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Pharmaceutical compositions of goserelin sustained release microspheres

Inactive Publication Date: 2016-01-28
SHANDONG LUYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present patent describes a way to improve the use of a drug called goserelin by adding a substance called poloxamer or polyethylene glycol (PEG) to it and making small particles called microspheres from it. This improves the amount of drug that can be trapped in the microspheres and increases the drug's bioavailability, which means it can be better absorbed by the body. This results in the drug having a higher effectiveness and being more effective in treating the condition it is designed to help with. The goserelin microspheres can have a high amount of drug entrapment and relatively high bioavailability in the body.

Problems solved by technology

When it is administrated with a non-physiological pulse frequency for a long period of time and at a large dose, it can inhibit the hypophysis from secreting luteinizing hormone (LH) and follicle stimulating hormone (FSH), resulting in a decrease in the hormone secretion capacity of gonad and the atrophy of sexual organs.
However, studies have shown that when microspheres are prepared from goserelin to which no pre-treatment is subjected, the drug entrapment efficiency is low and the loss in the manufacturing process is high, resulting in increasing in production cost.
Pharmacokinetic studies of the prepared microspheres in animals have shown that the bioavailability of goserelin is low, which makes the drug incapable of acting to its full effect.

Method used

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  • Pharmaceutical compositions of goserelin sustained release microspheres
  • Pharmaceutical compositions of goserelin sustained release microspheres
  • Pharmaceutical compositions of goserelin sustained release microspheres

Examples

Experimental program
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example 1

[0040]Appropriate amount of goserelin acetate and Poloxamer 188 were weighed and ball-mill mixed at frequency of 15 Hz for 5 min so as to obtain a mixture of solid powder. 430 mg mixture of goserelin and Poloxamer 188 (the measured amount of goserelin was 215 mg) was accurately weighed for later use. 1.721 g of PLGA (75 / 25, 0.35, 42,000) was weighed and dissolved in 10 ml of dichloromethane to form an oil phase; and then the pretreated drug mixture of solid powder was added into the oil phase, and subjected to emulsification in a high shear emulsifier (6,500 rpm, 3 min) so as to obtain a s / o primary emulsion. The primary emulsion was added into 1,000 ml of a 0.5% PVA solution at 6° C. under homogenization at 1,800 rpm, and then it was homogeneously emulsified for 2 min to obtain an S / O / W double emulsion. The double emulsion was stirred to volatilize and remove the organic solvent; the residue was washed and freeze-dried to obtain powdery microspheres. The microspheres had a drug loa...

example 2

[0041]The melting temperature of a melt extruder was set at 80° C. Appropriate amount of goserelin acetate and Poloxamer 407 were sifted and mixed. The mixture was fed into the cavity of the extruder. The stirring speed was set to n=60 and the stirring mixing time to 3 min. Then the valve handle was released to extrude the melted material, which was then allowed to become cool naturally. The material was ball-mill smashed for 2 min. 316 mg of the mixture of goserelin and Poloxamer 188 (the measured amount of goserelin was 158 mg) was accurately weighed for later use, 1.672 g of PLGA (25 / 75, 0.24, 25,000) was weighed and dissolved in 10 ml of dichloromethane to form an oil phase; and then the pretreated drug mixture of solid powder was added into the oil phase, and subjected to emulsification in a high shear emulsifier (6,500 rpm, 3 min) so as to obtain a s / o primary emulsion. The primary emulsion was added into 1,000 ml of a 0.5% PVA solution at 6° C. under homogenization at 1,800 r...

example 3

[0042]Appropriate amount of goserelin acetate and Poloxamer 188 were weighed and dissolved in water to form a clear solution, and then the solution was sprayed dried so as to obtain a mixture of solid powder. 47 mg spray-dried mixture of goserelin and Poloxamer 188 (the measured amount of goscrelin was 23 mg) was accurately weighed and put into a vial. 1.951 g of PLGA (65 / 35, 0.29, 32,000) was weighed and dissolved in 10 ml of dichloromethane to form an oil phase; and then the pretreated drug mixture of solid powder was added into the oil phase, and subjected to emulsification in a high shear emulsifier (6,500 rpm, 3 min) so as to obtain a s / o primary emulsion. The primary emulsion was added into 1,000 ml of a 0.5% PVA solution at 6° C. under homogenization at 1,800 rpm, and then it was homogeneously emulsified for 2 min to obtain an S / O / W double emulsion. The double emulsion was stirred to volatilize and remove the organic solvent; the residue was washed and freeze-dried to obtain ...

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Abstract

A composition of goserelin sustained release microspheres is provided. The microspheres comprise goserelin, at least one poly(lactide-co-glycolide) and poloxamer or PEG. The sustained release microspheres have comparatively high bioavailability, which promotes the drug taking its full effect and have entrapment efficiency over 90%.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]The application is a continuation application of International Application No. PCT / CN2014 / 075441, filed Apr. 16, 2014, which claims priority to Chinese Application No. 201310136505.6, filed Apr. 18, 2013, the contents of each of which are incorporated by reference in their entireties for all purposes.FIELD OF THE INVENTION[0002]The present disclosure relates to pharmaceutical preparations and, more particularly, to compositions of long-acting sustained release goserelin microspheres, methods for preparing the same and use of the same.BACKGROUND OF THE INVENTION[0003]Gonadotropin-releasing hormone (GnRH), also known as luteinizing hormone-releasing hormone (LHRH), is a hormone closely related to reproductive functions. When an exogenous LHRH or an analogue thereof is administrated with a physiological pulse frequency (once per 90 min) for a short period of time and at a small dose, it produces some promoting effects to the pituitary-gonada...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K38/09
CPCA61K9/1647A61K9/1682A61K38/09A61K9/1641A61K9/1694A61P5/00A61P5/06A61P13/00A61P13/08A61P15/00A61P15/08A61P35/00A61K47/34
Inventor SUN, WEIZHANG, XUEMEIWANG, TAOLENG, GUANGYISUN, KAOXIANGLI, YOUXINLIU, WANHUI
Owner SHANDONG LUYE PHARMA CO LTD
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