Department of Pharmaceutics, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur (C.G.) 495 009, India.
Curr Drug Deliv. 2021;18(5):654-668. doi: 10.2174/1567201817666201026105611.
Low bioavailability of anti-diabetic drugs results in the partial absorption of the drug as they are mainly absorbed from the stomach and the lower part of the GIT. Drug bioavailability of anti-diabetic drugs can be significantly increased by prolonging gastric retention time through gastro-retentive dosage form such as floating microspheres.
The study was aimed to develop and characterize resin based floating microspheres of Repaglinide and Metformin for superior and prolonged maintenance of normoglycaemia in type-2 diabetes mellitus.
Repaglinide and metformin were complexed with amberlite resin; later resin complexed drug was encapsulated in Ethylcellulose floating microspheres. Floating microspheres were characterized for morphology, particle size, IR spectroscopy, DSC, in vitro release and buoyancy studies. Further, floating microspheres were tested for in vivo blood glucose reduction potential in Streptozocin- induced diabetic mice.
Floating microspheres had a spherical shape and slightly rough surface with the entrapment efficiency in a range of 49-78% for metformin and 52-73% for repaglinide. DSC studies revealed that no chemical interaction took place between polymer and drugs. Floating microspheres showed good buoyancy behavior (P<0.05) and prolonged drug release as compared to plain drug (P<0.05). The blood glucose lowering effect of floating microspheres on Streptozocin induced diabetic rats was significantly greater (P<0.05) and prolonged (˃12h) and normoglycaemia was maintained for 6hr.
Floating microspheres containing drug resin complex were able to prolong drug release in an efficient way for a sustained period of time; as a result, profound therapeutic response was obtained.
抗糖尿病药物的生物利用度低，导致药物部分吸收，因为它们主要从胃和胃肠道的下部吸收。通过胃滞留剂型（如漂浮微球）延长胃滞留时间，可以显著提高抗糖尿病药物的药物生物利用度。
本研究旨在开发和表征瑞格列奈和二甲双胍的基于树脂的漂浮微球，以在 2 型糖尿病中更好地和延长维持正常血糖水平。
将瑞格列奈和二甲双胍与 Amberlite 树脂络合；随后将络合药物的树脂包裹在乙基纤维素漂浮微球中。对漂浮微球进行形态学、粒径、IR 光谱、DSC、体外释放和漂浮性研究。此外，还测试了漂浮微球在链脲佐菌素诱导的糖尿病小鼠体内降低血糖的潜力。
漂浮微球呈球形，表面略带粗糙，二甲双胍的包封效率在 49-78%之间，瑞格列奈的包封效率在 52-73%之间。DSC 研究表明聚合物和药物之间没有发生化学相互作用。漂浮微球表现出良好的漂浮行为（P<0.05）和延长的药物释放，与普通药物相比（P<0.05）。与普通药物相比，漂浮微球对链脲佐菌素诱导的糖尿病大鼠的降血糖作用显著更强（P<0.05）且持续时间更长（>12 小时），并能维持 6 小时的正常血糖水平。
含有药物树脂复合物的漂浮微球能够以有效的方式延长药物的释放时间，从而获得更深入的治疗效果。
