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Formulation variables affecting drug release from xanthan gum matrices at laboratory scale and pilot scale

机译:在实验室规模和中试规模影响黄原胶基质药物释放的配方变量

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摘要

The purpose of this research was to study processing variables at the laboratory and pilot scales that can affect hydration rates of xanthan gum matrices containing diclofenac sodium and the rate of drug release. Tablets from the laboratory scale and pilot scale proceedings were made by wet granulation. Swelling indices of xanthan gum formulations prepared with different amounts of water were measured in water under a magnifying lens. Granules were thermally treated in an oven at 60°C, 70°C, and 80°C to studythe effects of elevated temperatures on drug release from xanthan gum matrices. Granules from the pilot scale formulations were bulkier compared to their laboratory scale counterparts, resulting in more porous, softer tablets. Drug release was linear from xanthan gum matrices prepared at the laboratory scale and pilot scales, however, release was faster from the pilot scales. Thermal treatment of the granules did not affect the swelling index and rate of drug release from tablets in both the pilot and laboratory scale proceedings. On the other hand, the release from both proceedings was affected by the amount of water used for granulation and the speed of the impeller during granulation. The data suggest that processing variables that affect the degree of wetness during granulation, such as increase in impeller speed and increase in amount of water used for granulation, also may affect the swelling index of xanthan gum matrices and therefore the rate of drug release.
机译:这项研究的目的是研究实验室和中试规模的加工变量,这些变量可能会影响含有双氯芬酸钠的黄原胶基质的水合速率和药物释放速率。通过湿法制粒制备实验室规模和中试规模的片剂。用不同量的水制得的黄原胶制剂的溶胀指数在放大镜下在水中测量。将颗粒在60°C,70°C和80°C的烤箱中进行热处理,以研究高温对黄原胶基质药物释放的影响。与实验室规模的同类产品相比,中试规模的配方产品的颗粒更大,从而使片剂更多孔,更柔软。在实验室规模和中试规模下制备的黄原胶基质中的药物释放呈线性关系,但从中试规模上释放更快。在试验和实验室规模的程序中,对颗粒的热处理均不影响溶胀指数和片剂中药物的释放速率。另一方面,两个过程的释放都受到制粒用水量和制粒过程中叶轮速度的影响。数据表明,影响制粒过程中湿度程度的加工变量,例如叶轮速度的提高和制粒用水量的增加,也可能影响黄原胶基质的溶胀指数,从而影响药物释放速率。

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