Sustained release formulations using non-aqueous carriers

Details Sustained release formulations using non-aqueous carriers Sustained release formulations using non-aqueous carriers

A - Human Necessities

61

K

A61K 47/34 (2006.01) A61K 9/00 (2006.01)

Patent

CA 2734525

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, mono-glycerides, 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.

L'invention concerne des formulations à libération prolongée injectables à un composant qui comprennent des microsphères contenant des ingrédients pharmaceutiques actifs (par exemple, exénatide), les microsphères étant en suspension dans un support non aqueux. Le support non aqueux peut être constitué d'une huile, d'une huile fractionnée, de triglycérides, de diglycérides, de monoglycérides, de diesters d'acide gras de propylèneglycol et de substances similaires. Les formulations présentent des avantages spécifiques de longue durée de conservation favorables à la stabilité et à l'efficacité de la formulation et à la libération prolongée des ingrédients pharmaceutiques actifs permettant de réduire la fréquence d'administration des médicaments et d'augmenter la compliance du patient.

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