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Degarelix acetate injectable sustained release implant

A technology of degarelix acetate and sustained-release implants, which is applied in aerosol delivery, medical preparations with non-active ingredients, peptide/protein ingredients, etc. Treatment effect, low drug bioavailability and other issues, to achieve high drug loading capacity, maintain drug efficacy, and facilitate large-scale production.

Inactive Publication Date: 2018-03-09
南京星银药业集团有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For this class of drugs, there are many problems to be solved when the conventional drug delivery system is adopted: the patient needs to take the drug frequently or receive injections, and the interruption of the drug will cause the recurrence of the disease and bring great inconvenience to the patient; The "first-pass effect" and other effects, the bioavailability of the drug is low, and the individual differences are large; the stable blood drug concentration cannot be maintained for a long time, which reduces the therapeutic effect of the drug and increases the side effects
[0005] The existing degarelix acetate injection requires frequent dosing, and the patient's compliance is poor

Method used

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  • Degarelix acetate injectable sustained release implant
  • Degarelix acetate injectable sustained release implant
  • Degarelix acetate injectable sustained release implant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Take 24g of polylactide (Mw=15000Da), add it to an appropriate amount of benzyl benzyl ester, dissolve it ultrasonically, and configure it as a 10% polylactide solution, and then add 3.6g of degarelix acetate to the above solution , heated and stirred at constant temperature (temperature 30°C, 100 rpm) for 20 minutes to obtain a transparent and uniform drug-loaded sol system, which was sterilized by γ-ray irradiation to obtain degarelix acetate sustained-release implants for injection. Use a 1ml sterile syringe to draw an appropriate amount of gel, expel air bubbles, and seal it for use.

Embodiment 2

[0023] Take 6g of polylactide-caprolactone (Mw=8000Da), add it to an appropriate amount of N-methylpyrrolidone, dissolve it ultrasonically, and prepare a 25% polylactide-caprolactone solution, then add 3.6g of acetic acid Add the Rick raw material drug into the above solution, heat and stir at constant temperature (temperature 30°C, 100rpm) for 30 minutes to obtain a transparent and uniform drug-loaded sol system, and after γ-ray irradiation disinfection, the degarelix acetate injection delay release implants. Use a 1ml sterile syringe to draw an appropriate amount of gel, expel air bubbles, and seal it for use.

Embodiment 3

[0025] Take 4.5g of polylactic acid-glycolic acid (Mw=20000Da), add it to an appropriate amount of N-methylpyrrolidone, dissolve it ultrasonically, and configure it into a 18% polylactic acid-glycolic acid solution, and then add 1.8g of degarelix acetate raw material Add the drug into the above solution, heat and stir at a constant temperature (temperature 30°C, 100rpm) for 20 minutes to obtain a transparent and uniform drug-loaded sol system, which is sterilized by γ-ray irradiation to obtain degarelix acetate injection-type sustained-release implant agent. Use a 1ml sterile syringe to draw an appropriate amount of gel, expel air bubbles, and seal it for use.

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Abstract

The invention relates to an injectable sustained release implant comprising degarelix acetate and a preparation method of the injectable sustained release implant. The implant is a liquid preparationprepared by dissolving degarelix acetate and a biodegradable high-molecular polymer into an appropriate organic solvent. The liquid preparation is injected into the human body through local subcutaneous or muscular injection, the solvent is rapidly dispersed into the surrounding tissue water, the polymer is not soluble in water, is solidified on the administration part, wraps the medicine to forma semi-solid or solid medicine storage reservoir, the medicine is slowly released along with the degradation of the polymer, so that the effect of long-acting controlled release is achieved. The implant has the advantages that the troublesome of multiple administration for a patient is reduced, the untoward effect of the medicine is reduced and the compliance is improved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a degarelix acetate injection-type sustained-release implant and a preparation method thereof. Background technique [0002] Among the drugs used clinically, there is a class of drugs that need to be administered stably for a long time (several months or even years). For this class of drugs, there are many problems to be solved when the conventional drug delivery system is adopted: the patient needs to take the drug frequently or receive injections, and the interruption of the drug will cause the recurrence of the disease and bring great inconvenience to the patient; Influenced by the "first-pass effect", the bioavailability of the drug is low and the individual differences are large; the stable blood drug concentration cannot be maintained for a long time, which reduces the therapeutic effect of the drug and increases the side effects. Therefore, in order to...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K38/09A61K47/34A61P13/08A61P35/00
CPCA61K38/09A61K47/34A61K9/0024A61K9/06
Inventor 刘铠豪赵文华
Owner 南京星银药业集团有限公司
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