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Goserelin sustained release microsphere freeze-dried powder and preparation method thereof

A slow-release microsphere, freeze-dried powder technology, applied in freeze-dried delivery, powder delivery, microcapsules and other directions, can solve the problems of complex steps, serious burst release, etc., and achieve shortened peak time, high specificity, and convenient medication. Effect

Active Publication Date: 2019-03-01
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the existing slow-release implant has the following defects: first, this long-acting injection is an implant that requires special equipment, and professional personnel administer the drug
The preparation of goserelin microspheres by the solid-in-oil-in-water method (S / O / W method) requires the preparation of raw materials and pharmaceutical excipients such as poloxamers by freeze-drying, spray-drying, hot-melt extrusion, etc. Internal solid phase, the steps are relatively complicated
However, the spray-drying method to prepare microspheres loaded with water-soluble polypeptide drugs, the burst release is more serious

Method used

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  • Goserelin sustained release microsphere freeze-dried powder and preparation method thereof
  • Goserelin sustained release microsphere freeze-dried powder and preparation method thereof
  • Goserelin sustained release microsphere freeze-dried powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Weigh 100mg goserelin acetate, 150mg poloxamer 188, 50mg polyethylene glycol 4000 dissolved in 0.6mL water, the HLB value of poloxamer is 11, swell at 4 degrees Celsius for 10 hours to form a gel, As drug solution A. Weigh 0.8 g of lactide-glycolide copolymer (molecular weight: 5000 Dalton) and dissolve it in 5 mL of dichloromethane as solution B. Drug solution A was added to solution B, and colostrum was formed by high-speed shearing in an ice-water bath. The high-speed shearing speed was 12,000 rpm for 3 minutes. The shearing speed is 15000rpm, and the time is 4min. The double emulsion was poured into 200mL 5% NaCl solution, distilled under reduced pressure at 40°C for 30min, centrifuged, washed three times with water, and freeze-dried for 24 hours to obtain microspheres with a particle size of 20-90μm. 200 mesh, 400 mesh and 500 mesh combined standard sieve to obtain microsphere particle size are all within the limit of 25-74 μm, use 60 Sterilized by Co-gamma rays...

Embodiment 2

[0049] Weigh 120mg of goserelin acetate, 110mg of poloxamer 188, 50mg of poloxamer 407, dissolve in 0.9mL of water, the HLB value of poloxamer is 5, swell at 5 degrees Celsius for 8 hours to form a gel , Soluble in A as a drug. Weigh 1.2g of lactide-glycolide copolymer (molecular weight: 10,000 Daltons) and dissolve it in 5mL of dichloromethane as solution B. Drug solution A was added to solution B, and colostrum was formed by high-speed shearing in an ice-water bath. The high-speed shearing speed was 10,000 rpm, and the time was 4.6 minutes. The high-speed shearing speed is 20000rpm, and the time is 2min. The double emulsion was poured into 200mL 2% NaCl solution, distilled under reduced pressure at 70°C for 10min, centrifuged, washed three times with water, and freeze-dried for 24 hours to obtain microspheres. 200 mesh, 300 mesh and 500 mesh combined standard sieve to obtain microsphere particle size are all within the limit of 25-74 μm, use 60 Co-gamma ray sterilization,...

Embodiment 3

[0056] Weigh 200mg of goserelin acetate, 170mg of poloxamer 237, 20mg of poloxamer 228 dissolved in 1mL of water, the HLB value of poloxamer is 20, swell at 2 degrees Celsius for 12 hours to form a gel, as Drug solution A. Weigh 1.6g of lactide-glycolide copolymer (molecular weight: 30000 Daltons) and dissolve in 5mL of dichloromethane as solution B. Drug solution A was added to solution B, and colostrum was formed by high-speed shearing in an ice-water bath. The high-speed shearing speed was 6000 rpm for 5 minutes; The cutting speed was 17000rpm, and the time was 2.5min; the double emulsion was poured into 200mL 3% NaCl solution, distilled under reduced pressure at 35°C for 20min, centrifuged, washed three times with water, and freeze-dried for 24 hours to obtain microspheres. 90 μm, the freeze-dried microspheres passed through 200 mesh, 250 mesh and 500 mesh combined standard sieves to obtain microspheres with a particle size within the limit of 25-74 μm. 60Sterilized by C...

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Abstract

The invention relates to freeze-dried powder, in particular to goserelin sustained release microsphere freeze-dried powder and a preparation method thereof in the technical field of water-soluble polypeptide drug sustained release long-acting injections. Each microsphere in the freeze-dried powder comprises a shell, each shell wraps a core, each core is temperature-sensitive gel, when the temperature of the temperature-sensitive gel is lower than the body temperature of human bodies, the mobility of the temperature-sensitive gel is good, after the temperature of the temperature-sensitive gel is increased to be equal to the body temperature of the human bodies, the mobility is reduced, then the temperature-sensitive gel is gelatinized to form a gel core, and each shell is a biodegradable material. The goserelin sustained release microsphere freeze-dried powder has the advantages that the encapsulation efficiency reaches 90% or above, drug release is jointly controlled by the internal temperature-sensitive gel cores and external biodegradable sustained release framework materials, and the goserelin sustained release microsphere freeze-dried powder is a double-layered drug release system.

Description

technical field [0001] The invention relates to a freeze-dried powder, in particular to a water-soluble polypeptide drug slow-release long-acting injection technical field, goserelin slow-release microsphere freeze-dried powder and a preparation method thereof. Background technique [0002] Goserelin is a synthetic analogue of luteinizing hormone-releasing hormone, but compared with GnRH, it has better stability, strong affinity with GnRH receptors, long half-life, and its potency is about 100 times that of GnRH . Long-term use can inhibit the secretion of luteinizing hormone in the pituitary gland, thereby causing a decrease in serum testosterone in men and serum estradiol in women, and this effect is reversible after drug withdrawal. For male patients, the testosterone concentration can be reduced to the post-castration level about 21 days after the first medication, and the testosterone concentration has been kept within the post-castration concentration range during the...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/52A61K47/34A61K47/10A61K38/09A61P15/00A61P35/00G01N30/02
CPCA61K9/0019A61K9/19A61K9/5031A61K38/09A61K47/10A61P15/00A61P35/00G01N30/02
Inventor 唐星张宇何海冰尹湉苟靖欣戚盼
Owner SHENYANG PHARMA UNIVERSITY
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