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本文研究了尿与血浆中卡马西平(Ⅰ)浓度之间的关系,并以此推测了利用尿液对(Ⅰ)进行用药监测的可行性。实验方法:6名健康男性志愿者,每人单剂口服(Ⅰ)400mg,于服药后216h 内广泛收集血和尿样,置-20℃保存。未结合的血浆药物浓度(C_F)经超滤后测定。血浆、尿中(Ⅰ)的浓度(C_P、C_u)以及超滤液中游离(Ⅰ)的浓度均采用微孔 HPLC 法测定。9名癫痫病人单用(Ⅰ)或合用其它抗癫痫药后,同法测定 C_P、C_u 及 C_F。结果:6名志愿者的平均 C_u-t 曲线与C_P-t 曲线成比例,平均 C_F-t 曲线与 C_u-t 曲线非常接近,表明尿中(Ⅰ)与血浆中未结合的(Ⅰ)之间能迅速达到平衡。实验过程中尿流速变化很大(0.5~1.5ml/min),但并不影响 C_u 值。志愿者的平均 C_u/C_P 比值随时
In this paper, the relationship between urinary and plasma concentrations of carbamazepine (I) was investigated and the feasibility of using (i) urine for drug monitoring was estimated. Experimental Methods: Six healthy male volunteers, each single oral (Ⅰ) 400mg, within 216h after taking a wide range of blood and urine samples collected, stored at -20 ℃. Unbound plasma drug concentration (C_F) was determined by ultrafiltration. Plasma, urine (Ⅰ) concentration (C_P, C_u) and ultrafiltrate free (Ⅰ) concentrations were determined by microporous HPLC method. Nine patients with epilepsy alone (Ⅰ) or combined with other antiepileptic drugs, the same method for the determination of C_P, C_u and C_F. RESULTS: The average C_u-t curve of six volunteers was proportional to the C_Pt curve and the mean C_F-t curve was very close to the C_u-t curve, indicating that the difference between urine (I) and unbound (I) in plasma Can quickly reach equilibrium. Urine flow velocity during the experiment varied greatly (0.5 ~ 1.5ml / min), but it did not affect the C_u value. Volunteers average C_u / C_P ratio at any time