盐酸苯海拉明片在中国健康人体内的药动学研究

目的研究盐酸苯海拉明片在中国健康人体内的药动学。方法采用高效液相色谱-质谱法,以右美沙芬为内标,血样经液-液萃取后进样,电离源为ES+,选择性离子监测(SIR),苯海拉明及内标的M/Z分别为256.0、272.2。结果苯海拉明不受杂质干扰,线性范围浓度为3.33~200.00ng/ml;萃取回收率均大于90%,方法回收率均在80%~120%内,日内、日间精密度均小于15%。单次服用100mg盐酸苯海拉明片的AUC0~34为(770.37±251.64)(ng.h)/ml,AUC0~∞为(870.92±290.50)(ng.h)/ml,Cmax为(72.25±27.47)ng/ml,tmax为(2.99±0.91)h,t1/2为(9.89±2.04)h。结论盐酸苯海拉明片在中国健康人体中口服吸收快,消除较慢。

Pharmacokinetics of Diphenhydramine Hydrochloride Tablets in Healthy Chinese Volunteers

OBJECTIVE: To study the pharmacokinetics of diphenhydramine hydrochloride in healthy Chinese volunteers. METHODS :HPLC- MS was employed, and dextromethorphan was used as internal standard. Blood samples were injected after liquid-liquid extraction. The ionization source was ES+, and selected ion monitoring (SIR) was performed. M/Z of diphenhydramine and internal standard was 256.0 and 272.2, respectively. RESULTS: Determination of diphenhydramine was not interfered by material in plasma. The linear range was 3.33～200.00ng/ml. The extract recovery rate was more than 90%, and the method recovery rate was 80%～120%. The inter-day and intra-day RSD were less than 15.0%. The parameters of single dose of 100 mg of diphenhydramine were detected as follows: AUC0～34(770.37±251.64) (ng·h)/ml, AUC0～∞(870.92±290.50) (ng·h)/ml, Cmax(72.25±27.47)ng/ml, tmax(2.99±0.91) h , and t1/2 (9.89±2.04) h. CONCLUSION : Diphenhydramine hydrochloride taken orally was absorbed rapidly and eliminated slowly in healthy Chinese volunteers.