格列美脲控释微颗粒给药系统的设计与研制

Irisappan Sarath Chandiran , Balagani Pavan Kumar , Korlakanti Narasimha Jayaveera
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引用次数: 8

摘要

目的研制格列美脲载醋酸纤维素控释微颗粒。方法采用乳化溶剂蒸发法制备格列美脲微颗粒。考察了不同工艺参数对微颗粒中药物含量和药物释放的影响。从包封效率、粒径、载药量、FTIR、DSC、SEM分析和药物释放研究等方面对微颗粒进行表征。结果芯衣比由1:1增加到1:3,包封效率和平均粒径均有所提高。FTIR和DSC研究表明,药物和辅料之间没有相互作用。SEM研究清楚地表明,微颗粒具有良好的球形性质。在pH为7.8的磷酸盐缓冲液中,格列美脲的体外释放与分子量和共聚物类型有关。优化制剂格列美脲的释放动力学遵循零级和peppas机制。释放指数n值在0.95 ~ 1.07之间,表明微颗粒物的释放主要以非粘性运输机制为主。根据ICH指南评价稳定性研究前后优化制剂的溶出度。结论该模型在缓释剂型开发中是可行的。
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Design and development of microparticulate drug delivery system of Glimepiride for controlled release

Objective

The objective of the present investigation was to develop Glimepiride loaded cellulose acetate controlled release micro particulates.

Methods

The Glimepiride micro particles were prepared by emulsion solvent evaporation method. The effects of different parameters on the drug content and on the release of the drug from the micro particulates were investigated. Micro particulates were characterized in terms of encapsulation efficiency, particle size, drug loading, FTIR, DSC, SEM analysis and drug release studies.

Results

An increase in core:coat ratio from 1:1 to 1:3 caused an increase in the encapsulation efficiency and average particle size. FTIR and DSC studies exhibited there is no interaction between drug and excipients. The SEM studies clearly showed that the micro particles exhibited good spherical nature. The in vitro release of Glimepiride from micro particles in phosphate buffer of pH 7.8 was found to be dependent on molecular weight and copolymer type. The release kinetics of Glimepiride from optimized formulation followed zero order and peppas mechanism. The release exponent showed that the values of ‘n’ were between 0.95 and 1.07 indicating that the release from micro particulates was predominantly by non-fickian transport mechanism. The dissolution profiles of optimized formulation before and after stability studies were evaluated as per ICH guidelines.

Conclusion

The results demonstrate the feasibility of the model in the development of extended release dosage form.

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