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Inclusion complex of cyclodextrin/fe3o4 magnetic nanocomposite with ibuprofen

A magnetic nanometer and cyclodextrin technology, applied in the direction of drug combination, organic active ingredients, non-central analgesics, etc., can solve the problem of frequent medication to maintain therapeutic concentration, strong gastrointestinal stimulation, dissolution rate and bioavailability Low-level problems, to achieve significant solubilization effect and high solubility

Inactive Publication Date: 2011-11-30
SHANGHAI WUZHIFENG INFORMATION TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to its insolubility in water, low dissolution rate and bioavailability, frequent medication is required to maintain the therapeutic concentration, and it has a great stimulating effect on the gastrointestinal tract, which limits its application to a certain extent.

Method used

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  • Inclusion complex of cyclodextrin/fe3o4 magnetic nanocomposite with ibuprofen
  • Inclusion complex of cyclodextrin/fe3o4 magnetic nanocomposite with ibuprofen
  • Inclusion complex of cyclodextrin/fe3o4 magnetic nanocomposite with ibuprofen

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: β-Cyclodextrin / Fe 3 o 4 Preparation of magnetic nanocomposites

[0027] (1) Fe 3 o 4 Preparation of Magnetic Nanoparticles (MNPs)

[0028] Weigh FeCl with a molar ratio of 1:1 2 .4H2 O and FeCl 3 .6H 2 O (total iron concentration 0.3mol / L) is placed in a 250mL round bottom flask, add an appropriate amount of double distilled water 194mL, fully stir and dissolve at a speed of 600r / min at a temperature of 30°C, and add concentrated ammonia water (25-28%) dropwise at the same time When the pH is 9 to complete the precipitation, heat up to 80°C and mature for 30 minutes. The reactant is naturally cooled to room temperature, washed repeatedly with double distilled water and ethanol, separated by a permanent magnet, and vacuum-dried at 70°C for 24 hours to obtain Fe 3 o 4 magnetic nanoparticles.

[0029] Characterized by X-ray diffraction technique, it can be seen from the figure that the peaks at 2θ at 30.2, 35.6, 43.2, 53.7, 57.2 and 62.9 correspond to t...

Embodiment 2

[0037] Example 2: Hydroxypropyl-β-cyclodextrin / Fe 3 o 4 Preparation of magnetic nanocomposites

[0038] The first two steps reaction method sees embodiment 1

[0039] (3) Preparation of citric acid modified hydroxypropyl-β-cyclodextrin

[0040] Weigh 2.5g of hydroxypropyl-β-cyclodextrin, dissolve it in 1.8mL of twice-distilled aqueous solution containing 0.84g of citric acid, react in an oven at 100°C for 3.5 hours, and wash the product with isopropanol. Suction filtration and purification, vacuum drying at 55°C for 10 hours to obtain citric acid-modified hydroxypropyl-β-cyclodextrin (CA-HP-β-CD), which was sealed and stored.

[0041] (4) Hydroxypropyl-β-cyclodextrin / Fe 3 o 4 Preparation of magnetic nanocomposites

[0042] Weigh 1.0 g of GAMNP and dissolve it in buffer solution (0.1 g / mL, phosphate buffer pH=6.0). After ultrasonication for 20 minutes, add 0.25 g of carbodiimide solution (0.025 g / mL), continue ultrasonication for 30 minutes, and finally Add 1.0 g (0.05 g...

Embodiment 3

[0044] Embodiment 3 sulfobutyl ether-β-cyclodextrin / Fe 3 o 4 Preparation of magnetic nanocomposites

[0045] The first two steps reaction method sees embodiment 1

[0046] (3) Preparation of citric acid modified sulfobutyl ether-β-cyclodextrin

[0047] Weigh 2.0 g of sulfobutyl ether-β-cyclodextrin, dissolve it in 1 mL of double-distilled aqueous solution containing 0.68 g of citric acid, react in an oven at 100 ° C for 3.5 hours, wash the product with isopropanol, and pump Purify by filtration, and dry under vacuum at 55°C for 10 hours to obtain citric acid-modified sulfobutyl ether-β-cyclodextrin (CA-SBE-β-CD), which is sealed and stored.

[0048] (4) sulfobutyl ether-β-cyclodextrin / Fe 3 o 4 Preparation of magnetic nanocomposites

[0049] Weigh 1.0 g of GAMNP and dissolve it in buffer solution (0.1 g / mL, phosphate buffer pH=6.0). After ultrasonication for 20 minutes, add 0.25 g of carbodiimide solution (0.025 g / mL), continue ultrasonication for 30 minutes, and finally ...

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Abstract

The invention provides a clathrate compound of cyclodextrin / Fe3O4 magnetic nano compound and ibuprofen, prepared by adopting the following steps of: adding a cyclodextrin / Fe3O4 magnetic nano compound into ibuprofen ethanol solution in the weight ratio of (0.2-20): 1, and carrying out ultrasonic processing for 2-4 hours; washing products with secondary distilled water, separating by adopting a permanent magnet, and carrying out vacuum drying to obtain the clathrate compound. The cyclodextrin / Fe3O4 magnetic nano compound realizes targeting delivery on a medicine by simultaneously utilizing clathration characteristic of cyclodextrin and magnetic performance of a Fe3O4 magnetic nano particle; the ibuprofen is clathrated by the Fe3O4 magnetic nano compound, adverse effect of the medicine is reduced, peculiar and odour smells of the medicine are covered, solubility, bioavailability and stability are all improved, the clathrate compound can be used for targeting medicine delivery under the action of an external magnetic field, and curative effect of the medicine can be played to the utmost extent.

Description

technical field [0001] The present invention relates to the clathrate of ibuprofen, specifically by ibuprofen and cyclodextrin / Fe 3 o 4 Inclusion compound composed of magnetic nanocomposite and its preparation method. Background technique [0002] Ibuprofen (IBU), also known as ibuprofen, is odorless and tasteless. Insoluble in water, easily soluble in ethanol, ether, chloroform and acetone, easily soluble in sodium hydroxide and sodium carbonate solution. [0003] Ibuprofen is a good non-steroidal antipyretic, analgesic and anti-inflammatory drug, which produces analgesic and anti-inflammatory effects by inhibiting cyclooxygenase and reducing the synthesis of prostaglandins; thermal effect. It is widely used clinically to treat rheumatic and rheumatoid arthritis, osteoarthritis, gouty arthritis; joint and muscle pain, headache, dysmenorrhea and other mild and moderate pains; it is effective in treating fever in adults and children Thermal effects; one of the most used ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/02A61K31/192A61P29/00
Inventor 周叶红曹丽燕王海霞董川双少敏
Owner SHANGHAI WUZHIFENG INFORMATION TECH
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