Physical Stability of an Amorphous Sugar Matrix Dried From Methanol as an Amorphous Solid Dispersion Carrier and the Influence of Heat Treatment

Takeda, Koji; Sekitoh, Takanari; Fujioka, Akiho; Yamamoto, Kayoko; Okamoto, Takashi; Matsuura, Tsutashi; Imanaka, Hiroyuki; Ishida, Naoyuki; Imamura, Koreyoshi

doi:10.1016/j.xphs.2019.01.008

Cited by 11 publications

(7 citation statements)

References 47 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Our previous study (Sekitoh et al, 2021;Takeda et al, 2019) indicated that the thermal annealing of the amorphous sugar, vacuum foam dried from alcohols, markedly increased the T g value. Considering this, the T cry also is expected to be altered by thermal annealing, and furthermore, the temperature where amorphous sugar is solidified, namely drying temperature, may change (increase) the T g and possibly T cry values.…”

Section: Isothermal Crystallization Behaviormentioning

confidence: 92%

“…Differential scanning calorimetry (DSC) analyses of amorphous trehalose samples, obtained from alcohols (methanol, ethanol) as well as water, were conducted, using a TA Q2000 calorimeter (TA instruments Co., New Castle, DE) equipped with RCS90 cooling system (TA instruments Co.) according to the same procedures as was used in our previous study (Sekitoh et al, 2021;Takeda et al, 2017;Takeda et al, 2019).…”

Section: Differential Scanning Calorimetrymentioning

confidence: 99%

“…The glass transition temperature of the sample, T g , was determined as the onset of heat capacity change in the obtained DSC curve. The prewarming of the sample was omitted since it has been known to alter the characteristics of the amorphous sugar matrix dried from alcohol (Sekitoh et al, 2021;Takeda et al, 2019).…”

Section: Differential Scanning Calorimetrymentioning

confidence: 99%

“…The extents of formation of sugar-sugar hydrogen bonds in different amorphous sugar samples can be semi-quantitatively compared based on the peak frequency of the sugar O-H stretching vibration bands (Imamura et al, 2006;Kagotani et al, 2013;Wolkers, van Kilsdonk, & Hoekstra, 1998). Hence, the measured IR spectra for dried amorphous trehalose samples were smoothed at 80 points and the peak wavenumber of the IR band due to sugar O-H stretching vibration was determined at around 3300 cm -1 (Kagotani et al, 2013;Takeda et al, 2019).…”

Section: Fourier Transform Infrared Ray Spectroscopymentioning

confidence: 99%

See 3 more Smart Citations

Crystallization characteristics of amorphous trehalose dried from alcohol

Sekitoh

Okamoto

Fujioka

et al. 2021

Journal of Food Engineering

Self Cite

View full text Add to dashboard Cite

Trehalose forms a glass that can be used to preserve labile substances under desiccation.The crystallization characteristics, namely crystallization temperature (T cry ) and isothermal crystallization behavior of amorphous trehalose, dried from alcohol (methanol, ethanol), was analyzed and the results were compared with those for the amorphous trehalose freeze-dried from water. The use of alcohol as a drying solvent lowered the T cry by ~90˚C from the value for the case of an aqueous solvent. The formation of multiple forms of crystals and partial melting were suggested by the thermal analysis.Isothermal crystallization experiments showed that the alcohol-originated amorphous trehalose was eventually exclusively converted into ß-form crystals.The induction period (t ind ) before the start of isothermal crystallization was markedly shortened when alcohol was used as the solvent compared to water. The t ind values for various amorphous sugar samples including the alcohol-originated ones could be correlated with difference between T cry and the sample temperature.

show abstract

Section: Isothermal Crystallization Behaviormentioning

confidence: 92%

Section: Differential Scanning Calorimetrymentioning

confidence: 99%

Section: Differential Scanning Calorimetrymentioning

confidence: 99%

Section: Fourier Transform Infrared Ray Spectroscopymentioning

confidence: 99%

See 2 more Smart Citations

Crystallization characteristics of amorphous trehalose dried from alcohol

Sekitoh

Okamoto

Fujioka

et al. 2021

Journal of Food Engineering

Self Cite

View full text Add to dashboard Cite

show abstract

“…To address the issue of low T g , Takeda et al [57] devised a method involving the heat treatment of ASDs formed through the freeze-drying process. Specifically, SDs comprising α-maltose and hydrophobic drugs were prepared via freeze-drying and subjected to heat treatments between 30-120 • C for durations extending up to 120 min.…”

Section: Solid Dispersions Of Sugar Carriersmentioning

confidence: 99%

Sugars and Polyols of Natural Origin as Carriers for Solubility and Dissolution Enhancement

Poka,

Milne,

Wessels

et al. 2023

Pharmaceutics

View full text Add to dashboard Cite

Crystalline carriers such as dextrose, sucrose, galactose, mannitol, sorbitol, and isomalt have been reported to increase the solubility, and dissolution rates of poorly soluble drugs when employed as carriers in solid dispersions (SDs). However, synthetic polymers dominate the preparation of drugs: excipient SDs have been created in recent years, but these polymer-based SDs exhibit the major drawback of recrystallisation upon storage. Also, the use of high-molecular-weight polymers with increased chain lengths brings forth problems such as increased viscosity and unnecessary bulkiness in the resulting dosage form. An ideal SD carrier should be hydrophilic, non-hygroscopic, have high hydrogen-bonding propensity, have a high glass transition temperature (Tg), and be safe to use. This review discusses sugars and polyols as suitable carriers for SDs, as they possess several ideal characteristics. Recently, the use of low-molecular-weight excipients has gained much interest in developing SDs. However, there are limited options available for safe, low molecular excipients, which opens the door again for sugars and polyols. The major points of this review focus on the successes and failures of employing sugars and polyols in the preparation of SDs in the past, recent advances, and potential future applications for the solubility enhancement of poorly water-soluble drugs.

show abstract