Sustained release small molecule drug formulation

摘要

An injectable depot formulation includes a biocompatible polymer, an organic solvent combined with the biocompatible polymer to form a viscous gel, and a small molecule drug incorporated in the viscous gel such that the formulation exhibits an in vivo release profile having Cmax to Cmin ratio less than 200 and lag time less than 0.2.

主权项

1. An injectable depot formulation, comprising:
a biocompatible polymer comprising a copolymer of lactic acid and glycolic acid, wherein the biocompatible polymer has a number average molecular weight ranging from 1000 Daltons to 5000 Daltons; an organic solvent combined with the biocompatible polymer to form a viscous gel said solvent selected from the group consisting of benzyl alcohol, benzyl benzoate, ethyl benzoate, ethyl hydroxide, N-methy1-2-pyrrolidone, and mixtures thereof; and a small molecule drug selected from base and salt forms of risperidone incorporated in the viscous gel, wherein the small molecule drug is in the form of particles having a particle size less than 38 μm, wherein the salt forms of risperidone have less than 1 mg/mL solubility in water, and wherein the formulation exhibits an in vivo release profile having Cmax to Cmin ratio less than 200 over a period of one month.