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Linseed hydrogel based floating drug delivery system for fluoroquinolone antibiotics: Design, in vitro drug release and in vivo real-time floating detection.
Saudi Pharmaceutical Journal ( IF 4.1 ) Pub Date : 2020-03-19 , DOI: 10.1016/j.jsps.2020.03.005
Fatima Akbar Sheikh 1 , Muhammad Ajaz Hussain 2 , Muhammad Umer Ashraf 3 , Muhammad Tahir Haseeb 1 , Muhammad Farid-Ul-Haq 2
Affiliation  

Herein, we designed a novel gastroretentive drug delivery system as floating matrix tablets based on a polysaccharide material from linseeds (Linum usitatissimum 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. In vivo 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.



中文翻译:

基于亚麻籽水凝胶的氟喹诺酮类抗生素浮动药物输送系统:设计,体外药物释放和体内实时浮动检测。

本文中,我们基于亚麻籽(Linum usitatissimum)的多糖材料,设计了一种新型的胃滞留药物输送系统,作为漂浮基质片剂。L.)用于氟喹诺酮类抗生素。使用亚麻籽水凝胶(LSH)和不同的赋形剂组合设计了许多制剂,以获得所需的莫西沙星缓释曲线。药物释放研究基本上在pH 1.2下进行。但是,由于某些原因,片剂可能会通过胃部进入肠道,然后在肠道pH 4.5、6.8和7.4时也能持续释放药物。结果表明,莫西沙星的持续释放与LSH的浓度成正比,药物的释放遵循非Fickian扩散。片剂的SEM表明LSH具有延长的通道的多孔性质,其促成片剂的溶胀,然后促进莫西沙星从片剂核心的排出。体内进行了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可用于开发新型的胃滞缓缓释药物递送系统,其在GIT的所有pH下均具有缓释药物的双重优势。

更新日期:2020-03-19
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