Effect of the drug-matrix on the stability of enalapril maleate in tablet formulations

Al-Omari, Mahmoud M.H.; Abdelah, M.K; Badwan, Adnan A.; Jaber, A. M. Y.

doi:10.1016/s0731-7085(01)00399-5

Cited by 45 publications

(12 citation statements)

References 6 publications

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“…It degrades to two major degradation products, viz., enalaprilat and diketopiperazine derivative (Fig. 2), which are reported to be formed in solutions of pH above and below 3, respectively, and even in tablets [1,2]. Enalapril is also shown to be photolabile in solution, again yielding diketopiperazine derivative as the main degradation product [3].…”

Section: Introductionmentioning

confidence: 97%

“…The techniques include spectrophotometry [4], spectrofluorimetry [3], 1 H nuclear magnetic resonance (NMR) spectroscopy [5], atomic absorption spectroscopy (AAS) [4], etc. A number of high performance liquid chromatography (HPLC) methods have also been reported for this drug using ultraviolet (UV) as well as mass (MS) detectors [2,[6][7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%

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Study of forced degradation behavior of enalapril maleate by LC and LC–MS and development of a validated stability-indicating assay method

Bhardwaj

Singh

2008

Journal of Pharmaceutical and Biomedical Analysis

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Section: Introductionmentioning

confidence: 97%

Section: Introductionmentioning

confidence: 99%

Study of forced degradation behavior of enalapril maleate by LC and LC–MS and development of a validated stability-indicating assay method

Bhardwaj

Singh

2008

Journal of Pharmaceutical and Biomedical Analysis

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“…Furthermore, the presence of excipients could be another factor that compromises its stability yet there are no literature data to fully support this hypothesis. Several drug-excipients interactions have been, however, reported for other structurally-related ACE-Is, such as enalapril, quinapril, benazepril and moexipril (Al-Omari et al, 2001;Rezende et al, 2008;Simoncic et al, 2007;Stanisz, 2005Stanisz, , 2004aStanisz, ,b, 2003Stanisz et al, , 2010. Thus, by creating appropriate binary mixtures, we investigated the compatibility of CIL with the selected excipients used in its commercial dosage forms, i.e.…”

Section: Introductionmentioning

confidence: 99%

How to stabilize cilazapril-containing solid dosage forms? The optimization of a final drug formulation

Regulska¹,

Regulski²,

Paszun³

et al. 2017

Arabian Journal of Chemistry

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Cilazapril, a moisture-sensitive compound, is known to undergo rapid degradation which could be additionally facilitated by the presence of excipients that contain or absorb moisture. Hence we investigated the stability of cilazapril in two commercially-available dosage forms and in binary mixtures with the selected excipients used in the studied commercial formulations i.e.: hypromellose, lactose monohydrate, maize starch and talc in order to detect any possible, stability-affecting incompatibilities. Also the impact of the blister made of oriented polyamide/aluminum/polyvinyl chloride//aluminum on cilazapril-containing tablets was researched. A validated HPLC and HPLC-MS methods were used for analysis and the isothermal stress testing conditions were applied (temperature range 318-343 K, relative humidity 76.4% for tablets and temperature 333 K, relative humidity range 50.9-76.4% for binary mixtures). It was shown that the degradation of cilazapril in both, model mixtures and tablets follows the autocatalytic model kinetics and it is more rapid than that observed for pure substance, evidenced by higher degradation rate constants. The immediate packaging protects cilazapril in tablets from degradation only in case of the original drug while in its blistered generic counterpart a slight but statistically insignificant increase of cilazapril decay occurs when compared to bare tablets (p < 0.05). The degradation product of cilazapril in tablets and binary mixtures was identified as cilazaprilat. It was also observed that the increase of relative humidity or the presence of hypromellose, lactose and talc significantly impairs the stability of cilazapril in the aforementioned order. Only maize starch exhibited a positive effect on cilazapril stability (10.8% loss of cilazapril in binary mixture after 360 days of stressing compared to 35% loss of pure cilazapril in analogous test conditions) probably thanks to its moisture-scavenging

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“…5 It is reported that enalapril degrades to two major degradation products; enalaprilat and diketopiperazine derivative (DKP). [6][7][8][9][10][11] Most of the reported methods for quantitative determination of enalapril in pharmaceutical samples, [6][7][8][9][10][11][12][13][14] including official method, 2 are by liquid chromatography with UV detection using a high column temperature. Other techniques include liquid chromatography-mass spectrometry for analysis in biological samples.…”

Section: Introductionmentioning

confidence: 99%

Chemical stability of enalapril maleate drug substance and tablets by a stability-indicating liquid chromatographic method

Diego¹,

Godoy²,

Mennickent³

et al. 2011

Quím. Nova

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The chemical stability of enalapril drug substance and tablets was studied by a stability-indicating liquid chromatographic method. Stress testing was performed on drug substance under various conditions. Accelerated stability testing was carried out for different formulations of enalapril tablets. Chromatographic separation was achieved on a RP-18 column, using a mobile phase of methanolphosphate buffer at 1.0 mL min −1 and UV detection. Degradation of the drug substance was greater under hydrolytic conditions. After 180 days of accelerated stability testing most enalapril tablets showed more than 10% of degradation. Enalapril drug substance and tablets showed instability under stress and accelerated testing respectively, with possible implications on the therapeutic activity.

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Effect of the drug-matrix on the stability of enalapril maleate in tablet formulations

Cited by 45 publications

References 6 publications

Study of forced degradation behavior of enalapril maleate by LC and LC–MS and development of a validated stability-indicating assay method

Study of forced degradation behavior of enalapril maleate by LC and LC–MS and development of a validated stability-indicating assay method

How to stabilize cilazapril-containing solid dosage forms? The optimization of a final drug formulation

Chemical stability of enalapril maleate drug substance and tablets by a stability-indicating liquid chromatographic method

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