The Experts below are selected from a list of 315 Experts worldwide ranked by ideXlab platform
Eliana Martins Lima - One of the best experts on this subject based on the ideXlab platform.
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Improvement of Enalapril Maleate chemical stability by high shear melting granulation
Pharmaceutical development and technology, 2014Co-Authors: Ana Paula Montandon De Oliveira, Eliana Martins Lima, Talita A. Cunha, Luís Alexandre Pedro De Freitas, Raphael Caixeta Serpa, Stephânia Fleury Taveira, Danielle Guimarães Almeida Diniz, Ricardo Neves MarretoAbstract:Enalapril Maleate is a widely used drug, which is chemically unstable when mixed with excipients resulting in Enalaprilat and diketopiperazine as the main degradation products. The preparation of Enalapril sodium salt has been used to improve drug stability in solid dosage forms; however, product rejection is observed when the chemical reaction for obtaining the sodium salt is not completely finished before packaging. In this study, granules were prepared by melting granulation using stearic acid or glyceryl monostearate, with a view to developing more stable Enalapril Maleate solid dosage forms. The granules were prepared in a laboratory-scale high shear mixer and compressed in a rotary machine. Size distribution, flow properties, in vitro drug release and Enalapril Maleate chemical stability were evaluated and compared with data obtained from tablets prepared without hydrophobic binders. All formulations showed good physical properties and immediate drug release. The greatest improvement in the Enalapril Maleate stability was observed in formulations containing stearic acid. This study showed that hot melting granulation could be successfully used to prepare Enalapril Maleate granules which could substitute the in situ formation of Enalapril sodium salt, since they provided better Enalapril stability in solid dosage forms.
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stability and in vitro release profile of Enalapril Maleate from different commercially available tablets possible therapeutic implications
Journal of Pharmaceutical and Biomedical Analysis, 2008Co-Authors: Dione Marcal Lima, Leandro Dias Dos Santos, Eliana Martins LimaAbstract:Stability of Enalapril Maleate formulations can be affected when the product is exposed to higher temperature and humidity, with the formation of two main degradation products: Enalaprilat and a diketopiperazine derivative. In this work, stability and drug release profiles of 20 mg Enalapril Maleate tablets (reference, generic and similar products) were evaluated. After 180 days of the accelerated stability testing, most products did not exhibit the specified amount of drug. Additionally, drug release profiles were markedly different from that of the reference product, mainly due to drug degradation. Changes in drug concentration and drug release profile of Enalapril formulations are strong indicators of a compromised bioavailability, with possible interferences on the therapeutic response for this drug.
Jivaldo Do Rosário Matos - One of the best experts on this subject based on the ideXlab platform.
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Stability and compatibility study on Enalapril Maleate using thermoanalytical techniques
Journal of Thermal Analysis and Calorimetry, 2008Co-Authors: R. L. O. Rezende, M. I. R. M. Santoro, Jivaldo Do Rosário MatosAbstract:This paper demonstrates the application of thermal analysis in compatibility and stability studies between an ACE inhibitor (Enalapril Maleate) and excipients. The results have helped to elucidate the reason of a stability problem observed during the storage of Enalapril Maleate tablets. Incompatibility between Enalapril Maleate and colloidal silicon dioxide was detected. Besides, it was confirmed that the reaction between Enalapril Maleate and NaHCO3 increases the thermal stability of the drug. This study supports the importance of using thermoanalytical methods in the development of pharmaceuticals.
A M Y Jaber - One of the best experts on this subject based on the ideXlab platform.
