Preparation of Amorphous Composite Particles of Drugs with Ursodeoxycholic Acid as Preclinical Formulations

Tanida, Satoshi; Yoshimoto, Aika; Yoshida, Miyabi; Uchiyama, Hiromasa; Kadota, Kazunori; Tozuka, Yuichi

doi:10.1248/cpb.c18-00644

Cited by 3 publications

(1 citation statement)

References 40 publications

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“…For instance, the spray drying process is useful in producing solid dispersions that disperse the drug on a carrier to make it amorphous. [3][4][5] The production of solid dispersions is one of the most commonly applied pharmaceutical approaches to increase the bioavailability of water poorly soluble drugs. Moreover, spray-dried powders having a porous structure and well plastic deformability are effective for a direct compression.…”

Section: Introductionmentioning

confidence: 99%

Numerical Study on Spray Drying Process: Effect of Nonuniform Temperature Field and Interaction between Droplets on Evaporation Rates of Individual Droplets

Okada

Ohsaki

Nakamura

et al. 2021

CHEMICAL & PHARMACEUTICAL BULLETIN

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Spray drying process is widely used to produce particulate materials in the pharmaceutical industries, such as porous materials for direct compression, solid dispersion for improvement of drug dissolution properties, micro encapsulation to stabilize active compounds, taste masking, preparation of dry powder for inhalation. However, as many factors affect the physical properties of dried particles and the spray drying processes have complex behaviors in which heat and mass transfer occur simultaneously, the detailed mechanisms of dry particle generation have yet to be sufficiently elucidated. In this study, computational fluid dynamics was used to simulate water droplet evaporation in a spray dryer, and the evaporation kinetics of "individual droplets" in the droplet aggregate (group) were analyzed. The numerical simulation revealed that each droplet had different evaporation rates owing to the following two reasons. First, the driving force of evaporation, ΔT, changed every moment as the droplets traveled through different temperature fields in the drying tower. Second, it was calculated the driving force for droplet evaporation differed from the ideal system because the evaporation of other droplets changed the fluid characteristics around the droplets. The obtained results are important findings that lead to the understanding the spray drying process to design and manufacture the pharmaceutical products.

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Section: Introductionmentioning

confidence: 99%

Numerical Study on Spray Drying Process: Effect of Nonuniform Temperature Field and Interaction between Droplets on Evaporation Rates of Individual Droplets

Okada

Ohsaki

Nakamura

et al. 2021

CHEMICAL & PHARMACEUTICAL BULLETIN

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Probucol-Ursodeoxycholic Acid Otic Formulations: Stability and In Vitro Assessments for Hearing Loss Treatment

Ionescu,

Kovacevic,

Jones

et al. 2024

Journal of Pharmaceutical Sciences

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Effect of Solubility Improvement <i>via</i> Formation of an Amorphous Composite of Indomethacin and Sulindac on Membrane Permeability

Hatanaka

Uchiyama

Furukawa

et al. 2023

CHEMICAL & PHARMACEUTICAL BULLETIN

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The importance of permeability as well as solubility of the drug has been recognized in improving the solubility of poorly water-soluble drugs. This study investigated the impact of amorphous composites of indomethacin (IMC) and sulindac (SLD) on the membrane permeability of drugs. The IMC/SLD (1/1) formulation prepared by dry grinding was amorphous with a single glass transition temperature. The Fourier transform IR spectra and Raman spectra revealed formation of hydrogen bonds between the OH group of IMC and the carbonyl group of SLD. These results suggest that an amorphous composite was formed between IMC and SLD through hydrogen bonding. The amount of dissolved IMC and SLD from the amorphous composite of IMC/SLD (1/1) was higher than that of the untreated IMC or SLD in the dissolution test. The permeated amounts and permeation rates of both drugs were enhanced by increasing the solubility of the amorphous composite. Conversely, the apparent membrane permeability coefficients (P app ) were almost same for untreated drugs and amorphous composites. In the case of hydroxypropyl-β-cyclodextrin and sodium dodecyl sulfate, P app of the drugs decreased with the addition of these compounds, although the drug solubility was enhanced by the solubilization effect. This study revealed that an amorphous composite formed through hydrogen bonding is an attractive pharmaceutical way to enhance the permeated amount and permeation rate without changing the P app of both the drugs.

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Preparation of Amorphous Composite Particles of Drugs with Ursodeoxycholic Acid as Preclinical Formulations

Cited by 3 publications

References 40 publications

Numerical Study on Spray Drying Process: Effect of Nonuniform Temperature Field and Interaction between Droplets on Evaporation Rates of Individual Droplets

Numerical Study on Spray Drying Process: Effect of Nonuniform Temperature Field and Interaction between Droplets on Evaporation Rates of Individual Droplets

Probucol-Ursodeoxycholic Acid Otic Formulations: Stability and In Vitro Assessments for Hearing Loss Treatment

Effect of Solubility Improvement <i>via</i> Formation of an Amorphous Composite of Indomethacin and Sulindac on Membrane Permeability

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