Goserelin implant preparation and preparation method thereof

A technology of implants and preparations, applied in the directions of anti-inflammatory agents, pharmaceutical formulations, non-central analgesics, etc., can solve the problems of sudden drug release phenomenon, complex manufacturing process, high production cost, and achieve a flat release curve and a long release cycle. , The effect of low solvent residue

CN114209807APending Publication Date: 2022-03-22NANJING ANGGU PHARMA TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Publication Date
2022-03-22
Patent Text Reader

Abstract

The invention discloses a goserelin implant preparation and a preparation method thereof.The implant preparation is prepared from, by weight, 3-8 parts of dimethylformamide, 0.8-1.5 parts of oxidized proline, 2-4 parts of dimethyl sulfoxide, 3-7 parts of dioxane solution, 10-30 parts of lactic acid, 20-40 parts of glycolic acid and 3-12 parts of dimeticone. The goserelin sustained-release microsphere is low in solvent residue and has a long-acting sustained-release effect, and the goserelin sustained-release microsphere is fused with a goserelin solution, so that the goserelin sustained-release microsphere has the effects of small burst release effect, smooth release curve, long release period and the like.
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Description

technical field

[0001] The invention relates to the technical field of pharmacy, in particular to a goserelin implant preparation and a preparation method thereof. Background technique

[0002] Implants are a kind of sterile solid preparations made of drugs and auxiliary materials for value into the body. Implants are generally implanted into the body using a special syringe, or they can be implanted by surgical incision. The released drug is absorbed directly into the blood circulation through subcutaneous absorption or cavity absorption, thus avoiding the first-pass effect, high bioavailability, and a long acting time, even up to several years. Goserelin is currently the most researched drug. Gonadotropin-releasing hormone analogues are widely used in the treatment of premenopausal patients with hormone receptor-positive breast cancer. The drug acts as a medical castrate, reducing the patient's estrogen to postmenopausal levels. Goserelin is indicated for many diseases,...

Examples

Embodiment 1

[0024] The goserelin implant preparation proposed by the present invention has a raw material ratio of 8 parts of dimethylformamide, 1.5 parts of oxidized proline, 4 parts of dimethyl sulfoxide, and 7 parts of dioxane solution. , 30 parts of lactic acid, 40 parts of glycolic acid, 10 parts of simethicone.

[0025] The preparation method of goserelin implant preparation, the method comprises the following steps:

[0026] S1, placing dimethylformamide and dimethyl sulfoxide in the raw material in a stirrer, and preparing a mixed solvent under neutralization and stirring at a temperature of 0°C;

[0027] S2, suspending the oxidized proline in a mixed solvent, adding dioxane solution, and stirring for 5 minutes to obtain a clear goserelin solution;

[0028] S3, mixing and stirring lactic acid 1 and glycolic acid in the raw materials to obtain a mixed solution;

[0029] S4, injecting simethicone into the mixture, agglomerating to form microsphere embryos;

[0030] S5, transferri...

Embodiment 2

[0034] The goserelin implant preparation proposed by the present invention has a raw material ratio of 7 parts of dimethylformamide, 0.8 parts of oxidized proline, 3 parts of dimethyl sulfoxide, and 4 parts of dioxane solution. , 11 parts of lactic acid, 24 parts of glycolic acid, 7 parts of simethicone.

[0035] The preparation method of the goserelin implant preparation is the same as in Example 1.

Embodiment 3

[0037] The goserelin implant preparation proposed by the present invention has a raw material ratio of 8 parts of dimethylformamide, 0.9 parts of oxidized proline, 2.7 parts of dimethyl sulfoxide, and 4 parts of dioxane solution. , 15 parts of lactic acid, 22 parts of glycolic acid, 4 parts of simethicone.

[0038] The preparation method of the goserelin implant preparation is the same as in Example 1.