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使用乳化技术制备藻酸盐微球。

Formation of alginate microspheres produced using emulsification technique.

作者信息

Heng P W S, Chan L W, Wong T W

机构信息

Department of Pharmacy, Faculty of Science, National University of Singapore, 18 Science Drive 4, Singapore 117543.

出版信息

J Microencapsul. 2003 May-Jun;20(3):401-13. doi: 10.1080/0265204031000093069.

Abstract

This study investigated the formative process of alginate microspheres produced using an emulsification technique. The alginate microspheres were produced by cross-linking alginate globules dispersed in a continuous organic phase using various calcium salts: calcium chloride, calcium acetate, calcium lactate and calcium gluconate. The size, shape, drug content and Ca2+ content of the microspheres were evaluated. The tack, viscosity and pH of the calcium salt solution and percentage of Ca2+ partitioned into the organic phase were determined. Microscopic examination of the test emulsion at various stages of the emulsification process was also carried out. The propensity of cross-linking reaction was found to be dependent on successful collision between alginate and calcium salt globules. Examination of the characteristics of microspheres indicated that the formed microsphere was a resultant product of alginate globule clustering. The growth propensity of microspheres was promoted by the higher rate and extent of cross-linkage which was governed by the pH, tack and/or Ca2+ content of the cross-linking solution, as well as the dissociation constant and diffusivity of the calcium salt. Overall, the amount of free Ca2+ cross-linked with alginate in the formed microspheres was in the following order: calcium acetate > calcium chloride + calcium acetate > calcium chloride + calcium gluconate; calcium chloride + calcium lactate > calcium chloride. In microencapsulation by emulsification, the mean size of the microspheres produced can be modified by varying the tack, pH and Ca2+ content of the cross-linking solution and through the use of a combination of calcium salts. The shape of the microspheres produced was, nonetheless, unaffected by the physicochemical properties of the cross-linking solution.

摘要

本研究调查了采用乳化技术制备藻酸盐微球的形成过程。藻酸盐微球是通过使用各种钙盐(氯化钙、醋酸钙、乳酸钙和葡萄糖酸钙)交联分散在连续有机相中的藻酸盐小球而制备的。对微球的尺寸、形状、药物含量和Ca2+含量进行了评估。测定了钙盐溶液的粘性、粘度和pH值以及分配到有机相中的Ca2+百分比。还对乳化过程不同阶段的测试乳液进行了显微镜检查。发现交联反应的倾向取决于藻酸盐和钙盐小球之间的成功碰撞。对微球特性的检查表明,形成的微球是藻酸盐小球聚集的产物。交联的速率和程度越高,微球的生长倾向就越大,而交联的速率和程度由交联溶液的pH值、粘性和/或Ca2+含量以及钙盐的离解常数和扩散率决定。总体而言, 在形成微球中与藻酸盐交联的游离Ca2+量的顺序如下: 醋酸钙>氯化钙+醋酸钙>氯化钙+葡萄糖酸钙; 氯化钙+乳酸钙>氯化钙。在乳化微囊化过程中, 通过改变交联溶液的粘性、pH值和Ca2+含量以及使用钙盐组合, 可以改变所制备微球的平均尺寸。然而, 所制备微球的形状不受交联溶液物理化学性质的影响。

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