大鼠鼻腔药物吸收的体内系统评价。

IF 4.4 2区 医学 Q1 PHARMACOLOGY & PHARMACY European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-02-01 Epub Date: 2024-12-10 DOI:10.1016/j.ejpb.2024.114612
Ryosuke Tatsuta, Akiko Tanaka, Ken-Ichi Ogawara, Kazutaka Higaki, Tomoyuki Furubayashi, Toshiyasu Sakane
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引用次数: 0

摘要

尽管鼻腔给药有潜在的好处,但有必要对粘在鼻黏膜上的粉末制剂的疗效进行系统的评估。本研究旨在建立粉剂鼻腔药物吸收的系统评价方法。我们选择了三种模型化合物——安替比林、灰黄霉素和阿昔洛韦,并分析了它们在生理条件下经鼻给药的粉末制剂的药代动力学。我们的实验设计纳入了药物吸收模式的评估。安替比林仅从鼻腔被快速吸收。相反,灰黄霉素表现出从鼻腔和胃肠道吸收。这种现象可归因于药物的快速鼻腔清除率,初始半衰期为5 min。为了进一步确定我们的方法的生理有效性,我们进行了一项实验,研究改变粘膜纤毛清除率(MC)对鼻吸收的影响,导致延长MC后阿昔洛韦的生物利用度增加1.2倍。我们的研究结果支持了现有方法在评估鼻吸收及其在鼻腔中的行为方面的实用性。这项研究在通过鼻腔给药的有效给药方面取得了有希望的进展,可能导致靶向给药和改善治疗结果。
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In vivo systemic evaluation of nasal drug absorption from powder formulations in rats.

Despite the potential benefits of nasal drug delivery, there is a need for a systematic evaluation of the efficacy of powder formulations adhering to the nasal mucosa. This study aims to establish a systematic evaluation method for nasal drug absorption from powder formulations. We selected three model compounds-antipyrine, griseofulvin, and acyclovir-and analyzed their pharmacokinetics following nasal administration of powder formulations under physiological conditions. Our experimental design incorporated assessments of the drug absorption patterns. Antipyrine demonstrated rapid absorption exclusively from the nasal cavity. In contrast, griseofulvin exhibited absorption from the nasal cavity and the gastrointestinal tract. This phenomenon could be attributed to the rapid nasal clearance of the drug with an initial half-life of 5 min. To further establish the physiological validity of our method, we conducted an experiment to investigate the impact of changing the mucociliary clearance (MC) on nasal absorption that resulted in a 1.2-fold increase in the bioavailability of acyclovir upon prolonged MC. Our findings support the utility of established methods in evaluating nasal absorption and their behavior in the nasal cavity. This study holds a promising advancement toward effective drug delivery via nasal administration, potentially leading to targeted delivery and improved therapeutic outcomes.

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来源期刊
CiteScore
8.80
自引率
4.10%
发文量
211
审稿时长
36 days
期刊介绍: The European Journal of Pharmaceutics and Biopharmaceutics provides a medium for the publication of novel, innovative and hypothesis-driven research from the areas of Pharmaceutics and Biopharmaceutics. Topics covered include for example: Design and development of drug delivery systems for pharmaceuticals and biopharmaceuticals (small molecules, proteins, nucleic acids) Aspects of manufacturing process design Biomedical aspects of drug product design Strategies and formulations for controlled drug transport across biological barriers Physicochemical aspects of drug product development Novel excipients for drug product design Drug delivery and controlled release systems for systemic and local applications Nanomaterials for therapeutic and diagnostic purposes Advanced therapy medicinal products Medical devices supporting a distinct pharmacological effect.
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