Sheikh Fatima Akbar, Hussain Muhammad Ajaz, Ashraf Muhammad Umer, Haseeb Muhammad Tahir, Farid-Ul-Haq Muhammad
College of Pharmacy, University of Sargodha, Sargodha 40100, Pakistan.
Department of Chemistry, University of Sargodha, Sargodha 40100, Pakistan.
Saudi Pharm J. 2020 May;28(5):538-549. doi: 10.1016/j.jsps.2020.03.005. Epub 2020 Mar 19.
Herein, we designed a novel gastroretentive drug delivery system as floating matrix tablets based on a polysaccharide material from linseeds ( L.) for fluoroquinolone antibiotics. A number of formulations were designed with a combination of linseed hydrogel (LSH) and different excipients to obtain a desired sustained release profile of moxifloxacin. The drug release study was performed basically at pH 1.2. However, the tablet may pass through the stomach to intestine due to certain reasons then it also offered sustained drug release at intestinal pH 4.5, 6.8 and 7.4, as well. Results indicated that sustained moxifloxacin release was directly proportional to the concentration of LSH and the release of drug followed non-Fickian diffusion. SEM of the tablets indicated porous nature of LSH with elongated channels which contributed to the swelling of the tablet and then facilitated the discharge of moxifloxacin from the core of the tablet. X-ray study was performed to assess disintegration and real-time floating of tablet that confirmed its presence for 6 h in the stomach. These findings indicated that LSH can be used to develop novel gastroretentive sustained release drug delivery systems with the double advantage of sustained drug release at all pH of GIT.
在此，我们设计了一种新型胃滞留药物递送系统，即基于亚麻籽（Linum usitatissimum L.）中的多糖材料制成的漂浮型骨架片，用于递送氟喹诺酮类抗生素。设计了多种含有亚麻籽水凝胶（LSH）和不同辅料的制剂，以获得莫西沙星所需的缓释特性。药物释放研究基本在pH 1.2条件下进行。然而，由于某些原因，该片剂可能会通过胃进入肠道，因此它在肠道pH 4.5、6.8和7.4条件下也能实现药物的持续释放。结果表明，莫西沙星的持续释放与LSH的浓度成正比，且药物释放遵循非菲克扩散。片剂的扫描电子显微镜（SEM）显示LSH具有多孔性质，带有细长通道，这有助于片剂膨胀，进而促进莫西沙星从片剂核心释放。进行了X射线研究以评估片剂的崩解和实时漂浮情况，证实其在胃中存在6小时。这些发现表明，LSH可用于开发新型胃滞留缓释药物递送系统，具有在胃肠道所有pH值下均能持续释放药物的双重优势。
