Preparation of Apixaban Solid Dispersion for the Enhancement of Apixaban Solubility and Permeability

(1) Background: Solid dispersion (SD) can help increase the bioavailability of poorly water-soluble drugs. Meanwhile, apixaban (APX)-a new anticoagulation drug-has low water solubility (0.028 mg/mL) and low intestinal permeability (0.9 × 10 cm/s across Caco-2 colonic cells), thus resulting in a low...

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Published inPharmaceutics Vol. 15; no. 3; p. 907
Main Authors Lee, Juseung, Lee, Jong-Ju, Lee, Seungyeol, Dinh, Linh, Oh, Hangyu, Abuzar, Sharif Md, Ahn, Jun-Hyun, Hwang, Sung-Joo
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 01.03.2023
MDPI
Subjects
Aluminum
anticoagulation
Apixaban
Bioavailability
bioavailability enhancement
Chemical properties
Drug dosages
Evaluation
Fourier transforms
Permeability
Polymers
Potassium
Pulmonary embolisms
solid dispersion
Solubility
solubility enhancement
Solvents
Spectrum analysis
Testing
Thrombosis
South Korea
United States > US
Japan
Germany
bioavailability enhancement
solubility enhancement
solid dispersion
apixaban
anticoagulation
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Summary:(1) Background: Solid dispersion (SD) can help increase the bioavailability of poorly water-soluble drugs. Meanwhile, apixaban (APX)-a new anticoagulation drug-has low water solubility (0.028 mg/mL) and low intestinal permeability (0.9 × 10 cm/s across Caco-2 colonic cells), thus resulting in a low oral bioavailability of <50%; (2) Methods: To solve the drawbacks of conventional APX products, a novel SD of APX in Soluplus was prepared, characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infrared (FTIR) spectroscopy techniques and evaluated for its solubility, intestinal permeability and pharmacokinetic performance. (3) Results: The crystallinity of the prepared APX SD was confirmed. The saturation solubility and apparent permeability coefficient increased 5.9 and 2.54 times compared to that of raw APX, respectively. After oral administration to the rats, the bioavailability of APX SD was improved by 2.31-fold compared to that of APX suspension (4) Conclusions: The present study introduced a new APX SD that potentially exhibits better solubility and permeability, thus increasing APX's bioavailability.
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ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics15030907