Abstract
Firstly, metformin and repaglinide were degraded under high temperature/humidity, UV/VIS light, in different pH and oxidative conditions. Secondly, a new validated LC-UV method was examined, as to whether it validly determined these drugs in the presence of their degradation products and whether it is suitable for estimating degradation kinetics. Finally, the respective LC-MS method was used to identify the degradation products. In addition, using FT-IR method, the stability of metformin and repaglinide was scrutinized in the presence of polyvinylpyrrolidone (PVP), mannitol, magnesium stearate, and lactose. Significant degradation of metformin, following the first order kinetics, was observed in alkaline medium. In the case of repaglinide, the most significant and quickest degradation, following the first order kinetics, was observed in acidic and oxidative media (0.1 M HCl and 3% H2O2). Two new degradation products of metformin and nine new degradation products of repaglinide were detected and identified when the stressed samples were examined by our LC-MS method. What is more, the presence of PVP, mannitol, and magnesium stearate proved to affect the stability of metformin, while repaglinide stability was affected in the presence of PVP and magnesium stearate.
Highlights
Metformin hydrochloride, 3-(diaminomethylidene)-1,1-dimethylguanidine (Figure 1A), is an oral antidiabetic drug that is used for the treatment of type 2 diabetes, for overweight or obese patients with normal kidney function
Our results proved that repaglinide was significantly sensitive to acidic and oxidative conditions
Taking our results presented above into consideration, it could be supposed that the non-ionized forms of metformin and repaglinide are more susceptible to degradation
Summary
3-(diaminomethylidene)-1,1-dimethylguanidine (Figure 1A), is an oral antidiabetic drug that is used for the treatment of type 2 diabetes, for overweight or obese patients with normal kidney function. It reduces the serum glucose level by several actions, notably through non-pancreatic mechanisms without increasing insulin secretion. This agent mainly works by reducing gluconeogenesis and opposing glucagon-mediated signaling in the liver and, to a lesser extent, by increasing glucose uptake in skeletal muscles [1]. Metformin and repaglinide are available in fixed-dose combinations because of their complementary actions in diabetes.
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