Goserelin slow release microsphere preparation and preparation method thereof

A sustained-release microsphere preparation and technology of sustained-release microspheres, which are applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Lin microsphere injection implant patent reports and other issues, to achieve the effect of reducing the frequency of administration, eliminating the phenomenon of drug concentration peaks and valleys, and reducing the dosage of administration

Inactive Publication Date: 2012-05-09
SHENZHEN JYMED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Goserelin slow release microsphere preparation and preparation method thereof
  • Goserelin slow release microsphere preparation and preparation method thereof
  • Goserelin slow release microsphere preparation and preparation method thereof

Examples

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Embodiment 1

[0022] Weigh 15 mg of goserelin acetate and dissolve it in distilled water to obtain an internal aqueous phase; weigh 200 mg of PLA and 800 mg of PLGA (polymerization ratio = 1:1) and dissolve in dichloromethane to obtain an oil phase. Prepare 50 ml of a 5% PVA solution and 500 ml of a 0.5% PVA solution. First transfer the goserelin acetate solution into the dichloromethane solution with PLA and PLGA, and place it on an emulsifying disperser at room temperature at high speed (30000rpm) for 30 seconds, and then transfer the resulting W / O emulsion to a concentration of 20ml In a 5% PVA solution, place it on an emulsifying disperser at 5000 rpm and homogenize the milk for 1 minute to obtain a W / O / W type double emulsion. Transfer it into 500 ml of 0.5% PVA solution and place it on a mechanical stirrer. Stir at low speed at 500 rpm for 2 hours, centrifuge, collect the resulting microspheres, wash with distilled water several times, and then collect by centrifugation, freeze-dry, and...

Embodiment 2

[0030] Weigh 15 mg of goserelin acetate and dissolve it in distilled water to obtain the internal water phase; weigh 1000 mg of PLGA (polymerization ratio = 1:1) and dissolve it in dichloromethane to obtain the oil phase. Prepare 50 ml of a 5% PVA solution and 500 ml of a 0.5% PVA solution. First transfer the goserelin acetate solution into the dichloromethane solution with PLGA, and place it on an emulsifying disperser at high speed (30000rpm) for 30 seconds at room temperature, and then transfer the obtained W / O emulsion to 20ml with a concentration of 5 % PVA solution, place it on the emulsifying disperser at 5000 rpm and homogenize the milk for 1 minute to obtain W / O / W type double emulsion, transfer it into 500ml 0.5% PVA solution, place it on a mechanical stirrer at 500 rpm Stir at low speed for 2 hours, centrifuge, collect the microspheres, wash them with distilled water several times, then collect them by centrifugation, freeze-dry them, and dispense them into Goserelin ...

Embodiment 3

[0038] Weigh 25 mg of goserelin acetate and dissolve it in distilled water to obtain an internal aqueous phase; weigh 500 mg of PLA and 1500 mg of PLGA (polymerization ratio = 3: 2) and dissolve in dichloromethane to obtain an oil phase. Prepare 100ml of PVA solution with a concentration of 5% and 1000ml of PVA solution with a concentration of 0.5%. First transfer the goserelin acetate solution into the dichloromethane solution with PLA and PLGA, and place it on an emulsifying disperser at room temperature at high speed (30000rpm) for 30 seconds, and then transfer the resulting W / O emulsion to a concentration of 20ml In a 5% PVA solution, place it on an emulsifying disperser at 5000 rpm and homogenize the milk for 1 minute to obtain a W / O / W type double emulsion. Transfer it into 500 ml of 0.5% PVA solution and place it on a mechanical stirrer. Stir at low speed at 500 rpm for 2 hours, centrifuge, collect the resulting microspheres, wash with distilled water several times, and t...

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Abstract

The invention discloses a goserelin slow release microsphere preparation and a preparation method thereof. The slow release microsphere preparation comprises, based on the weight of microspheres, 0.5% to 30% (w/w) of goserelin or a salt thereof, 70% to 99.5% of a biodegradable and biocompatible high-molecular material with a molecular weight of 5, 000 to 300, 000 Dalton and 0.1% to 10% of other pharmaceutically acceptable accessories. The slow release microspheres in the invention have an average particle size of 5 to 40 mu m and an entrapment rate of greater than 80%. The slow release microspheres have a slow release period as long as a plurality of days or months, obviously reduce usage frequency of the preparation, improve bioavailability of goserelin, reduce toxic and side effects of the preparation and benefit clinical treatment.

Description

Technical field: [0001] The invention relates to the technical field of sustained-release microsphere preparations, in particular to a sustained-release preparation containing goserelin or its salt and a preparation method. Background technique: [0002] Goserelin is a synthetic analogue of LHRH, which can promote the release of gonadal hormones. Its effect is 50-100 times stronger than that of LHRH secreted by the human body. LH-RH analogues bind to most of the pituitary LH-RH receptors through competition , Feedback inhibition of the secretion of LH and FSH, thereby inhibiting the production of ovarian estrogen, to achieve the therapeutic effect of drug-induced ovariectomy. [0003] The Goserelin dosage form currently available on the market is an implant. It is a product developed by AstraZeneca Pharmaceutical Co., Ltd. in the United Kingdom. It is a polymer sustained-release implant that can be gradually biodegraded in the body. Reid". It was approved for listing in France in...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K38/08A61K47/34A61K47/38A61K47/42A61P35/00
Inventor 支钦姚志勇李新宇
Owner SHENZHEN JYMED TECH
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