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采用天然聚合物和直接压片法制备水溶性药物基质。

Matrices of water-soluble drug using natural polymer and direct compression method.

作者信息

Rosario Nery L, Ghaly Evone S

机构信息

School of Pharmacy, University of Puerto Rico, P.O. Box 365067, San Juan, Puerto Rico 00936-5067.

出版信息

Drug Dev Ind Pharm. 2002 Sep;28(8):975-88. doi: 10.1081/ddc-120006429.

Abstract

The objective of this research was to find an optimum Carrageenan matrix formulation with the desired drug release and physical properties prepared by direct compression. In order to achieve this, matrices containing 10% theophylline, different Carrageenan level, and different excipient were prepared and evaluated. A selected matrix containing 40% Carrageenan and lactose fast flo was tested for dissolution in three different dissolution media (distilled water, 0.1 N HCl, and phosphate buffer pH 7.4). The same formulation was also tested for dissolution at 50 rpm, 100 rpm, and 150 rpm, and using different dissolution apparatus (Apparatus 1 and 2). All matrices showed a decrease in drug release as the polymer level was increased. Only Avicel PH-101 did not show any significant difference between matrices prepared with 30% and 40% polymer. At 10% polymer level, it appears that the type of diluent used controls the drug release. However, at high polymer level, 30% and 40%, it appears that the polymer level controls the drug release. Phosphate buffer pH 7.4 and 0.1 N HCl increase drug release and appear to increase Carrageenan solubility and decrease gel formation. Also, as the rotational speed of the apparatus was increased, the integrity of the gel layer was decreased, and the release of drug was increased. The drug release from Carrageenan matrices appears to follow the diffusion model for inert matrix up to 90 min. After 90 min, the drug release follows a zero-order model. This study demonstrated that matrices using Carrageenan can be successfully prepared by direct compression.

摘要

本研究的目的是通过直接压片法找到一种具有所需药物释放特性和物理性质的最佳卡拉胶基质配方。为实现这一目标,制备并评估了含有10%茶碱、不同水平卡拉胶和不同辅料的基质。对一种含有40%卡拉胶和乳糖速溶粉的选定基质在三种不同的溶出介质(蒸馏水、0.1 N盐酸和pH 7.4的磷酸盐缓冲液)中进行溶出度测试。还对相同配方在50 rpm、100 rpm和150 rpm转速下以及使用不同的溶出装置(装置1和装置2)进行溶出度测试。随着聚合物水平的提高,所有基质的药物释放均降低。只有微晶纤维素PH - 101在含30%和40%聚合物制备的基质之间未显示出任何显著差异。在聚合物水平为10%时,所用稀释剂的类型似乎控制着药物释放。然而,在高聚合物水平(30%和40%)时,似乎聚合物水平控制着药物释放。pH 7.4的磷酸盐缓冲液和0.1 N盐酸可增加药物释放,似乎还能增加卡拉胶的溶解度并减少凝胶形成。此外,随着装置转速的增加,凝胶层的完整性降低,药物释放增加。卡拉胶基质的药物释放在90分钟内似乎遵循惰性基质的扩散模型。90分钟后,药物释放遵循零级模型。本研究表明,使用卡拉胶的基质可通过直接压片法成功制备。

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