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目的:比较两种国产卡马西平(Carbamazepine,CBZ)片(B,C)与北京CIBA-GEIGY产得理多(Tegretol)片(A)的人体相对生物利用度。方法:采用FPIA测定人血清CBZ浓度。12名健康志愿者口服300mgCBZ片,采用随机单盲同体交叉试验,进行B,C与A人体相对生物利用度研究。结果:B,C对A的相对生物利用度分别为(100.7±20.9)%,(110.2±23.1)%;A,B,C的Ka分别为(0.15±0.11),(5.3±6.6)和(8.0±15.3)h-1,达峰时间(Tmax)分别为(16.3±5.4),(3.4±3.8)和(2.3±1.9)h;消除半衰期(T1/2)分别为(42.0±9.9),(42.1±13.9)和(41.6±13.4)h;血药浓度曲线下面积(AUC0→∞)分别为(265.2±59.4),(265.6±82.3)和(286.1±73.6)mg.h.L-1。经统计学分析B,C与A的Tmax,Ka差异有极显著性(P<0.01),其余各参数差异均无显著性(P>0.05)。单次给药后,CBZ血药浓度-时间曲线出现双峰或多峰现象。结论:B,C生物等效,与A生物不等效
OBJECTIVE: To compare the relative bioavailability of Carbamazepine (CBZ) tablets (B, C) with Beijing CIBA-GEIGY Tegretol tablets (A). Methods: The serum concentration of CBZ was measured by FPIA. 12 healthy volunteers oral administration of 300mgCBZ tablets, using a single-blind randomized cross-crossover study of B, C and A relative bioavailability of the human body. Results: The relative bioavailabilities of B and C to A were (100.7 ± 20.9)% and (110.2 ± 23.1)%, respectively. The Ka of A, B and C were (0.15 ± 0.11), (5.3 ± 6.6) and (8.0 ± 15.3) h-1 respectively. The peak time (Tmax) were (16.3 ± 5.4) and ± 3.8 and 2.3 ± 1.9 h respectively; the elimination half-lives (T1 / 2) were (42.0 ± 9.9), (42.1 ± 13.9) and ± 13.4) h. The area under the plasma concentration curve (AUC0 → ∞) were (265.2 ± 59.4), (265.6 ± 82.3) and (286.1 ± 73.6) mg . h L-1. Statistical analysis of B, C and A Tmax, Ka significant difference (P <0.01), the remaining parameters were no significant difference (P> 0.05). After a single dose, the CBZ plasma concentration-time curve appears bimodal or multimodal phenomenon. Conclusion: B and C are bioequivalent and not equivalent to A organisms