Harrower A
Monklands Hospital, Scotland, United Kingdom.
Metabolism. 2000 Oct;49(10 Suppl 2):7-11. doi: 10.1053/meta.2000.17823.
Although sulfonylureas have been used for more than 40 years, it is only recently that their molecular mechanisms of action have been elucidated. Gliclazide modified release, whose introduction comes soon after the sequencing and cloning of the sulfonylurea receptor, is the first sulfonylurea for which it is possible to detail its action from the moment of oral administration through to its effects on long-term glycemic control. Piecing together these steps for this new agent underlines the rationality of its development and the important differences from other members of the sulfonylurea class. Employing an innovative pharmaceutical form based on a hydrophilic matrix to deliver this short-acting sulfonylurea, gliclazide modified release is associated with an unsurpassed efficacy:acceptability ratio, with the potential additional advantages inherent in reduced dosage and once-daily administration.
尽管磺脲类药物已使用了40多年,但直到最近其分子作用机制才得以阐明。格列齐特缓释片在磺脲类受体测序和克隆后不久就被推出,它是首个能够详细阐述从口服给药时刻到其对长期血糖控制效果的整个作用过程的磺脲类药物。梳理这种新药的这些作用步骤突显了其研发的合理性以及与磺脲类药物其他成员的重要差异。基于亲水性基质的创新剂型用于递送这种短效磺脲类药物,格列齐特缓释片具有无与伦比的疗效与可接受性比率,还有减少剂量和每日一次给药所固有的潜在额外优势。