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Human relaxin-2 lyophilized powder preparation for injection

A technology for relaxin and injection, which is applied in the field of pharmaceutical preparations of human relaxin-2, and can solve problems such as easy collapse, destruction, and poor stability of ordinary injection preparations

Inactive Publication Date: 2011-07-27
山东长肽医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] As a polypeptide drug, human relaxin-2 has the general characteristics of this type of drug, that is, low oral bioavailability, easy to be degraded and destroyed by various enzymes in the body, and low stability, easy to degrade and denature
Therefore, similar to other protein peptide drugs, human relaxin-2 is not suitable for oral administration, and human relaxin-2 has a larger molecular weight, more amino acid residues than insulin, and there are three disulfide bonds. The complexity is far greater than that of the listed peptide drugs, and its stability is also low. It is sensitive to light, heat, humidity, oxidants, strong acids, and strong alkalis. The stability of ordinary injection preparations is poor.
[0007] Freeze-dried powder for injection can improve the stability of polypeptide medicine to a certain extent, but the document (Effects of reducing sugars on the chemical stability of human relaxin in the lyophilized state.1996 Journal of Pharmaceutical Science) published in 1996 Vol. 85, No. 8, pp. 873-877) showed that human relaxin-2 itself reacts easily with a variety of commonly used lyoprotectants, resulting in changes in amino acid residues or breaking of peptide chains from specific peptide bonds
It changes its primary structure and reduces its chemical stability, thus affecting its biological activity
The conformation of human relaxin-2 will also be destroyed during the freeze-drying process, and the destruction of conformation will lead to the complete loss of biological activity of human relaxin-2 spatial structure
In addition, the lyophilized product of human relaxin-2 lyophilized powder preparation is not plump and easy to collapse, and opalescence often appears in a short time after dissolving
Therefore, there is currently no proven technology that can improve the stability and bioavailability of human relaxin-2

Method used

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  • Human relaxin-2 lyophilized powder preparation for injection
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  • Human relaxin-2 lyophilized powder preparation for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 Preparation of the lyophilized powder preparation for injection of human relaxin-2

[0025] The formula is as follows:

[0026] Human Relaxin - 2 5g

[0027] Trehalose 3g

[0028] Calcium phosphate 0.9g

[0029] The preparation method is as follows:

[0030] 1) Dosing: mix human relaxin-2 with excipients, add 1000ml of water for injection, stir to dissolve at room temperature, and adjust the pH value to 4.0-6.0 with phosphate buffer;

[0031] 2) Decolorization: Add 0.03 g of activated carbon for needles to the solution prepared in step 1) according to the ratio of 0.03 g of activated carbon for needles per 100 ml of solution, stir at room temperature for 20 minutes for decolorization, filter to remove carbon, measure the pH value or further adjust the pH value , ensure that it is at 4.0-6.0, add water for injection to 1500ml, then filter with a 0.22μm microporous membrane, pack in vials, and half stopper;

[0032] 3) freeze-drying:

[0033] a. Pre-freezi...

Embodiment 2

[0036] Example 2 Preparation of the lyophilized powder preparation for injection of human relaxin-2

[0037] The formula is as follows:

[0038]

[0039] The preparation method is as follows:

[0040] 1) Dosing: mix human relaxin-2 with excipients, add 1000ml of water for injection, stir to dissolve at room temperature, and adjust the pH value to 4.0-6.0 with phosphate buffer;

[0041] 2) Decolorization: Add 0.03 g of activated carbon for needles to the solution prepared in step 1) according to the ratio of 0.03 g of activated carbon for needles per 100 ml of solution, stir at room temperature for 15 minutes for decolorization, filter to remove carbon, measure the pH value or further adjust the pH value , ensure that it is at 4.0-6.0, add water for injection to 1500ml, then filter with a 0.22μm microporous membrane, pack in vials, and half stopper;

[0042] 3) freeze-drying:

[0043] a. Pre-freezing: quickly freeze the solution in the vials to -40°C, and keep freezing fo...

Embodiment 3

[0046] Example 3 Preparation of Injectable Freeze-dried Powder Preparation of Human Relaxin-2

[0047] The formula is as follows:

[0048] Human Relaxin - 2 5g

[0049] Trehalose 3g

[0050] Calcium phosphate 1.5g

[0051]The preparation method is as follows:

[0052] 1) Dosing: mix human relaxin-2 with excipients, add 1000ml of water for injection, stir to dissolve at room temperature, and adjust the pH value to 4.0-6.0 with phosphate buffer;

[0053] 2) Decolorization: Add 0.03 g of activated carbon for needles to the solution prepared in step 1) according to the ratio of 0.03 g of activated carbon for needles per 100 ml of solution, stir at room temperature for 20 minutes for decolorization, filter to remove carbon, measure the pH value or further adjust the pH value , ensure that it is at 4.0-6.0, add water for injection to 1500ml, then filter with a 0.22μm microporous membrane, pack in vials, and half stopper;

[0054] 3) freeze-drying:

[0055] a. Pre-freezing: qui...

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Abstract

The invention discloses a human relaxin-2 lyophilized powder preparation for injection, which is composed of human relaxin-2 and medically acceptable medicinal auxiliary materials, wherein the mass ratio of the medically acceptable medicinal auxiliary materials to the human relaxin-2 is (0.2-1.5):1; and the medically acceptable medicinal auxiliary materials are selected from one or more of mannitol, trehalose, polyvinylpyrrolidone, dodecyl-beta-D-maltoside, hydroxypropyl-beta-cyclodextrin, calcium phosphate and zinc carbonate. The inventors of the invention perform a large number of pharmaceutical and animal experiments, and indicated by research, the human relaxin-2 lyophilized powder preparation for injection disclosed by the invention has good stability and full appearance, does not degrade, aggregate or generate conformational change under accelerated test conditions, and has good safety in vivo.

Description

technical field [0001] The invention relates to a pharmaceutical preparation of human relaxin-2, in particular to a freeze-dried powder preparation of human relaxin-2 for injection. Background technique [0002] Human relaxin-2, usually abbreviated as RLN2, and the drug name is also named Relaxin, namely relaxin, is a polypeptide hormone found in the human body. Human relaxin-2 consists of two chains, the A chain contains 24 amino acids and has intra-chain disulfide bonds, the B chain contains 29 amino acids, and the A chain and the B chain are connected by two disulfide bonds. Its structural formula is as follows : [0003] [0004] Where pGlu is pyroglutamic acid, Tyr is tyrosine, Ser is serine, Asn is asparagine, Cys is cysteine, His is histidine, Val is valine, Gly is glycine, Thr is threonine Amino acid, Lys is lysine, Arg is arginine, Leu is leucine, Phe is phenylalanine, Asp is aspartic acid, Trp is tryptophan, Met is methionine, Glu is glutamic acid , Ile is is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K38/22A61P9/04
Inventor 厉保秋厉凌子
Owner 山东长肽医药科技有限公司
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