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A kind of dexamethasone nano-preparation for targeted treatment of rheumatoid arthritis and preparation method thereof

A technology of dexamethasone and nano-preparation, applied in the field of medicine, can solve problems such as poor patient compliance, inconvenient administration, adverse reactions, etc., achieve high bioavailability, improve drug safety, and improve anti-inflammatory effects

Active Publication Date: 2022-02-15
ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional oral administration methods can cause serious adverse reactions such as osteoporosis, increased chance of infection, and even myocardial infarction
The reason is that in order to maintain a certain drug concentration in the lesion, the drug concentration in the blood circulation is maintained at a high level, which causes serious adverse reactions, which leads to serious restrictions on the use of this type of drug, and is only used for short-term rapid relief of symptoms. "
However, the local intra-articular drug administration method cannot solve the problems faced by drug therapy in clinical application due to reasons such as inconvenient administration, poor patient compliance, and too long intervals between administrations (each interval is not less than 3-4 months).

Method used

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  • A kind of dexamethasone nano-preparation for targeted treatment of rheumatoid arthritis and preparation method thereof
  • A kind of dexamethasone nano-preparation for targeted treatment of rheumatoid arthritis and preparation method thereof
  • A kind of dexamethasone nano-preparation for targeted treatment of rheumatoid arthritis and preparation method thereof

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preparation example Construction

[0033] A preparation method of dexamethasone nano-preparation for targeted treatment of rheumatoid arthritis, the preparation steps of the dexamethasone nano-preparation for targeted treatment of rheumatoid arthritis are as follows:

[0034] (1) the cyclodextrin modified by dexamethasone and 4-hydroxymethylphenylboronic acid pinacol ester is dissolved in methanol mixed solution;

[0035] (2) ultrasonically disperse lecithin, distearoylphosphatidylethanolamine-polyethylene glycol 2000 and distearoylphosphatidylethanolamine-polyethylene glycol 3500-folic acid conjugates in an organic solvent, and then add water Continue ultrasonic dispersion, and heat at 65 degrees Celsius for 30 minutes, and cool to room temperature;

[0036] (3) Titrate the solution obtained in step (1) into the solution in step (2), stir quickly after titration for 3 minutes, then continue to stir slowly at room temperature for self-assembly for 1.5 hours to obtain a suspension of dexamethasone nano preparati...

Embodiment 1

[0049] Mix methanol and acetonitrile at a ratio of 1:1 by volume to prepare a methanol-acetonitrile mixed solution, and use 3.0 mg of dexamethasone drug and 30.0 mg of 4-hydroxymethylphenylboronic acid pinacol ester modified α-cyclodextrin with Dissolve in 3.0ml methanol-acetonitrile mixed solution;

[0050] Sonicate 6.0 mg lecithin and 6.0 mg distearoylphosphatidylethanolamine-polyethylene glycol 2000 and 6.0 mg distearoylphosphatidylethanolamine-polyethylene glycol 3500-folic acid conjugate with 1.0 ml absolute ethanol Disperse, then add 10.0ml of water to continue ultrasonic dispersion, and heat at 65°C for 30 minutes, then cool to room temperature to obtain lecithin and distearoylphosphatidylethanolamine-polyethylene glycol 2000 and distearoyl Aqueous solution of phosphatidylethanolamine-polyethylene glycol 3500-folic acid conjugate.

[0051] The methanol-acetonitrile mixed solution dissolved with dexamethasone and cyclodextrin modified with 4-hydroxymethylphenylboronic a...

Embodiment 2

[0054] Methanol and dimethyl sulfoxide were mixed according to the volume ratio of 1:1.5 to prepare a methanol-dimethyl sulfoxide mixed solution, and 3.5 mg of dexamethasone and 35.0 mg of 4-hydroxymethylphenylboronic acid pinacol ester modified γ - Dissolve the cyclodextrin with 4.0ml methanol-dimethyl subpeak mixed solution;

[0055] Sonicate 7.0 mg lecithin and 10.0 mg distearoylphosphatidylethanolamine-polyethylene glycol 2000 and 10.0 mg distearoylphosphatidylethanolamine-polyethylene glycol 3500-folate conjugate with 1.0 ml absolute ethanol Disperse, then add 15.0ml of water to continue ultrasonic dispersion, and heat at 65°C for 30 minutes, then cool to room temperature to obtain lecithin and distearoylphosphatidylethanolamine-polyethylene glycol 2000 and distearoyl Aqueous solution of phosphatidylethanolamine-polyethylene glycol 3500-folic acid conjugate.

[0056] The methanol-dimethylsulfoxide mixed solution dissolved with dexamethasone and cyclodextrin modified with...

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Abstract

The invention discloses a dexamethasone nano preparation for targeted treatment of rheumatoid arthritis. Dexamethasone is loaded on a cyclodextrin drug carrier modified based on 4-hydroxyphenylboronic acid pinacol ester, and the outer layer is covered with A nano-formulation of lecithin and distearoyl phosphatidyl ethanolamine-polyethylene glycol 2000 and distearoyl phosphatidyl ethanolamine-polyethylene glycol 3500-folate conjugate, the nano-formulation has a spherical structure with a particle size of 200 ‑300 nm. A preparation method of a dexamethasone nano preparation for targeted treatment of rheumatoid arthritis, the disclosed dexamethasone nano preparation of the present invention has active targeting, high dispersibility and long-term circulation, and can effectively improve dexamethasone The invention also discloses the preparation method of the dexamethasone nano preparation, which is simple and easy to popularize.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a dexamethasone nano-preparation for targeted treatment of rheumatoid arthritis and a preparation method thereof. Background technique [0002] In addition to surgical treatments such as joint replacement, the treatment of rheumatoid arthritis mainly uses anti-inflammatory and immune-reducing drug treatments, so as to alleviate the pain of patients and prevent further damage to joint morphology and function. Commonly used therapeutic drugs mainly include non-steroidal anti-inflammatory drugs, disease-modifying antirheumatic drugs (such as methotrexate, biological drugs, etc.) and glucocorticoid drugs (such as dexamethasone, prednisone, etc.). Although these drugs can control the inflammation of the lesion site and relieve the pain of patients to a certain extent, they are all limited due to serious side effects. As a non-steroidal hormone, dexamethasone (DMS) can have an important impact...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K9/127A61K47/24A61K31/573A61P19/02A61P29/00
CPCA61K47/24A61K47/6951A61P19/02A61P29/00A61K9/1273A61K31/573
Inventor 黄刚张定林倪荣容刘涵孙凤军胡俊付晓红
Owner ARMY MEDICAL UNIV