Blood level profile in man following chronic oral administration of flurazepam hydrochloride. J. Pharm. Sci.62, 1932–1935 (1973)

    Google Scholar 

  10. Klotz, U., Antonin, K. H., Bieck, P. R.: Comparison of the pharmacokinetics of diazepam after single and subchronic doses. Europ. J. clin. Pharmacol.10, 121–126 (1976)

    Google Scholar 

  11. Linnoila, M., Saario, I., Maki, M.: Effect of treatment with diazepam or lithium and alcohol on psychomotor skills related to driving. Europ. J. clin. Pharmacol.7, 337–342 (1974)

    Google Scholar 

  12. Maccagnani, G., Ambrosini, G.: Sperimentazione clinica controllata di un nuovo derivato benzodiazepinico, il temazepam (ER 115) versus placebo, in terapia psichiatrica. Rass. Studi Psichiat.59, 33–58 (1970)

    Google Scholar 

  13. Maggini, C., Murri, L., Sacchetti, G.: Evaluation of the effectiveness of temazepam on the insomnia of patients with neurosis and endogenous depression. Arzneim. Forsch. (Drug Res.)19, 1647–1652 (1969)

    Google Scholar 

  14. Nicholson, A. N., Stone, B. M.: Effect of a metabolite of diazepam, 3-hydroxydiazepam (temazepam), on sleep in man. Brit. J. clin. Pharmacol.3, 543–550 (1976)

    Google Scholar 

  15. Nicholson, A. N., Stone, B. N., Clarke, C. H., Ferres, H. M.: Effect of N-desmethyldiazepam and a precursor, potassium chlorazepate, on sleep in man. Brit. J. clin. Pharmacol.3, 429–438 (1976)

    Google Scholar 

  16. Riccioni, R., Gallevi, M., Sacchetti, G., Castrogiovanni, P., Cassano, G. B.: Il temazepam: nuovo ansiolitico della serie 1–4 benzodiazepinica. Studio pilota nell'uomo. Neuropsichiatria34, 838–848 (1968)

    Google Scholar 

  17. Rieder, J., Gernot, W.: Pharmacokinetics and metabolism of the hypnotic nitrazepam. In “The Benzodiazepines” (ed. Garattini, S., Mussini, E. & Randall, L. O.), p. 99. New York: Raven Press 1973

    Google Scholar 

  18. Sarteschi, P., Cassano, G. B., Castrogiovanni, P., Placidi, G. F., Sacchetti, G.: Major and minor transquillizers in the treatment of anxiety states. Arzneim. Forsch. (Drug Res.)22, 93–97 (1972)

    Google Scholar 

  19. Tansella, M., Siciliani, O., Burti, L., Schiavon, M., Zimmermann Tansella, C. H., Gerna, M., Tognoni, G., Morselli, P. L.: N-desmethyldiazepam and amylobarbitone sodium as hypnotics in anxious patients. Plasma levels, clinical efficacy and residual effects. Psychopharmacologia (Berl.)41, 81–85 (1975)

    Google Scholar 

  20. Tansella, M., Zimmermann Tansella, C. H., Lader, M.: The residual effects of N-desmethyldiazepam in patients. Psychopharmacologia (Berl.)38, 81–90 (1974)

    Google Scholar 

  21. Tognoni, G., Gomeni, R., De Maio, D., Alberti, G. G., Franciosi, P., Scieghi, G.: Pharmacokinetics of N-desmethyldiazepam in patients suffering from insomnia and treated with nortriptyline. Brit. J. clin. Pharmacol.2, 227–232, 1975.

    Google Scholar 

  22. Wagner, J. G. Fundamental of clinical pharmacokinetics, p. 461. Hamilton, IL: Drug Intelligence Publications 1975

    Google Scholar 

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Fuccella, L.M., Bolcioni, G., Tamassia, V. et al. Human pharmacokinetics and bioavailability of temazepam administered in soft gelatin capsules. Eur J Clin Pharmacol 12, 383–386 (1977). https://doi.org/10.1007/BF00562455

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  • DOI: https://doi.org/10.1007/BF00562455

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