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了解新型直接压片辅料(包含辊压甲壳素)的性能。

Understanding the Performance of a Novel Direct Compression Excipient Comprising Roller Compacted Chitin.

机构信息

Chemical Engineering Department, School of Engineering, University of Jordan, Amman 11942, Jordan.

Research and Innovation Centre, The Jordanian Pharmaceutical Manufacturing Company (JPM), P.O. Box 94, Naor 11710, Jordan.

出版信息

Mar Drugs. 2020 Feb 17;18(2):115. doi: 10.3390/md18020115.

DOI:10.3390/md18020115
PMID:32079246
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7073602/
Abstract

Chitin has been investigated in the context of finding new excipients suitable for direct compression, when subjected to roller compaction. Ball milling was concurrently carried out to compare effects from different energy or stress-inducing techniques. Samples of chitin powders (raw, processed, dried and humidified) were compared for variations in morphology, X-ray diffraction patterns, densities, FT-IR, flowability, compressibility and compactibility. Results confirmed the suitability of roller compaction to convert the fluffy powder of raw chitin to a bulky material with improved flow. X-ray powder diffraction studies showed that, in contrast to the high decrease in crystallinity upon ball milling, roller compaction manifested a slight deformation in the crystal lattice. Moreover, the new excipient showed high resistance to compression, due to the high compactibility of the granules formed. This was correlated to the significant extent of plastic deformation compared to the raw and ball milled forms of chitin. On the other hand, drying and humidification of raw and processed materials presented no added value to the compressibility and compactibility of the directly compressed excipient. Finally, compacted chitin showed direct compression similarity with microcrystalline cellulose when formulated with metronidazole (200 mg) without affecting the immediate drug release action of the drug.

摘要

甲壳素在寻找适合直接压片的新辅料方面受到了研究关注,尤其是在经受滚轮压实处理时。同时进行球磨处理,以比较来自不同能量或应力诱导技术的效果。比较了甲壳素粉末(原始、加工、干燥和加湿)的样品,以观察形态、X 射线衍射图谱、密度、FT-IR、流动性、可压缩性和压缩性的变化。结果证实了滚轮压实适用于将原始甲壳素的蓬松粉末转化为具有改善流动性的块状材料。X 射线粉末衍射研究表明,与球磨过程中结晶度大幅下降相反,滚轮压实使晶格发生轻微变形。此外,由于形成的颗粒具有高压缩性,这种新辅料表现出对压缩的高抵抗力。这与与原始和球磨形式的甲壳素相比,塑性变形的显著程度相关。另一方面,干燥和加湿原始和加工材料对直接压片辅料的可压缩性和压缩性没有增值作用。最后,压结甲壳素与微结晶纤维素在与甲硝唑(200mg)配方时具有直接压片相似性,而不会影响药物的即时药物释放作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/7073602/aa08eb542c4d/marinedrugs-18-00115-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/7073602/033d5d3389e6/marinedrugs-18-00115-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/7073602/b718675907bc/marinedrugs-18-00115-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/7073602/bab5982e53ee/marinedrugs-18-00115-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/7073602/c35270ce43eb/marinedrugs-18-00115-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/7073602/aa08eb542c4d/marinedrugs-18-00115-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/7073602/033d5d3389e6/marinedrugs-18-00115-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/7073602/b718675907bc/marinedrugs-18-00115-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/7073602/bab5982e53ee/marinedrugs-18-00115-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/7073602/c35270ce43eb/marinedrugs-18-00115-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/7073602/aa08eb542c4d/marinedrugs-18-00115-g008.jpg

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