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润湿、干燥及微晶纤维素类型对微丸机械强度和崩解的综合影响

Combined effects of wetting, drying, and microcrystalline cellulose type on the mechanical strength and disintegration of pellets.

作者信息

Balaxi Maria, Nikolakakis Ioannis, Kachrimanis Kyriakos, Malamataris Stavros

机构信息

Department of Pharmaceutical Technology, School of Pharmacy, University of Thessaloniki, Thessaloniki, Greece.

出版信息

J Pharm Sci. 2009 Feb;98(2):676-89. doi: 10.1002/jps.21454.

DOI:10.1002/jps.21454
PMID:18548618
Abstract

Effects of wetting and drying conditions on micromeritic, mechanical and disintegration properties of microcrystalline cellulose (MCC) pellets were evaluated. Extrusion/spheronization and three drying methods (fluidized bed, microwaves, and freeze drying) were applied using two wetting liquids (water or water-isopropanol 60:40 w/w) and three MCC types: (standard, silicified, and modified). Additionally, the effects of drying method were compared on highly porous pellets prepared by the incorporation and extraction of pore former (NaCl). It was found that the drying method has the greatest effect on the pellet size and porosity followed by the wetting liquid. The modification of MCC resulted in reduced water retention ability, implying hornification, increased porosity, reduced resistance to deformation and tensile strength of pellets. The disintegration time also decreased markedly due to the modification but only in the low porosity range <37%. Silicification increased greatly the disintegration time of the low porosity pellets (<14%). Combination of water-isopropanol, freeze drying and modified MCC gave the greatest increase in pellet size and porosity. The increase in pellet porosity caused exponential reduction in the resistance to deformation, tensile strength and disintegration time, as expected. Compared to fluidized bed, the freeze drying resulted in 20-30% higher porosity for pellets prepared without pore former and 6% for those with pore former, indicating the possibility of preparing highly porous pellets by employing freeze drying.

摘要

评估了润湿和干燥条件对微晶纤维素(MCC)微丸的粉体学、机械性能及崩解性能的影响。使用两种润湿液体(水或水-异丙醇60:40 w/w)和三种MCC类型(标准型、硅化型和改性型),采用挤出/滚圆法及三种干燥方法(流化床干燥、微波干燥和冷冻干燥)。此外,还比较了干燥方法对通过加入和提取致孔剂(NaCl)制备的高孔隙率微丸的影响。结果发现,干燥方法对微丸尺寸和孔隙率的影响最大,其次是润湿液体。MCC的改性导致保水能力降低,意味着角质化,孔隙率增加,微丸的抗变形性和拉伸强度降低。由于改性,崩解时间也显著缩短,但仅在低孔隙率范围(<37%)内。硅化极大地增加了低孔隙率微丸(<14%)的崩解时间。水-异丙醇、冷冻干燥和改性MCC的组合使微丸尺寸和孔隙率增加最多。正如预期的那样,微丸孔隙率的增加导致抗变形性、拉伸强度和崩解时间呈指数下降。与流化床干燥相比,冷冻干燥使未添加致孔剂制备的微丸孔隙率提高20-30%,添加致孔剂的微丸孔隙率提高6%,这表明采用冷冻干燥制备高孔隙率微丸是可能的。

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