Microspheres for controlled- or sustained-release delivery of therapeutics

摘要

A new microsphere formulation (composition) for controlled- or sustained-release delivery of therapeutic ingredient(s), mainly peptides and proteins not over 10K in molecular weight, comprises at least a therapeutic ingredient, a helping agent (such as PH sensitive agent whose solubility is a function of pH) and a biodegradable polymer. The therapeutic ingredient(s) and the helping agent are in the form of fine particles, less than 1O um in diameter, encapsulated in the polymer which forms the microsphere matrix. A method for preparing the composition comprises a step of in-situ precipitating the therapeutic ingredient(s) and the helping agent to the fine particles and successive steps for forming the microspheres. Such a microsphere formulation offers a well-controlled release profile for prolonged period and encapsulation efficiency over 95%.

主权项

1. A composition comprising a plurality of microspheres, each microsphere comprising:
a) a biodegradable polymer forming a matrix of the microsphere; b) a particulate GLP-1 receptor agonist distributed in the matrix of the microsphere; and c) a particulate helping agent selected from Mg(OH)2, MgCO3, and Zn(OH)2 distributed in the matrix of the microsphere, wherein the particulate helping agent is less than 8.82 w/w % of the total mass of the microsphere wherein the particulate GLP-1 receptor agonist and the particulate helping agent are less than 10 μm in size and are encapsulated by the biodegradable polymer; and wherein the GLP-1 receptor agonist is exenatide.