Protein drug solid preparation and preparation method thereof

A protein drug and solid preparation technology, which is applied in the direction of drug combination, pharmaceutical formula, peptide/protein composition, etc., to achieve good protein encapsulation efficiency and maintain the effect of protein drug activity

Active Publication Date: 2021-08-13
康汉医药(广州)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no universal protein solid preparation for improving protein pharmacokinetic behavior and pharmacodynamics

Method used

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  • Protein drug solid preparation and preparation method thereof
  • Protein drug solid preparation and preparation method thereof
  • Protein drug solid preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The preparation of embodiment 1 amphiphilic polymer

[0042] Prepare amphiphilic polymers as follows:

[0043] S01. Dissolving the hydrophobic polymer material in an organic solvent, adding a hydrophilic polymer material for a mixed reaction, removing the organic solvent and other impurities in the reaction system to obtain a mixture A;

[0044] S02. The mixture A was redissolved in water, and the product was collected after purification.

[0045] S03. Collect the dialysis product, freeze overnight at -80°C, and then freeze-dry on a freeze dryer to obtain a white flocculent substance.

[0046] Hydrophilic polymer materials include polyethylene glycol, polyoxyethylene, mPEG-NH2-400, mPEG-NH2-600, mPEG-NH2-800, mPEG-NH2-1000, mPEG-NH2-2000, mPEG-NH2- 4000, mPEG-NH2-5000 or mPEG-NH 2 -At least one in 10000; Select polyethylene glycol for use in the present embodiment.

[0047]The hydrophobic polymer material preferably comprises polymaleic anhydride, poly(maleic anhydr...

Embodiment 2

[0055] Example 2 Preparation of Amphiphilic Polymer and Detection of Self-Assembly

[0056] Follow the steps below to prepare amphiphilic polymers

[0057] S01. Dissolve poly(maleic anhydride-ALT-1-octadecene) in organic solvent, add mPEG-NH in proportion 2 Mixing reaction, removing the organic solvent and other impurities in the reaction system, to obtain mixture A;

[0058] S02. Reconstitute the mixture A with water, put it into a dialysis bag and perform dialysis in pure water;

[0059] S03. Collect the dialysis product, freeze overnight at -80°C, and then freeze-dry on a freeze dryer to obtain a white flocculent substance.

[0060] The organic solvent generally selects dichloromethane, dimethyl sulfoxide, acetone, ethanol, and selects dichloromethane in this embodiment.

[0061] mPEG-NH 2 Grafting ratio P with poly(maleic anhydride-ALT-1-octadecene) m m n For (1:10)~(2:1), respectively prepare P 1 m 10 ,P 1 m 5 ,P 2 m 1 ,P 1 m 1 ,P 2 m 1 Five amphiphilic po...

Embodiment 3

[0067] The preparation of embodiment 3 insulin solid preparations

[0068] Insulin pharmaceutical preparations are prepared according to the following steps:

[0069] S11. Dissolving insulin in a buffer solution to obtain a protein drug solution;

[0070] S12. adding the amphiphilic polymer prepared in Example 1 to the protein drug solution described in step S11 to obtain a mixture;

[0071] S13. Put the mixture into a dialysis bag for dialysis in pure water, collect the dialysis product, and freeze-dry to obtain a solid insulin preparation.

[0072] The volume ratio of the amphiphilic polymer solution to the protein solution is (1:10)˜(10:1).

[0073] A magnetic stirrer can be used for mixing, the rotation speed of the magnetic stirrer is about 800rpm, and the reaction time is about 24h. The "approximately" mentioned in the summary of the invention all represent the original number and the upper and lower error is 20%, for example, "about 800rpm" is 800±160rpm.

[0074] F...

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Abstract

The invention discloses a protein drug solid preparation and a preparation method thereof, and discloses a polymer which is formed by polymerizing a hydrophilic high-molecular material and a hydrophobic high-molecular material. The polymer has good protein wrapping efficiency, and the biological activity of freeze-dried protein is kept unchanged. Therefore, the polymer can be used for preparing a protein solid preparation which is easy to preserve at normal temperature. The invention also provides a preparation method and application of the polymer, and provides a protein drug solid preparation prepared from the polymer, and a protein drug solution can be freeze-dried into a solid preparation and maintain the activity of the protein drug, and can be preserved at normal temperature and even high temperature. The protein drug solid preparation can be re-dissolved into a protein drug solution with undamaged activity, and the activity of the protein drug is maintained.

Description

technical field [0001] The invention belongs to the technical field of biomedical preparations, and more specifically relates to a protein drug solid preparation and a preparation method thereof. Background technique [0002] As a relatively new type of treatment, protein drugs have broad application prospects in the treatment of tumors and other diseases. For example, according to statistics, the US Food and Drug Administration (Food and Drug Administration, FDA) and the European Medicines Agency, EMA) has approved a total of 128 antibody drugs, 33 of which have anti-tumor indications, and many are still in the clinical research stage. The development of protein drugs has become a hot field pursued by various countries to occupy the commanding heights of biomedicine. However, due to the particularity of the structure of protein drugs, protein drugs often require relatively harsh storage conditions such as low temperature after they are made into drugs. A little carelessnes...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/02A61K9/19A61K38/28A61K47/32A61P3/10A61K38/00
CPCC08G81/025A61K9/19A61K38/28A61K47/32A61P3/10A61K38/00Y02A50/30
Inventor 刘小文
Owner 康汉医药(广州)有限公司
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