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Development and Evaluation of oral multiple-unit and single-unit hydrophilic controlled-release systems

机译:口服多单位和单单位亲水控释系统的开发和评估

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摘要

This study compared the release behavior of single-unit (tablets, capsules) and multiple-unit (minitablets in capsules) controlled-release systems of furosemide. The swelling and erosion behaviors of these systems, which contained the swellable hydrophilic polymers sodium alginate (high viscosity) and Carbopol 974P, were compared. Swelling and erosion experiments showed a high degree of swelling and limited erosion for the Carbopol preparations, whereas less swelling but greater erosion was observed for the sodium alginate preparations. The sodium alginate preparations were eroded in 6 hours, while Carbopol preparations exhibited limited erosion within this period of time. These results appear to be attributed to the physicochemical characteristics of the polymers used in this study. Polymer characteristics greatly influenced the release of furosemide (model drug) from the formulations prepared and tested. Sodium alginate had a less pronounced sustained release effect compared with Carbopol (ie, in 8 hours all 3 sodium alginate dosage forms displayed complete release of furosemide, while only 30% of the drug was released from Carbopol dosage forms). Finally, all 3 Carbopol dosage forms (single- and multiple-unit) displayed similar release behavior while sodium alginate dosage forms displayed a different and more distinctive behavior. Minitablets and tablets showed a greater sustained release effect compared with capsules. Evaluation of the release data indicates that the release mechanism for sodium alginate formulations may be attributed to erosion/dissolution, while for Carbopol it may be attributed mainly to polymer relaxation and diffusion of the drug from the polymer surface.
机译:这项研究比较了速尿的单单位(片剂,胶囊)和多单位(胶囊中的迷你片剂)控释系统的释放行为。比较了这些系统的溶胀和侵蚀行为,这些系统包含可溶胀的亲水性聚合物海藻酸钠(高粘度)和Carbopol 974P。溶胀和侵蚀实验表明,Carbopol制剂具有较高的溶胀度和有限的溶蚀度,而藻酸钠制剂则具有较小的溶胀度和较大的溶蚀度。海藻酸钠制剂在6小时内被侵蚀,而Carbopol制剂在这段时间内显示出有限的侵蚀。这些结果似乎归因于这项研究中使用的聚合物的理化特性。聚合物的特性极大地影响了速尿(模型药物)从制备和测试的制剂中的释放。与Carbopol相比,海藻酸钠的缓释作用不太明显(即,所有3种海藻酸钠剂型在8小时内均表现出呋塞米的完全释放,而仅30%的药物从Carbopol剂型中释放)。最后,所有3种Carbopol剂型(单单位和多单位)均显示出相似的释放行为,而藻酸钠剂型则表现出不同且更独特的行为。与胶囊相比,小型片剂和片剂显示出更大的持续释放效果。对释放数据的评估表明,藻酸钠制剂的释放机理可能归因于侵蚀/溶解,而对于卡波普而言,其释放机理可能主要归因于聚合物松弛和药物从聚合物表面的扩散。

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