注射用长效制剂 (ILAF) 和制造技术。

Expert opinion on drug delivery Pub Date : 2024-06-01 Epub Date: 2024-07-17 DOI:10.1080/17425247.2024.2374807
Kosheli Thapa Magar, Hamza Boucetta, Zongmin Zhao, Ying Xu, Zhengxia Liu, Wei He
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引用次数: 0

摘要

简介:大多数使用短效制剂给药的治疗药物都需要重复给药,这会损害患者的依从性,并增加因治疗不连贯而导致治疗失败的风险。注射用长效制剂(ILAFs)是一种控释/缓释制剂,用于递送活性药物成分(APIs),并将其半衰期延长数天至数月。长效制剂的半衰期可最大限度地减少频繁给药的必要性,提高患者的依从性,并降低静脉注射副作用的风险。利用 ILAF 技术,还可以控制药物的即时释放,从而最大限度地减少因初始药物血药浓度过高而导致的潜在不良反应:在这篇综述中,我们讨论了各种 ILAF 及其理化性质、制造技术、优势和实际问题,并探讨了其应用中的一些主要挑战。特别强调了已获批准的 ILAF:ILAF是一种具有延长活性的缓释制剂,可以提高患者的依从性。ILAF 的设计目的是输送蛋白质和肽等原料药,并延长其数天至数月的半衰期。每种 ILAF 制剂都具有延长释放时间和提高药物靶向能力等特殊性能,因此是精确和集中治疗的有效方法。此外,这对生物半衰期短、稳定性低的生物制药尤其有帮助,因为大多数环境条件都能保护它们不受缓释给药方法的影响。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Injectable long-acting formulations (ILAFs) and manufacturing techniques.

Introduction: Most therapeutics delivered using short-acting formulations need repeated administration, which can harm patient compliance and raise failure risks related to inconsistent treatment. Injectable long-acting formulations (ILAFs) are controlled/sustained-release formulations fabricated to deliver active pharmaceutical ingredients (APIs) and extend their half-life over days to months. Longer half-lives of ILAFs minimize the necessity for frequent doses, increase patient compliance, and reduce the risk of side effects from intravenous (IV) infusions. Using ILAF technologies, the immediate drug release can also be controlled, thereby minimizing potential adverse effects due to high initial drug blood concentrations.

Area covered: In this review, we have discussed various ILAFs, their physiochemical properties, fabrication technologies, advantages, and practical issues, as well as address some major challenges in their application. Especially, the approved ILAFs are highlighted.

Expert opinion: ILAFs are sustained-release formulations with extended activity, which can improve patient compliance. ILAFs are designed to deliver APIs like proteins and peptides and extend their half-life over days to months. The specific properties of each ILAF preparation, such as extended-release and improved drug targeting capabilities, make them an effective approach for precise and focused therapy. Furthermore, this is especially helpful for biopharmaceuticals with short biological half-lives and low stability since most environmental conditions can protect them from sustained-release delivery methods.

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