The invention provides microparticles for sustained release formulation for physostigmine, pyridostigmine and other therapeutically active carbamates. The microparticles comprise the active compound and a biodegradable polymer such as polyester, poly(phosphate), poly(anhydride), poly(ortho ester), or mixture thereof. In one embodiment, the polymer is poly(d,l-lactide-co-glycolide). The desired release pattern of the active compound may be readily attained by varying the type and amount of the polymer used, including by using a mixture of two polymers, one of which is more hydrophobic. The invention also provides a method of preparing the microparticles and in one embodiment, the microparticles may be prepared by spray drying.
本发明提供了用于持续释放制剂的微颗粒,可用于
吡咯斯的明、
吡啶斯的明和其他具有治疗活性的
氨基甲酸酯类药物。微颗粒由活性化合物和可
生物降解的聚合物(如聚酯、聚
磷酸酯、聚酸酐、聚原酯或它们的混合物)组成。在一个实施方案中,聚合物是聚(d,l-内酯-共聚
乙二醇)。通过改变聚合物的种类和用量,包括使用两种聚合物的混合物(其中一种更疏
水),可以很容易地获得所需的活性化合物释放模式。本发明还提供了制备微颗粒的方法,在一个实施方案中,微颗粒可以通过喷雾干燥法制备。