Polymorph compositions, methods of making, and uses thereof

摘要

The described invention provides a biodegradable, biocompatible delivery system of flowable sustained release microparticulate composition of a substantially pure crystalline form of a bioactive agent such as, for example, nimodipine, a process of preparing a therapeutic form of a substantially pure crystalline form of the bioactive agent and a method for treating an interruption of a cerebral artery in a subarachnoid space at risk of interruption caused by brain injury in a mammal, which reduces signs or symptoms of at least one delayed complication associated with brain injury.

主权项

1. A process for producing microparticles encapsulating a crystalline polymorphic Form I of Nimodipine that has an X-ray Powder Diffraction (XRPD) spectrum substantially the same as the X-ray Powder Diffraction (XRPD) spectrum shown in FIG. 11, the process comprising:
(a) providing the polymorphic Form I of Nimodipine; (b) adding the polymorphic Form I of Nimodipine to a polymer solution, thereby creating a mixture of the polymorphic Form I of Nimodipine and the polymer solution; (c) homogenizing the mixture to form a disperse phase; (d) mixing the disperse phase with a continuous phase comprising a continuous process medium, thereby forming an emulsion comprising the polymorphic Form I of Nimodipine; (e) forming and extracting the microparticles comprising the polymorphic Form I of Nimodipine; and (f) drying the microparticles, the microparticles being characterized by: (i) dispersal of the polymorphic Form I of Nimodipine throughout each microparticle; and (ii) at least 70 percent by weight relative to the total weight of Nimodipine of Form I of Nimodipine.