Modified‐release systems have been evaluated as an option to formulations that employ the conventional delivery system and, therefore, may present side effects and reduced therapeutic efficacy. In general, it is more convenient to modify the release of existing drugs to overcome their drawbacks, since developing a new drug can be a quite expensive and time‐consuming process. Furosemide, a drug for hypertension treatment, when administered in the conventional form, can cause inconvenience to patients due to short and intense periods of diuresis and the need for multiple daily administrations due to its short half‐life. In order to modify its release, in the present work, furosemide was successfully incorporated into sericin/alginate matrix prepared by ionic gelation and modified by thermal or covalent cross‐linking, through the addition of proanthocyanidin, achieving high incorporations rates. This polymeric matrix provided a delayed and sustained release form for furosemide, which could improve patients' compliance to treatment and decrease its side effect. Furosemide release study demonstrated that the cross‐linking method affects the amount of dosage release and does not affect the release time, but the presence of sericin does. scanning electron microscopy, X‐ray diffraction, and FT‐IR analyses confirmed furosemide incorporation. The drug thermal stability was not affected by its incorporation and the particle size was considered suitable for multiparticulate system.

中文翻译：

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负载呋塞米的丝胶/藻酸盐微珠的合成和表征，经过热或化学交联以延迟和持续释放

改良释放系统已被评估为采用传统递送系统的制剂的一种选择，因此可能会出现副作用并降低治疗效果。通常，修改现有药物的释放以克服它们的缺点更为方便，因为开发新药可能是一个非常昂贵且耗时的过程。速尿是一种用于高血压治疗的药物，当以常规形式给药时，由于利尿的时间短而激烈，会给患者带来不便，并且由于其半衰期短，因此需要每日多次给药。为了改变其释放效果，在目前的工作中，速尿成功地通过离子凝胶化并通过热或共价交联改性了的丝胶蛋白/藻酸盐基质中，通过添加原花色素，达到很高的掺入率。这种聚合物基质为呋塞米提供了缓释和持续释放的形式，可改善患者对治疗的依从性并减少其副作用。速尿释放研究表明，交联方法影响剂量释放的量，并且不影响释放时间，但是丝胶的存在会影响剂量释放。扫描电子显微镜，X射线衍射和FT-IR分析证实了呋塞米的结合。药物的热稳定性不受其掺入的影响，并且其粒径被认为适用于多颗粒系统。顺应治疗并减少其副作用。速尿释放研究表明，交联方法影响剂量释放的量，并且不影响释放时间，但是丝胶的存在会影响剂量释放。扫描电子显微镜，X射线衍射和FT-IR分析证实了呋塞米的结合。药物的热稳定性不受其掺入的影响，并且其粒径被认为适用于多颗粒系统。顺应治疗并减少其副作用。速尿释放研究表明，交联方法影响剂量释放的量，并且不影响释放时间，但是丝胶的存在会影响剂量释放。扫描电子显微镜，X射线衍射和FT-IR分析证实了呋塞米的结合。药物的热稳定性不受其掺入的影响，并且认为粒径适合于多颗粒系统。