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Self-assembled polypeptide, preparation method and application thereof

A self-assembly and self-selection technology, applied in the field of pharmaceutical excipients, can solve problems such as poor water solubility

Inactive Publication Date: 2014-06-04
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Therefore, the purpose of the present invention is to provide a self-assembled polypeptide capable of forming complexes with other polar materials, which can effectively improve the water solubility of the current polar drugs.

Method used

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  • Self-assembled polypeptide, preparation method and application thereof
  • Self-assembled polypeptide, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] The preparation of embodiment 1 polypeptide

[0067] Chloromethyl polystyrene resin is used as an insoluble solid-phase self-assembly. First, the amino acid whose amino group is protected by a blocking group (G) is covalently linked to the solid-phase self-assembly. Under the action of trifluoroacetic acid, the protective group of the amino group is removed, so that the first amino acid is connected to the solid phase self-assembly. Then the carboxyl group of the second amino acid whose amino group is blocked is activated by N,N'-dicyclohexylcarbodiimide (DCC, Dicyclohexylcarbodiimide), and the carboxyl group is activated by DCC. The amino group of the first assembled amino acid reacts to form a peptide bond, thus generating a dipeptide with a protecting group on solid-phase self-assembly. Repeat the above peptide bond formation reaction to grow the peptide chain from the C-terminus to the N-terminus until the desired length of the peptide chain is reached. Using th...

Embodiment 2

[0076] The complex of embodiment 2 paclitaxel and self-assembling polypeptide

[0077] Paclitaxel (purchased from Shanghai Demo Chemical Co., Ltd.) and the self-assembled polypeptide 1 prepared in Example 1 were respectively 25:1, 1:100, 10:1, 1:25 and 1:50 (the following ratios do not indicate the same is the molar ratio), dissolved in an appropriate amount of normal saline, mixed thoroughly, and mixed ultrasonically for 5 minutes at 4°C to obtain a complex solution, and the monomer and complex were measured by HPLC method, the specific HPLC The instrument is (Agilent 1100), the mobile phase is A acetonitrile (1 / 1000 trifluoroacetic acid), mobile phase B water (1 / 1000 trifluoroacetic acid), filler octadecylsilane bonded silica gel, detection The conditions are: detection wavelength: 214nm, gradient conditions for elution: mobile phase A changes from 35 vol% to 50 vol%, and mobile phase B changes from 65 vol% to 50 vol% within 50 minutes.

[0078] Violatriol monomer see f...

Embodiment 3

[0079] The preparation of embodiment 3 pharmaceutical compositions

[0080] Put 0.05g of poloxamer, 0.2g of mannitol, 0.1g of lactose, and 3mL of water for injection into a 10mL container, stir to dissolve, add 1mol / L citric acid to adjust the pH to 6.0, cool to 5°C, Add 5 mL of the self-assembling polypeptide complex solution containing the amino acid sequence shown in SEQ ID NO: 2 prepared by the method in Example 2 into it, continue to adjust the pH to 6.0, and add water to 10 mL. Add 10mg of activated carbon, stir at 5°C for 20 minutes, remove the activated carbon by filtration, filter and sterilize with a microporous membrane (Millipore, Inc), and divide the filtrate into 0.2mL per tube, pre-freeze for 2 hours, then freeze Press and dry for 12 hours until the temperature of the sample reaches 5°C, then dry for 2 hours to obtain a white loose block, seal it to obtain the pharmaceutical composition of the complex, put it in a prefilled syringe, and the specification is 10...

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Abstract

The present invention provides a self-assembled polypeptide, a preparation method and an application thereof, wherein the sequence of the polypeptide is an amino acid sequence represented by SEQ ID NO:1, the self-assembled polypeptide is synthesized through a chemical synthesis method, and the application is an application of the self-assembled polypeptide in drug self-assembly or pharmaceutical composition preparation. According to the present invention, the water solubility of the drug can be increased with the complex formed from the self-assembled polypeptide; and the drug intake can be easily reduced with the pharmaceutical composition prepared from the complex formed by adopting the self-assembled polypeptide so as to reduce the medical cost.

Description

technical field [0001] The invention relates to the field of pharmaceutical excipients, in particular, the invention relates to a self-assembled polypeptide and its preparation method and application, and the polypeptide can increase the water solubility of medicines. Background technique [0002] The water solubility of injectable drugs has always been an insurmountable drug delivery barrier in the field of medicine, which limits the clinical use of many drugs. Self-assembled peptides can spontaneously form nanostructures, and increase their water solubility after inclusion of drugs in their lumens. Self-assembled polypeptides have different polar ends, and their structure causes microsphere structures to be formed automatically in polar solutions. Self-assembled polypeptides have attracted widespread attention in the field of pharmacy in recent years, and they are considered to be developed as a substitute for liposomes. [0003] Self-assembled polypeptides are derived fr...

Claims

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Application Information

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IPC IPC(8): C07K14/00C07K1/06C07K1/04A61K47/48A61K9/08A61K9/19A61K31/337A61K38/22A61P3/10
CPCC07K14/00A61K31/337A61K47/42
Inventor 王玉丽郑学敏黄长江龚珉徐为人汤立达
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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