Design and evaluation of oral formulation for apixaban

Chien-Chiao Wang; Yu-Li Chen; Ta-Chien Lu; Catherine Lee; Yu-Chia Chang; Yen-Fan Chan; Philip Mathew; Xing-Rong Lin; Wen-Rung Hsieh; Ting-Yun Huang; Hsin-Lan Huang; Tsong-Long Hwang

doi:10.1016/j.heliyon.2023.e18422

Design and evaluation of oral formulation for apixaban

Heliyon. 2023 Jul 19;9(8):e18422. doi: 10.1016/j.heliyon.2023.e18422. eCollection 2023 Aug.

Authors

Chien-Chiao Wang^{1

2}, Yu-Li Chen³, Ta-Chien Lu², Catherine Lee², Yu-Chia Chang³, Yen-Fan Chan³, Philip Mathew⁴, Xing-Rong Lin², Wen-Rung Hsieh², Ting-Yun Huang², Hsin-Lan Huang³, Tsong-Long Hwang^{1

3

5

6

7}

Affiliations

¹ Graduate Institute of Biomedical Sciences, College of Medicine, Chang Gung University, Taoyuan City, 333, Taiwan.
² TAHO Pharmaceuticals Ltd. Neihu Dist., Taipei City, 114, Taiwan.
³ Research Center for Chinese Herbal Medicine, Graduate Institute of Healthy Industry Technology, College of Human Ecology, Chang Gung University of Science and Technology, Taoyuan City, 333, Taiwan.
⁴ Novum Pharmaceutical Research Inc. Toronto, ON, M1L 4S4, Canada.
⁵ Graduate Institute of Natural Products, College of Medicine, Chang Gung University, Taoyuan City, 333, Taiwan.
⁶ Department of Anesthesiology, Chang Gung Memorial Hospital, Taoyuan City, 333, Taiwan.
⁷ Department of Chemical Engineering, Ming Chi University of Technology, New Taipei City, 243, Taiwan.

Abstract

Non-valvular atrial fibrillation (NVAF) is a common form of cardiac arrhythmia that affects 1-1.5% of adults and roughly 10% of elderly adults with dysphagia. Apixaban is an anticoagulant referred to as a factor Xa inhibitor, which has been shown to reduce the risk of stroke and systemic embolism in cases of NVAF. Our objective in the current study was to formulate an orally disintegrating film to facilitate the administration of apixaban to elderly patients who have difficulty swallowing. Researchers have used a wide variety of cellulose-based or non-cellulose-based polymers in a variety of combinations to achieve specific characteristics related to film formation, disintegration performance, drug content, in vitro drug release, and stability. One of the two formulations in this study was specify that bioequivalence criteria met with respect to Cmax of the reference drug (ELIQUIS®) in terms of pharmacokinetic profile. Further research will be required to assess the applicability of orodispersible films created using colloidal polymers of high and low molecular weights to other drugs with poor solubility in water.

Keywords: Apixaban; Non-valvular atrial fibrillation (NVAF); Oral disintegrating film; Pharmacokinetics.