Sustained release compositions, process for producing the same and utilization thereof
View Patent ↗A sustained-release composition containing a hydroxynaphthoic acid salt of a biologically active substance and a biodegradable polymer, a method of its production, and a pharmaceutical composition containing said sustained-release composition.
1. A method of producing a sustained-release composition containing an LH-RH derivative or salt thereof, a hydroxynaphthoic acid or salt thereof and a biodegradable polymer or salt thereof, comprising removing an organic solvent from a mixture comprising the organic solvent, an LH-RH derivative or salt thereof, a biodegradable polymer or salt thereof, and hydroxynaphthoic acid or a salt thereof.
2. The method of claim 1 , comprising mixing and dispersing an LH-RH derivative or salt thereof in an organic solvent solution containing a biodegradable polymer or salt thereof and hydroxynaphthoic acid or a salt thereof, and subsequently removing the organic solvent.
3. The method of claim 2 , wherein the LH-RH derivative or salt thereof is in the form of an aqueous solution.
4. The method of claim 1 , wherein the salt of the LH-RH derivative is a salt with a free base or acid.
5. A method of suppressing initial burst of an LH-RH derivative from a sustained-release composition by maintaining a retention rate, comprising adding hydroxynaphthoic acid or a salt thereof to the sustained-release composition.
6. A method of prolonging the efficiency of an LH-RH derivative in a sustained-release composition, comprising adding hydroxynaphthoic acid or a salt thereof to the sustained-release composition.
7. A hydroxynaphthoate of an LH-RH derivative.
8. The hydroxynaphthoate of an LH-RH derivative claim 7 , which is soluble in water or very slightly soluble in water.
9. A sustained-release composition containing the hydroxynaphthoate of an LH-RH derivative.