乳液溶剂蒸发法制备格列本脲负载醋酸纤维素微颗粒的表征

Sarath Chandiran Irisappan , Balagani Pavan Kumar , Korlakanti Narasimha Jayaveera
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引用次数: 7

摘要

目的制备格列本脲微囊化制剂,并对其进行评价。方法以醋酸纤维素为原料,采用乳液溶剂蒸发法制备微颗粒,并对微颗粒性能、包封效率、粒径、载药量、FTIR、DSC、SEM等进行表征。在磷酸盐缓冲液(pH 7.4)中进行体外释放研究。稳定性研究是按照ICH指南进行的。结果溶剂蒸发法制备的微颗粒具有自由流动性质。微颗粒的平均粒径为132.54 ~ 178.44 μm,封装效率为89.96 ~ 98.48%。红外光谱和差示扫描量热图证实了格列本脲在载药微粒中的稳定性。扫描电镜显示,微颗粒为球形。体外释放实验表明,格列本脲的释放持续时间长达12 h。优化后的格列本脲释放动力学遵循零级和peppas机制。发现微颗粒的药物释放机制为非菲克型。结论乳状溶剂蒸发技术可成功制备含格列本脲的醋酸纤维素微颗粒,该微颗粒既能缓释药物,又能较好地控制糖尿病的复杂性。
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Characterization of Glibenclamide loaded cellulose acetate microparticles prepared by an emulsion solvent evaporation method

Aim

The objective of the present investigation was to formulate and evaluate microencapsulated Glibenclamide produced by the emulsion–solvent evaporation method.

Methods

Microparticles were prepared using cellulose acetate by emulsion solvent evaporation method and characterized for their micromeritic properties, encapsulation efficiency, particle size, drug loading, FTIR, DSC, SEM analysis. In vitro release studies were performed in phosphate buffer (pH 7.4). Stability studies were conducted as per ICH guidelines.

Results

The resulting microparticles obtained by solvent evaporation method were free flowing in nature. The mean particle size of microparticles ranges from 132.54 to 178.44 μm and encapsulation efficiency ranges from 89.96 to 98.48%. The infrared spectra and differential scanning calorimetry thermographs confirmed the stable character of Glibenclamide in the drug-loaded microparticles. Scanning electron microscopy revealed that the microparticles were spherical in nature. In vitro release studies revealed that the drug release was sustained up to 12 h. The release kinetics of Glibenclamide from optimized formulation followed zero-order and peppas mechanism. The mechanism of drug release from the microparticles was found to be non-Fickian type.

Conclusion

Cellulose Acetate microparticles containing Glibenclamide could be prepared successfully by using an emulsion solvent evaporation technique, which will not only sustain the release of drug but also manage complicacy of the diabetes in a better manner.

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