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2
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本文引用的文献

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1. Commentary on an exponential model for the analysis of drug delivery: Original research article: a simple equation for description of solute release: I II. Fickian and non-Fickian release from non-swellable devices in the form of slabs, spheres, cylinders or discs, 1987.1. 药物递送分析指数模型述评:原创研究文章:溶质释放描述的一个简单方程:I II. 平板、球体、圆柱体或圆盘形式的非溶胀装置中的菲克和非菲克释放,1987年。
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A sugar cane native dextran as an innovative functional excipient for the development of pharmaceutical tablets.一种甘蔗天然葡聚糖作为开发药物片剂的创新功能性辅料。
Eur J Pharm Biopharm. 2008 Feb;68(2):319-29. doi: 10.1016/j.ejpb.2007.04.015. Epub 2007 Apr 29.
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Polysaccharide hydrogels for modified release formulations.用于控释制剂的多糖水凝胶
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Hydrogels in controlled release formulations: network design and mathematical modeling.控释制剂中的水凝胶:网络设计与数学建模
Adv Drug Deliv Rev. 2006 Nov 30;58(12-13):1379-408. doi: 10.1016/j.addr.2006.09.004. Epub 2006 Sep 22.
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Estimation of the percolation thresholds in acyclovir hydrophilic matrix tablets.阿昔洛韦亲水骨架片中渗透阈值的估算
Eur J Pharm Biopharm. 2006 Nov;64(3):336-42. doi: 10.1016/j.ejpb.2006.05.009. Epub 2006 Jul 28.
6
Study of the critical points in lobenzarit disodium hydrophilic matrices for controlled drug delivery.用于控释药物的洛苯达唑二钠亲水基质中的临界点研究。
Chem Pharm Bull (Tokyo). 2006 May;54(5):598-602. doi: 10.1248/cpb.54.598.
7
Development and optimization of a novel sustained-release dextran tablet formulation for propranolol hydrochloride.新型盐酸普萘洛尔缓释右旋糖酐片剂制剂的研发与优化
Int J Pharm. 2006 Jul 6;317(1):32-9. doi: 10.1016/j.ijpharm.2006.02.049. Epub 2006 Apr 11.
8
Study of the critical points of HPMC hydrophilic matrices for controlled drug delivery.用于控释药物的羟丙基甲基纤维素亲水基质的临界点研究。
Int J Pharm. 2006 Mar 27;311(1-2):75-81. doi: 10.1016/j.ijpharm.2005.12.012. Epub 2006 Jan 30.
9
Analysis of macromolecular changes and drug release from hydrophilic matrix systems.亲水性基质系统的大分子变化及药物释放分析
Int J Pharm. 2005 Mar 23;292(1-2):75-85. doi: 10.1016/j.ijpharm.2004.11.011.
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Fronts movement as a useful tool for hydrophilic matrix release mechanism elucidation.前沿运动作为阐明亲水性基质释放机制的有用工具。
Int J Pharm. 2000 Jul 20;202(1-2):21-8. doi: 10.1016/s0378-5173(00)00407-5.

来氟米特二钠天然右旋糖酐基质片剂中渗滤阈值的估算

Estimation of the percolation thresholds in lobenzarit disodium native dextran matrix tablets.

作者信息

Gil Eddy Castellanos, Colarte Antonio Iraizoz, Bataille Bernard, Caraballo Isidoro

机构信息

Center of Pharmaceutical Chemistry, Calle 200, esq 21, Atabey, Playa, Havana, Cuba.

出版信息

AAPS PharmSciTech. 2007 Dec 28;8(4):E115. doi: 10.1208/pt0804115.

DOI:10.1208/pt0804115
PMID:18181536
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2750701/
Abstract

The objective of the present work is to estimate for the first time the percolation threshold of a new series of dextran (native dextran of high molecular weight [B110-1-2, Mw = 2 x 10(6)]), in matrices of lobenzarit disodium (LBD) and to apply the obtained result to the design of hydrophilic matrices for the controlled delivery of this drug. The formulations studied were prepared with different amounts of excipient in the range of 20% to 70% wt/wt. Dissolution studies were performed using the paddle method (100 rpm) and one face water uptake measurements were performed using a modified Enslin apparatus. The Higuchi, zero-order, and Hixson-Crowell models as well as the nonlinear regression model were employed as empiric methods to study the release data. Values of diffusion exponent 0.563 < n < 0.786 (Korsmeyer equation) for dissolution profile and water uptake mechanism 0.715 < n < 1 (Davidson and Peppas equation) suggested anomalous or complex mechanisms. On the other hand, the contribution of the relaxation or erosion and of the diffusive mechanism in Peppas-Sahlin equation indicated that the main mechanism for drug delivery from tablets is swelling controlled delivery (K(r)/K(d) < 1). The critical points observed in kinetic parameters above 58.63% vol/vol of native dextran B110-1-2 plus initial porosity in the LBD-dextran matrices with a relative polymer/drug particle size of 4.17 were attributed to the existence of an excipient percolation threshold.

摘要

本研究的目的是首次估算一系列新型右旋糖酐(高分子量天然右旋糖酐[B110-1-2,Mw = 2×10⁶])在氯苯扎利二钠(LBD)基质中的渗滤阈值,并将所得结果应用于该药物控释亲水基质的设计。所研究的制剂是用20%至70% wt/wt范围内不同量的辅料制备的。使用桨法(100 rpm)进行溶出度研究,并使用改良的恩斯林装置进行单面吸水测量。采用Higuchi模型、零级模型、Hixson-Crowell模型以及非线性回归模型作为经验方法来研究释放数据。溶出曲线的扩散指数值0.563 < n < 0.786(Korsmeyer方程)和吸水机制的扩散指数值0.715 < n < 1(Davidson和Peppas方程)表明存在异常或复杂机制。另一方面,Peppas-Sahlin方程中松弛或侵蚀以及扩散机制的贡献表明,片剂药物释放的主要机制是溶胀控释(K(r)/K(d) < 1)。在天然右旋糖酐B110-1-2体积分数高于58.63%加上LBD-右旋糖酐基质中的初始孔隙率且聚合物/药物颗粒相对尺寸为4.17时观察到的动力学参数临界点,归因于辅料渗滤阈值的存在。