SUSTAINED-RELEASING INJECTABLE FORMULATION FOR THE TREATMENT OR PREVENTION OF BONE-RELATED DISEASES COMPRISING BISPHORENATE-CONTAINING POLYMERIC MICROPARTICLES

摘要

Disclosed is a sustained-release injectable formulation for treating or preventing bone-related diseases, comprising bisphosphonate-containing polymeric microparticles prepared by dissolving and dispersing a bisphosphonate in an aqueous solution containing a water-soluble polymer and a hydrophilic surfactant to provide a polymer solution; adding the polymer solution to another polymer solution, prepared by adding a secondary organic solvent to a primary organic solvent containing a biodegradable polymer and a hydrophobic surfactant, to provide a primary emulsion (water-in oil (W/O) type); and dispersing the primary emulsion in an external continuous phase. The injectable formulation has an effect of sustaining drug release in vivo for a period of 4 weeks or more using only a single administration, thereby reducing administration frequency and total dosage compared to conventional oral formulations administered every day, as well as remarkably reducing local irritation compared to a directly injected non-encapsulated bisphosphonate. Therefore, this sustained-release injectable formulation is more useful in the treatment or prevention of diseases against which bisphosphonate drugs have therapeutic or preventive effects than conventional oral formulations and direct injections of bisphosphonates.