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| In this article, we established a rapid and feasible gas chromatography method for the detection of tilidine and its active metabolite nortilidine in human plasma, and investigated the pharmacokinetics of tilidine in Chinese healthy subjects. The drug concentration of plasma sample from the 9 volunteers was determined by GC method and ketamine was used as internal standard. The method has been validated over a liner range from 2.5 to 160 ng/ml for tilidine, and from 5 to 160 ng/ml for nortilidine. After validation, the method was used to study the pharmacokinetic profile of tilidine and its active metabolite nortilidine in 9 Chinese healthy volunteers following administration of a single oral dose 50mg tilidine hydrochloride oral solution, the main pharmacokinetics data (mean±SD) for tilidine and nortilidine were Cmax 63.39±28.99 and 122.53±23.23 ng/ml; Tmax 0.37±0.07 and 0.64±0.30 h; t1/2 2.83±135 and 5.72±1.37 h; AUC0-∞101.59±41.85 and 577.13±189.77 ng•h•ml-1, respectively. The method is simple, sensitive, accurate and can be used for pharmacokinetics studies of tilidine and its active metabolite nortilidine. |
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| Keywords:tilidine;nortilidine;GC-NPD;clinical pharmacokinetics |
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