Literature DB >> 8161719

Single-dose bioavailability of oral and intramuscular thiocolchicoside in healthy volunteers.

P Sandouk1, M Bouvier d'Yvoire, P Chretien, J P Tillement, J M Scherrmann.   

Abstract

A single dose of 8 mg of thiocolchicoside was administered to 12 healthy volunteers according to a Latin square design, either as tablets (reference), oral solution, or intramuscular injection. Serum thiocolchicoside concentrations showed an absorption phase followed by a biexponential decay with a terminal half-life (t1/2 beta) of approximately 5 h, similar for the three formulations. The relative bioavailability of both oral formulations was approximately 25%, compared to the intramuscular formulation. There was a trend for the oral solution to have a slightly larger AUC and Cmax, as well as a slightly shorter Tmax, than the tablet formulation. However, the comparison of the two oral forms did not show statistically significant differences in the pharmacokinetic parameters Cmax, Tmax, and AUC, suggesting that the Coltramyl tablets have an adequate in vivo dissolution profile.

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Year:  1994        PMID: 8161719     DOI: 10.1002/bdd.2510150108

Source DB:  PubMed          Journal:  Biopharm Drug Dispos        ISSN: 0142-2782            Impact factor:   1.627


  3 in total

1.  Thiocolchicoside exhibits anticancer effects through downregulation of NF-κB pathway and its regulated gene products linked to inflammation and cancer.

Authors:  Simone Reuter; Sahdeo Prasad; Kanokkarn Phromnoi; Jayaraj Ravindran; Bokyung Sung; Vivek R Yadav; Ramaswamy Kannappan; Madan M Chaturvedi; Bharat B Aggarwal
Journal:  Cancer Prev Res (Phila)       Date:  2010-10-26

2.  Comparative bioavailability and tolerability study of two intramuscular formulations of thiocolchicoside in healthy volunteers.

Authors:  M P Ferrari; G Gatti; C Fattore; G Fedele; R Novellini
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2001 Oct-Dec       Impact factor: 2.441

3.  Comparative pharmacokinetics and bioavailability of two oral formulations of thiocolchicoside, a GABA-mimetic muscle relaxant drug, in normal volunteers.

Authors:  E Perucca; P Poitou; G Pifferi
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1995 Oct-Dec       Impact factor: 2.441

  3 in total

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