头孢地尼颗粒剂与胶囊的人体生物等效性

Bioequivalence of cefdinir granule and capsule in healthy volunteers

目的 本试验旨在对头孢地尼颗粒剂和胶囊进行生物等效性研究 ,为头孢地尼颗粒剂 (50mg/0 .5g)的临床应用提供参考依据。方法 2 4名健康志愿者分别随机交叉口服 1 0 0mg颗粒剂 (50mg/0 .5g× 2 )和对照药头孢地尼胶囊 (1 0 0mg/粒× 1 ) ,用微生物法测定血清中头孢地尼浓度。结果 头孢地尼颗粒剂和参比药头孢地尼胶囊剂的达峰时间Tmax分别为 (2 771± 0 579)、(3 2 50± 0 60 0 )h ;峰浓度Cmax分别为 (0 875± 0 1 91 )、(0 832± 0 1 70 )mg/L ;消除半衰期T1 /2 分别为 (1 967± 0 42 8)、(1 957± 0 60 3)h ;药时曲线下面积AUC0～∞ 分别为 (3 360± 0 0 952 )、(3 381± 0 80 8)h·mg/L。两种制剂的主要药物动力学参数AUC及Cmax经双单侧检验无显著性差异 (P >0 0 5)。结论 头孢地尼颗粒剂的相对生物利用度为 (99 2 9±1 5 52 ) %,说明两种制剂为生物等效制剂。

The relative bioavailability of cefdinir granule were studied in 24 Chinese healthy volunteers after a single oral dose (100mg) compared with cefdinir capsule. In this paper, Providencia stuartii CMCC(B)42066 3 as test strain, plasma cefdinir concentration was determined by microbiological assay. The concentration time curves of cefdinir fitted to two compartment model estimated by 3p87 program. The main pharmacokinetic parameters of the two preparations, granule and capsule were as follows: T max (2.771±0 589), (3 250±0 608)h, C max were (0.875 ±0.191), (0.832±0.170)mg/L; T 1/2 were (1.967±0.428), (1.957±0 603)h; AUC 0～t were (3.360±0.952), (3.381±0.808)h·mg/L, respectively. There was statisitical significant difference between T max of two formulations, but AUC and C max showed no significant difference ( P >0 05). The relative bioavailability of cefdinir granule was (99.29±15.52)%. Results demonstrated that two formulations of cefdinir were bioequivalent.