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食管用粘膜粘附膜的生物相关释放测试的改进及增加粘膜接触时间的制剂策略的开发

Modification of the Biorelevant Release Testing of Esophageal Applied Mucoadhesive Films and Development of Formulation Strategies to Increase the Mucosal Contact Time.

作者信息

Brokmann Friederike, Simonek Paul, Rosenbaum Christoph

机构信息

Department of Biopharmaceutics and Pharmaceutical Technology, Institute of Pharmacy, University of Greifswald, Felix-Hausdorff-Straße 3, 17489 Greifswald, Germany.

出版信息

Pharmaceutics. 2024 Aug 1;16(8):1021. doi: 10.3390/pharmaceutics16081021.

DOI:10.3390/pharmaceutics16081021
PMID:39204366
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11360207/
Abstract

The increasing prevalence of esophageal disease highlights the clinical relevance of novel, long-lasting mucoadhesive oral dosage forms. The EsoCap device enables targeted local application of films in the esophagus. Biorelevant test systems such as EsoPeriDiss are essential for early formulation development. To this end, the developed and already described release model for simulating the esophagus is being further developed for its potential for biorelevant mapping of the application site through complete tempering and investigation of biorelevant release media. Particularly viscous saliva formulations led to an extension of the retention time. In addition, possible formulation strategies for increasing the retention time of esophageal applied films are being evaluated, such as different film thicknesses, polymer grades and the influence of different active ingredient properties on the retention time. For highly soluble active ingredients, the film thickness represents an option for extending the retention time, while for less soluble substances, the choice of polymer grade may be of particular interest.

摘要

食管疾病患病率的不断上升凸显了新型长效粘膜粘附口服剂型的临床相关性。EsoCap装置能够将薄膜靶向局部应用于食管。诸如EsoPeriDiss等生物相关测试系统对于早期制剂开发至关重要。为此,已开发并已描述的用于模拟食管的释放模型正在进一步开发,以通过完全调温和研究生物相关释放介质来实现对应用部位进行生物相关映射的潜力。特别粘稠的唾液制剂导致保留时间延长。此外,正在评估增加食管应用薄膜保留时间的可能制剂策略,例如不同的薄膜厚度、聚合物等级以及不同活性成分特性对保留时间的影响。对于高溶解性活性成分,薄膜厚度是延长保留时间的一种选择,而对于低溶解性物质,聚合物等级的选择可能特别重要。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/6605abc9eb98/pharmaceutics-16-01021-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/a3326c20b247/pharmaceutics-16-01021-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/ff1e391c61c7/pharmaceutics-16-01021-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/20bb1d35c533/pharmaceutics-16-01021-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/752df95951d6/pharmaceutics-16-01021-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/57bd77fe7264/pharmaceutics-16-01021-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/6605abc9eb98/pharmaceutics-16-01021-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/a3326c20b247/pharmaceutics-16-01021-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/ff1e391c61c7/pharmaceutics-16-01021-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/20bb1d35c533/pharmaceutics-16-01021-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/752df95951d6/pharmaceutics-16-01021-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/57bd77fe7264/pharmaceutics-16-01021-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4ea/11360207/6605abc9eb98/pharmaceutics-16-01021-g006.jpg

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本文引用的文献

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Development of Test Programs for the Biorelevant Characterization of Esophageal-Applied Dosage Forms.用于食管给药剂型生物相关性表征的测试程序的开发
Polymers (Basel). 2023 Aug 17;15(16):3430. doi: 10.3390/polym15163430.
2
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Pharmaceutics. 2021 Jun 2;13(6):828. doi: 10.3390/pharmaceutics13060828.
3
Establishment of a Dissolution Test System for the Biorelevant Characterization of Esophageal Applied Dosage Forms.
建立用于生物相关特征描述的食管应用剂型的溶出度测试体系。
J Pharm Sci. 2022 Jan;111(1):62-68. doi: 10.1016/j.xphs.2021.05.011. Epub 2021 Jun 5.
4
Topically applied mometasone furoate improves dysphagia in adult eosinophilic esophagitis - results from a double-blind, randomized, placebo-controlled trial.局部应用莫米松糠酸酯可改善成人嗜酸性食管炎的吞咽困难 - 来自一项双盲、随机、安慰剂对照试验的结果。
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Development and optimisation of simulated salivary fluid for biorelevant oral cavity dissolution.模拟唾液液体制备及其优化用于口腔生物相关性溶出度研究
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J Control Release. 2020 Nov 10;327:1-7. doi: 10.1016/j.jconrel.2020.08.011. Epub 2020 Aug 8.
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