University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160014, India.
Expert Opin Drug Deliv. 2012 Apr;9(4):403-16. doi: 10.1517/17425247.2012.663080. Epub 2012 Feb 25.
α-Glucosidase inhibitors (AGIs) are an important category of oral antidiabetic agents being extensively exploited for the effective management of type 2 diabetes and associated disorders. These drugs significantly reduce the postprandial rise in glycemic and plasma insulin levels both in nondiabetics and in type 2 diabetic patients. Currently only three drugs belonging to this category, viz, acarbose, miglitol and voglibose are in the market. The major limitations associated with the administration of AGIs are the stringent repetitive dosing schedule at specified time intervals, along with a high incidence of gastrointestinal disturbances that mainly include flatulence, abdominal distension, borborygmus and diarrhea. All these factors tend to decrease patient compliance.
This review focuses on the various formulation approaches being targeted for the effective delivery of AGIs, viz, unit matrix systems, bioadhesive pellets, hydrogels and lipid-based granules.
It is concluded that development of a successful controlled-release delivery system for these drugs will obviate the need of repeated administration, which in turn will improve patient compliance.
α-葡萄糖苷酶抑制剂(AGIs)是一类重要的口服抗糖尿病药物,广泛用于有效治疗 2 型糖尿病和相关疾病。这些药物可显著降低非糖尿病患者和 2 型糖尿病患者餐后血糖和血浆胰岛素水平的升高。目前,该类药物仅有阿卡波糖、米格列醇和伏格列波糖 3 种药物上市。AGIs 给药的主要局限性是必须在规定的时间间隔内严格重复给药,同时胃肠道紊乱的发生率很高,主要包括胀气、腹胀、肠鸣音亢进和腹泻。所有这些因素都可能降低患者的顺应性。
本综述重点介绍了针对 AGIs 有效传递的各种制剂方法,即单位基质系统、生物粘附微丸、水凝胶和基于脂质的颗粒。
结论是,为这些药物开发成功的控释传递系统将消除重复给药的需要,这反过来又将提高患者的顺应性。