Innovative approach for improved sustained delivery of metformin hydrochloride for its anti-hyperglycemic activity

M. K. Pillai, S. Pillai, S. Jain
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Abstract

Metformin hydrochloride, an antidiabetic agent, is useful in reducing the blood glucose concentration in Type II diabetes. It is also finding its use as a repurposed drug. The formulations consisted of micro drug delivery systems prepared by emulsification method and were evaluated in-vitro and in-vivo. Process variables like amount of polymer, speed of agitation and stirring, presence or absence of surfactant and cross linker offered a versatile approach towards obtaining the formulation though affected physicochemical properties of formulations. Discrete, spherical, and free-flowing microspheres, in the size range and granularity of 250 to 700µ were used to control the drug release rate. Drug release was diffusion controlled as evident from the Higuchi kinetics. The physical characteristics of the formulations were reproducible. Healthy and alloxan induced hyperglycaemic male albino mice were used for in-vivo experimentation by evaluating plasma glucose level reduction and % reduction in the blood glucose level after administration of pure drug and formulations. The results indicate significant sustained fall in the blood glucose level for about 10 hrs following formulation administration as compared to the pure drug.
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改进盐酸二甲双胍持续给药以提高其抗高血糖活性的创新方法
盐酸二甲双胍是一种抗糖尿病药物,有助于降低 II 型糖尿病患者的血糖浓度。它还被用作再利用药物。制剂由乳化法制备的微给药系统组成,并在体外和体内进行了评估。聚合物用量、搅拌速度、表面活性剂和交联剂的有无等工艺变量为制备配方提供了多种方法,但也影响了配方的理化性质。为控制药物释放率,我们使用了大小和颗粒度在 250 微米到 700 微米之间的离散、球形和自由流动微球。从樋口动力学可以看出,药物释放是由扩散控制的。制剂的物理特性具有可重复性。使用健康和阿脲诱导的高血糖雄性白化小鼠进行体内实验,评估服用纯药物和制剂后血浆葡萄糖水平的降低情况以及血糖水平降低的百分比。结果表明,与纯药相比,制剂给药后血糖水平在约 10 小时内持续明显下降。
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