Calcitonin long-acting sustained-release microspheres and preparation method and combination thereof

A technology for sustained-release microspheres and calcitonin, which is applied in the directions of drug combinations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Small burst release, high encapsulation rate, simple and flexible method of regulating release

Active Publication Date: 2015-08-19
SHANGHAI JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The first object of the present invention is to provide a kind of calcitonin long-acting slow-release microspheres, to solve the problem of difficult release faced in the preparation of calcitonin long-acting slow-release microsphere dosage forms in the prior art
[0005] The second object of the present invention is to provide a preparation method of calcitonin long-acting sustained-release microspheres to solve the problem of difficult release in the preparation of calcitonin long-acting sustained-release microspheres in the prior art
[0006] The third object of the present invention is to provide a combination of calcitonin long-acting sustained-release microspheres to solve the problems of difficult release and burst release in the preparation of calcitonin long-acting sustained-release microsphere dosage forms in the prior art

Method used

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  • Calcitonin long-acting sustained-release microspheres and preparation method and combination thereof
  • Calcitonin long-acting sustained-release microspheres and preparation method and combination thereof
  • Calcitonin long-acting sustained-release microspheres and preparation method and combination thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032] The preparation of calcitonin long-acting slow-release microspheres includes:

[0033] 1. Preparation of carboxylic acid dextran (Dextran-COOH)

[0034] Weigh a certain amount of dextran sodium carboxylate, select a dialysis bag with a molecular weight of 3500, and dialyze in a hydrochloric acid solution with pH=2 for 24 hours, then replace with a new solution, continue to dialyze with a hydrochloric acid solution with pH=2 for 24 hours, and then use pure water Dialyze for 24 hours, transfer to a small beaker and pre-freeze in a -20°C refrigerator for 12 hours, and finally freeze-dry in a freeze dryer before use.

[0035] Preparation of calcitonin microspheres by 2W / O / W method

[0036] This step includes the preparation of five kinds of calcitonin microspheres, wherein the type and content of PLGA are different, see Table 1, the preparation process of these five kinds of calcitonin microspheres is the same, including the following steps:

[0037] Weigh an appropriate ...

Embodiment 2

[0064] The preparation of calcitonin long-acting slow-release microspheres includes:

[0065] 1. Dextran sulfate (Dextran-SO 3 OH) and preparing granules from calcitonin and dextran sulfate

[0066] Weigh 50g of dextran sodium sulfate, select a dialysis bag with a molecular weight of 3500, and dialyze in a hydrochloric acid solution with pH=2 for 24 hours, then replace with a new solution, continue to dialyze with a hydrochloric acid solution with pH=2 for 24 hours, and then dialyze with pure water for 24 hours , transferred to a beaker and added with a mass concentration of 5% calcitonin solution and 500g of PEG (molecular weight: 8000Da) with a mass concentration of 10%, pre-freezing in a refrigerator at -20°C for 12 hours, and finally putting it into a lyophilizer for lyophilization. PEG was removed with dichloromethane for later use.

[0067] Preparation of calcitonin microspheres by 2S / O / W method

[0068] This step includes the preparation of five kinds of calcitonin m...

Embodiment 3

[0078] 1. Dextran sulfate (Dextran-SO 3 OH) preparation

[0079] Weigh a certain amount of dextran sodium sulfate, select a dialysis bag with a molecular weight of 3500, and dialyze in a hydrochloric acid solution of pH=2 for 24 hours, then replace with a new solution, continue to dialyze with a hydrochloric acid solution of pH=2 for 24 hours, and then dialyze with pure water 24h, transferred to a small beaker and pre-frozen in a -20°C refrigerator for 12h, and finally placed in a lyophilizer for freeze-drying before use.

[0080] Preparation of Calcitonin Long-acting Sustained-release Microspheres by 2W / O / W Method

[0081] This step includes the preparation of five kinds of calcitonin long-acting sustained-release microspheres, wherein the type and content of PLGA are different, see Table 5, the preparation process of these five kinds of calcitonin long-acting sustained-release microspheres is the same, including the following steps:

[0082] Weigh an appropriate amount of ...

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Abstract

The invention relates to calcitonin long-acting slow-release microspheres which comprise the following components in percentage by weight: 0.5%-4% of acidic glucosan, 1.5%-12% of calcitonin and 84%-98% of slow-release or controlled-release high molecules. The particle diameter of each calcitonin long-acting slow-release microsphere is 1-200 micrometers. A plurality of calcitonin long-acting slow-release microspheres which contain different slow-release or controlled-release high molecules are combined and different calcitonin long-acting slow-release microspheres which are mutually separated and mutually continued in the concentrated release time are selected for combination to obtain the calcitonin long-acting slow-release microsphere combination. The invention also discloses a preparation method of the calcitonin long-acting slow-release microspheres. The preparation method disclosed by the invention has the advantage that the slow-release or controlled-release high molecules can be completely released by reducing the adsorption of the calcitonin on the slow-release or controlled-release high molecules by causing a local acid environment by adding the acidic glucosan, thereby overcoming the defect that a protein polypeptide medicament is easy to be adsorbed in a slow-release material without being released; and the calcitonin long-acting slow-release microsphere combination which has the advantages of stability, long action, slow release and less burst release through the combination of the calcitonin microspheres in different prescriptions can be obtained.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations and relates to a cytokine drug calcitonin, in particular to a calcitonin long-acting slow-release microsphere and a preparation method, combination and application thereof. Background technique [0002] Osteoporosis is a systemic disease characterized by decreased bone mass, microarchitectural destruction of bone tissue, increased bone fragility, and susceptibility to fracture. The incidence of osteoporosis in the elderly is relatively high. With the aging of society, the incidence of osteoporosis is on the rise, and it is expected to increase to 221 million by 2050. Osteoporosis is a leading cause of pain, bone deformation, fractures and even death in older adults. Calcitonin (a polypeptide composed of 32 amino acids) is one of the first-choice drugs for the treatment of osteoporosis. The advantage of calcitonin is that it inhibits the activity of osteoclasts, reduces the number of ost...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/23A61K9/16A61K47/36A61K47/34A61P19/10
Inventor 袁伟恩金拓吴飞郑瑞媛洪晓芸
Owner SHANGHAI JIAOTONG UNIV
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