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Preparation method of goserelin acetate microspheres

A technology of goserelin acetate and microspheres, which can be applied to medical preparations containing active ingredients, microcapsules, nanocapsules, etc., can solve the problem of reducing the residual amount of organic solvents, reducing the residual amount of organic solvents, and the phenomenon of drug burst release and other problems, to achieve the effect of low solvent residue, long release cycle and smooth release curve

Inactive Publication Date: 2019-04-30
QILU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The residual amount of organic solvents in the microsphere preparation process developed above needs to be further controlled and reduced
In addition, the use of an aqueous solution containing an emulsifier during the preparation of water-soluble drug microspheres is likely to cause drug burst release.
In order to reduce the sudden release of drugs, the double emulsion method adopted by Livzon Pharmaceutical Group Co., Ltd. (CN201510208322.X) is to add a small amount of organic solvent to the aqueous solution, and then remove the organic solvent by evaporation, but this method reduces the organic The advantage of solvent residue is not obvious

Method used

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  • Preparation method of goserelin acetate microspheres
  • Preparation method of goserelin acetate microspheres
  • Preparation method of goserelin acetate microspheres

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Weigh 0.2 g of goserelin acetate, dissolve 4 g of PLGA 7525 in 196 g of dichloromethane, add goserelin acetate into the PLGA in dichloromethane solution, and disperse homogeneously at 1000 rpm for 2 minutes to form a white suspension. The suspension was placed in an ice-water bath, under stirring at 500 rpm, simethicone at 5° C. was added through a syringe, and kept for 1 minute to form microsphere embryos. Transfer the mixture containing the microspheroids to n-heptane at 6 °C at 800 rpm, and stir for 60 minutes to complete the quench hardening. The hardened microspheres were collected by filtration, washed with an appropriate amount of methanol, vacuum-dried and lyophilized to obtain microsphere powder. Solvent residues: 0.12% dichloromethane, 0.75% n-heptane, 0.45% methanol.

Embodiment 2

[0043]Weigh 0.2g of goserelin acetate, dissolve 4g of PLGA 7525 in 133g of dichloromethane, add goserelin acetate into the solution of PLGA in dichloromethane, and disperse homogeneously at 1000rpm for 2 minutes to form a white suspension. The suspension was placed in an ice-water bath, under stirring at 500 rpm, simethicone at 7° C. was added through a syringe, and kept for 1 minute to form microsphere embryos. The mixture containing microspheroids was transferred to n-heptane at 5 °C at 800 rpm, and quenched and hardened after stirring for 60 minutes. The hardened microspheres were collected by filtration, washed with an appropriate amount of methanol, vacuum-dried and lyophilized to obtain microsphere powder. Solvent residues: 0.07% dichloromethane, 0.38% n-heptane, 0.61% methanol.

Embodiment 3

[0045] Weigh 0.2 g of goserelin acetate, dissolve 4 g of PLGA 7525 in 96 g of dichloromethane, add goserelin acetate into the PLGA in dichloromethane solution, and disperse homogeneously at 1000 rpm for 2 minutes to form a white suspension. The suspension was placed in an ice-water bath, under stirring at 500 rpm, simethicone at 6° C. was added through a syringe, and kept for 1 minute to form microsphere embryos. The mixture containing microspheroids was transferred to n-heptane at 8°C with a rotation speed of 800rpm, and quenched and hardened after stirring for 60 minutes. The hardened microspheres were collected by filtration, washed with an appropriate amount of methanol, vacuum-dried and lyophilized to obtain microsphere powder. Solvent residue: dichloromethane 0.05%, n-heptane 0.53%, methanol 0.34%

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Abstract

The invention provides a preparation method of goserelin acetate microspheres, which comprises the following three steps: step 1): adding a goserelin acetate bulk drug having a suitable particle sizeto an organic solvent in which PLGA is dissolved, homogenizing or performing shear dispersion to uniformly form a mixture A; step 2): injecting a coagulant into the mixture A to form a microsphere embryo; and step 3): transferring the formed microsphere embryo to a quenching liquid, stirring and quenching and hardening the materials, and then rinsing the hardened microspheres with a rinsing liquid, and performing collecting and drying, and lyophilizing to obtain microsphere powder. The preparation method of the invention has simple process, short preparation period, and low residual amount ofthe organic solvent. The prepared goserelin acetate microspheres have the advantages of small burst release effect, gentle release curve and long sustained release period.

Description

technical field [0001] The invention relates to the technical field of sustained-release microsphere preparations, in particular to a preparation method of goserelin acetate sustained-release microspheres. Background technique [0002] Gonadotropin-releasing hormone, also known as luteinizing hormone-releasing hormone (LHRH), is synthesized in the hypothalamus. It is a polypeptide hormone whose main function is to cause the pituitary gland to release follicular estrogen (FSH) and luteinizing hormone (LH), which can be used to treat certain cancers. LHRH analogues that are currently widely used for the treatment of cancer mainly include goserelin, triptorelin, leuprolide and the like. Among them, goserelin is a synthetic decapeptide of gonadotropin-releasing hormone, which is used to control the clinical symptoms and signs of endometriosis and adenomyosis, and to prevent the recurrence of endometriosis after surgery. good effect. Long-term use of goserelin can inhibit the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/09A61K9/51A61P15/00
CPCA61K38/09A61K9/5146
Inventor 李太行孙彦华杨清敏张明会
Owner QILU PHARMA CO LTD
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