O'Donnell P B, Iwata M, McGinity J W
College of Pharmacy, University of Texas at Austin 78712-1074, USA.
J Microencapsul. 1995 Mar-Apr;12(2):155-63. doi: 10.3109/02652049509015286.
Multiphase microspheres of poly(D,L-lactic-co-glycolic acid) (PLGA) were prepared by a multiple emulsion potentiometric dispersion technique. Water-soluble compounds were dissolved in the aqueous phase (W) and emulsified in soybean oil (O) to form a stable emulsion. This primary emulsion was dispersed in a solution of PLGA and acetonitrile (O) to form a W/O/O emulsion. The W/O/O emulsion was then dispersed in a hardening solution of light mineral oil (O) using a potentiometric dispersion technique to produce microspheres of the W/O/O/O type with a very narrow and selective size distribution. The size of the microspheres was controlled by varying the internal diameter of the conductive infusion tube or by the variation of voltage applied to the conductive tube. Particle size analysis revealed a particle size distribution of 1-50 microns for microspheres made by this method as compared to a distribution of 50-500 microns for microspheres made by conventional agitation methods. Chlorpheniramine maleate was encapsulated with a loading efficiency of 88.9% with the potentiometric method as compared with a loading efficiency of 74.3% for the agitation method.
采用多重乳液电位分散技术制备了聚(D,L-乳酸-乙醇酸共聚物)(PLGA)多相微球。将水溶性化合物溶解于水相(W)中,并在大豆油(O)中乳化以形成稳定乳液。将该初级乳液分散于PLGA和乙腈的溶液(O)中以形成W/O/O乳液。然后使用电位分散技术将W/O/O乳液分散于轻质矿物油的硬化溶液(O)中,以制备具有非常窄且选择性的尺寸分布的W/O/O/O型微球。通过改变导电输液管的内径或通过改变施加于导电管的电压来控制微球的尺寸。粒度分析表明,通过该方法制备的微球的粒度分布为1-50微米,而通过传统搅拌方法制备的微球的粒度分布为50-500微米。与搅拌法74.3%的载药效率相比,采用电位法包封马来酸氯苯那敏的载药效率为88.9%。