Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens.
Acta Pharm. 2020 Mar 1;70(1):49-61. doi: 10.2478/acph-2020-0010.
Modified release of furosemide from tablet formulations is preferred by patients, because of physiological problems, acute diuresis being the most serious, compared to the forms designed for immediate release. With this in view, we aimed at achieving furosemide's longer gastric retention and waste minimization by preparing matrix and compression coated tablets incorporating different grades of Eudragit® and poly(ethylene oxide) (PEO), polyvinylpyrrolidone (PVP) and lactose monohydrate. Dissolution profiles of the new formulations were compared with that of the main stream drug Lasix®, 40 mg tablets. The results indicate that the use of Eudragit® in conjunction with either PVP or lactose monohydrate led to a slower release rate in the intestinal fluids compared to Lasix®. Moreover, furosemide release in the intestinal pH from matrix tablets and compression coated tablets was not noticeably different. Formulations incorporating PEO led to sustained release, in intestinal fluids, which depended on the molecular weight of PEO.
与设计为即刻释放的剂型相比，患者更喜欢将呋塞米制成控释剂型，因为控释剂型可以解决生理方面的问题，其中以急性利尿反应最为严重。基于这一目的，我们旨在通过制备包含不同等级的 Eudragit®和聚环氧乙烷（PEO）、聚乙烯吡咯烷酮（PVP）和乳糖一水合物的基质和压制包衣片剂，实现呋塞米在胃中更长时间的滞留和最小化浪费。将新制剂的溶出曲线与主要药物速尿（Lasix®）40mg 片剂进行了比较。结果表明，与速尿（Lasix®）相比，Eudragit®与 PVP 或乳糖一水合物联合使用，可导致在肠液中的释放速度减慢。此外，基质片剂和压制包衣片剂中在肠道 pH 下的呋塞米释放没有明显差异。包含 PEO 的制剂在肠液中呈现持续释放，其释放速度取决于 PEO 的分子量。
