首页> 外国专利> SOLID LIPID NANOPARTICLES AS A CARRIER FOR LERCANIDIPINE, A MECHANISM FOR TWO-WAY ENHANCEMENT OF ORAL BIOAVILABILITY

SOLID LIPID NANOPARTICLES AS A CARRIER FOR LERCANIDIPINE, A MECHANISM FOR TWO-WAY ENHANCEMENT OF ORAL BIOAVILABILITY

机译:固体脂质纳米粒作为莱卡尼定的载体,是双向增强口服生物利用度的机制

摘要

In this invention, lercanidipine entrapped solid lipid nanoparticles was developed comprising of Glyceryl Monostearate as solid lipid and Gelucire 44/14 as surfactant to yield a stable formulation with enhanced oral bioavailability and extended release of action. Preparation of drug loaded formulation involves the Hot-Homogenisation method. Lipid solubility of drug is an added benefit to the high entrapment efficiency. Solid lipid formulation provides enhanced physical and chemical stability of the drug molecule. High Pressure Homogenisation method is less time consuming, involves less metal contamination as compared to sonication method and hence more economical. The size of formulation was achieved between 100 - 200 nm, which is optimum to bypass the First-pass metabolism. The stability of the formulation was more than 6 months. Drug loading was achieved to be more than 90%. The Pharrnacodynamic activity was found to be controlled for more than 36 hours.
机译:在本发明中,开发了包被有雷卡地平的固体脂质纳米颗粒,其包含单硬脂酸甘油酯作为固体脂质和Gelucire 44/14作为表面活性剂,以产生具有增强的口服生物利用度和延长的作用释放的稳定制剂。载药制剂的制备涉及热均质方法。药物的脂溶性是高包封率的另一个好处。固体脂质制剂提供了增强的药物分子物理和化学稳定性。与超声处理方法相比,高压均质化方法耗时少,金属污染少,因此更经济。制剂的大小在100-200 nm之间,这是绕过首过代谢的最佳选择。制剂的稳定性超过6个月。载药量达到90%以上。发现可控制咽气动力学活动超过36小时。

著录项

  • 公开/公告号IN2013DE00264A

    专利类型

  • 公开/公告日2014-08-22

    原文格式PDF

  • 申请/专利权人

    申请/专利号IN264/DEL/2013

  • 发明设计人 MD SABIR;SAIMA AMIN;

    申请日2013-01-30

  • 分类号

  • 国家 IN

  • 入库时间 2022-08-21 15:57:29

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