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芋艿球茎粘液-海藻酸盐奥卡西平微球:设计、优化与评价

COLOCASIA ESCULENTA CORMS MUCILAGE-ALGINATE MICROSPHERES OF OXCARBAZEPINE: DESIGN, OPTIMIZATION AND EVALUATION.

作者信息

Ghumman Shazia Akram, Bashir Sajid, Ahmad Jamshed, Hameed Huma, Khan Ikram Ullah

出版信息

Acta Pol Pharm. 2017 Mar;74(2):505-517.

Abstract

The present investigation was undertaken with an objective of formulating sustained release microspheres of oxcarbazepine (OXC), an anti-epileptic drug, to overcome poor patient compliance and exposure to high doses associated with currently marketed OXC dosage forms. Ionic gelation technique was used to prepare OXC microspheres by using sodium alginate along with rate controlling polymer Colocasia esculenta mucilage (CEM) matrix as well coated form. The microspheres have been characterized by differential scanning calorimetry (DSC) for understanding thermal stability and Fourier transform infrared (FT-IR) spectroscopy to investigate the chemical interaction as well as to assess the structure of drug-loaded formulation. Surface morphology of the microspheres was investigated by scanning electron microscope (SEM). The size distribution of OXC microspheres as studied by optical microscopy was in the range of 394-575 pm. The microspheres exhibited encapsulating efficiency from 75 to 92%. The release of drug from the microspheres at pH 1.2 is negligible. Under neutral conditions, the microspheres were swell and release was attributed mainly to polymer relaxation. The release pattern from microspheres followed Korsmeyer-Peppas model and the value of n > 1 showed that drug released by anomalous (non-Fickian) diffusion. The data obtained thus suggest that a microparticulate system can be successfully designed by using CEM with alginate for sustained delivery of OXC.

摘要

本研究旨在制备抗癫痫药物奥卡西平(OXC)的缓释微球,以克服患者依从性差以及目前市售奥卡西平剂型存在的高剂量暴露问题。采用离子凝胶技术,以海藻酸钠与控速聚合物香芋黏液(CEM)基质共同制备奥卡西平微球,并制成包衣形式。通过差示扫描量热法(DSC)对微球进行表征,以了解其热稳定性;利用傅里叶变换红外光谱(FT-IR)研究化学相互作用,并评估载药制剂的结构。通过扫描电子显微镜(SEM)研究微球的表面形态。用光学显微镜研究的奥卡西平微球的粒径分布在394 - 575 µm范围内。微球的包封率为75%至92%。在pH 1.2条件下,微球中药物的释放可忽略不计。在中性条件下,微球膨胀,释放主要归因于聚合物松弛。微球的释放模式符合Korsmeyer-Peppas模型,n > 1的值表明药物通过非菲克扩散方式释放。由此获得的数据表明,使用CEM与海藻酸钠可成功设计出用于奥卡西平持续递送的微粒系统。

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