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Design and in vitro evaluation of controlled release alginate beads of diltiazem hydrochloride

机译:盐酸地尔硫卓控释藻酸盐微珠的设计与体外评价

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Objective:Oral slow and sustained release drug delivery system can release their drug content with a controlled manner,producing a desirable blood serum level,reduction in drug toxicity and improving the patient compli-ance by prolonging dosing intervals.The major drawback of orally administered drug like diltiazem as a calcium channel blocker for the treatment of angina pectoris,arrhythmia and hypertension.Its has higher aqueous solu-bility and shorter elimination half-life.Methods:To overcome these drawbacks associated with diltiazem,an attempt has been made to develop a sustained release dosage form of diltiazem embedded alginate microbeads by ionotropic gelation technique employing various concentrations of polymer and keeping the drug concentra-tion constant.Results:The beads were characterized for its particle size,drug content and in vitro release stud-ies.The results revealed that the surface adhering drug was found to release immediately and a steady state of release was obtained up to 12 h from all the batches.The results indicated there was an inverse relationship be-tween the concentration of alginate and drug release.The drug release was found to follow non-fickian diffusion obeying first order kinetics.Conclusion:The developed alginate microbeads offered a sustained release of dilti-azem.Hence,the formulated microbeads were found to be potential,cost effective,possess satisfactory in vitro release studies.
机译:目的:口服缓释和缓释给药系统可以通过延长给药间隔来控制药物的释放,产生理想的血清水平,降低药物毒性并改善患者依从性。口服给药的主要缺点如地尔硫卓作为钙通道阻滞剂,用于治疗心绞痛,心律不齐和高血压。它具有更高的水溶性和较短的消除半衰期。方法:为克服与地尔硫卓有关的这些缺点,已尝试开发一种采用离子浓度不同的聚合物通过离子凝胶法,将地尔硫卓包埋的藻酸盐微珠缓释剂型进行了研究。结果:对微珠的粒径,药物含量和体外释放规律进行了表征。揭示发现表面粘附的药物可立即释放并且稳定释放状态不明显结果表明,藻酸盐的浓度与药物释放呈反比关系,发现其释放遵循服从一阶动力学的非菲尼克斯扩散规律。因此,发现配制的微珠是潜在的,具有成本效益的,具有令人满意的体外释放研究。

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  • 来源
    《亚太热带医药杂志(英文版)》 |2009年第004期|46-49|共4页
  • 作者单位

    Department ofPharmaceutics,JSS College ofPharmacy,00TY-643001,Tamil Nadu,India;

    Department ofPharmaceutics,JSS College ofPharmacy,00TY-643001,Tamil Nadu,India;

    Department ofPharmaceutics,JSS College ofPharmacy,00TY-643001,Tamil Nadu,India;

    Department ofPharmaceutics,JSS College ofPharmacy,00TY-643001,Tamil Nadu,India;

    Department ofPharmaceutics,JSS College ofPharmacy,00TY-643001,Tamil Nadu,India;

    Department ofPharmaceutics,JSS College ofPharmacy,00TY-643001,Tamil Nadu,India;

    Department ofPharmaceutics,JSS College ofPharmacy,00TY-643001,Tamil Nadu,India;

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