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将纤维素衍生物的特性粘数与溶胀亲水性基质片剂的机械敏感性相关联。

Correlating cellulose derivative intrinsic viscosity with mechanical susceptibility of swollen hydrophilic matrix tablets.

机构信息

Lek Pharmaceuticals d.d, Verovškova 57, 1526, Ljubljana, Slovenia.

出版信息

AAPS PharmSciTech. 2012 Sep;13(3):903-10. doi: 10.1208/s12249-012-9811-6. Epub 2012 Jun 19.

Abstract

Hydrophilic matrix tablets are prone to mechanical stress while passing through the gastrointestinal tract, which may result in inappropriate drug-release characteristics. Intrinsic viscosity is a physical polymer property that can be directly compared across various types and grades of polymers and correlated with the mechanical susceptibility of swollen matrix tablets. Five tablet formulations containing different HPMC and HPC polymers were prepared and analyzed using an in vitro glass bead manipulation test. The dissolution rate results were modeled using the Korsmeyer-Peppas equation and a correlation was found between the fit constants k and n, goodness-of-fit measure parameters, and intrinsic viscosity. Moreover, the dissolution profiles were used to calculate the degree of mechanical susceptibility for each formulation, defined as the ratio of the average dissolution rate after manipulation and the initial dissolution rate before manipulation. It was confirmed that an increased intrinsic viscosity polymer value resulted in a decrease in mechanical susceptibility. Considering this, two simple rules were defined for designing robust matrix tablets with respect to mechanical stresses.

摘要

亲水基质片剂在通过胃肠道时容易受到机械应力的影响,这可能导致药物释放特性不合适。特性黏度是一种物理聚合物性质,可以在不同类型和等级的聚合物之间直接比较,并与溶胀基质片剂的机械敏感性相关。制备了包含不同 HPMC 和 HPC 聚合物的五种片剂配方,并使用体外玻璃珠操作测试进行了分析。使用 Korsmeyer-Peppas 方程对溶出速率结果进行建模,并发现拟合常数 k 和 n、拟合度参数以及特性黏度之间存在相关性。此外,还使用溶出曲线计算了每个配方的机械敏感性程度,定义为操作后平均溶出速率与操作前初始溶出速率的比值。证实了聚合物特性黏度值的增加会导致机械敏感性降低。考虑到这一点,针对机械应力,定义了两个设计稳健基质片剂的简单规则。

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本文引用的文献

1
Thermo sensitive behavior of cellulose derivatives in dilute aqueous solutions: from macroscopic to mesoscopic scale.
J Colloid Interface Sci. 2011 May 15;357(2):372-8. doi: 10.1016/j.jcis.2011.02.041. Epub 2011 Feb 22.
2
Physiological parameters for oral delivery and in vitro testing.
Mol Pharm. 2010 Oct 4;7(5):1388-405. doi: 10.1021/mp100149j. Epub 2010 Sep 7.
3
Magnetic marker monitoring: high resolution real-time tracking of oral solid dosage forms in the gastrointestinal tract.
Eur J Pharm Biopharm. 2010 Jan;74(1):93-101. doi: 10.1016/j.ejpb.2009.07.007. Epub 2009 Jul 18.
4
5
Gut instincts: explorations in intestinal physiology and drug delivery.
Int J Pharm. 2008 Dec 8;364(2):213-26. doi: 10.1016/j.ijpharm.2008.05.012. Epub 2008 May 20.
9
A novel in vitro and numerical analysis of shear-induced drug release from extended-release tablets in the fed stomach.
Pharm Res. 2005 Aug;22(8):1215-26. doi: 10.1007/s11095-005-5272-x. Epub 2005 Aug 3.

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