A kind of injection preparation containing exendin-4 Fc fusion protein

A fusion protein and injection preparation technology, applied in the field of biomedicine, can solve the problems of adverse effects, short shelf life, high production cost, etc., and achieve the effect of reducing surface interaction, ensuring quality and activity, and ensuring solubility

Active Publication Date: 2020-03-17
BEIJING DONGFANG BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These four drugs are all small-molecule chemical drugs, among which Exenatide Microsphere Injection (Bida Yang) is a long-acting sustained-release drug, and the other three drugs are all short-acting GLP-1 analogues, which not only have a short half-life, but also give The high frequency of medication increases the patient’s medication burden and pain, and the patient has obvious gastrointestinal reactions after each administration, and long-term administration will bring great inconvenience and pain to the patient; exenatide microspheres Injection (Baidayang), its preparation uses polyethylene lactide and sucrose as auxiliary materials, although it has a sustained release effect and can reduce the frequency of medication, but the microsphere preparation has a burst release effect, which is likely to cause unstable blood drug concentrations in patients , because the microspheres cannot be sterilized and filtered, the entire aseptic process is required, the production cost is high, the process and quality controllability is poor, and there is a risk of microbial contamination. In addition, recent studies have confirmed that exenatide microspheres and exenatide common Compared with injections, it can significantly increase the risk of thyroid C-cell cancer, and has significant adverse effects. The drug has been marked with a black box warning in the instructions by the US Food and Drug Administration
In addition, the existing injections or microsphere injections have a short storage period, and the stability of the drug molecules in the injection cannot be guaranteed during storage. Therefore, there is an urgent need for a long-term storage that can ensure the stability of the drug during long-term storage. GLP-1 analog preparation products with high quality, long-acting, small side effects, safe and reliable preparation process, and low adverse reactions

Method used

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  • A kind of injection preparation containing exendin-4 Fc fusion protein
  • A kind of injection preparation containing exendin-4 Fc fusion protein
  • A kind of injection preparation containing exendin-4 Fc fusion protein

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] An injection preparation containing Exendin-4 Fc fusion protein, the injection preparation comprises Exendin-4 Fc fusion protein and injection mixture, the pH value of the injection mixture is 6.5, and each mL injection preparation contains 2mg Exendin-4 Fc fusion protein, The injection mixture consists of the following ingredients in grams by weight:

[0037]

[0038]

[0039] The balance is water for injection, which is added to a vial to prepare 1 mL of injection preparation.

[0040] Wherein, the amino acid sequence of the Exendin-4 Fc fusion protein is shown in SEQ ID NO.1.

Embodiment 2

[0042] An injection preparation containing Exendin-4 Fc fusion protein, the injection preparation includes Exendin-4 Fc fusion protein and injection mixture, the pH value of the injection mixture is 6.0, and each mL injection preparation contains 1.5mg Exendin-4 Fc fusion protein , the injection mixture consists of the following ingredients in grams by weight:

[0043] Select specific ingredients Surfactant 0.1mg Tween 40: 0.04mg, Poloxamer 0.06mg Solution buffer 0.1mg Phosphoric acid: 0.05mg, succinic acid: 0.05mg Osmotic regulator 5mg Fructose 2.5mg, sodium chloride 2.5mg Stabilizer 50mg Trehalose 10mg, Mannitol 10mg, Chitosan 30mg

[0044] The balance is water for injection, which is added to a vial to prepare 1 mL of injection preparation.

[0045] Wherein, the amino acid sequence of the Exendin-4 Fc fusion protein is shown in SEQ ID NO.1.

Embodiment 3

[0047] An injection preparation containing Exendin-4 Fc fusion protein, the injection preparation includes Exendin-4 Fc fusion protein and injection mixture, the pH value of the injection mixture is 6.7, and each mL injection preparation contains 2.5mg Exendin-4 Fc fusion protein , the injection mixture consists of the following ingredients in grams by weight:

[0048] Specific ingredients Surfactant 2mg Glycerin Fatty Acid Ester 1.5mg, Poloxamer 0.5mg Solution buffer 0.8mg Citric acid 0.4mg, phosphoric acid 0.4mg Osmotic regulator 10mg Sodium chloride 5mg, glucose 5mg Stabilizer 90mg Trehalose 10mg, Mannitol 50mg, Chitosan 30mg

[0049] The balance is water for injection, which is added to a vial to prepare 1 mL of injection preparation.

[0050] Wherein, the amino acid sequence of the Exendin-4 Fc fusion protein is shown in SEQ ID NO.1.

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PUM

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Abstract

The invention relates to the field of biological medicines, and particularly provides an injection preparation containing Exendin-4Fc fusion protein. The injection preparation is prepared from the Exendin-4Fc fusion protein and injection mixed liquid, wherein a pH value of the injection mixed liquid is 6.0-6.7, each millilitre of the injection preparation contains 1.5-2.5 mg of the Exendin-4Fc fusion protein, and the injection mixed liquid is prepared from the following components in parts by weight: 0.1-2.0 parts of surfactant, 0.1-0.8 part of a solution buffering agent, 5-10 parts of an osmotic pressure adjusting agent and 50-90 parts of stabilizer. The injection preparation containing the Exendin-4Fc fusion protein can be stably stored for at least 36 months under circumstances in whichvarious detection indexes are stable, and corresponding physicochemical quality standards are met, so that a storage life of the Exendin-4Fc fusion protein is effectively prolonged.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to an injection preparation containing Exendin-4 Fc fusion protein. Background technique [0002] Diabetes is a chronic metabolic disorder that occurs when the human pancreas cannot produce enough insulin or cannot effectively use the insulin produced. At present, diabetes is one of the four major non-communicable diseases of human beings. Global public health has posed a serious threat. [0003] Diabetes mainly includes type I and type II. Among them, type I diabetes, also known as insulin-dependent diabetes, is an insulin deficiency caused by the body's immune system damaging pancreatic β cells. Type II diabetes is a complex disease caused by factors such as relative insulin deficiency, or insulin resistance in liver, muscle and adipocytes, or excessive glucagon secretion. [0004] GLP-1 (glucagon-like peptide-1) is a peptide hormone composed of 31 amino acids encoded by the...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/26A61K47/14A61K47/12A61K47/24A61K38/22A61K47/64A61P3/10
CPCA61K9/0019A61K9/08A61K38/2278A61K47/12A61K47/14A61K47/24A61K47/26A61K47/42A61P3/10
Inventor 白义王康孙宇石
Owner BEIJING DONGFANG BIOTECH
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