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Method for preparing nonapeptide microspheres without sensitized auxiliary materials

A technology of sensitization and excipients, applied in the field of preparation of nonapeptide microspheres, to achieve the effects of increasing the range, reducing the frequency of medication, and improving the compliance and medication level.

Inactive Publication Date: 2014-12-24
周晓庆 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aiming at the deficiencies in the above problems, the present invention provides a method for preparing nonapeptide microspheres without allergenic excipients. The method is simple in process and solves the immune reaction of gelatin excipients in microsphere preparations by optimizing process parameters. problems, adapted to industrial production

Method used

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  • Method for preparing nonapeptide microspheres without sensitized auxiliary materials
  • Method for preparing nonapeptide microspheres without sensitized auxiliary materials
  • Method for preparing nonapeptide microspheres without sensitized auxiliary materials

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Investigate the influence of the volume of the external water phase on the encapsulation of leuprolide acetate

[0039] Pretreatment of the raw material leuprolide acetate;

[0040] Put the pretreated 100 mg leuprolide acetate raw material into 300 mg of water and dissolve it as the inner water phase W solution, and the inner water phase W solution is not added with the allergenic auxiliary material gelatin;

[0041] Add 2.0g of lactic acid-glycolic acid polymer to 20g of methylene chloride as the oil phase O solution. The molecular weight of the lactic acid-glycolic acid polymer used is 12000-15000, the molar ratio of lactic acid to glycolic acid is 75:25, and lactic acid-ethanol The acid polymer is an acid end-blocking polymer;

[0042] The prepared inner water phase W solution and oil phase O solution are mixed, and the phacoemulsification method is adopted. The phacoemulsification method includes first-stage ultrasound and second-stage ultrasound. The first-stage ultrasonic...

Embodiment 2

[0050] Investigate the effect of double emulsion temperature on the surface morphology of microspheres

[0051] Pretreatment of the raw material leuprolide acetate;

[0052] Put the 100 mg pretreated leuprolide acetate raw material into 300 mg of water and dissolve it as the inner aqueous phase W solution, and the inner aqueous phase W solution is not added with the allergenic auxiliary material gelatin;

[0053] Add 2.0 g of lactic acid-glycolic acid polymer to 20 g of dichloromethane as an oil phase O solution, the molecular weight of lactic acid-glycolic acid used is 12000-15000, the molar ratio is 75:25, and acidic end-capped polymer is selected;

[0054] The prepared inner water phase W solution and oil phase O solution are mixed, and the ultrasonic emulsification method is adopted. The ultrasonic power in the first stage is 10W, and the ultrasonic power in the second stage is 30W. Adjust the ultrasonic power to make the mixture become milky white, namely Get colostrum

[0055] Po...

Embodiment 3

[0063] Investigate the effect of speed on the particle size of microspheres during mixing of double emulsion

[0064] Pretreatment of the raw material leuprolide acetate;

[0065] Put the 100 mg pretreated leuprolide acetate raw material into 300 mg of water and dissolve it as the inner aqueous phase W solution, and the inner aqueous phase W solution is not added with the allergenic auxiliary material gelatin;

[0066] Add 2.0 g of lactic acid-glycolic acid polymer to 20 g of dichloromethane as an oil phase O solution. The molecular weight of lactic acid-glycolic acid used is 12000-15000 and the molar ratio is 75:25;

[0067] The prepared inner water phase W solution and oil phase O solution are mixed, and the ultrasonic emulsification method is adopted. The ultrasonic power in the first stage is 10W, and the ultrasonic power in the second stage is 30W. Adjust the ultrasonic power to make the mixture become milky white, namely To obtain colostrum, the temperature of the colostrum solu...

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Abstract

The invention relates to a method for preparing nonapeptide microspheres without sensitized auxiliary materials. The method comprises the following steps: pretreating a raw material leuprolide acetate; dissolving the treated leuprolide acetate into water to serve as an inner water phase solution, adding a lactic-glycolic acid polymer into dichloromethane to serve as an oil phase solution; mixing the prepared two-phase solution, and regulating the ultrasonic power, so that the mixed solution becomes milk white, pouring the mixed solution into polyvinyl alcohol for stirring at a high speed, transferring the stirred solution into evaporation equipment, so that the dichloromethane volatilizes out; centrifugally screening, washing and collecting semi-finished nonapeptide microspheres, adding a certain amount of mannitol into the washed semi-finished microspheres, starting prefreezing at the temperature of 35 DEG C below zero, preserving the heat at 37 DEG C for 8 hours, ending, performing freeze-drying for 51 hours, thereby obtaining the freeze-dried powder, namely the product. According to the preparation method disclosed by the invention, the problem of immunoreaction of gelatin auxiliary materials in the microsphere preparation is solved by optimizing the process parameters, and the method is suitable for industrialized production.

Description

Technical field [0001] The invention relates to a medical preparation technology, in particular to a preparation method of nonapeptide microspheres without allergenic auxiliary materials. Background technique [0002] Microsphere refers to the spherical or quasi-spherical particles prepared by the microencapsulation technology of drugs and suitable carrier materials. Generally, the materials of pharmaceutical raw materials with pharmacological activity and biodegradable polymers without pharmacological activity are used as materials The carrier is packaged together and usually equipped with a dedicated solvent when used. China is actively developing microsphere technology with independent intellectual property rights. In recent years, the research of microspheres in the fields of protein and peptide drugs, natural drugs, drugs for treating special diseases such as drug addiction or schizophrenia has attracted attention. The methods for preparing microspheres mainly include spra...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K38/08A61K47/32
Inventor 周晓庆王魁罗翰文
Owner 周晓庆
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