首页> 美国卫生研究院文献>Iranian Journal of Pharmaceutical Research : IJPR >Preparation and Characterization of Salbutamol Sulphate Loaded Ethyl Cellulose Microspheres using Water-in-Oil-Oil Emulsion Technique
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Preparation and Characterization of Salbutamol Sulphate Loaded Ethyl Cellulose Microspheres using Water-in-Oil-Oil Emulsion Technique

机译:油包水油乳化技术制备硫酸沙丁胺醇负载的乙基纤维素微球及其表征

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摘要

The aim of this study was to formulate and evaluate microencapsulated controlled release preparations of a highly water/soluble drug, salbutamol sulphate by (water in oil) in oil emulsion technique using ethyl cellulose as the retardant material. Various processing and formulation parameters such as drug/polymer ratio, stirring speed, volume of processing medium were optimized to maximize the entrapment. The release of salbutamol sulphate from ethyl cellulose microsphere was compared and possible release mechanism proposed. Microspheres were prepared by water in oil emulsion technique using acetonitrile/dichloromethane (1:1 ratio) solvent system. Span 80 was used as the dispersing agent and n-hexane was added to harden the microspheres. The prepared microspheres were characterized for their micromeritic properties and drug loading, as well as compatibility by infrared spectroscopy, differential scanning calorimetry (DSC), X-ray powder diffractometry and scanning electron microscopy (SEM). The in-vitro release studies were carried out in phosphate buffer at pH 7.4. The prepared microspheres were white, free flowing and spherical in shape. The drug-loaded microspheres showed 55.7 - 76.6 % of entrapment and release was extended up to 10 h. Various processing and formulation parameters such as drug/polymer ratio, stirring speed, volume of processing medium, etc. significantly affect the drug release from the microspheres. The best/fit release kinetics was achieved with Higuchi plot followed by zero order and first order. The release of salbutamol sulphate was influenced by altering the drug to polymer ratio and the drug release was found to be diffusion controlled.
机译:这项研究的目的是使用乙基纤维素作为缓释材料,通过油包水乳化技术(油包水),配制和评估高度水溶性/水溶性药物硫酸沙丁胺醇的微囊控释制剂。优化了各种加工和配方参数,例如药物/聚合物的比例,搅拌速度,加工介质的体积,以使截留量最大化。比较了硫酸沙丁胺醇从乙基纤维素微球中的释放,并提出了可能的释放机理。通过使用乙腈/二氯甲烷(1:1比例)溶剂系统的油包水乳化技术制备微球。使用Span 80作为分散剂,并添加正己烷以硬化微球。通过红外光谱,差示扫描量热法(DSC),X射线粉末衍射法和扫描电子显微镜(SEM)对制得的微球的微链性质和载药量以及相容性进行了表征。在pH 7.4的磷酸盐缓冲液中进行了体外释放研究。制备的微球为白色,自由流动且呈球形。载有药物的微球显示出55.7-76.6%的截留,释放时间延长至10 h。各种加工和配制参数,例如药物/聚合物的比例,搅拌速度,加工介质的体积等,都会显着影响药物从微球中的释放。最佳/适合的释放动力学是通过Higuchi图实现的,其后为零阶和一阶。沙丁胺醇硫酸盐的释放受到药物与聚合物比例的改变的影响,并且药物的释放受到扩散控制。

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