Goserelin release microsphere preparation, preparation method and detecting method thereof

A slow-release microsphere preparation and microsphere technology, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., can solve problems that have not been reported, and achieve convenient clinical use, The effect of improving compliance and reducing the number of injections

Inactive Publication Date: 2010-06-09
RESEARCH INSTITUTE OF TSINGHUA UNIVERSITY IN SHENZHEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] Under normal renal function, the plasma clearance half-life is 2-4 hours. In order to maintain the effective blood concentration, it needs to be administered once a day. Because castration requires long-term administration, long-term administration is required. In order to reduce the adverse effects caused by administration Discomfort, it is necessary to design goserelin to be administered o...

Method used

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  • Goserelin release microsphere preparation, preparation method and detecting method thereof
  • Goserelin release microsphere preparation, preparation method and detecting method thereof
  • Goserelin release microsphere preparation, preparation method and detecting method thereof

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preparation example Construction

[0053] The preparation method of microsphere preparation can be realized by methods such as phase separation method, drying method in water, spray drying method, wherein the drying method in water is preferred, and its basic process: dissolve lactide-glycolide copolymer in dichloromethane or acetic acid An organic solvent such as ethyl ester is used to obtain an organic phase, and goserelin is dissolved in a gelatin solution to form a water phase. Mix well to form colostrum, prepare an aqueous solution of a stable emulsifier, disperse the W / O colostrum in the solution containing a stable emulsifier, stir to form a W / O / W double emulsion, evaporate the film, stir and centrifuge for washing, and add manna Alcohol is used as a skeleton agent and freeze-dried to obtain goserelin microspheres containing double-layer organic phases.

[0054] The preparation method of the goserelin sustained-release microsphere preparation of the present invention is characterized in that two polymer ...

Embodiment 1

[0058] Weigh 750mg lactide-glycolide copolymer (75:25, molecular weight 15000) and dissolve in 5ml dichloromethane as organic phase. 1 , Weigh 125mg goserelin and dissolve in 2.5ml 20% gelatin aqueous solution as the water phase W 1 , the organic phase and the aqueous phase are dispersed at a high speed at 40°C to become W 1 / O colostrum, then stir and disperse the colostrum in 250mg / 2ml polylactic acid (molecular weight 25000) dichloromethane solution, slowly add the above solution dropwise to 500ml containing 0.1% polyvinyl alcohol 205, stir and disperse at a temperature of about 40°C 1h, lower the temperature and stir for 6h, volatilize to remove the organic solvent, filter and wash with water, add 20% mannitol in total as the skeleton agent to freeze-dry, and pack into goserelin microsphere preparations with an actual drug loading of 36mg, particle size 50 -100um, sterilization method, using 60 Sterilized by Co gamma radiation. One dose is injected subcutaneously once a...

Embodiment 2

[0061] Dissolve 1000 mg of lactide-glycolide copolymer (50:50, molecular weight 20000) in 5 ml of dichloromethane as organic phase O 1 , Weigh 150mg goserelin and dissolve in 2.5ml 20% gelatin aqueous solution as the water phase W 1 , heated to 50°C, and the organic phase and the aqueous phase were dispersed ultrasonically (35HZ) at 50°C for 5min to become W 1 / O colostrum, then the colostrum is stirred and dispersed in the dichloromethane solution of the polylactic acid (molecular weight 25000) of 300mg / 2ml, the above solution is slowly added dropwise to 20ml containing 0.5% polyvinyl alcohol 205, and the homogenizer is dispersed at a high speed (10000rpm / min), evaporating on a rotary evaporator at 0°C for 30min, transferring to an open instrument and stirring at room temperature for 12h, volatilizing to remove the organic solvent, filtering and washing with water, adding 20% ​​mannitol as a skeleton agent to freeze-dry, and subpackaging into actual drug loading Goserelin m...

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Abstract

The invention discloses a Goserelin release microsphere preparation, wherein the Goserelin microsphere contains Goserelin or salt thereof which is 0.1% to 40% of the weight of the microsphere, high molecular material which is biodegradable and biocompatible, has the molecular weight ranged from 5000 to 100,000 daltons and is 60% to 99.9% of the weight of the microsphere, and other medical acceptable auxiliary materials which are 0% to 15% of the weight of the microsphere. The Goserelin or salt thereof is packed or embedded in the high molecular material. The size of the microsphere is 1 to 10 microns and the average size is 5 to 50 microns. The invention further discloses a preparation method and a detecting method for the Goserelin release microsphere preparation. The Goserelin release microsphere preparation of the invention can work for days, weeks, even months by just injecting for one time so the injection times is reduced, the compliance of patient is promoted, and the clinical use is convenient. Furthermore, the patient is convenient to take medicine.

Description

technical field [0001] The invention relates to the technical field of sustained-release pharmaceutical preparations, in particular to a sustained-release preparation containing goserelin and a preparation method thereof. Background technique [0002] Studies have confirmed that the hypothalamus releases gonadotropin-releasing hormone GnRH to the pituitary in the form of small pulses, and GnRH binds to the GnRH receptor on the pituitary cell membrane to form a ligand-receptor complex, and the transfer of the complex to the cell triggers a series of reactions , leading to the release of luteinizing hormone and follicle-stimulating hormone, which stimulates the ovary to secrete estrogen and progesterone. However, GnRH is not combined with all GnRH receptors on the cell membrane, and there is always a part of GnRH receptors that are vacant, thus ensuring that there are enough receptors to respond to the next release of GnRH. [0003] Since sex hormone-releasing hormone product...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K38/08A61K47/30A61P35/00A61P13/08
Inventor 阎玺庆李荣先贾强裴渭静刘西京
Owner RESEARCH INSTITUTE OF TSINGHUA UNIVERSITY IN SHENZHEN
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