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Published on:July 2016
RGUHS Journal of Pharmaceutical Sciences, 2016; 6(3):54-62
Review Article | doi:10.5530/rjps.2016.3.1


Formulation Strategies for Enhancement of Solubility and Dissolution Rate and limitation for oral bioavailability of Repaglinide: A Review


Authors and affiliation (s):

Vivekanand Kishan Chatap and Savita Dattatray Patil

Department of Pharmaceutics & Pharmacology, H R Patel Institute of Pharmaceutical Education and Research, Shirpur, Dist-Dhule, Maharashtra, INDIA, 425405.

Abstract:

Diabetes mellitus is a disorder of glucose metabolism that results from an absolute or relative lack of insulin and it shows complication in the body. Thus, Diabetes has considered being a dangerous incurable disease in the world. The International Diabetes Federation is recently reported in 2015, that India was a country with the largest numbers of people with diabetes cases of 69.1 million. Therefore pharmaceutical industries take this challenge to resolve this issue by the discovery of new molecules with new approaches for the effective treatment of diabetes-like Glipizide, Repaglinide (RPGD), Pioglitazone, Glibenclamide etc. RPGD (2-ethoxy-4-[[3-methyl-1-[2-(1-piperidyl) phenyl] -butyl] carbamoylmethyl] benzoic acid) is a potent second generation oral hypoglycemic agent broadly used to treat type 2 diabetes mellitus, which acts on the beta cell to induced insulin secretion and reduce blood glucose concentration. As this drug belongs to BCS class-II its dissolution rate is low in the gastrointestinal fluids and its high permeability. Hence, there is need to improve solubility and dissolution rate of poorly water-soluble drugs leads to enhanced oral bioavailability. The dissolution rate of the orally administered poorly water-soluble drug is a long lasting problem of pharmaceutical industries. As the low dissolution rate of RPGD leads to poor bioavailability, this acts as a barrier for the development of therapeutic applications of poorly water soluble drug. This review fulfills the requirement of those researchers who work on solubility, dissolution enhancement for RPGD and poorly water soluble drugs i.e. BCS class-II drugs.

Key words: Repaglinide, Pharmacokinetic, Solubility, Dissolution, Bioavailability, Limitations, and Approaches.

 

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