Abstract
Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily.
 Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies.
 Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for.
 Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release
Highlights
Nateglinide, a D-phenylalanine derivative is an anti-diabetic drug that is quick but short acting and controls postprandial blood glucose (PBG) effectively
HPMC K15M and HPMC K100M were selected for formulation and their release profile compared with HPMC K4M matrix tablets
Results indicate that the tablet formulations HA-1(HPMC K4M), HB-1(HPMC K15M) and HC-1(HPMC K100M) released 7.31, 3.39 and 1.02% at the end of 0.5 h and 91.14%, 85.28% and 64.75% of nateglinide at the end of 24 h
Summary
Nateglinide, a D-phenylalanine derivative is an anti-diabetic drug that is quick but short acting and controls postprandial blood glucose (PBG) effectively. By using a higher 24-hr dose of nateglinide in a single matrix tablet, the drug is released at a slower rate preventing extremely high and low concentrations of nateglinide in plasma. This helps to avoid the side effects of hypoglycemia and hepatic impairment associated with high concentration and the lack of drug activity when its concentration in plasma is low. The prepared tablets were evaluated with respect to physicochemical parameters including in-vitro drug release, stability, surface morphology and in vivo pharmacokinetics in rabbits
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