Medicine for enhancing osteoblast bone formation in targeting manner and synthesis method thereof

A technology of osteoblasts and synthetic methods, applied in the direction of drug combinations, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve non-bone tissue or organ toxic side effects, reduce drug therapeutic index, lack bone specificity of drugs, etc. problems, achieve high targeting, promote osteogenesis, and reduce side effects

Inactive Publication Date: 2016-11-09
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the lack of bone specificity of the drug, it not only reduces the therapeutic index of the drug, but also causes unnecessary toxic side effects to the patient's non-bone tissues or organs, as shown in recent reports of long-term side effects of hormone replacement therapy, to represent the drug parathyroid Adrenaline as an example, after more than two years of application, the curative effect decreases, bone mass loss, and even severe side effects may include neurological symptoms, renal failure, etc.

Method used

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  • Medicine for enhancing osteoblast bone formation in targeting manner and synthesis method thereof
  • Medicine for enhancing osteoblast bone formation in targeting manner and synthesis method thereof
  • Medicine for enhancing osteoblast bone formation in targeting manner and synthesis method thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0031] A drug for targeting and enhancing bone formation of osteoblasts, the active ingredient is a polypeptide, the polypeptide is composed of 3 serines and 2 aspartic acids, and its sequence is Ser Asp Ser Ser Asp, wherein, Ser represents serine, Asp Represents aspartic acid, wherein the surface of the polypeptide is modified with PEG.

[0032] The drug also includes physiological saline with a content of 55% of the active ingredient, which, when used, is injected directly into the human body by intravenous injection.

[0033] The above-mentioned medicine for targeting and enhancing osteoblast bone formation, its synthesis method is as follows figure 1 shown, including the following steps:

[0034] (1) Preparation of polypeptides: Condensed amino acids into polypeptides at the ratio of Ser:Asp=2:3 by a twelve-channel semi-automatic polypeptide synthesizer, and set aside for use;

[0035] (2) Activation of the polypeptide: dissolve the polypeptide obtained in step (1) in de...

Embodiment 2

[0044] A drug targeted at enhancing osteoblast bone formation, its active ingredient is a polypeptide, the polypeptide is composed of 1 serine and 1 aspartic acid, and its sequence is Ser Asp, where Ser stands for serine, and Asp stands for aspartate Amino acid, wherein the surface of the polypeptide is modified with PEG.

[0045] The medicine also includes physiological saline, the content of the active ingredient is 50%, and when used, it enters the human body directly through intravenous injection.

[0046] The above-mentioned drugs targeted to enhance bone formation of osteoblasts include the following steps:

[0047] (1) Preparation of polypeptides: condense amino acids into polypeptides by using a 12-channel semi-automatic polypeptide synthesizer according to the ratio of Ser:Asp=1:1, and wait for use;

[0048] (2) Activation of the polypeptide: dissolve the polypeptide obtained in step (1) in deionized water, then add EDC and NHS equal in mass to the polypeptide to act...

Embodiment 3

[0053] A drug targeted at enhancing bone formation of osteoblasts, the active ingredient of which is a polypeptide, which consists of 10 serines and 40 aspartic acids, and its sequence is:

[0054] Ser Asp Asp Asp Asp Ser Asp Asp Asp Ser AspAsp Asp Asp Asp Ser Asp Asp Asp Ser Asp Asp Asp Asp Asp Ser Asp Asp Asp Asp Ser Asp Asp Asp Asp Asp Ser Asp Asp Asp Ser AspAsp Asp Asp Asp Ser Asp Asp Asp Ser Asp Asp Asp Asp Asp Asp, where , Ser represents serine, Asp represents aspartic acid, wherein the surface of the polypeptide is modified with PEG.

[0055] The medicine also includes physiological saline, and the content of the active ingredient is 60%. When used, it enters the human body directly through intravenous injection.

[0056] The above-mentioned drugs targeted to enhance bone formation of osteoblasts include the following steps:

[0057] (1) Preparation of polypeptides: condense amino acids into polypeptides according to the ratio of Ser:Asp=1:4 through a twelve-channel se...

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Abstract

The invention provides a medicine for enhancing osteoblast bone formation in a targeting manner. An effective component of the medicine is a polypeptide; the polypeptide is composed of two amino acids including serine and aspartic acid; the polypeptide contains 2-50 amino acids; the quantity ratio of the serine to the aspartic acid is (0.25-4) to 1; and the mass content of effective components in the medicine is 50%-60%. Compared with the prior art, osteoporosis treatment is taken as a target, and a micro-molecular active polypeptide derived from in-vivo natural protein is used as a bone target treatment medicine; and the target medicine has a bone formation cell targeting property, a good bone formation promoting capability, low cell toxicity and side effect and relatively low medicine dosage, and provides important medicine selection for osteoporosis treatment in the future.

Description

technical field [0001] The invention relates to the field of biological materials, in particular to a drug for targeting and enhancing bone formation of osteoblasts and a synthesis method thereof. Background technique [0002] Bone is a highly specific connective tissue in higher vertebrates that provides support and muscle attachment sites for the body. It is also a major source of inorganic ions and actively participates in calcium and phosphorus balance in the body. The normal development and maintenance of bone requires continuous bone resorption and reconstruction. Under physiological conditions, this balance is coordinated, the function of osteoblasts, osteoclasts and osteocytes is normal, and the integrity of bone mass and microstructure is maintained in a stable state. However, this imbalance of bone remodeling is an important cause of numerous bone diseases including osteoporosis, Paget's disease, osteoporosis, bone metastases, rheumatoid arthritis, osteomyelitis,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/05A61K38/08A61K38/16A61K47/48A61P19/08
CPCA61K38/05A61K38/08A61K38/16
Inventor 孙瑶王晓刚蔡明详
Owner TONGJI UNIV
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