A Novel Accelerated Oxidative Stability Screening Method for Pharmaceutical Solids

Zhu, Donghua; Zhang, Geoff G. Z.; George, Karen L.S.T.; Zhou, Deliang

doi:10.1002/jps.22580

Cited by 17 publications

(8 citation statements)

References 19 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The reactive excipient impurities mediated oxidative degradation in a solid-state is challenging to investigate and rarely reported. Some oxidative methods have been reported for the stress studies [8,9], which barely represent the actual solid-state environment in the presence of the relevant excipient.…”

Section: Introductionmentioning

confidence: 99%

PVP-H2O2 Complex as a New Stressor for the Accelerated Oxidation Study of Pharmaceutical Solids

2019

View full text Add to dashboard Cite

Reactive impurities, such as hydrogen peroxide in excipients, raise a great concern over the chemical stability of pharmaceutical products. Traditional screening methods of spiking impurities into solid drug-excipient mixtures oversimplify the micro-environment and the physical state of such impurities in real dosage form. This can lead to an inaccurate prediction of the long-term product stability. This study presents the feasibility of using a polyvinylpyrrolidone-hydrogen peroxide complex (PVP-H2O2) as an oxidative agent for the solid state forced degradation of a selected drug, vortioxetine HBr. The PVP-H2O2 complex was prepared and characterized using FT-IR spectroscopy. The tablet compacts were made using a mixture of solid PVP-H2O2 complex and crystalline vortioxetine HBr powder. The compacts were exposed to 40 °C/75% RH condition in open and closed states for different time intervals. The extent and the type of drug degradation were analysed using LC and LC-MS. The extent of degradation was higher in the samples stored at the open state as compared to the close state. The solution state forced oxidation was conducted to verify the peroxide induced degradation reactions. The results evidence the utility of the proposed solid-state stressor and the method for screening the sensitivity of drugs to the excipient reactive impurities involving peroxides in solid-state.

show abstract

Section: Introductionmentioning

confidence: 99%

PVP-H2O2 Complex as a New Stressor for the Accelerated Oxidation Study of Pharmaceutical Solids

2019

View full text Add to dashboard Cite

show abstract

“…The peroxide‐mediated oxidative stress in solid state of samples was performed according to Ref. . To evaluate the oxidative stability against hydrogen peroxide, the solid samples were exposed to hydrogen peroxide vapor at 20°C.…”

Section: Methodsmentioning

confidence: 99%

Stabilization of conjugated linoleic acid via complexation with arabinogalactan and β‐glucan

Veverka

Dubaj

Jorı́k

et al. 2017

Euro J Lipid Sci & Tech

View full text Add to dashboard Cite

Conjugated linoleic acid (CLA) was stabilized via its complexation with arabinogalactan or beta‐glucan by freeze‐drying. The complexes were characterized by infrared spectroscopy, X‐ray diffraction, differential scanning calorimetry, and scanning electron microscopy. The results have shown that only a fraction of CLA is present in the form of inclusion complex while the rest is adsorbed on the surface of the polysaccharide matrix. Even though the materials prepared contain relatively high amount of uncomplexed CLA, the complexation yields products with significantly increased stability toward thermal and oxidative stress compared to pristine CLA. Practical applications: The results demonstrate that it is possible to integrate dietary fibre and dietary fat into a single solid functional food material with increased shelf life. Moreover, the combination of CLA with polysaccharide matrix allows preparation of stable O/W emulsions of CLA. Interaction between polysaccharides (beta‐glucan and arabinogalactan) and CLA allows preparation of materials with high CLA loading of up to 30% while maintaining improved oxidative stability compared to free CLA or physical mixture.

show abstract

“…There are fewer methods available for the prediction of oxidation in solids. Previous studies have reported solid‐state‐based methods in which 2,2′‐azobis(‐amidinopropane) dihydrochloride was simply added to a mixture of a drug and excipients; in which hydrogen peroxide (H 2 O 2 ) was spiked into a mixture of a drug and excipients before tablet formation; in which a drug was exposed to the vapor from H 2 O 2 dissolved in water in a sealed container filled with oxygen; and in which urea‐H 2 O 2 was used to expose a drug to H 2 O 2 vapor . The present study proposes and describes a novel solid‐state‐based forced oxidation system that can be used for a realistic prediction of oxidation products.…”

Section: Introductionmentioning

confidence: 99%

“…12,13 For this reason, oxidation is associated with a high risk of generating potentially genotoxic impurities. Many previous studies have described approaches for studying oxidative mechanisms, including autoxidation prediction using free radical initiators, [14][15][16][17] the use of N-methylpyrrolidone 18 and Tween80/Fe 3+ , 19 nucleophilic/ electrophilic oxidation prediction with peroxides, 3,4,20,21 electron transfer oxidation prediction with transition metals, 5 electro-oxidation prediction with voltammetry, 22 and prediction of photochemically induced oxidation with a photosensitizer. 6 Indeed, these approaches have been used in the pharmaceutical industry, often producing useful information relating to oxidation susceptibility that has been helpful in pharmaceutical development.…”

Section: Introductionmentioning

confidence: 99%

Realistic Prediction of Solid Pharmaceutical Oxidation Products by Using a Novel Forced Oxidation System

Ueyama

Tamura

Mizukawa

et al. 2014

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

A Novel Accelerated Oxidative Stability Screening Method for Pharmaceutical Solids

Cited by 17 publications

References 19 publications

PVP-H2O2 Complex as a New Stressor for the Accelerated Oxidation Study of Pharmaceutical Solids

PVP-H2O2 Complex as a New Stressor for the Accelerated Oxidation Study of Pharmaceutical Solids

Stabilization of conjugated linoleic acid via complexation with arabinogalactan and β‐glucan

Realistic Prediction of Solid Pharmaceutical Oxidation Products by Using a Novel Forced Oxidation System

Contact Info

Product

Resources

About