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药物的离子化对使用Capmul MCM和辛酸制备的自微乳化药物传递系统（SMEDDS）中药物增溶的影响。

Effect of ionization of drug on drug solubilization in SMEDDS prepared using Capmul MCM and caprylic acid.

作者信息

Li Suhua, Madan Parshotam, Lin Senshang

机构信息

College of Pharmacy and Health Sciences, St. John's University, Queens, NY, USA.

出版信息

Asian J Pharm Sci. 2017 Jan;12(1):73-82. doi: 10.1016/j.ajps.2016.10.001. Epub 2016 Nov 3.

DOI:10.1016/j.ajps.2016.10.001
PMID:32104316
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7032218/
Abstract

The purpose of this study was to investigate the effect of ionization of drug on drug solubilization in SMEDDS (self-microemulsifying drug delivery system) prepared using Capmul MCM and caprylic acid. Solubilization capacity of blank SMEDDS dispersions for danazol, indomethacin and haloperidol as model drugs was determined. Based on the outcomes of solubilization capacity study, drug-loaded SMEDDS formulations were prepared and subjected to dispersion/precipitation study and droplet size analysis. Blank SMEDDS dispersions exhibited the highest solubilization capacity for haloperidol followed by indomethacin and danazol. Furthermore, the solubilization of the three drugs in blank SMEDDS dispersions was explained by a modified mathematical model. Dispersion/precipitation studies indicate that drug-loaded SMEDDS formulations exhibited superiority in solubilizing the drugs in comparison to their respective drug powder. In addition, indomethacin and haloperidol were found to reduce the droplet size of the microemulsions while danazol did not affect droplet size formation for drug-loaded SMEDDS formulations. These findings suggest that ionization of drug affects drug solubilization, droplet size formation, drug loading and drug dispersion/precipitation profiles for the SMEDDS formulations.

摘要

本研究的目的是考察药物离子化对使用Capmul MCM和辛酸制备的自微乳化药物递送系统（SMEDDS）中药物增溶的影响。测定了空白SMEDDS分散体对作为模型药物的达那唑、吲哚美辛和氟哌啶醇的增溶能力。基于增溶能力研究的结果，制备了载药SMEDDS制剂，并进行了分散/沉淀研究和粒径分析。空白SMEDDS分散体对氟哌啶醇的增溶能力最高，其次是吲哚美辛和达那唑。此外，用改进的数学模型解释了三种药物在空白SMEDDS分散体中的增溶情况。分散/沉淀研究表明，载药SMEDDS制剂在增溶药物方面比其各自的药物粉末表现出优势。此外，发现吲哚美辛和氟哌啶醇可减小微乳液的粒径，而达那唑对载药SMEDDS制剂的粒径形成没有影响。这些发现表明，药物离子化会影响SMEDDS制剂的药物增溶、粒径形成、药物负载和药物分散/沉淀情况。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/99e6530d1758/ajps412-fig-0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/4a7f6597f96f/ajps412-ga-5001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/dec621e038bf/ajps412-fig-0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/f6519783057d/ajps412-fig-0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/2dd63a2166ad/ajps412-fig-0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/9bdc3cf53e55/ajps412-fig-0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/e9f7563094eb/ajps412-fig-0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/421c50bcd75e/ajps412-fig-0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/99e6530d1758/ajps412-fig-0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/4a7f6597f96f/ajps412-ga-5001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/dec621e038bf/ajps412-fig-0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/f6519783057d/ajps412-fig-0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/2dd63a2166ad/ajps412-fig-0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/9bdc3cf53e55/ajps412-fig-0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/e9f7563094eb/ajps412-fig-0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/421c50bcd75e/ajps412-fig-0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36bc/7032218/99e6530d1758/ajps412-fig-0007.jpg

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本文引用的文献

1
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Pharm Dev Technol. 2015 Nov;20(7):886-896. doi: 10.3109/10837450.2014.943408. Epub 2014 Jul 25.
2
Supersolubilization and amorphization of a model basic drug, haloperidol, by interaction with weak acids.通过与弱酸相互作用实现模型碱性药物氟哌啶醇的超增溶和非晶化。
Pharm Res. 2013 Jun;30(6):1561-73. doi: 10.1007/s11095-013-0994-7. Epub 2013 Feb 21.
3
Enhancing the intestinal absorption of poorly water-soluble weak-acidic compound by controlling local pH.通过控制局部pH值提高难溶性弱酸性化合物的肠道吸收。
Drug Dev Ind Pharm. 2013 Dec;39(12):1887-94. doi: 10.3109/03639045.2012.668911. Epub 2012 Mar 26.
4
To evaluate the effect of addition of an anionic surfactant on solid dispersion using model drug indomethacin.评价在固体分散体中加入阴离子表面活性剂对模型药物吲哚美辛的作用。
Drug Dev Ind Pharm. 2012 Aug;38(8):930-9. doi: 10.3109/03639045.2011.633264. Epub 2011 Nov 15.
5
A comparative evaluation of mono-, di- and triglyceride of medium chain fatty acids by lipid/surfactant/water phase diagram, solubility determination and dispersion testing for application in pharmaceutical dosage form development.通过脂质/表面活性剂/水相图、溶解度测定和分散试验对中链脂肪酸的单、二和三甘油酯进行比较评价，用于药物剂型开发。
Pharm Res. 2012 Jan;29(1):285-305. doi: 10.1007/s11095-011-0541-3. Epub 2011 Aug 23.
6
Design of lipid-based formulations for oral administration of poorly water-soluble drugs: precipitation of drug after dispersion of formulations in aqueous solution.用于口服难溶性药物的基于脂质的制剂设计：制剂在水溶液中分散后药物的沉淀。
J Pharm Sci. 2009 Oct;98(10):3582-95. doi: 10.1002/jps.21659.
7
Salt formation to improve drug solubility.通过盐形成来提高药物溶解度。
Adv Drug Deliv Rev. 2007 Jul 30;59(7):603-16. doi: 10.1016/j.addr.2007.05.010. Epub 2007 May 29.
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When poor solubility becomes an issue: from early stage to proof of concept.当溶解度差成为一个问题时：从早期阶段到概念验证。
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Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs.脂质及基于脂质的制剂：优化亲脂性药物的口服给药
Nat Rev Drug Discov. 2007 Mar;6(3):231-48. doi: 10.1038/nrd2197.
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Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system.口服难溶性药物的制剂：物理化学和生理学问题以及脂质制剂分类系统
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