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Evaluation of Chitosan-Microcrystalline Cellulose Blends as Direct Compression Excipients

机译:壳聚糖-微晶纤维素共混物作为直接压缩赋形剂的评估

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摘要

This study was aimed at evaluating chitosan-microcrystalline cellulose blends as direct compression excipients. Crab shell chitosan, α-lactose monohydrate, and microcrystalline cellulose powders were characterized. Blends of the microcrystalline cellulose and chitosan in ratios 9 : 1, 4 : 1, 2 : 1, and 1 : 1 as direct compression excipients were made to constitute 60% of metronidazole tablets. Similar tablets containing blends of the microcrystalline cellulose and α-lactose monohydrate as well as those containing pure microcrystalline cellulose were also produced. The compact density, tensile strength, porosity, disintegration time, and dissolution rate of tablets were determined. Chitosan had higher moisture content (7.66%) and higher moisture sorption capacity (1.33%) compared to microcrystalline cellulose and lactose. It also showed better flow properties (Carr's index of 18.9% and Hausner's ratio of 1.23). Compact density of tablets increased but tensile strength decreased with increase in the proportion of chitosan in the binary mixtures. In contrast to lactose, the disintegration time increased and the dissolution rate decreased with increase in the proportion of chitosan. This study has shown that chitosan promotes flowability of powder mix and rapid disintegration of tablet. However, incorporation of equal proportions of microcrystalline cellulose and chitosan leads to production of extended-release tablet. Therefore, chitosan promotes tablet disintegration at low concentration and enables extended-release at higher concentration.
机译:这项研究旨在评估壳聚糖-微晶纤维素共混物作为直接压片赋形剂。表征了壳壳聚糖,α-乳糖一水合物和微晶纤维素粉末。使微晶纤维素和壳聚糖以直接压缩赋形剂的比例为9 1:1,4 -1 ∶1、2 2:1,和1 ∶1:1的共混物构成甲硝唑片剂的60%。还生产了包含微晶纤维素和α-乳糖一水合物的混合物的类似片剂以及包含纯微晶纤维素的片剂。测定片剂的紧密密度,抗张强度,孔隙率,崩解时间和溶解速率。与微晶纤维素和乳糖相比,壳聚糖具有较高的水分含量(7.66%)和较高的水分吸收能力(1.33%)。它还显示出更好的流动性能(卡尔指数为18.9%,豪斯纳比为1.23)。随着二元混合物中壳聚糖比例的增加,片剂的致密密度增加,但抗张强度降低。与乳糖相反,随着壳聚糖比例的增加,崩解时间增加,溶出度降低。这项研究表明,壳聚糖可促进粉末混合物的流动性和片剂的快速崩解。然而,等比例的微晶纤维素和壳聚糖的掺入导致生产缓释片剂。因此,壳聚糖在低浓度下促进片剂崩解,并在较高浓度下可延长释放。

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