Cyclic peptide glass and pharmaceutical composition glass containing cyclic peptide

A technology of composition and cyclic peptide, which is applied in the field of medicine, can solve the problems of unpublished reports of cyclic peptide glass, which have not been disclosed, and achieve high thermal/chemical stability, increase the dissolution rate of drugs, and reduce the effects of drug side effects

Active Publication Date: 2022-02-08
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no published report on cyclic peptide glass, especially the glass based on pharmaceutical composition with biological / pharmacological activity and sustained release function, and the method of converting insoluble cyclic peptide into glass state.

Method used

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  • Cyclic peptide glass and pharmaceutical composition glass containing cyclic peptide
  • Cyclic peptide glass and pharmaceutical composition glass containing cyclic peptide
  • Cyclic peptide glass and pharmaceutical composition glass containing cyclic peptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0106] A kind of preparation method of the cyclopeptide glass based on cyclosporine A (CsA) comprises the steps:

[0107] (1) Put the CsA powder in a ball mill to grind evenly, control the constant temperature of the ball mill to 25°C, and then transfer it to a crucible;

[0108] (2) Place the crucible containing CsA powder in step (1) under N 2 placed in the heating equipment under the atmosphere;

[0109] (3) heat treatment is carried out to the equipment of step (2), with 10Kmin -1 Raise the temperature of the crucible from room temperature to 573.15K at a heating rate of 20 minutes at this temperature;

[0110] (4) The equipment of step (3) is cooled down, with 10Kmin -1 Lower the crucible to an annealing furnace at 273.15K at a constant temperature for 30 minutes to anneal the glass to obtain CsA glass.

[0111] figure 1 The physical picture (a) of the CsA glass prepared in Example 1 at room temperature and the physical picture (b) of the CsA glass obtained by the po...

Embodiment 2

[0119] A kind of preparation method of the pharmaceutical composition glass based on phenylalanine-proline cyclic dipeptide (CFP) and paclitaxel (PTX) comprises the steps:

[0120] (1) Put the CFP powder in a ball mill to grind and mix evenly, control the constant temperature of the ball mill to 37°C, and then transfer it to a container;

[0121] (2) heat treatment is carried out to the container of step (1), with 20K min -1 The heating rate is to raise the temperature of the container from room temperature to 473.15K, and keep it warm for 30 minutes at this temperature;

[0122] (3) The container of step (2) is cooled down, with 10K min -1 The cooling rate reduces the container to a temperature of 333.15K;

[0123] (4) Put the PTX powder in a ball mill to grind evenly, control the constant temperature of the ball mill to 37°C, then add ethanol to completely dissolve, and the molar ratio of CFP to PTX is 25:1;

[0124] (5) Add the solution of step (4) dropwise into the cont...

Embodiment 3

[0134] A kind of preparation method of the pharmaceutical composition glass based on vancomycin, gramicidin S and penicillin comprises the steps:

[0135] (1) Put vancomycin, gramicidin S and penicillin in a ball mill, grind and mix evenly, control the constant temperature of the ball mill to 37°C, and then transfer to a container, the mass ratio of the three is 2:2:1;

[0136] (2) Add a mixed organic solvent of hexafluoroisopropanol and ethanol to the mixed powder in step (1), and stir until completely dissolved;

[0137] (3) The mixed solution obtained in step (2) is placed in a vacuum rotary evaporator, and the mixture is heated at 50K min -1 The heating rate is raised from room temperature to 443.15K temperature, and the temperature is kept at this temperature for 30 minutes to remove the organic solvent;

[0138] (4) The equipment of step (3) is cooled down, with 10K min -1 The cooling rate is reduced to 243.15K temperature, and the temperature is kept at this temperatu...

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Abstract

The invention discloses a cyclic peptide glass and a pharmaceutical composition glass containing a cyclic peptide. The cyclopeptide glass can simultaneously exert the drug effect and the function of a drug auxiliary material, and compared with a crystal and a traditional drug dosage form or an auxiliary material, the cyclic peptide glass can effectively increase the drug dissolution rate and improve the drug bioavailability, and is widely applied to the drug delivery and slow release fields of tumor resistance, virus / bacterium resistance, blood glucose control, immunoregulation, neuroregulation and the like.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to a new dosage form and a new auxiliary material of cyclopeptide medicine, in particular to a cyclopeptide glass and a cyclopeptide medicine composition glass. At the same time, it involves related technologies for effectively utilizing insoluble drugs, and in particular relates to a preparation method for converting insoluble cyclic peptide drugs into glass states to form glass drugs. This cyclic peptide glass can be used in the field of drug delivery such as anti-tumor, anti-virus / anti-bacterial, blood sugar control, immune regulation, neuromodulation, etc., especially to achieve drug sustained release therapy. Background technique: [0002] Cyclic peptides are formed by condensation and cyclization of multiple amino acids through peptide bonds, and their structures have certain conformational constraints. The unique topology of cyclic peptides makes them exceptionally stable ag...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/12C07K7/66C07K7/62C07K7/58C07K11/00C07K7/60C07K7/56C07K9/00C07K7/64C07K7/06C07K5/103C07K14/605A61K9/00A61K38/05A61K38/12A61K38/14A61K47/18A61K47/42A61P3/10A61P31/04A61P31/12A61P35/00A61P37/02C07D498/18C07D498/22A61K31/439
CPCC07K5/12C07K7/66C07K7/62C07K7/58C07K11/00C07K7/60C07K7/56C07K9/008C07K7/64C07K7/06C07K7/645C07K5/101C07K14/605A61K9/0087A61K38/05A61K38/12A61K38/14A61K47/42A61K47/183A61P31/04A61P31/12A61P35/00A61P3/10A61P37/02C07D498/18C07D498/22A61K31/439Y02A50/30
Inventor 闫学海邢蕊蕊袁成前
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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