Sustained-release injection comprising deslorelin, and preparation method therefor
AssigneeG2Gbio, Inc.
InventorsHeeyong LEE, Eunyoung SEOL, Yongha NA, Juhan LEE
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Abstract
The present disclosure relates to a sustained-release injection formulation comprising biodegradable polymer microspheres containing deslorelin as an active ingredient, and a preparation method therefor. The sustained-release microsphere injection containing deslorelin, according to the present disclosure, has good administrability and enables, with a single administration, a deslorelin drug to be maintained at an effective concentration for 6 months without rapid temporary release into the blood of an animal.
Claims23
A sustained-release microsphere containing deslorelin, comprising 5 to 25% by weight of deslorelin based on the total weight of the microsphere, and two or more polymers selected from the group consisting of poly(lactide-co-glycolide) and polylactide polymers.
A method for preparing a sustained-release microsphere containing deslorelin, the method comprising the steps of:
- (a) dissolving deslorelin and two or more polymers selected from the group consisting of poly(lactide-co-glycolide) and polylactide polymers in a mixed organic solvent to prepare a deslorelin-polymer solution (dispersed phase);
- (b) adding the deslorelin-polymer solution prepared in step (a) to an aqueous solution phase (continuous phase) containing a surfactant to prepare a dispersed phase in an emulsion state;
- (c) extracting the organic solvent from the dispersed phase in the emulsion state phase prepared in step (b) into a continuous phase and evaporating the organic solvent to form a microsphere;
- and
- (d) recovering the microsphere from the continuous phase of step (c) to prepare a deslorelin microsphere.
A method for preparing sustained release microspheres including deslorelin, comprising the steps of:
- preparing two or more different preliminary microspheres using two or more different poly(lactide-co-glycolide) or polylactide polymer and deslorelin;
- and mixing the two or more different preliminary microspheres,
- wherein the step of preparing the two or more different preliminary microspheres comprises the following steps:
- (a) dissolving deslorelin and poly(lactide-co-glycolide) or polylactide polymer in a mixed organic solvent to prepare a deslorelin-polymer solution (dispersed phase);
- (b) adding the deslorelin-polymer solution prepared in step (a) to an aqueous solution phase (continuous phase) containing a surfactant to prepare a dispersed phase in an emulsion state;
- (c) extracting the organic solvent from the dispersed phase in the emulsion state prepared in step (b) into a continuous phase and evaporating the organic solvent to form a microsphere;
- and
- (d) recovering the microsphere from the continuous phase of step (c) to prepare the preliminary microsphere.
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Dependencies are inferred from the claim text.