Preparation method of goserelin acetate microspheres

A technology of goserelin acetate and sustained-release microspheres, which is applied in the field of medicine, can solve the problems of increased adverse drug reactions, etc., and achieve the effects of gentle sustained-release curve, reduced diffusion, and small burst release effect
CN104840429BActive Publication Date: 2017-12-01LIVZON PHARM GRP INC
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
LIVZON PHARM GRP INC
Publication Date
2017-12-01

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Abstract

The invention provides a preparation method of acetic acid goserelin microspheres. The preparation method includes: step 1), mixing acetic acid goserelin with water to obtain a drug solution A, and mixing PLGA (polylactic-co-glycolic acid) with an organic solution to obtain a solution B; step 2), mixing the solution A with the solution B to form colostrum through ultrasound, and adding the colostrum to a PVA (polyvinyl acetate) water solution saturated by an organic mixed solution to obtain a compound emulsion through homogeneous emulsification; step 3), stirring the compound emulsion at the room temperature for one hour, increasing the temperature to 40-45 DEG C, keeping the compound emulsion for one hour, reducing the temperature to 10 DEG C, sieving the compound emulsion to collect particles and subjecting the particles to freeze-frying. The preparation method has the advantages that the problem of adverse drug reaction increase caused by high sudden release effect of the acetic acid goserelin microspheres can be solved, and the microspheres prepared by the method have quite smooth and stable blood concentration and are beneficial to long-term medication.
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Description

technical field

[0001] The invention belongs to the field of medicine, in particular, the invention relates to a preparation method of goserelin acetate sustained-release microspheres and the goserelin acetate sustained-release microspheres prepared therefrom. Background technique

[0002] Goserelin acetate is a synthetic 10-peptide of gonadotropin-releasing hormone. Goserelin is used to control the clinical symptoms and signs of endometriosis and adenomyosis, and to prevent the recurrence of endometriosis after surgery, all of which have good results. Long-term use of goserelin acetate can inhibit the synthesis of luteinizing hormone in the pituitary gland, thereby causing a decrease in serum testosterone in men and serum estradiol in women. Increased concentrations of serum testosterone in men and serum estradiol in women.

[0003] According to the medication characteristics of the clinical indications of goserelin acetate, patients often need long-term administration. T...

Claims

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