Miskolczi P, Vereczkey L, Frenkl R
Chemical Works of Gedeon Richter Ltd., Department of Pharmacokinetics and Drug Metabolism, Budapest, Hungary.
J Pharm Biomed Anal. 1987;5(7):695-700. doi: 10.1016/0731-7085(87)80082-1.
A new capillary GLC method for the determination of tolperisone in human plasma was developed. Pharmacokinetic and comparative bioavailability studies were carried out after i.v. administration and after oral administration of two different preparations of tolperisone. After i.v. administration of the drug the elimination half-life was found to be 1.55 +/- 0.7 h (mean +/- S.D.), the apparent volume of distribution to be 5.1 +/- 1.0 l/kg (mean +/- S.D.) and total body clearance to be 140.8 +/- 33.8 l/h (mean +/- S.D.). The oral bioavailability was found to be 22.3 +/- 6.3% for Mydeton tablets and 16.7 +/- 8.9% for Mydocalm tablets. There was no significant difference between the bioavailability of two oral tablets.
建立了一种测定人血浆中托哌酮的新型毛细管气相色谱法。在静脉注射和口服两种不同制剂的托哌酮后进行了药代动力学和比较生物利用度研究。静脉注射该药物后,消除半衰期为1.55±0.7小时(平均值±标准差),表观分布容积为5.1±1.0升/千克(平均值±标准差),全身清除率为140.8±33.8升/小时(平均值±标准差)。发现米多君片的口服生物利用度为22.3±6.3%,米多卡因片为16.7±8.9%。两种口服片剂的生物利用度之间无显著差异。