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CD-MOF preparation of allyl isothiocyanate, method and application

A technology of -CD-MOF and -CD-MOF-AITC, which is applied in the field of dry powder inhalation, can solve problems such as toxicity and application restrictions, and achieve the effects of reducing systemic effects, improving bioavailability, and increasing drug solubility

Pending Publication Date: 2021-08-20
ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] As a promising drug delivery system, metal-organic framework (MOF) has been attracting much attention in the field of biomedicine. However, most MOFs are currently assembled from heavy metals and non-degradable ligands, which have certain toxicity, making them widely used in the field of biomedicine. Applications in biomedicine are limited

Method used

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  • CD-MOF preparation of allyl isothiocyanate, method and application
  • CD-MOF preparation of allyl isothiocyanate, method and application
  • CD-MOF preparation of allyl isothiocyanate, method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] β-CD-MOF and γ-CD-MOF were synthesized using β-CD and γ-CD as organic ligands, and AITC was loaded with β-CD-MOF and γ-CD-MOF as carriers.

[0049] 1. Preparation of CD-MOF-AITC

[0050] ① Preparation of β-CD-MOF

[0051] Weigh β-CD (4.54g, 4mmol) and KOH (1.80g, 32mmol) respectively in a 250mL beaker, add 46mL of ultrapure water, and filter the dissolved solution through a 0.45μm organic filter membrane, and add an equal volume of methanol, placed in a 50°C water bath and heated for 20min. Transfer the supernatant to a clean beaker, and immediately add PEG 20000 (12 mg·mL -1 ), react for 10 min after PEG 20000 is completely dissolved, place the beaker in a water bath at 15°C and incubate overnight. The above reactions are all carried out in airtight glass containers. After the reaction is completed, centrifuge at 4000rpm for 5min, collect the precipitate after centrifugation, and wash with absolute ethanol and CH 2 Cl 2 After washing twice, vacuum drying at 40°C f...

Embodiment 2

[0061] The drug-loading conditions of the obtained two kinds of β-CD-MOF-AITC and γ-CD-MOF-AITC crystals were investigated (using a single factor investigation); the AITC in each CD-MOF-AITC sample was preliminarily determined by UV spectrophotometry. The influence of drug loading method, drug loading time, drug loading temperature, drug molar ratio and other factors on drug loading was investigated.

[0062] ①Inspection of drug loading method: UV spectrophotometry was used to preliminarily measure the drug loading of each sample obtained by co-crystallization method and magnetic stirring heating method. CD-MOF-AITC not only has a low drug loading (<5%), but also greatly reduces the yield of crystals obtained. Compared with the co-crystallization method, the magnetic stirring heating method is more controllable, which can avoid the degradation of AITC in contact with alkaline aqueous solution. The drug and the carrier are fully contacted and mixed, so that the drug enters the ...

Embodiment 3

[0075]The characterization of β-CD-MOF, β-CD-MOF-AITC, γ-CD-MOF and γ-CD-MOF-AITC were carried out respectively.

[0076] ①Scanning Electron Microscope (SEM)

[0077] The morphology of CD-MOF was characterized by scanning electron microscopy, and the two CD-MOF powders before and after drug loading were observed under scanning electron microscope.

[0078] The result is as Figure 6 As shown, the morphologies of β-CD-MOF and γ-CD-MOF are quite different. Both γ-CD-MOF and γ-CD-MOF-AITC were regular cubic crystals, which indicated that the loading of AITC by magnetic stirring and heating did not change the morphology of γ-CD-MOF; on the contrary, the loading of β-CD-MOF After drug treatment, the microscopic morphology changed greatly, which may be due to the layered structure of β-CD-MOF, which caused its side surface to be not connected with K + Covalent bonds are formed, and the drug-loaded drug is stirred by magnetic force for a long time to change its structure.

[0079...

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Abstract

The invention discloses a CD-MOF preparation of allyl isothiocyanate, a method and application thereof. The preparation takes gamma-CD-MOF as a carrier to load allyl isothiocyanate, and the preparation method of the preparation comprises the following steps: selecting beta-CD and gamma-CD as organic ligands to synthesize beta-CD-MOF and gamma-CD-MOF crystals; adjusting the beta-CD-MOF crystal and the gamma-CD-MOF crystal to be neutral; taking the neutral beta-CD-MOF and gamma-CD-MOF as carriers to load allyl isothiocyanate to obtain beta-CD-MOF-AITC and gamma-CD-MOF-AITC. According to the preparation quality evaluation method, evaluation is carried out one by one from the micromeritics property, in-vitro release, cytotoxicity and lung local tolerance, and the preparation can be applied to preparation of drugs or kits for treating COPD and can also be used for production of medicinal preparations, medical instruments or disinfection articles for treating COPD.

Description

technical field [0001] The field of the invention belongs to the field of dry powder inhalers, and in particular relates to a CD-MOF preparation, method and application of allyl isothiocyanate. Background technique [0002] Chronic obstructive pulmonary disease (COPD) is a common and frequently-occurring disease in the respiratory system, characterized by persistent respiratory symptoms and airflow limitation, with high morbidity and mortality. At present, there are a variety of drugs that can be used to relieve or alleviate the symptoms of COPD clinically. Most of the drugs are administered by pulmonary inhalation, and bronchodilators are still the cornerstone of COPD treatment. Pulmonary drug delivery is the most effective drug delivery method for the treatment of lung diseases. However, the lung phagocytes and mucociliary clearance of foreign bodies exposed in the airway have become the biggest obstacle to pulmonary drug delivery. Therefore, to achieve effective aerosoli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K9/72A61K47/22A61K47/10A61K31/26A61P35/00A61P11/00C12Q1/02G01N30/02
CPCA61K47/6951A61K9/0073A61K47/22A61K47/10A61K31/26A61P35/00A61P11/00G01N33/5014G01N33/5044G01N30/02C12N2503/02G01N2500/10
Inventor 汪电雷张敏李泽庚
Owner ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE