Intestinal medicine-release preparation taking thymopertin PEGylation derivative as active composition and application

A technology of active ingredients and derivatives, which is applied in the field of enteric release drug preparations and uses of thymopentin PEGylated derivatives as active ingredients, and can solve problems such as large doses, unbearable patient tolerance, and poor compliance

Inactive Publication Date: 2014-07-16
张保格
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The dosage of thymopentin injection is large, the frequency is high, and the cycle is long, which makes it unbearable for patients and poor compliance

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] PEGylated thymopentin enteric-coated capsules: PEGylated thymopentin and auxiliary materials such as microcrystalline cellulose, starch, mannitol, povidone and micronized silica gel are sieved, mixed and granulated, granulated, and filled into enteric-coated capsules In the shell.

Embodiment 2

[0024] PEGylated thymopentin enteric-coated tablets: PEGylated thymopentin and auxiliary materials such as microcrystalline cellulose, starch, sodium citrate, povidone and magnesium stearate are sieved, mixed and granulated, granulated, compressed Tablets, enteric-coated.

Embodiment 3

[0026] PEGylated thymopentin enteric-coated microspheres: PEGylated thymopentin and glycolide-lactide are mixed to form microspheres, which are packed into enteric capsule shells.

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PUM

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Abstract

The invention discloses an intestinal medicine-release preparation taking a thymopertin PEGylation derivative as an active composition and application. The oral preparation of the thymopertin PEGylation derivative employs an enteric form, so that the degradation of the preparation caused by pepsin is avoided. Thymopertin linked with polyethylene glycol is increased in molecular weight, the kidney clearance is reduced and the in-vivo retention time is increased. Thymopertin linked with polyethylene glycol is degraded by in-vivo protease and amino-peptidase with a reduced speed and is retained in blood for an increased time, so that the treatment effect is improved. Injection is replaced by oral administration or a suppository, the compliance of patients is increased, and the treatment cost is reduced. The polyethylene glycol derivative of thymopertin can be used as an immunomodulator.

Description

Technical field [0001] The present invention relates to the use method and effect of PEGylated thymopentin derivatives as medicines. Background technique [0002] Thymopentin (TP5) is a synthetic pentapeptide whose amino acid sequence and structure are the same as those of thymopoietin (TP) at positions 32-36. It is an important functionally active part of TP and has similar biological activities to TP. TP5 can promote the differentiation and development of thymus and peripheral T cells, has a two-way regulatory effect on the body's immune function, and can make the immune response that is too high or too low tend to be normal. Animal experiments and clinical studies have proved that TP5 has an important regulatory effect on the immune function of patients with low immune function and autoimmune diseases. [0003] Thymopoietin (TP) is a 49-amino acid polypeptide isolated from human thymus tissue. It has biological activities such as promoting the differentiation and development of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K47/48A61K9/02A61K9/00A61P37/02A61P35/00A61P1/16
Inventor 张保格曹秀格张翕
Owner 张保格
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