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Int. J. Mol. Sci. 2017, 18(1), 164; doi:10.3390/ijms18010164

Comparative Solid-State Stability of Perindopril Active Substance vs. Pharmaceutical Formulation

1
Faculty of Pharmacy, Victor Babes University of Medicine and Pharmacy, 2 Eftimie Murgu, 300041 Timisoara, Romania
2
Faculty of Medicine, Victor Babes University of Medicine and Pharmacy, 2 Eftimie Murgu, 300041 Timisoara, Romania
3
Research Centre for Thermal Analysis in Environmental Problems, West University of Timisoara, 300115 Timisoara, Romania
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Chang Won Choi
Received: 7 August 2016 / Revised: 28 December 2016 / Accepted: 10 January 2017 / Published: 15 January 2017
(This article belongs to the Section Bioactives and Nutraceuticals)
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Abstract

This paper presents the results obtained after studying the thermal stability and decomposition kinetics of perindopril erbumine as a pure active pharmaceutical ingredient as well as a solid pharmaceutical formulation containing the same active pharmaceutical ingredient (API). Since no data were found in the literature regarding the spectroscopic description, thermal behavior, or decomposition kinetics of perindopril, our goal was the evaluation of the compatibility of this antihypertensive agent with the excipients in the tablet under ambient conditions and to study the effect of thermal treatment on the stability of perindopril erbumine. ATR-FTIR (Attenuated Total Reflectance Fourier Transform Infrared) spectroscopy, thermal analysis (thermogravimetric mass curve (TG—thermogravimetry), derivative thermogravimetric mass curve (DTG), and heat flow (HF)) and model-free kinetics were chosen as investigational tools. Since thermal behavior is a simplistic approach in evaluating the thermal stability of pharmaceuticals, in-depth kinetic studies were carried out by classical kinetic methods (Kissinger and ASTM E698) and later with the isoconversional methods of Friedman, Kissinger-Akahira-Sunose and Flynn-Wall-Ozawa. It was shown that the main thermal degradation step of perindopril erbumine is characterized by activation energy between 59 and 69 kJ/mol (depending on the method used), while for the tablet, the values were around 170 kJ/mol. The used excipients (anhydrous colloidal silica, microcrystalline cellulose, lactose, and magnesium stearate) should be used in newly-developed generic solid pharmaceutical formulations, since they contribute to an increased thermal stability of perindopril erbumine. View Full-Text
Keywords: perindopril erbumine; perindopril tert-butylamine; thermal stability; decomposition; pharmaceutical formulation; comparative stability; isoconversional kinetic study; ASTM E698 perindopril erbumine; perindopril tert-butylamine; thermal stability; decomposition; pharmaceutical formulation; comparative stability; isoconversional kinetic study; ASTM E698
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MDPI and ACS Style

Buda, V.; Andor, M.; Ledeti, A.; Ledeti, I.; Vlase, G.; Vlase, T.; Cristescu, C.; Voicu, M.; Suciu, L.; Tomescu, M.C. Comparative Solid-State Stability of Perindopril Active Substance vs. Pharmaceutical Formulation. Int. J. Mol. Sci. 2017, 18, 164.

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