Pharmacokinetics and bioequivalence of trimebutine dispersive tablet in healthy subjects / 药学学报
Acta Pharmaceutica Sinica
;
(12): 208-211, 2004.
Artigo
em Chinês
| WPRIM
| ID: wpr-301113
ABSTRACT
<p><b>AIM</b>To develop an HPLC-ESI-MS assay for determination of trimebutine in human plasma and to investigate the pharmacokinetics and bioequivalence of two trimebutine tablets in human.</p><p><b>METHODS</b>After being made alkaline with saturated sodium bicarbonate, plasma was extracted by cyclohexane and separated by HPLC on a reversed-phase C18 column with a mobile phase of 10 mmol x L(-1) ammonium acetate buffer solution (pH 3.5)-methanol (1882). HPLC-ESI-MS was performed in the selected ion monitoring (SIM) mode using target ions at m/z 388 for trimebutine and m/z 280 for the internal standard (sibutramine, IS). The fragmentor voltage was 50 V. A randomized cross-over design was performed in 20 healthy volunteers. In the two study periods, a single 100 mg dose of each tablet was administered to each volunteer.</p><p><b>RESULTS</b>Calibration curve was linear over the range of 0.3 - 150 microg x L(-1). The main pharmacokinetic parameters of T1/2, Tmax and Cmax were (9.2 +/- 2.8) h, (1.0 +/- 0.3) h and (40 +/- 20) microg x L(-1) for the reference tablet; (9.2 +/- 2.3) h, (0.9 +/- 0.4) h and (41 +/- 20) microg x L(-1) for the test tablet. The relative bioavalability of the test tablet was (97 +/- 13)%. The results of variance analysis and two one-sided t-test showed that there was no significant difference between the two formulations in the AUC and Cmax.</p><p><b>CONCLUSION</b>The assay was proved to be sensitive, accurate and convenient. The two formulations were bioequivalent.</p>
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Comprimidos
/
Trimebutina
/
Fármacos Gastrointestinais
/
Farmacocinética
/
Equivalência Terapêutica
/
Cromatografia Líquida de Alta Pressão
/
Área Sob a Curva
/
Espectrometria de Massas por Ionização por Electrospray
Tipo de estudo:
Ensaio Clínico Controlado
/
Estudo prognóstico
Limite:
Adulto
/
Humanos
/
Masculino
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2004
Tipo de documento:
Artigo
Similares
MEDLINE
...
LILACS
LIS