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低聚合度和高聚合度纤维素I与纤维素II辅料的粉末及压片特性的比较评估

Comparative evaluation of powder and tableting properties of low and high degree of polymerization cellulose I and cellulose II excipients.

作者信息

de la Luz Reus Medina Maria, Kumar Vijay

机构信息

Division of Pharmaceutics, College of Pharmacy, The University of Iowa, Iowa City, IA 52242, USA.

出版信息

Int J Pharm. 2007 Jun 7;337(1-2):202-9. doi: 10.1016/j.ijpharm.2007.01.008. Epub 2007 Jan 14.

Abstract

Low and high degree of polymerization (DP) cellulose II powders have been prepared from Avicel PH-102 and Solka Floc 40NF (low and high DP cellulose I powders, respectively), respectively, by treatment with sodium hydroxide (5N) for 24h and their powder and tableting properties investigated. Cellulose II powders, compared to the respective cellulose I counterpart, exhibited lower crystallinity, true density, and specific surface area. They were denser and showed higher moisture uptake. The Heckel analyses revealed both low and high DP cellulose II powders to be less ductile than the low DP cellulose I powder and more ductile compared to the high DP cellulose I powder. The crushing strengths of low and high DP cellulose II powders were comparable to that of the high DP cellulose I powder but lower than the low DP cellulose I powder. When compressed to comparable crushing strengths, the low and high DP cellulose II compacts disintegrated faster in comparison to the corresponding cellulose I compacts. Low DP cellulose I and II powders, compared to the high DP cellulose I counterparts were more sensitive to magnesium stearate. Magnesium stearate decreased the disintegration times of low DP cellulose I compacts but had no effect on the low and high DP cellulose II and high DP cellulose I compacts. In conclusion, low and high DP cellulose II powders, despite their different powder properties, show similar tableting properties, leading to the formation of rapidly disintegrating compacts. The low and high DP cellulose I excipients, in contrast, differ in their powder properties as well as tableting characteristics.

摘要

分别以微晶纤维素PH - 102和Solka Floc 40NF(分别为低聚合度和高聚合度的纤维素I粉末)为原料,通过用5N氢氧化钠处理24小时制备了低聚合度和高聚合度的纤维素II粉末,并对其粉末和压片性能进行了研究。与相应的纤维素I相比,纤维素II粉末表现出较低的结晶度、真密度和比表面积。它们更致密,吸湿率更高。Heckel分析表明,低聚合度和高聚合度的纤维素II粉末的韧性均低于低聚合度的纤维素I粉末,但高于高聚合度的纤维素I粉末。低聚合度和高聚合度的纤维素II粉末的抗压强度与高聚合度的纤维素I粉末相当,但低于低聚合度的纤维素I粉末。当压缩至相当的抗压强度时,低聚合度和高聚合度的纤维素II片剂相比相应的纤维素I片剂崩解更快。与高聚合度的纤维素I相比,低聚合度的纤维素I和II粉末对硬脂酸镁更敏感。硬脂酸镁缩短了低聚合度纤维素I片剂的崩解时间,但对低聚合度和高聚合度的纤维素II以及高聚合度的纤维素I片剂没有影响。总之,低聚合度和高聚合度的纤维素II粉末尽管粉末性质不同,但压片性能相似,可形成快速崩解的片剂。相比之下,低聚合度和高聚合度的纤维素I辅料在粉末性质和压片特性方面存在差异。

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