Title |
Comparative pharmacokinetics and bioavailability of two oral formulations of thiocolchicoside, a GABA-mimetic muscle relaxant drug, in normal volunteers
|
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Published in |
European Journal of Drug Metabolism and Pharmacokinetics, December 1995
|
DOI | 10.1007/bf03190249 |
Pubmed ID | |
Authors |
E. Perucca, P. Poitou, G. Pifferi |
Abstract |
The comparative pharmacokinetic and bioavailability profile of two different formulations (tablets and capsules) of thiocolchicoside was investigated in 8 healthy male volunteers after administration of single oral 8 mg doses. Plasma samples were assayed by a capillary gas chromatography--mass spectrometry (GC-MS) method following enzymatic hydrolysis of thiocolchicoside to its aglycone (3-demethylthiocolchicine) and no attempt was made to account for the possible occurrence of hydrolysis in vivo. Irrespective of the formulation used, the drug was rapidly absorbed from the gastrointestinal tract, peak levels of about 17 ng/ml being detected within 1 h in most subjects. Elimination was rapid, with mean MRT values of 5-6 h. All kinetic parameters showed considerable interindividual variability but none differed significantly between the two formulations. Relative to the tablet formulation, the oral bioavailability of the capsule formulation was 1.06 +/- 0.39. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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Unknown | 10 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
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Researcher | 2 | 20% |
Lecturer > Senior Lecturer | 1 | 10% |
Other | 1 | 10% |
Student > Ph. D. Student | 1 | 10% |
Student > Doctoral Student | 1 | 10% |
Other | 2 | 20% |
Unknown | 2 | 20% |
Readers by discipline | Count | As % |
---|---|---|
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Pharmacology, Toxicology and Pharmaceutical Science | 1 | 10% |
Chemistry | 1 | 10% |
Biochemistry, Genetics and Molecular Biology | 1 | 10% |
Unknown | 4 | 40% |