Gel drug sustained-release preparation and preparation method and application thereof

A slow-release preparation and gel technology, applied in the field of medicine, to achieve the effect of reducing systemic side effects, long-term anti-inflammation and anti-fibrosis

Active Publication Date: 2020-05-15
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, how to effectively use colchicine to treat myocardial infarction without causing obvious systemic side effects is still a huge clinical challenge.

Method used

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  • Gel drug sustained-release preparation and preparation method and application thereof
  • Gel drug sustained-release preparation and preparation method and application thereof
  • Gel drug sustained-release preparation and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Weigh 15g of dihydroxypolyethylene glycol (PEG1500) in a 250mL three-necked bottle, seal each port with vacuum ester, and remove water under vacuum at 130°C for 3h under mechanical stirring. Then cool down to 80°C with argon gas, add 37g of D,L-lactide and glycolide with a molar ratio of 1:1 in total, stir well; add toluene solution containing 50mg of stannous octoate, and repeatedly vacuumize 3 times After removing the toluene, the temperature was raised to 150°C and reacted for 12h under the protection of argon. Then lower the temperature to 120°C and vacuumize for 3 hours to remove unreacted monomers, pour it out while it is hot, wash the crude product with 80°C deionized water three times, and obtain the final product after freeze-drying to obtain the BAB type triblock polymer PLGA - PEG-PLGA (copolymer-1), about 85% yield. Measure the number average and weight average molecular weight (M) of the above-mentioned BAB type triblock polymer by gel permeation chromatog...

Embodiment 2

[0049] Weigh 10 g of dihydroxypolyethylene glycol (PEG1000) in a 250 mL three-necked bottle, seal each port with vacuum ester, and remove water under vacuum at 130°C for 3 hours under mechanical stirring. Then cool down to 80°C with argon, add 25g of D,L-lactide, stir well; add toluene solution containing 50mg of stannous octoate, repeat vacuuming 3 times to remove toluene, then heat up to 150°C under the protection of argon Reaction 12h. Then lower the temperature to 120°C and vacuumize for 3 hours to remove unreacted monomers, pour it out while it is hot, wash the crude product with 80°C deionized water three times, and obtain the final product after freeze-drying to obtain the BAB type triblock polymer PLA - PEG-PLA (copolymer-2), about 80% yield. Measure the number average and weight average molecular weight (M) of the above-mentioned BAB type triblock polymer by gel permeation chromatography (GPC, polystyrene is a standard sample) n ,M w ) are 4750 and 6120 respectivel...

Embodiment 3

[0051] Weigh 15 g of monomethoxypolyethylene glycol (mPEG750) in a 250 mL three-necked bottle, seal each port with vacuum ester, and remove water under vacuum at 130° C. for 3 h under mechanical stirring. Then cool down to 80°C with argon gas, add 30g of D,L-lactide and 10g of glycolide, stir well; add toluene solution containing 40mg of stannous octoate, repeat vacuuming 3 times to remove toluene, then heat up to 150°C The reaction was carried out under the protection of argon for 12h. Then lower the temperature to 120°C and vacuumize for 3 hours to remove unreacted monomers, pour it out while it is hot, wash the crude product with 80°C deionized water three times, and obtain the final product after freeze-drying to obtain the AB type block polymer mPEG- PLGA (copolymer-3), about 79% yield. Measure the number average and weight average molecular weight (M) of the above-mentioned AB type block polymer by gel permeation chromatography (GPC, polystyrene is a standard sample) n...

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Abstract

The present invention discloses a gel drug sustained-release preparation and a preparation method and an application thereof, and belongs to the field of medicines. The disclosed gel drug sustained-release preparation is mainly composed of a gel carrier material, an effective amount of a drug and a solvent, and the gel drug sustained-release preparation can realize sustained release of the colchicine drug, besides, the gel drug sustained-release preparation has a thermally induced gelation property, is in a solution state at room temperature, turns into a gel state at 4-37 DEG C, and can be conveniently administered by injection. In addition, after the gel drug sustained-release preparation is gelled in situ in body, the drug can be released in situ for local administration, systemic toxicand side effects are reduced, through the sustained release, long-term anti-inflammatory and anti-fibrotic effects can be achieved, and the gel drug sustained-release preparation is suitable for promotion and application in the market.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a gel medicine slow-release preparation and its preparation method and application, in particular to a long-acting slow-release preparation for treating myocardial infarction and its preparation method. [0002] technical background [0003] Myocardial infarction is the necrosis of myocardial ischemia and hypoxia due to interruption of coronary blood flow, which can cause heart failure, cardiogenic shock or cardiac arrest, and is one of the leading causes of death in the world. [0004] In addition to the myocardial injury caused by ischemia and hypoxia, excessive local inflammatory response in myocardial infarction is an important factor for the deterioration of cardiac structure and function. Inflammation can promote the apoptosis of cardiomyocytes and accelerate the synthesis of extracellular matrix, leading to myocardial fibrosis, myocardial remodeling and cardiac dysfunction. Exploring...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/165A61K47/34A61P9/10A61P29/00
CPCA61K9/0024A61K9/06A61K31/165A61K47/34A61P9/10A61P29/00
Inventor 俞麟沈成兴时家悦陈昱丁建东
Owner FUDAN UNIV
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