Thymopentin sustained release microsphere and its preparation method and application

A technology of slow-release microspheres and thymus, which is used in pharmaceutical formulations, peptide/protein components, medical preparations containing active ingredients, etc., and can solve the problems of large porosity and low drug loading of thymopentin sustained-release microspheres. , to achieve the effect of small total amount and high drug loading

Inactive Publication Date: 2017-09-26
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The thymopentin slow-release microspheres disclosed in CN1714861A have lower drug loading and larger porosity

Method used

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  • Thymopentin sustained release microsphere and its preparation method and application
  • Thymopentin sustained release microsphere and its preparation method and application
  • Thymopentin sustained release microsphere and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Using the W / O / W double emulsion solvent volatilization method, feed the external water phase osmotic pressure regulator sodium chloride at 10, 20, 40, 60, 80 mg / mL, and polymerize the monomer of biodegradable pharmaceutical polymer material PLGA The molar ratio is 50:50 and the viscosity is 0.59dL / g. Microsphere samples were prepared as follows:

[0040]Weigh 2.0g PLGA (polymerization molar ratio 50:50, viscosity 0.59dL / g) and dissolve in 8.0mL dichloromethane to make the oil phase in double emulsion; dissolve 600mg TP-5 in 1.2mL water for injection to make inner water phase; the inner water phase is added to the organic phase of dichloromethane as the middle oil phase, placed in a high-shear emulsification disperser, and treated at 17,000rpm for 2.0min to form W / O type colostrum; with 0.5% poly Vinyl alcohol (PVA) as the emulsifier, a predetermined amount of sodium chloride (NaCl) as the osmotic pressure regulator 80mL aqueous solution as the external water phase, pou...

Embodiment 2

[0043] Using the W / O / W double emulsion solvent evaporation method, fluorescein isothiocyanate-labeled thymopentin (FITC-TP5, prepared by polypeptide solid-phase synthesis, purity ≥ 95%, kept away from light) and thymopentin ( TP-5) Feed and mix according to the weight ratio of 1:5, the concentration of sodium chloride in the external aqueous phase is 40mg / mL, the monomer polymerization molar ratio of the biodegradable pharmaceutical polymer material PLGA is 50:50, and the viscosity is 0.59dL / g. Prepare microsphere samples under dark conditions as follows:

[0044] Weigh 2.0g PLGA (polymerization molar ratio 50:50, viscosity 0.59dL / g) and dissolve it in 8.0mL dichloromethane to make the oil phase in double emulsion; dissolve 100mg FITC-TP5 and 500mg TP-5 in 1.2mL Prepare the inner water phase in water for injection; add the inner water phase to the organic phase of dichloromethane as the middle oil phase, place it in a high-shear emulsification disperser, and process it at 17...

Embodiment 3

[0047] Using the W / O / W double emulsion solvent volatilization method, the external water phase osmotic pressure regulator sodium chloride is fed at 70, 100 mg / mL, and the monomer polymerization molar ratio of the biodegradable pharmaceutical polymer material PLGA is 50:50 , the viscosity is 0.38dL / g. Prepare microsphere samples under dark conditions as follows:

[0048] Weigh 2.0g PLGA (polymerization molar ratio 50:50, viscosity 0.38dL / g) and dissolve in a mixed solvent of 6.5mL dichloromethane and 1.5mL ethyl acetate to make the oil phase in double emulsion; 600mg isothiocyanate Fluorescein-labeled thymopentin (FITC-TP5, prepared by polypeptide solid-phase synthesis, purity ≥ 95%, stored away from light) was dissolved in 1.2mL water for injection to make the inner water phase; the inner water phase was added to the oil phase In the organic phase of the mixed solvent, place it in a high-shear emulsifying disperser, and treat it at 17,000rpm for 2.0min to form W / O colostrum; ...

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Abstract

The invention discloses a thymopentin sustained release microsphere and its preparation method and application. The thymopentin sustained release microsphere comprises thymopentin and biodegradable pharmaceutical polymers; the drug loading capacity and porosity of the sustained release microsphere have specific scale. Through controlling the porosity and the drug loading capacity in the scale of the invention, the long-cycle release of the drug can be realized and the internal drug release characteristics of the thymopentin sustained release microsphere can be controlled; thus the thymopentin sustained release microsphere capable of meeting various clinical application demands is prepared.

Description

technical field [0001] The invention relates to thymopentin sustained-release microspheres, a preparation method and application thereof. Background technique [0002] Protein peptide drugs have the advantages of high curative effect and small dosage. The rapid development of modern biotechnology has made it possible to produce large-scale and efficient bioactive protein peptide drugs, making them more and more widely used in clinical practice. However, protein and polypeptide drugs have the disadvantages of poor stability, easy degradation in vivo, and short half-life, which lead to limited administration forms and single administration routes in clinical application. Most of the current clinical dosage forms are injection solutions and freeze-dried powder injections. Long-term frequent injections are required during use, and patient compliance is poor. The sustained-release microspheres of this type of drug are prepared with biodegradable pharmaceutical polymer materials ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K9/16A61P1/16A61P31/20A61P37/02A61P35/00
CPCA61K9/0002A61K9/1635A61K9/1641A61K38/08
Inventor 刘玉玲王洪亮郝华珍谢兰桂夏学军董武军汪仁芸马盼盼李琳金笃嘉胡俊
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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