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effect of the drug matrix on the stability of Enalapril Maleate in tablet formulations
Journal of Pharmaceutical and Biomedical Analysis, 2001Co-Authors: M M Alomari, M K Abdelah, Adnan Badwan, A M Y JaberAbstract:Abstract The chemical stability of Enalapril Maleate in tablet dosage forms consisting of different formulation excipients has been studied in this work. The influence of various parameters such as heat, moisture, light and the drug-matrix was investigated. The degradation of Enalapril Maleate has been followed by using an HPLC method, which was demonstrated to be specific, stability indicating, accurate and precise. The degradation kinetics of enalalpril Maleate in phosphate buffer solutions of pH values in the range of 2.2–10.5 were observed to be psuedo first order throughout the whole pH range studied. Enalapril Maleate alone showed high stability for temperature under dry and humid conditions, however it became unstable when mixed with the drug-matrix in its tablet formulations and exposed to the same conditions. The pathway of degradation of Enalapril Maleate was found to be pH dependent. The extent of degradation of two different Enalapril Maleate tablet formulations (product A of a basic drug-matrix and product B of an acidic drug-matrix) has been investigated. The degree of degradation of the product with acidic matrix was significantly less than that of the basic matrix under same temperature and humidity conditions. Infact, diketopiperazine and Enalaprilat degradants were mainly associated with the degradation of the product with the acidic matrix and that with the basic matrix, respectively. Dry Enalapril Maleate powder showed some photolysis, which was more significant with daylight (3.3%) compared with that under UV light (0.2%). Although the product with the acidic matrix showed some photolysis but the effect was not pronounced and the % recovery of Enalapril was almost complete and within the acceptable experimental errors. However, the product with the basic matrix showed almost no response for photolysis.
Dione Marcal Lima - One of the best experts on this subject based on the ideXlab platform.
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stability and in vitro release profile of Enalapril Maleate from different commercially available tablets possible therapeutic implications
Journal of Pharmaceutical and Biomedical Analysis, 2008Co-Authors: Dione Marcal Lima, Leandro Dias Dos Santos, Eliana Martins LimaAbstract:Stability of Enalapril Maleate formulations can be affected when the product is exposed to higher temperature and humidity, with the formation of two main degradation products: Enalaprilat and a diketopiperazine derivative. In this work, stability and drug release profiles of 20 mg Enalapril Maleate tablets (reference, generic and similar products) were evaluated. After 180 days of the accelerated stability testing, most products did not exhibit the specified amount of drug. Additionally, drug release profiles were markedly different from that of the reference product, mainly due to drug degradation. Changes in drug concentration and drug release profile of Enalapril formulations are strong indicators of a compromised bioavailability, with possible interferences on the therapeutic response for this drug.
Beata Stanisz - One of the best experts on this subject based on the ideXlab platform.
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Kinetics of degradation of Enalapril Maleate in dosage forms.
Acta poloniae pharmaceutica, 2004Co-Authors: Beata StaniszAbstract:The effect of humidity and temperature on the stability of Enalapril Maleate (ENA) in tablets have been studied. Tablets with ENA were stored in final packs (blisters) and without final packs in the atmosphere of increased humidity (76.4 % RH) and in the temperature range from 313 K to 333 K (forced degradation test). Degradation of ENA in tablets stored in final packs and without final packs followed the first order reaction model. During this study, the product of hydrolysis of the ester group and intramolecular cyclization have been observed. Thermodynamic parameters (activation energies, enthalpy and entropy) for the decomposition of ENA in tablets were calculated.
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Evaluation of stability of Enalapril Maleate in solid phase
Journal of pharmaceutical and biomedical analysis, 2003Co-Authors: Beata StaniszAbstract:Abstract The influence of temperature (from 383 to 348 K) and relative humidity (from 25.0 to 76.4%) on the stability of Enalapril Maleate in the solid phase was investigated. Changes in the concentration Enalapril Maleate were followed by a HPLC method with UV detection. The kinetic and thermodynamic parameters [ E a (kJ mol −1 )=168.5±27 for RH=0% and 149.1±48 for RH=76.4%; Δ H ≠ (kJ mol −1 )=166.1±30 for RH=0% and 146.6±50 for RH=76.4%; Δ S ≠ (J (K −1 mol −1 ))=120.3±169 for RH=0% and 82.1±110 for RH=76.4%) of the decomposition reaction were calculated.