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亲脂性膜与尺寸排阻膜的比较：供体室中搅拌和环糊精的影响。

Comparison of lipophilic and size-exclusion membranes: the effect of stirring and cyclodextrin in the donor compartment.

作者信息

Tőzsér Petra, Kádár Szabina, Szabó Edina, Dobó Máté, Tóth Gergő, Balogh György T, Sóti Péter, Sinkó Bálint, Borbás Enikő

机构信息

Department of Organic Chemistry and Technology, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, 3 Műegyetem Quay, H-1111, Budapest, Hungary.

Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Semmelweis University, 9 Hőgyes Endre Street., H-1092, Budapest, Hungary.

出版信息

ADMET DMPK. 2025 Jul 5;13(4):2753. doi: 10.5599/admet.2753. eCollection 2025.

DOI:10.5599/admet.2753
PMID:40786063
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12335304/
Abstract

BACKGROUND AND PURPOSE

The effective transport of an active pharmaceutical ingredient across various membrane systems is critical for enhancing its bioavailability, especially in formulations involving solubilizing agents. This study aims to investigate the permeability differences of carvedilol (CAR) between lipophilic and size-exclusion membranes in the presence of hydroxypropyl-beta-cyclodextrin (HP-β-CD) using side-by-side diffusion cell assays.

EXPERIMENTAL APPROACH

Solubility and permeability assays confirmed that HP-β-CD significantly enhanced the solubility of CAR, while simultaneously decreasing its permeability, indicating an interplay between the two parameters.

KEY RESULTS

A mathematical model based on Fick's first law of diffusion was developed to describe drug transport across the UWL, and generally through the UWL-membrane system, with a particular focus on the role of solubilizing agents.

CONCLUSION

Results from both the UWL and membrane limited transport conditions demonstrated that the supersaturation ratio (SSR, defined as the ratio of the drug concentration present in solution to its thermodynamic solubility measured in exactly the same media) between donor and acceptor compartments is the real driving force of the transport, when the complexing agent and the drug- HP-β-CD complex does not penetrate the membrane or the permeation of the solubilizing additive through the membrane is relatively slow, so it does not affect the transport of the API substantially.

摘要

背景与目的

活性药物成分在各种膜系统中的有效转运对于提高其生物利用度至关重要，尤其是在涉及增溶剂的制剂中。本研究旨在使用并排扩散池试验，研究在羟丙基-β-环糊精（HP-β-CD）存在的情况下，卡维地洛（CAR）在亲脂性膜和尺寸排阻膜之间的渗透性差异。

实验方法

溶解度和渗透性试验证实，HP-β-CD显著提高了CAR的溶解度，同时降低了其渗透性，表明这两个参数之间存在相互作用。

关键结果

建立了一个基于菲克第一扩散定律的数学模型，以描述药物通过未搅拌层的转运，以及一般通过未搅拌层-膜系统的转运，特别关注增溶剂的作用。

结论

未搅拌层和膜限制转运条件下的结果均表明，当络合剂与药物-HP-β-CD络合物不穿透膜或增溶添加剂通过膜的渗透相对较慢，因此基本不影响活性药物成分的转运时，供体和受体隔室之间的过饱和比（SSR，定义为溶液中药物浓度与其在完全相同介质中测得的热力学溶解度之比）是转运的真正驱动力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/791033847c57/ADMET-13-2753-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/a84b09d2301a/ADMET-13-2753-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/bcb276af6a9d/ADMET-13-2753-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/52fee275569d/ADMET-13-2753-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/81293c27609a/ADMET-13-2753-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/1502dcc03965/ADMET-13-2753-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/1e61a8be0ce3/ADMET-13-2753-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/71dca44f0d1a/ADMET-13-2753-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/a67a6848163d/ADMET-13-2753-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/b8fbe6888e52/ADMET-13-2753-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/791033847c57/ADMET-13-2753-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/a84b09d2301a/ADMET-13-2753-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/bcb276af6a9d/ADMET-13-2753-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/52fee275569d/ADMET-13-2753-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/81293c27609a/ADMET-13-2753-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/1502dcc03965/ADMET-13-2753-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/1e61a8be0ce3/ADMET-13-2753-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/71dca44f0d1a/ADMET-13-2753-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/a67a6848163d/ADMET-13-2753-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/b8fbe6888e52/ADMET-13-2753-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e64/12335304/791033847c57/ADMET-13-2753-g010.jpg

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