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首页> 美国卫生研究院文献>AAPS PharmSciTech >The effect of drug concentration and curing time on processing and properties of calcium alginate beads containing metronidazole by response surface methodology
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The effect of drug concentration and curing time on processing and properties of calcium alginate beads containing metronidazole by response surface methodology

机译：响应面法研究药物浓度和固化时间对甲硝唑海藻酸钙微珠加工及性能的影响

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摘要

The purpose of present research work was to prepare calcium alginate beads containing water-soluble drug metronidazole using 32 factorial design, with drug concentration and curing time as variables. Curing time was kept as low as possible to improve entrapment with increasing drug concentration. Mostly the drugs which had been encapsulated were water insoluble to facilitate drug encapsulation; a characteristic drug release as whole process is aqueous based. Entrapment efficiency was in the range of 81% to 96% wt/wt, which decreased with decrease in polymer concentration and increase in curing time. The beads were spherical with size range between 1.4 and 1.9 mm. Scanning electron microscope (SEM) photomicrographs revealed increase in the leaching of drug crystals with increased curing time and high drug concentrations. In acidic environment, the swelling ratio was 200% in 30 minutes, but in basic medium, it increased to a maximum of 1400% within 120 minutes. In acidic medium, the swelling and drug release properties were influenced by drug solubility, whereas in phosphate buffer these properties were governed by the gelling of polymer and exhibited curvilinear and quadratic functions of both the variables, respectively.
机译：本研究的目的是采用3 2 因子设计，以药物浓度和固化时间为变量，制备含有水溶性甲硝唑的海藻酸钙珠。固化时间应保持尽可能短，以提高药物浓度，从而改善包封率。多数情况下，已被封装的药物是水不溶性的，以利于药物的封装。整个过程中典型的药物释放是基于水的。包封率在81％至96％wt / wt的范围内，其随着聚合物浓度的降低和固化时间的增加而降低。珠为球形，尺寸范围在1.4至1.9mm之间。扫描电子显微镜（SEM）显微照片显示，随着固化时间的增加和药物浓度的升高，药物晶体的浸出也增加了。在酸性环境中，溶胀率在30分钟内达到200％，但在碱性介质中，溶胀率在120分钟内达到最大值1400％。在酸性介质中，溶胀和药物释放特性受药物溶解度的影响，而在磷酸盐缓冲液中，这些特性则受聚合物的胶凝作用控制，并分别表现出这两个变量的曲线和二次函数。

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