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聚丙烯酸树脂(尤特奇缓释型)微胶囊作为一种控释给药系统——改进的非溶剂添加相分离工艺

Polyacrylate resin (Eudragit retard) microcapsules as a controlled release drug delivery system-improved non-solvent addition phase separation process.

作者信息

Benita S, Hoffman A, Donbrow M

机构信息

Pharmacy Department, School of Pharmacy, Hebrew University of Jerusalem, Israel.

出版信息

J Microencapsul. 1985 Jul-Sep;2(3):207-22. doi: 10.3109/02652048509038526.

Abstract

Eudragit retard microcapsules were prepared using an improved non-solvent addition phase separation process with tetrahydrofuran as the solvent. The evolution of microcapsule wall formation was studied by direct methodology. Eudragit coacervation was effected by progressive uptake of tetrahydrofuran by the non-solvent cyclohexane in the presence of a protective colloid, polyisobutylene (PIB). The core materials had a higher affinity for the acrylic that the PIB phase, thus ensuring encapsulation. Microcapsule batch reproducibility depended mainly on the variation in particle size distribution of the recrystallized core material. All batches gave apparent first-order release profiles, confirmed by regression procedures. The release rate was decreased by raising the wall/core ratio, holding constant concentration of either the wall polymer or the core material. Increase in the non-solvent addition rate elevated the release rate, probably due to structural changes in the microcapsule wall. The velocity fell, however, with decrease in particle size of the core material, contrary to expectations. PIB concentration increase elevated the release rate by enhancing wall porosity, shown by scanning electron microscopy.

摘要

采用改进的非溶剂添加相分离法,以四氢呋喃为溶剂制备了Eudragit缓释微胶囊。通过直接方法研究了微胶囊壁形成的过程。在保护胶体聚异丁烯(PIB)存在下,非溶剂环己烷逐渐吸收四氢呋喃,实现了Eudragit凝聚。与PIB相相比,芯材对丙烯酸具有更高的亲和力,从而确保了包封。微胶囊批次的重现性主要取决于重结晶芯材粒径分布的变化。所有批次均呈现明显的一级释放曲线,经回归程序确认。在壁聚合物或芯材浓度保持不变的情况下,提高壁/芯比可降低释放速率。非溶剂添加速率的增加提高了释放速率,这可能是由于微胶囊壁的结构变化所致。然而,与预期相反,芯材粒径减小导致释放速率下降。扫描电子显微镜显示,PIB浓度增加通过提高壁孔隙率提高了释放速率。

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