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鼻内给药:制剂因素及用户体验洞察

Intranasal Delivery: Formulation Factors and Insights Into User Experience.

作者信息

Lobo Shabbir, Xi Zhangjie, Das Debanjan, Hadzimichalis Norell M, Creek John A

机构信息

Bayer U.S. LLC, R&D Global Consumer Health, 36 Columbia Drive, Morristown, NJ, 07860, USA.

出版信息

AAPS PharmSciTech. 2025 Jul 1;26(6):179. doi: 10.1208/s12249-025-03171-y.

DOI:10.1208/s12249-025-03171-y
PMID:40593387
Abstract

Improving nasal spray use experience is typically not addressed as a key product requirement even though sensations of bitterness, sourness, astringency, or burning after intranasal application can cause significant repulsion, consumer non-compliance from recommended usage and product rejection. Extensive studies have been carried out by academia and industry alike into the formulation characteristics of sprays and consumer preferences to make nasal sprays more "acceptable" by patients. Due to lack of a collative synopsis of these works, this review article attempts to gather and summarize these studies, address the various attributes that impact post spray experience, and provide suggestions towards maximizing user compliance. We systematically categorized a range of factors which can contribute to unpleasant experiences using nasal sprays including anatomical characteristics of the nose, formulation and device properties, formulation components and dosages, etc. Furthermore, we collated relevant information from pharmaceutical and non-pharmaceutical domains to create a comprehensive knowledge base to frame the scope of the issue. Unpleasant sensorial attributes can be controlled by designing the formulation with a thorough understanding of product-device interactions and novel use of excipients. By choosing excipients such as taste masking agents, flavors, and novel polymers the behavior of the product in the nasal canal can be modulated to block the burning, astringent or bitterness sensation on spray use. This paper discusses these factors in comprehensive detail while offering solutions to ensure a superior product experience. The paper also discusses challenges to adoption and compliance strategies of some newer techniques and excipients.

摘要

改善鼻喷雾剂的使用体验通常并未被视为一项关键的产品要求,尽管鼻内给药后出现的苦味、酸味、涩味或灼烧感会导致明显的反感、消费者不遵循推荐用法以及拒绝使用产品。学术界和业界都已针对喷雾剂的配方特性以及消费者偏好展开了广泛研究,以使鼻喷雾剂更易于被患者“接受”。由于缺乏对这些研究的整理综述,本文试图收集并总结这些研究,探讨影响喷雾后体验的各种属性,并就最大限度提高用户依从性提供建议。我们系统地对一系列可能导致使用鼻喷雾剂产生不愉快体验的因素进行了分类,包括鼻子的解剖特征、配方和装置特性、配方成分及剂量等。此外,我们整理了来自制药和非制药领域的相关信息,以创建一个全面的知识库,从而界定该问题的范围。通过深入了解产品 - 装置相互作用并创新性地使用辅料来设计配方,可以控制不愉快的感官属性。通过选择诸如掩味剂、香料和新型聚合物等辅料,可以调节产品在鼻腔内的行为,以阻止喷雾使用时的灼烧感、涩味或苦味。本文详细讨论了这些因素,同时提供了确保卓越产品体验的解决方案。本文还讨论了一些较新技术和辅料在采用和依从策略方面面临的挑战。

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本文引用的文献

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Visualization of nasal powder distribution using biomimetic human nasal cavity model.使用仿生人类鼻腔模型可视化鼻用粉剂分布情况。
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