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通过加入聚乙二醇对微晶纤维素微丸压片行为的调节

Modulation of the tabletting behaviour of microcrystalline cellulose pellets by the incorporation of polyethylene glycol.

作者信息

Nicklasson F, Alderborn G

机构信息

Department of Pharmacy, Uppsala University, Box 580, SE-751 23, Uppsala, Sweden.

出版信息

Eur J Pharm Sci. 1999 Oct;9(1):57-65. doi: 10.1016/s0928-0987(99)00042-1.

Abstract

This study investigated the effect of incorporating a soft material (polyethylene glycol; PEG) into pellets of microcrystalline cellulose (MCC) on the compression behaviour and compactability of the pellets. Low and high porosity MCC pellets were formed. Pellets were also formed from a 1:1 (w/w) mixture of MCC and PEG 6000 to have a porosity equal to that of the low porosity MCC pellets. The degree of compression of the pellets and the porosity, permeability to air and tensile strength of the resulting tablets were determined. Some of the tablets were also deaggregated, and the thickness and porosity of the retrieved pellets were determined. The lowest total tablet porosity was seen with tablets made from pellets containing PEG. The intergranular porosity and the permeability of these tablets were similar to those of tablets made of the high porosity MCC pellets. However, the thickness and porosity of retrieved MCC/PEG pellets were similar to those of the low porosity MCC pellets. The degree of compression levelled off at a lower pressure for the MCC/PEG pellets than for the MCC pellets. Tablet strength values for the MCC/PEG pellets was intermediate between the MCC pellet types and not greatly affected by the applied pressure. It was concluded that the deformation propensity of the pellets was, in general terms, increased due to the presence of the soft material. However, the character of the deformation behaviour changed towards an increased tendency for local deformation during compression, i.e., the ability of adjacent pellet surfaces to conform to each other increased, without marked changes in the main dimensions and porosity of the pellets.

摘要

本研究考察了将软质材料(聚乙二醇;PEG)混入微晶纤维素(MCC)颗粒中对颗粒压缩行为和可压性的影响。制备了低孔隙率和高孔隙率的MCC颗粒。还由MCC与PEG 6000按1:1(w/w)的混合物制成颗粒,使其孔隙率与低孔隙率MCC颗粒的孔隙率相等。测定了颗粒的压缩程度以及所得片剂的孔隙率、透气率和抗张强度。还将一些片剂解聚,并测定回收颗粒的厚度和孔隙率。含PEG颗粒制成的片剂的片剂总孔隙率最低。这些片剂的晶间孔隙率和透气率与高孔隙率MCC颗粒制成的片剂相似。然而,回收的MCC/PEG颗粒的厚度和孔隙率与低孔隙率MCC颗粒的相似。MCC/PEG颗粒在比MCC颗粒更低的压力下压缩程度趋于平稳。MCC/PEG颗粒的片剂强度值介于MCC颗粒类型之间,且受施加压力的影响不大。得出的结论是,一般来说,由于软质材料的存在颗粒的变形倾向增加。然而,变形行为的特征朝着压缩过程中局部变形趋势增加的方向变化,即相邻颗粒表面相互贴合的能力增加,而颗粒的主要尺寸和孔隙率没有明显变化。

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