SOLUBILITY EFFECTS ON DRUG TRANSPORT THROUGH PH-SENSITIVE, SWELLING-CONTROLLED RELEASE SYSTEMS - TRANSPORT OF THEOPHYLLINE AND METOCLOPRAMIDE MONOHYDROCHLORIDE
SOLUBILITY EFFECTS ON DRUG TRANSPORT THROUGH PH-SENSITIVE, SWELLING-CONTROLLED RELEASE SYSTEMS - TRANSPORT OF THEOPHYLLINE AND METOCLOPRAMIDE MONOHYDROCHLORIDE
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DOI：
10.1016/0168-3659(95)00069-k
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发表时间：
1995-11-01
影响因子：
10.8
通讯作者：
PEPPAS, NA
中科院分区：
文献类型：
--
作者：
BETTINI, R;COLOMBO, P;PEPPAS, NA
研究了不同组成的甲基丙烯酸羟乙酯与甲基丙烯酸可溶胀离子共聚物的溶胀行为和溶质迁移。溶胀行为是通过研究溶胀和侵蚀前沿位置以及相关凝胶层随离子组分(MAA)百分比的时间变化来确定的。考察了茶碱和甲氧氯普胺的释药规律。根据受试药物的显著溶解性和它们可能与聚合物基质的结合来解释溶胀和释放行为。结果表明，水凝胶的吸水率主要受电离度的影响，而非电离药物在水凝胶中的扩散仅受聚合物的体积膨胀率控制。对于一元盐酸甲氧氯普胺，药物扩散系数随共聚物组成不同而不同。
The swelling behavior of and solute transport in swellable, ionic copolymers of 2-hydroxyethyl methacrylate and methacrylic acid was studied for a wide range of copolymer compositions. The swelling behavior was determined by investigating the time-dependent change of the swelling and erosion front positions and the associated gel layer as a function of the percentage of the ionic component (MAA). Release of theophylline and metoclopramide-HCl were studied as a function of time. The swelling and release behavior were interpreted in terms of the significant solubility of the drugs tested and their possible association with the polymer matrices. It was concluded that the water uptake was mainly governed by the degree of ionization, and that the diffusion of non-ionized drugs in the hydrogels was controlled only by the volume swelling ratio of the polymer. For metoclopramide monohydrochloride, the drug diffusivity varied with copolymer composition.