聚乙二醇-6000 -硬脂酸共磨法制备二水阿奇霉素固体分散体及评价

Q2 Pharmacology, Toxicology and Pharmaceutics Science and Technology Indonesia Pub Date : 2023-04-15 DOI:10.26554/sti.2023.8.2.312-320
M. Mardiyanto, Budi Untari, A. Mara, Nauval Hady Prasetyo
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引用次数: 0

摘要

阿奇霉素是一种窄谱细菌生长抑制抗生素,来源于大环内酯类,在水中的溶出度较低。已经采用了几种方法来提高药物的溶解性,其中之一是固体分散。固体分散体是由一种或多种活性物质在惰性载体中组成的混合物。本研究的目的是确定用PEG-6000聚合物和硬脂酸形成固体分散体对提高阿奇霉素溶解速率的影响。形成固体分散体的方法使用共研磨方法。阿奇霉素的固体分散体以四种配方制备,PEG 6000的量不同。对阿奇霉素固体分散体样品进行了XRD、FTIR、SEM、溶解度测试和溶出度测试。对共研磨制备的阿奇霉素固体分散体的测试结果表明,PEG 6000的用量对降低阿奇霉素晶体强度有影响,阿奇霉素与载体之间没有化学相互作用,纯阿奇霉素粉末和固体分散体形态存在差异,以及固体分散体在介质SIF中的溶解增加。
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Formulation and Evaluation of Azithromycin Dihydrate Solid Dispersion with Esther of Polyethylene Glycol-6000 and Stearic Acid Using A Co-Grinding Technique
Azithromycin is a narrow-spectrum bacterial growth inhibitory antibiotic derived from macrolides with low dissolution in water. Several methods have been carried out to increase the dissolution of medicinal substances, one of which is solid dispersion. Solid dispersions are mixtures consisting of one or more active substances in an inert carrier. The purpose of this study was to determine the effect of formatting solid dispersions with PEG 6000 polymer and stearic acid on increasing the dissolution rate of azithromycin. The method of formatting solid dispersions uses the co-grinding method. Solid dispersion of azithromycin was prepared in four formulas with variations in the amount of PEG 6000. Tests carried out on solid dispersion samples of azithromycin were XRD, FTIR, SEM, solubility tests, and dissolution tests. Test results on azithromycin solid dispersions prepared by co-grinding showed that there was an effect of the amount of PEG 6000 on decreasing the intensity of azithromycin crystals, there was no chemical interaction between azithromycin and the carrier, differences in the morphology of pure azithromycin powder and solid dispersions, and an increase in the dissolution of solid dispersions in medium SIF.
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来源期刊
Science and Technology Indonesia
Science and Technology Indonesia Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.80
自引率
0.00%
发文量
72
审稿时长
8 weeks
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