Insulin derivative formulations for pulmonary delivery
View Patent ↗Aerosolizable formulations comprising: an insulin derivative having an isoelectric point (pI) ranging from about 6 to about 8; and a pharmaceutically acceptable excipient including a precipitating agent.
1. An aerosolized formulation, comprising:
a first insulin derivative having an isoelectric point (p1) ranging from about 6.5 to about 7.5, wherein the first insulin derivative is glargine insulin;
a second insulin or insulin derivative;
Trehalose;
Leucine;
a liquid carrier, which is water, ethanol, ethanol-water, or saline; and
a precipitating agent, which is a free cation selected from at least one of zinc, copper, cobalt, iron, manganese, vanadium, cadmium, magnesium, calcium, and barium;
wherein the first insulin derivative and the precipitating agent are dissolved in the liquid carrier;
wherein the molar ratio of the precipitating agent to the first insulin derivative is from about 1:3 to about 5:1;
wherein the first insulin derivative is present in an amount of from about 20 weight % to about 99 weight %.
2. The aerosolized formulation of claim 1 , wherein the molar ratio of the precipitating agent to the first insulin derivative is about 5:3.
3. The aerosolized formulation of claim 1 , wherein the second insulin or insulin derivative has a different isoelectric point than that of the first insulin derivative.