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Preparation and Characterization of a Novel Co-processed Excipient of Chitin and Crystalline Mannitol

机译:甲壳素和甘露醇结晶共处理新型辅料的制备与表征

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摘要

A co-processed excipient was prepared from commercially available crystalline mannitol and α-chitin using direct compression as well as spray, wet, and dry granulation. The effect of the ratio of the two components, percentage of lubricant and particle size, on the properties of the prepared co-processed excipient has been investigated. α-Chitin forms non-hygroscopic, highly compactable, disintegrable compacts when co-processed with crystalline mannitol. The compaction properties of the co-processed mannitol–chitin mixture were found to be dependent upon the quantity of mannitol added to chitin, in addition to the granulation procedure used. Optimal physicochemical properties of the excipient, from a manufacturing perspective, were obtained using a co-processed mannitol–chitin (2:8, w/w) mixture prepared by wet granulation (Cop-MC). Disintegration time, crushing strength, and friability of tablets, produced from Cop-MC using magnesium stearate as a lubricant, were found to be independent of the particle size of the prepared granules. The inherent binding and disintegration properties of the compressed Cop-MC are useful for the formulation of poorly compressible, high-strength, and low-strength active pharmaceutical ingredients. The ability to co-process α-chitin with crystalline mannitol allows chitin to be used as a valuable industrial pharmaceutical excipient.
机译:使用直接压制以及喷雾,湿法和干法制粒,由市售的结晶甘露醇和α-几丁质制备共处理的赋形剂。研究了两种组分的比例(润滑剂的百分比和粒度)对制备的共加工的赋形剂性能的影响。当与结晶甘露醇共加工时,α-甲壳质形成非吸湿性,高致密性,可崩解的压块。发现共处理的甘露醇-几丁质混合物的压实性能取决于所用的制粒程序,还取决于添加至几丁质的甘露醇的量。从制造的角度来看,使用通过湿法制粒(Cop-MC)制备的共处理的甘露醇-甲壳素(2:8,w / w)混合物可以获得辅料的最佳理化特性。发现使用硬脂酸镁作为润滑剂由Cop-MC生产的片剂的崩解时间,压碎强度和脆性与制备的颗粒的粒径无关。压缩的Cop-MC的固有结合和崩解性质可用于配制可压缩性差,高强度和低强度的活性药物成分。 α-几丁质与结晶甘露醇共加工的能力使几丁质可用作有价值的工业药物赋形剂。

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