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氢氯噻嗪的药物组合物：β-环糊精：通过三种不同方法制备、物理化学特性描述和体内利尿活性评价。

Pharmaceutical composition of hydrochlorothiazide:β-cyclo-dextrin: preparation by three different methods, physico-chemical characterization and in vivo diuretic activity evaluation.

机构信息

Departamento de Química, ICEx, Universidade Federal de Minas Gerais, Avenida Pres. Antônio Carlos 6627, 31270-901 Belo Horizonte, Brazil.

出版信息

Molecules. 2011 May 27;16(6):4482-99. doi: 10.3390/molecules16064482.

DOI:10.3390/molecules16064482
PMID:21623317
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6264165/
Abstract

Hydrochlorothiazide is a common diuretic antihypertensive drug of the thiazide family. Its poor aqueous solubility is one of the reasons for its limited bioavailability after oral administration. This work aimed at the development of a hydrochlorothiazide:β-cyclodextrin (HTZ:β-CD) pharmaceutical composition in order to improve water solubility and bioavailability of the drug. The HTZ:β-CD complexes were prepared by three different methods: spray-drying, freeze-drying and fluid bed. Complexes were characterized by thermal analysis, Fourier transform-infrared (FTIR) spectroscopy, powder X-ray diffractometry, NMR (2D-ROESY), scanning electron microscopy (SEM), particle analysis and intrinsic dissolution. The findings reveal that three binary systems prepared presented better solubility results in comparison with free HTZ. Increased diuretic effect was observed to HTZ:β-CD obtained by fluid bed in comparison to free drug in rats. Results taken together suggest that pharmacological effect of HTZ in complex was increased by solubility improvement promoted by cyclodextrin.

摘要

氢氯噻嗪是噻嗪类家族中常见的一种利尿剂降压药。其较差的水溶性是口服后生物利用度有限的原因之一。本工作旨在开发氢氯噻嗪：β-环糊精（HTZ：β-CD）药物组合物，以提高药物的水溶性和生物利用度。通过三种不同的方法制备 HTZ：β-CD 配合物：喷雾干燥、冷冻干燥和流化床。通过热分析、傅里叶变换红外（FTIR）光谱、粉末 X 射线衍射、NMR（2D-ROESY）、扫描电子显微镜（SEM）、颗粒分析和内部分散度对配合物进行了表征。研究结果表明，与游离 HTZ 相比，三种二元体系的制备表现出更好的溶解度。与游离药物相比，在大鼠中发现流化床制备的 HTZ：β-CD 具有更好的利尿效果。综合结果表明，通过环糊精促进的溶解度提高，HTZ 在复合物中的药理作用增强。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/9875c50c89db/molecules-16-04482-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/444fbf366766/molecules-16-04482-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/ac7a9b19e4c1/molecules-16-04482-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/3778c07b784f/molecules-16-04482-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/720322f33053/molecules-16-04482-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/b4bbcf9998f2/molecules-16-04482-g005a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/6d3230e86dfc/molecules-16-04482-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/0e5f29b4b1f6/molecules-16-04482-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/f03ef7d5f90a/molecules-16-04482-g008a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/d958f1e51975/molecules-16-04482-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/ac1cbcbacc01/molecules-16-04482-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/7c99332e51b5/molecules-16-04482-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/516f756d3261/molecules-16-04482-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/9875c50c89db/molecules-16-04482-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/444fbf366766/molecules-16-04482-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/ac7a9b19e4c1/molecules-16-04482-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/3778c07b784f/molecules-16-04482-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/720322f33053/molecules-16-04482-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/b4bbcf9998f2/molecules-16-04482-g005a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/6d3230e86dfc/molecules-16-04482-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/0e5f29b4b1f6/molecules-16-04482-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/f03ef7d5f90a/molecules-16-04482-g008a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/d958f1e51975/molecules-16-04482-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/ac1cbcbacc01/molecules-16-04482-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/7c99332e51b5/molecules-16-04482-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/516f756d3261/molecules-16-04482-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ea6/6264165/9875c50c89db/molecules-16-04482-g013.jpg

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