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生物药剂学分类系统III类药物的口腔吸收:制剂方法与机制见解

Buccal Absorption of Biopharmaceutics Classification System III Drugs: Formulation Approaches and Mechanistic Insights.

作者信息

Sabra Rayan, Kirby Daniel, Chouk Vikram, Malgorzata Kleta, Mohammed Afzal R

机构信息

Aston Pharmacy School, Aston University, Birmingham B4 7ET, UK.

Catalent Pharma Solutions U.K. Swindon Zydis® Limited, Swindon SN5 8RU, UK.

出版信息

Pharmaceutics. 2024 Dec 6;16(12):1563. doi: 10.3390/pharmaceutics16121563.

DOI:10.3390/pharmaceutics16121563
PMID:39771541
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11676059/
Abstract

Buccal drug delivery emerges as a promising strategy to enhance the absorption of drugs classified under the Biopharmaceutics Classification System (BCS) Class III, characterized by high solubility and low permeability. However, addressing the absorption challenges of BCS Class III drugs necessitates innovative formulation strategies. This review delves into optimizing buccal drug delivery for BCS III drugs, focusing on various formulation approaches to improve absorption. Strategies such as permeation enhancers, mucoadhesive polymers, pH modifiers, ion pairing, and prodrugs are systematically explored for their potential to overcome challenges associated with BCS Class III drugs. The mechanistic insight into how these strategies influence drug absorption is discussed, providing a detailed understanding of their applicability. Furthermore, the review advocates for integrating conventional buccal dosage forms with these formulation approaches as a potential strategy to enhance absorption. By emphasizing bioavailability enhancement, this review contributes to a holistic understanding of optimizing buccal absorption for BCS Class III drugs, presenting a unified approach to overcome inherent limitations in their delivery.

摘要

口腔给药成为一种有前景的策略,可增强生物药剂学分类系统(BCS)III类药物的吸收,这类药物的特点是高溶解性和低渗透性。然而,应对BCS III类药物的吸收挑战需要创新的制剂策略。本综述深入探讨了优化BCS III类药物的口腔给药,重点关注各种改善吸收的制剂方法。系统地探索了渗透促进剂、黏膜黏附聚合物、pH调节剂、离子对和前药等策略克服与BCS III类药物相关挑战的潜力。讨论了这些策略如何影响药物吸收的作用机制,详细阐述了它们的适用性。此外,本综述提倡将传统口腔剂型与这些制剂方法相结合,作为增强吸收的潜在策略。通过强调提高生物利用度,本综述有助于全面理解优化BCS III类药物的口腔吸收,提出一种统一的方法来克服其给药过程中的固有局限性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2b6b/11676059/6336d6a1c73d/pharmaceutics-16-01563-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2b6b/11676059/0d6255022d6c/pharmaceutics-16-01563-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2b6b/11676059/6336d6a1c73d/pharmaceutics-16-01563-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2b6b/11676059/0d6255022d6c/pharmaceutics-16-01563-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2b6b/11676059/6336d6a1c73d/pharmaceutics-16-01563-g002.jpg

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2
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Buccal Permeation of Polysaccharide High Molecular Weight Compounds: Effect of Chemical Permeation Enhancers.
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Pharmaceuticals (Basel). 2022 Dec 19;15(12):1585. doi: 10.3390/ph15121585.
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