Sustained release formulations using non-aqueous carriers

摘要

The disclosure provides one-component, injectable, sustained release formulations which comprise microspheres containing active pharmaceutical ingredients (e.g., exenatide), wherein the microspheres are suspended in a non-aqueous carrier. The non-aqueous carrier can be an oil, a fractionated oil, triglycerides, diglycerides, monoglycerides, propylene glycol fatty acid diesters, and the like. The formulations offer distinct advantages of long shelf life for the stability and potency of the formulation and sustained release of active pharmaceutical ingredients to reduce the frequency of medication dosing and to increase patient compliance.

主权项

1. A manufactured pre-mixed formulation for injection comprising a suspension of (i) a pharmaceutically acceptable non-aqueous carrier comprising one or more triglycerides and (ii) microspheres which comprise a biocompatible, biodegradable polymer and an active pharmaceutical ingredient, and wherein the pharmaceutically acceptable non-aqueous carrier comprises from 0 to 2 wt % of C6 fatty acid, from 50 to 65 wt % of C8 fatty acid, from 30 to 45 wt % of C10 fatty acid, and form 0 to 2 wt % of C12 fatty acid based on the total fatty acid content of the one or more triglycerides.