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制备和评价明胶/羧甲基纤维素钠聚电解质复合微球用于异烟肼的控制释放。

Preparation and evaluation of gelatin/sodium carboxymethyl cellulose polyelectrolyte complex microparticles for controlled delivery of isoniazid.

机构信息

Department of Chemical Sciences, Tezpur University, Napaam, 784028, India.

出版信息

AAPS PharmSciTech. 2009;10(4):1412-9. doi: 10.1208/s12249-009-9344-9. Epub 2009 Nov 24.

Abstract

The ratio of gelatin to sodium carboxymethyl cellulose (SCMC) at which maximum yield was obtained was optimized. This optimized ratio of gelatin to SCMC along with other parameters was used to prepare microparticles of different sizes. Vegetable oil was used as emulsion medium. Effect of various factors like amount of surfactant, concentration of polymer on the formation, and size of the microparticles was investigated. These microparticles were used as carrier for isoniazid. Among different cross-linkers, glutaraldehyde was found to be the most effective cross-linker at the temperature and pH at which the reaction was carried out. The loading efficiency and release behavior of loaded microparticles were found to be dependent on the amount of cross-linker used, concentration of drug, and time of immersion. Maximum drug loading efficiency was observed at higher immersion time. The release rate of isoniazid was more at higher pH compared to that of at lower pH. The sizes of the microparticles were investigated by scanning electron microscope. In all the cases, the microparticles formed were found spherical in shape except to those at low stirring speed where they were agglomerated. Fourier transform infrared study indicated the successful incorporation of isoniazid into the microparticles. Differential scanning calorimetry study showed a molecular level dispersion of isoniazid in the microparticles. X-ray diffraction study revealed the development of some crystallinity due to the encapsulation of isoniazid.

摘要

优化了获得最大产率的明胶与羧甲基纤维素钠(CMC)的比例。使用该明胶与 CMC 的最佳比例以及其他参数来制备不同大小的微球。植物油被用作乳化介质。研究了各种因素,如表面活性剂的用量、聚合物浓度对微球形成和大小的影响。这些微球被用作异烟肼的载体。在不同的交联剂中,戊二醛在反应进行的温度和 pH 值下被发现是最有效的交联剂。载药微球的载药效率和释放行为取决于所用交联剂的量、药物的浓度和浸泡时间。在较高的浸泡时间下观察到最大的药物载药效率。与较低 pH 值相比,较高 pH 值下异烟肼的释放速率更高。通过扫描电子显微镜研究了微球的大小。在所有情况下,形成的微球均呈球形,除了在较低搅拌速度下,微球发生团聚。傅里叶变换红外研究表明异烟肼已成功掺入微球中。差示扫描量热法研究表明异烟肼在微球中呈分子水平分散。X 射线衍射研究表明由于异烟肼的包封,出现了一些结晶度。

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