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Polypeptide microsphere with effects of quick release and slow release and preparation method of polypeptide microsphere

A mild and microsphere technology, which is applied in the field of polypeptide microspheres and its preparation, can solve the problems of slow onset of action, low release, and major safety issues, and achieve the effects of good shape, maintaining blood drug concentration, and improving safety

Active Publication Date: 2019-06-28
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to the 2015 edition of the Chinese Pharmacopoeia, glacial acetic acid (acetic acid) and dimethyl sulfoxide are both third-class solvents, and both need to pass the detection of residual solvents to prove their safety, and there are large safety problems
In addition, the release profile shown in the patent is too low in the initial stage, and the effect is slow after injection

Method used

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  • Polypeptide microsphere with effects of quick release and slow release and preparation method of polypeptide microsphere
  • Polypeptide microsphere with effects of quick release and slow release and preparation method of polypeptide microsphere
  • Polypeptide microsphere with effects of quick release and slow release and preparation method of polypeptide microsphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Weigh 15 mg of triptorelin acetate and 2 mg of Tween 80 and co-lyophilize, the cold trap temperature is -50°C, and the lyophilization pressure is 0.52 mbar. Weigh 500 mg of PLGA and dissolve it in 20 g of dichloromethane, and directly disperse the obtained co-lyophilized product in the dichloromethane solution of PLGA. After ultrasonic dispersion, stir at a speed of 1000 rpm and add 12.5 g of simethicone, so that PLGA is wrapped on the surface of triptorelin acetate. The resulting mixture was then added to a 750 mL n-heptane bath, solidified at a rotation speed of 400 rpm, and solidified for 30 min. Stand still, and after the suspended matter settles to the bottom, remove the upper layer to clarify n-heptane, wash with petroleum ether three times, dry, and collect the polypeptide microspheres.

Embodiment 2

[0041] Weigh 15 mg of triptorelin acetate and 4 mg of Tween 80 and co-lyophilize, the cold trap temperature is -50°C, and the lyophilization pressure is 0.52 mbar. Weigh 500 mg of PLGA and dissolve it in 20 g of dichloromethane, and disperse the co-lyophilized product directly in the dichloromethane solution of PLGA. After ultrasonic dispersion, stir at a speed of 1000 rpm and add 12.5 g of simethicone, and then dissolve the obtained The mixture was added to a 750mL n-heptane bath, solidified at a speed of 400rpm, and solidified for 30min. Stand still, and after the suspended matter settles to the bottom, remove the upper layer to clarify n-heptane, wash with petroleum ether three times, dry, and collect the polypeptide microspheres.

Embodiment 3

[0043] Weigh 40mg of exenatide and 2mg of Tween 20 and co-lyophilize, the temperature of the cold trap is -60°C, and the lyophilization pressure is 0.37mbar. Weigh 400 mg of PLA and dissolve it in 20 g of ethyl acetate, and disperse the co-lyophilized product directly in the PLA ethyl acetate solution. After ultrasonic dispersion, stir at a speed of 1000 rpm and add 12.5 g of simethicone, and then dissolve the obtained The mixture was added to a 750mL n-heptane bath, solidified at a speed of 400rpm, and solidified for 30min. Stand still, and after the suspended matter settles to the bottom, remove the upper layer to clarify n-heptane, wash with petroleum ether three times, dry, and collect the polypeptide microspheres.

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Abstract

The invention relates to a polypeptide microsphere with effects of quick release and slow release and a preparation method of the polypeptide microsphere. The method comprises the following steps thatwater-soluble polypeptide and a surfactant are co-freeze-dried to obtain a powdery co-freeze-dried product, then the co-freeze-dried product is dispersed in an organic solvent to obtain an oil-phasesolution, and a high-molecular polymer containing hydrophobic chain segments is dissolved in an organic solvent; the oil-phase solution and the poor solvent of the high-molecular polymer are mixed uniformly to obtain the polypeptide microsphere wrapped with the high-molecular polymer, then the mixture is added into a curing agent, so that the polypeptide microsphere is completely cured to obtain the polypeptide microsphere with the effects of quick release and slow release. The polypeptide microsphere with the effects of quick release and slow release and the preparation method of the polypeptide microsphere have the advantages that the polypeptide microsphere is prepared by adopting a phase separation method, the use of a polar solvent is avoided, the security is effectively improved, andthe prepared polypeptide microsphere has the effects of both quick release and slow release.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a polypeptide microsphere with quick-release and sustained-release effects and a preparation method thereof. Background technique [0002] Peptide protein drugs usually require long-term frequent injections due to their stability and half-life, resulting in poor patient compliance. In recent years, sustained and controlled release preparations have developed rapidly, and the development of slow and controlled release long-acting injection preparations of polypeptide protein drugs has also made some progress, mainly including implants and microsphere injection preparations. [0003] The preparation of protein and polypeptide drugs into microspheres can achieve taste masking, improve the stability of protein and polypeptide drugs, and the targeting effect of the preparation can prolong the drug action time and improve the curative effect. Microsphere preparation methods ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/09A61K9/50A61K47/26A61K47/34A61P15/00
Inventor 曹青日陈利清
Owner SUZHOU UNIV
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