Department of Pharmaceutical Technology and Raw Materials Development, National Institute for Pharmaceutical Research and Development, Abuja, Nigeria.
Int J Pharm. 2010 Mar 30;388(1-2):159-67. doi: 10.1016/j.ijpharm.2009.12.056. Epub 2010 Jan 8.
The choice of excipients remains a critical factor in pharmaceutical formulations. Microcrystalline cellulose-maize starch composites (MCC-Mst) have been prepared by mixing colloidal dispersions of microcrystalline cellulose (MCC) with 10% (w/w) of chemically gelatinized maize starch (Mst) at controlled temperature conditions for use as multifunctional excipients with direct compression and enhanced disintegration abilities. The novel excipient was evaluated for its direct compression and enhanced disintegrant properties and the result compared with the properties of the individual components. Some of its physicochemical and thermal properties were also determined together with effects of freeze-thaw cycles of processing on the functional and physicochemical properties. The scanning electron micrograph (SEM) shows that the particles of the MCC-Mst were irregular in shape and multiparticulate with a marked degree of asperity. The indirect assessment of the powder flow properties as determined by Carr's compressibility index and angle of repose showed that the MCC-Mst possesses better flow compared with MCC and Mst. MCC-Mst is moderately hygroscopic and shows a Type III moisture sorption isotherm. The FT-IR spectra and DSC thermograms of the composite were different from those of MCC and Mst. The hardness of aspirin tablets was enhanced by incorporating MCC-Mst and MCC, but was reduced by Mst. While the tablets prepared with MCC-Mst and Mst disintegrated within 7min, aspirin compacts devoid of any excipient and those prepared with MCC did not disintegrate even after 2h. Acetaminophen compacts prepared with MCC and MCC-Mst showed similar compact hardness characteristics and loading properties. The loading capacity of the different samples of the composite decreased with increase in the freeze-thaw cycles. The loading capacity of the different materials as assessed by their compact hardness efficiency can be represented as follows (MCC>T0>T1>T4>T3>T2>Mst). Generally, the different samples of MCC-Mst are characterized by physicochemical and functional properties that are similar at different degrees to MCC and Mst.
辅料的选择仍然是药物制剂的一个关键因素。微晶纤维素-玉米淀粉复合材料（MCC-Mst）是通过将胶体分散的微晶纤维素（MCC）与 10%（w/w）化学胶凝化的玉米淀粉（Mst）混合在受控温度条件下制备的，用作具有直接压缩和增强崩解能力的多功能赋形剂。该新型赋形剂的直接压缩和增强崩解性能进行了评价，并与各成分的性能进行了比较。还确定了其一些物理化学和热性质，以及加工过程中冻融循环对功能和物理化学性质的影响。扫描电子显微镜（SEM）显示，MCC-Mst 的颗粒形状不规则，呈多颗粒状，表面粗糙度明显。通过 Carr 可压缩性指数和休止角间接评估粉末流动性能表明，MCC-Mst 的流动性能优于 MCC 和 Mst。MCC-Mst 具有中等吸湿性，并表现出 III 型水分吸附等温线。复合材料的 FT-IR 光谱和 DSC 热图谱与 MCC 和 Mst 的不同。阿司匹林片剂的硬度通过加入 MCC-Mst 和 MCC 得到增强，但通过 Mst 降低。虽然含有 MCC-Mst 和 Mst 的片剂在 7 分钟内崩解，但不含任何赋形剂的阿司匹林片剂和含有 MCC 的片剂甚至在 2 小时后也没有崩解。含有 MCC 和 MCC-Mst 的对乙酰氨基酚片剂表现出相似的片剂硬度特性和载药量。不同样品的载药量随着冻融循环次数的增加而降低。通过其片剂硬度效率评估不同材料的载药量，可以表示为如下顺序（MCC>T0>T1>T4>T3>T2>Mst）。一般来说，不同样品的 MCC-Mst 具有物理化学和功能性质，在不同程度上与 MCC 和 Mst 相似。
