氯沙坦钾纳米颗粒的制备及评价

Amar Singh, A. Deep
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引用次数: 5

摘要

氯沙坦钾是一种用于治疗高血压的降压药,其血药峰浓度低,半衰期短。它已被选为缓释剂型制剂的候选物。本文通过壳聚糖与三聚磷酸阴离子凝胶法制备了氯沙坦钾负载壳聚糖纳米颗粒。制备了不同芯包比的纳米颗粒,并对其药物含量、载药效率、粒径、zeta电位、体外释药和稳定性进行了研究。扫描电镜结果表明,所制备的纳米颗粒在纳米级范围内,具有理想的表面形貌。差示扫描量热分析表明,药物与聚合物无化学相互作用,药物稳定性良好。所有载药批次的体外释放行为均遵循零顺序,并在24小时内持续释放。在不同温度下储存的60天内,纳米颗粒的降解程度没有明显的差异。在氯沙坦钾的缓释剂型方面,所开发的制剂克服并可能具有优势。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and Evaluation of Nanoparticles containing Losartan Potassium 
Losartan potassium is an antihypertensive agent used in the treatment of hypertension which has low peak plasma concentration and half-life. It has been selected as candidate for the formulation of sustained release dosage forms. In the present work losartan potassium loaded chitosan nanoparticles were prepared by ionic gelation of chitosan with tripolyphosphate anions. Nanoparticles of different core: coat ratio were formulated and evaluated for drug content, loading efficiency, particles size, zeta potential, In vitro drug release and stability studies. Scanning Electron Microscopy indicated that the nanoparticles were found to be in nanometer range and showed ideal surface morphology. Differ ential scanning calorimetry analysis indicated that there were no chemical interactions between drug and polymer and stability of drug. In vitro release behavior from all the drug loaded batches were found to follow zero order and provided sustained release over a period of 24 hours. No appreciable difference was observed in the extent of degradation of product during 60 days in which nanoparticles were stored at various temperatures. The developed formulation overcomes and could possibility be advantageous in terms of sustained release dosage forms of losartan potassium.
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