Abstract
Repaglinide is an oral blood-glucose-lowering drug used to manage type-2 diabetes mellitus by lowering post-prandial glucose by stimulating insulin secretion from pancreatic beta cells. According to the biopharmaceutical classification system, repaglinide falls under the class II category. For such drugs, limited solubility and poor dissolution rate are the major hurdles to overcome by formulation scientists, as they hinder drug absorption and lead to inadequate therapeutic effects. Therefore, this review aims to discuss in depth the various approaches investigated in the past five years to improve the solubility and dissolution of orally administered repaglinide: namely, solid dispersion, co-amorphous technology, cyclodextrin complexation, phospholipid complexes and polymeric micelles, nanocrystals, nanosuspensions and nanofibers.
Highlights
Review ArticleRecent solubility and dissolution enhancement techniques for repaglinide a biopharmaceutics classification system (BCS) class II drug: a review
Diabetes mellitus (DM) is a chronic and complex metabolic disorder that has reached epidemic levels globally, representing an important concern: in particular for poorly developed nations, as DM adds to already existing burdens within health care (Olokoba et al 2012; Standl et al 2019)
Falling into the second class within the biopharmaceutics classification system (BCS), RPG suffers from low aqueous solubility: 34.6 μg/mL at a temperature of 37 °C, while being highly lipophilic ( Mandić and Gabelica 2006; Bhanja et al 2011), meaning that it is characterized by poor solubility, but have an excellent ability to cross membranes, to improve the bioavailability of RPG, it is necessary to increase RPG solubility and/or the drug dissolution rate
Summary
Recent solubility and dissolution enhancement techniques for repaglinide a BCS class II drug: a review.
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