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Pharmaceutics
Article . 2023 . Peer-reviewed
License: CC BY
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Other literature type . 2023
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Pharmaceutics
Article . 2023
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Preparation of Apixaban Solid Dispersion for the Enhancement of Apixaban Solubility and Permeability

Authors: Juseung Lee; Jong-Ju Lee; Seungyeol Lee; Linh Dinh; Hangyu Oh; Sharif Md Abuzar; Jun-Hyun Ahn; +1 Authors

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

Abstract

(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 × 10−6 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.

Keywords

solid dispersion, RS1-441, Pharmacy and materia medica, bioavailability enhancement, apixaban; anticoagulation; solid dispersion; solubility enhancement; bioavailability enhancement, solubility enhancement, apixaban, anticoagulation, Article

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citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
15
Top 10%
Average
Top 10%
Green
gold