摘要
格列齐特（Ｇｌｉｃｌａｚｉｄｅ）系第二代口服磺酰脲类降血糖药，可使非胰岛素依赖型糖尿病得到良好的控制。为了正确评价和使用该药，作者根据中华人民共和国药典１９９０年版二部的有关规定，对国产益公牌格列齐特和进口格列齐特（商品名达美康）的体外溶出度和正常人体内药物动力学进行了研究。结果表明，国产益公牌格列齐特的体外试验符合中国药典规定，进口达美康却相差甚远。正常人体内药物动力学测定结果，国产格列齐特和进口达美康片的Ｔ１／２ｋ分别为１０．１６和１１．４１ｈ；Ｔｍａｘ分别为３．２８和８．１８ｈ；Ｃｍａｘ分别为５．５８和１．１２μｇ／ｍｌ；ＡＵＣ分别为１０１．４７和３０．１３ｈ·μｇ／ｍｌ。若以口服国产格列齐特片８０ｍｇ的生物利用度为１００％，则进口达美康相对生物利用度仅为２９．７７％。
The dissolution behaviours in vitro and pharmacokinetics of gliclazide, a potential hypoglycemic drug, were investigated in 18 healthy Chinese volunteers. The blood levels of gliclazide at different times after single oral administration of 80 mg of the domestic and imported tablets were determined by high performance liquid chromatography. The PKBP-N1 pharmacokinetic program was used for the selection of optimal compartment model and calculation of pharmacokinetic parameters using weighted noulinear least square regession. The results showed that the plasma drug was in line with the one-compartment open model. T1/2k, Tmax, Cmax and AUC of domestic and imported tablets were 10.16±2.50 h and 11.41±4.05 h , 3.28±1.18 h and 8.18±4.29 h, 5.58±2.45 h and 1.12±1.45 μg/ml, 101.47±41.31 and 30. 13±25.33 h·μg/ml, respectively. The relative bioavailability of the imported gliclazide was 29.7% compared with that of the domestic.
出处
《第二军医大学学报》
CAS
CSCD
北大核心
1994年第1期52-57,共6页
Academic Journal of Second Military Medical University
关键词
降血糖药
格列齐特
药物动力学
hypoglycemic agents
gliclazide
dissolution
pharmacokinetic
bioavailability
