Physical aging in pharmaceutical polymers and the effect on solid oral dosage form stability

Kucera, Shawn A.; Felton, Linda A.; McGinity, James W.

doi:10.1016/j.ijpharm.2013.01.069

Cited by 26 publications

(11 citation statements)

References 45 publications

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“…The small movements of molecules within the glassy matrix can be a source of ‘physical ageing’ of the structure, which has been implicated in the deterioration of foods, plastics and pharmaceutical compounds (e.g. Cicerone et al, 2003; Roudaut et al, 2004; Kucera et al, 2013; Cowie and Arrighi, 2014). Over time, molecules that were entrapped by neighbouring molecules budge (or relax) and begin to fill in the pores.…”

Section: The Role Of Glassy Matrices In Survival and Deterioration Ofmentioning

confidence: 99%

Dry architecture: towards the understanding of the variation of longevity in desiccation-tolerant germplasm

Ballesteros

Pritchard

Walters³

2020

Seed Sci. Res.

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Desiccation-tolerant (DT) plant germplasm (i.e. seeds, pollen and spores) survive drying to low moisture contents, when cytoplasm solidifies, forming a glass, and chemical reactions are slowed. DT germplasm may survive for long periods in this state, though inter-specific and intra-specific variation occurs and is not currently explained. Such variability has consequences for agriculture, forestry and biodiversity conservation. Longevity was previously considered in the context of morphological features, cellular constituents or habitat characteristics. We suggest, however, that a biophysical perspective, which considers the molecular organization – or structure – within dried cytoplasm, can provide a more integrated understanding of the fundamental mechanisms that control ageing rates, hence the variation of longevity among species and cell types. Based on biochemical composition and physical–chemical properties of dried materials, we explore three types of the interplay between structural conformations of dried cytoplasm and ageing: (1) cells that lack chlorophyll and contain few storage lipids may exhibit long shelf life, with ageing probably occurring through slow autoxidative processes within the glassy matrix as it relaxes; (2) cells with active chlorophyll may die quickly, possibly because they are prone to oxidative stress promoted by the photosynthetic pigments in the absence of metabolic water and (3) cells that lack chloroplasts but contain high storage lipids may die quickly during storage at −20°C, possibly because lipids crystallize and destabilize the glassy matrix. Understanding the complex variation in structural conformation in space and time may help to design strategies that increase longevity in germplasm with generally poor shelf life.

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Section: The Role Of Glassy Matrices In Survival and Deterioration Ofmentioning

confidence: 99%

Dry architecture: towards the understanding of the variation of longevity in desiccation-tolerant germplasm

Ballesteros

Pritchard

Walters³

2020

Seed Sci. Res.

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“…Amorphous drugs may crystallize or, in the absence of a crystalline form, undergo physical aging process during storage at a temperature below the glass transition. Aged amorphous materials are characterized by increased fragility, and the aging process may result in a slower dissolution rate of the API [11][12][13][14][15][16]. Standalone amorphous APIs are rather not used in formulation development.…”

Section: (I)mentioning

confidence: 99%

Physical aging of polylactide-valsartan system investigated by differential scanning calorimetry

2020

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The polylactide-valsartan systems with a mass ratio of 20 : 80, 50 : 50 and 80 : 20 were obtained and characterized by standard Differential Scanning Calorimetry (DSC). The isothermal physical aging process of polylactide-valsartan with a mass ratio of 50 : 50 was investigated at the aging temperature of 50°C and 70°C for different aging times. The enthalpy of relaxation values for each of the aging times and for all investigated components were determined experimentally and fitted to the Kohlrausch-Williams-Watts equation.

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“…This phenomenon has been shown to cause changes in the mechanical, permeability and drug release properties of polymeric films due to a densification and decrease in free volume of the polymer. A variety of techniques have been used to stabilize polymeric films and prevent aging [107]. For example, the storage temperature was critical for the stability of theophylline pellets coated with a blend of Eudragit ® RS 30 D and NE 30 D [108].…”

Section: Synthetic Polymers Used As Excipient In Floating Formulationsmentioning

confidence: 99%

In-Depth Study into Polymeric Materials in Low-Density Gastroretentive Formulations

et al. 2020

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The extensive use of oral dosage forms for the treatment of diseases may be linked to deficient pharmacokinetic properties. In some cases the drug is barely soluble; in others, the rapid transit of the formulation through the gastrointestinal tract (GIT) makes it difficult to achieve therapeutic levels in the organism; moreover, some drugs must act locally due to a gastric pathology, but the time they remain in the stomach is short. The use of formulations capable of improving all these parameters, as well as increasing the resident time in the stomach, has been the target of numerous research works, with low-density systems being the most promising and widely explored, however, there is further scope to improve these systems. There are a vast variety of polymeric materials used in low-density gastroretentive systems and a number of methods to improve the bioavailability of the drugs. This works aims to expedite the development of breakthrough approaches by providing an in-depth understanding of the polymeric materials currently used, both natural and synthetic, their properties, advantages, and drawbacks.

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Physical aging in pharmaceutical polymers and the effect on solid oral dosage form stability

Cited by 26 publications

References 45 publications

Dry architecture: towards the understanding of the variation of longevity in desiccation-tolerant germplasm

Dry architecture: towards the understanding of the variation of longevity in desiccation-tolerant germplasm

Physical aging of polylactide-valsartan system investigated by differential scanning calorimetry

In-Depth Study into Polymeric Materials in Low-Density Gastroretentive Formulations

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