Effect of pharmaceutical excipients on the stability of angiotensin-converting enzyme inhibitors in their solid dosage formulations

Stanisz, Beata; Regulska, Katarzyna; Kania, Jagoda; Garbacki, Piotr

doi:10.3109/03639045.2012.657644

Cited by 19 publications

(20 citation statements)

References 23 publications

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“…Stability studies have received considerable attention in recent years because of their importance in the development and quality control of pharmaceutical products [25][26][27][28][29][30][31][32][33][34][35] . They make part of a development strategy under ICH requirements and should be carried out to establish the inherent or intrinsic stability characteristics of the molecule in a variety of suggested degradation conditions.…”

Section: Resultsmentioning

confidence: 99%

Stability of cefozopran hydrochloride in aqueous solutions

Zalewski

Skibiński

Paczkowska

et al. 2015

Drug Development and Industrial Pharmacy

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The influence of pH on the stability of cefozopran hydrochloride (CZH) was investigated in the pH range of 0.44-13.00. Six degradation products were identified with a hybrid ESI-Q-TOF mass spectrometer. The degradation of CZH as a result of hydrolysis was a pseudo-first-order reaction. As general acid-base hydrolysis of CZH was not occurred in the solutions of hydrochloric acid, sodium hydroxide, acetate, borate and phosphate buffers, kobs = kpH because specific acid-base catalysis was observed. Specific acid-base catalysis of CZH consisted of the following reactions: hydrolysis of CZH catalyzed by hydrogen ions (kH+), hydrolysis of dications (k1H2O), monocations (k2H2O) and zwitter ions (k3H2O) and hydrolysis of zwitter ions (k1OH-) and monoanions (k2OH-) of CZH catalyzed by hydroxide ions. The total rate of the reaction was equal to the sum of partial reactions: [Formula: see text]. CZH similarly like other fourth generation cephalosporin was most stable at slightly acidic and neutral pH and less stable in alkaline pH. The cleavage of the β-lactam ring resulting from a nucleophilic attack on the carbonyl carbon in the β-lactam moiety is the preferred degradation pathway of β-lactam antibiotics in aqueous solutions.

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Section: Resultsmentioning

confidence: 99%

Stability of cefozopran hydrochloride in aqueous solutions

Zalewski

Skibiński

Paczkowska

et al. 2015

Drug Development and Industrial Pharmacy

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“…They can help increase the solubility/compatibility/patient acceptability of the API and help maintain the physicochemical stability of the API in the formulated products. [1][2][3][4] A number of excipients with diverse functions are frequently used in vaginally administered drug products, including the vaginal microbicides tested in preclinical and clinical studies for topical preexposure prophylaxis (PrEP) of sexually transmitted HIV-1. [5][6][7][8] In the design and development of vaginal formulations, the effect of formulation ingredients on the integrity of the cervicovaginal epithelium should be carefully evaluated.…”

mentioning

confidence: 99%

The Effect of Commonly Used Excipients on the Epithelial Integrity of Human Cervicovaginal Tissue

Zhou

Dezzutti

et al. 2016

AIDS Research and Human Retroviruses

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Pharmaceutical excipients are widely used in vaginal drug products. The epithelial integrity of the cervicovaginal tissue is important for HIV-1 prevention. However, the effects of excipients on cervicovaginal epithelium remain unknown. This study aims at assessing the effects of vaginal product excipients on the integrity of human cervicovaginal epithelium and on a lead HIV prevention antiretroviral drug, tenofovir (TFV). In the current study, nine excipients commonly used in vaginal formulations were incubated for 6 h with excised human ectocervical tissue. The effects of the excipients were examined by measuring the transepithelial electrical resistance (TEER), epithelial morphology, paracellular/transcellular permeability, and cell viability. The efficacy of TFV for preventing HIV-1 infection in the ex vivo cultured ectocervix was also tested. We found that disodium ethyl-enediaminetetraacetate (EDTA), sorbic acid, and benzoic acid had no effect on the tissue TEER. Butylated hydroxyanisole, glycerin, propylene glycol, methylparaben, and propylparaben slightly to moderately decreased tissue TEER, whereas citric acid significantly decreased the TEER in a time-dependent manner. Tissue morphology observed post-exposure strongly correlated with TEER data; however, a less strong correlation was observed between paracellular permeability and TEER data after exposure to different excipients. In addition, treatment with EDTA, methylparaben, and propylene glycol at tested levels had no effect on the efficacy of TFV in preventing tissue HIV-1 infection. In conclusion, the combined measurements of TEER, morphology, permeability, and viability using human cervicovaginal tissue represent a clinically relevant platform for safety evaluation of excipients and formulated products for HIV-1 prevention.

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“…Results obtained by the proposed method for the determination of pure samples of MOX and MOXT are statistically compared to those obtained by the reported methods 4 . The calculated t and F values were found to be less than their corresponding theoretical ones confirming good accuracy and excellent precision (Table 4).…”

Section: Discussionmentioning

confidence: 99%

“…It is reported that MOX was identified by HPLC [4][5][6], spectrophotometry [7,8], gas chromatography mass spectrometry [9], and liquid chromatography tandem mass spectrometry [10,11]. In 2006, Koti, J. et al developed a LC-MASS spectrometry method just to monitor the metabolism of MOX to MOXT [10].…”

Section: Moexipril (3s)-2-[(2s)-2-[[(1s)-1-(ethoxycarbonyl)-3-phenylpmentioning

confidence: 99%

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Liquid chromatography-electro spray ionization tandem mass spectrometry for simultaneous determination of Moexipril and its active metabolite Moexiprilat in human plasma

et al. 2014

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A selective, sensitive, and rapid liquid chromatography-electro spray ionization tandem mass spectrometry method has been developed and subsequently validated for the simultaneous determination of Moexipril (MOX), and its active metabolite Moexiprilat (MOXT) in spiked human plasma, using Benazepril (BENZ) as an internal standard (IS). Various modes were tried and the Multiple Reaction Monitoring (MRM) mode was found the most suitable one. The two analytes and Benazepril (IS) were extracted from human plasma by simple protein precipitation using acetonitrile as the precipitating solvent. The stationary phase used was a C18 Sunfire column while water and acetonitrile at 0.1% formic acid (30:70, v:v) was used as a mobile phase. The flow rate used was 0.8 mL/min. Food and Drug Administration guidelines were followed for the method validation. The linearity range was found to be 0.5-100 ng/mL for MOX and 5-200 ng/mL for MOXT and the correlation coefficient was more than 0.9980 for each analyte. Results for accuracy and precision showed satisfactory results. Also the method was compared with reported HPLC method and no significant difference was found.

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Effect of pharmaceutical excipients on the stability of angiotensin-converting enzyme inhibitors in their solid dosage formulations

Cited by 19 publications

References 23 publications

Stability of cefozopran hydrochloride in aqueous solutions

Stability of cefozopran hydrochloride in aqueous solutions

The Effect of Commonly Used Excipients on the Epithelial Integrity of Human Cervicovaginal Tissue

Liquid chromatography-electro spray ionization tandem mass spectrometry for simultaneous determination of Moexipril and its active metabolite Moexiprilat in human plasma

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