Cui H D, Jiang W D, Zhu X X, Guo Y, Karras H O
Institute of Clinical Pharmacology, Shanghai Medical University, China.
Zhongguo Yao Li Xue Bao. 1993 May;14(3):193-7.
Pharmacokinetic characteristics and relative bioavailability of the regular preparation (RG) and micronized preparation (MG) of glibenclamide (Gli) were studied in 4 Chinese healthy men. Each volunteer entered 2 consecutive experiments at the same dose (10.5 mg) of RG and MG tablets given orally. Blood samples were drawn before and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 h after po. A selective HPLC method with a uv spectrophotometric detector (sensitivity: 16 ng.ml-1) was established for determining serum Gli concentration. Cmax for RG was 212 +/- 41 ng.ml-1, for MG 529 +/- 73 ng.ml-1. Tmax for RG and MG were 3.5 +/- 0.6 and 2.2 +/- 0.3 h, respectively. The relative oral bioavailability of MG was found to be 77%, increased approximately 1.7-fold that of RG. The other pharmacokinetic parameters (Vd, Cl, T1/2) were substantially the same after ingestion of GR and MG.
对4名中国健康男性进行了格列本脲（Gli）常规制剂（RG）和微粉化制剂（MG）的药代动力学特征及相对生物利用度研究。每位志愿者以相同剂量（10.5mg）口服RG和MG片剂，连续进行2次实验。口服给药前及给药后0.5、1、2、3、4、6、8、10和12小时采集血样。建立了一种采用紫外分光光度检测器的选择性高效液相色谱法（灵敏度：16ng.ml-1）测定血清Gli浓度。RG的Cmax为212±41ng.ml-1，MG的Cmax为529±73ng.ml-1。RG和MG的Tmax分别为3.5±0.6小时和2.2±0.3小时。发现MG的相对口服生物利用度为77%，约为RG的1.7倍。摄入GR和MG后，其他药代动力学参数（Vd、Cl、T1/2）基本相同。
