Formulation and in vitro Evaluation of Eudragit ® Microspheres of Stavudine
Formulation and in vitro Evaluation of Eudragit ® Microspheres of Stavudine
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Eudragit ® 司他夫定微球的配方及体外评价
DOI：
10.4314/tjpr.v4i1.14622
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发表时间：
2007
影响因子：
0.6
通讯作者：
P. Senapati
中科院分区：
文献类型：
--
作者：
K. Sahoo;A. A. Mallick;B. Barik;P. Senapati
目的：本研究的目的是制定和评价微囊化控制释放制剂的高度水溶性药物，司他夫定，使用共聚物合成的丙烯酸酯和甲基丙烯酸酯（Eudragit RS 100和RL 100）作为阻滞材料。.方法：采用丙酮/液体石蜡溶剂挥发法制备微球。硬脂酸镁被用作液滴稳定剂，并加入正己烷以硬化微球。采用傅里叶变换红外光谱（FTIR）、差示扫描量热法、X射线粉末衍射法和扫描电子显微镜对制备的微球的粉体性质和载药量进行了表征。在pH 6.8磷酸盐缓冲液中进行体外释放研究。结果：制备的微球呈白色，流动性好，呈球形。载药微球的包封率为67-91%，释放时间延长至6 ~ 8h。红外光谱和差示扫描量热热分析表明司他夫定在载药微球中性质稳定，没有药物-聚合物相互作用。X-射线衍射图谱显示药物结晶度降低。扫描电子显微镜研究表明，微球是球形和多孔的性质。结论：Higuchi曲线拟合最佳，其次为零级和一级。司他夫定的释放受药物与聚合物的比例和粒径的影响，并被发现是扩散控制的。
Purpose: The aim of this study was to formulate and evaluate microencapsulated controlled release preparations of a highly water-soluble drug, stavudine, using Copolymers synthesized from acrylic and methacrylic acid esters (Eudragit RS 100 and RL 100) as the retardant material. . Methods: Microspheres were prepared by solvent evaporation method using an acetone / liquid paraffin system. Magnesium stearate was used as the droplet stabilizer and n-hexane was added to harden the microspheres. The prepared microspheres were characterized for their micromeritic properties and drug loading, as well by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry, x-ray powder diffractometry and scanning electron microscopy. The in vitro release studies were performed in pH 6.8, phosphate buffer. Results: The prepared microspheres were white, free flowing and spherical in shape. The drug-loaded microspheres showed 67-91% of entrapment and release was extended upto 6 to 8 h. The infrared spectra and differential scanning calorimetry thermographs showed stable character of stavudine in the drug-loaded microspheres and revealed the absence of drugpolymer interactions. X-ray diffraction patterns showed that there was decrease in crystallinity of the drug. Scanning electron microscopy study revealed that the microspheres were spherical and porous in nature. Conclusion: The best-fit release kinetics was achieved with Higuchi plot followed by zero order and First order. The release of stavudine was influenced by the drug to polymer ratio and particle size & was found to be diffusion controlled.