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阿哌沙班口服制剂的设计与评价

Design and evaluation of oral formulation for apixaban.

作者信息

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

机构信息

Graduate Institute of Biomedical Sciences, College of Medicine, Chang Gung University, Taoyuan City, 333, Taiwan.

TAHO Pharmaceuticals Ltd. Neihu Dist., Taipei City, 114, Taiwan.

出版信息

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

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, 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.

摘要

非瓣膜性心房颤动(NVAF)是一种常见的心律失常形式,影响1%至1.5%的成年人,在吞咽困难的老年人中约占10%。阿哌沙班是一种抗凝剂,被称为Xa因子抑制剂,已被证明可降低NVAF患者中风和全身性栓塞的风险。我们在当前研究中的目标是制备一种口腔崩解膜,以便于向吞咽困难的老年患者给药阿哌沙班。研究人员使用了多种基于纤维素或非纤维素的聚合物,并进行了各种组合,以实现与成膜、崩解性能、药物含量、药物释放和稳定性相关的特定特性。本研究中的两种制剂之一明确规定,在药代动力学方面,相对于参比药物(艾乐妥®)的Cmax符合生物等效性标准。还需要进一步研究,以评估使用高分子量和低分子量胶体聚合物制成的口腔崩解膜对其他水溶性差的药物的适用性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79bd/10391955/5b842301573a/ga1.jpg

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