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鼓室内注射类乳剂分散体以增加健康兔内耳模型中的肉桂嗪含量。

Intratympanic injections of emulsion-like dispersions to augment cinnarizine amount in a healthy rabbit inner ear model.

机构信息

Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research- Guwahati, Sila Katamur (Halugurisuk), Changsari, Kamrup, Assam 781101, India.

Department of Pharmaceutical Analysis, National Institute of Pharmaceutical Education & Research- Guwahati, Sila Katamur (Halugurisuk), Changsari, Kamrup, Assam 781101, India.

出版信息

Nanomedicine (Lond). 2024;19(21-22):1717-1741. doi: 10.1080/17435889.2024.2373042. Epub 2024 Jul 23.

DOI:10.1080/17435889.2024.2373042
PMID:39041668
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11418292/
Abstract

To investigate eutectic liquid-based emulsion-like dispersions for intratympanic injections to augment cinnarizine permeability across round window membrane in a healthy rabbit inner ear model. Two-tier systematic optimization was used to get the injection formula. The drug concentrations in perilymph and plasma were analyzed via. Ultra-performance liquid chromatography-tandem mass spectrometry method after 30-, 60-, 90- and 120-min post intratympanic injection time points in rabbits. A shear-thinning behavior, immediate drug release (∼98.80%, 10 min) and higher cell viability (>97.86%, 24 h) were observed in dispersions. The cinnarizine level of 8168.57 ± 1236.79 ng/ml was observed in perilymph at 30 min post intratympanic injection in rabbits. The emulsion-like dispersions can augment drug permeability through round window membrane.

摘要

研究了共晶液体型乳剂样分散体用于鼓室内注射,以增加辛那嗪通过健康兔内耳模型圆窗膜的渗透性。采用两阶段系统优化法得到注射配方。通过超高效液相色谱-串联质谱法分析了兔鼓室内注射后 30、60、90 和 120 分钟时外淋巴液和血浆中的药物浓度。分散体表现出剪切稀化行为、即刻药物释放(约 98.80%,10 分钟)和更高的细胞活力(>97.86%,24 小时)。在兔鼓室内注射 30 分钟后,外淋巴液中的辛那嗪水平为 8168.57±1236.79ng/ml。乳剂样分散体可增加药物通过圆窗膜的渗透性。

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