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Vitamin A and derivative thereof-loaded cyclodextrin-metal organic framework complex and deep processing method of vitamin A and derivative thereof

A metal-organic framework and cyclodextrin technology, which can be used in drug combinations, active ingredients of hydroxyl compounds, inactive ingredients of polymer compounds, etc., can solve problems such as unfavorable packaging, storage and transportation, and achieve uniform, controllable and safe particle size. High performance and high stability

Active Publication Date: 2017-05-10
BY HEALTH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there are mainly vitamin A nanoemulsion (CN103520101 B), vitamin A liposome (CN1245153C and CN105496801 A) and vitamin A micelles (CN103565676 B) about the liquid preparation patent reports of improving vitamin A stability, and these liquid preparations contain emulsified additives and preservatives, and the resulting product is in a liquid state, which is not conducive to packaging, storage and transportation

Method used

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  • Vitamin A and derivative thereof-loaded cyclodextrin-metal organic framework complex and deep processing method of vitamin A and derivative thereof
  • Vitamin A and derivative thereof-loaded cyclodextrin-metal organic framework complex and deep processing method of vitamin A and derivative thereof
  • Vitamin A and derivative thereof-loaded cyclodextrin-metal organic framework complex and deep processing method of vitamin A and derivative thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Preparation of acidified CD-MOFs-VAP composites with different particle sizes

[0067] Dissolve 3.26g of γ-CD and 1.12g of KOH in 100mL of water, pre-add 60mL of methanol to the mixed solution of γ-CD and KOH, seal it, and heat it at 50°C for 2h. After reacting for a certain period of time, 1.28g of polyethylene glycol 20000 was added, and after standing at room temperature for a period of time, it was washed with ethanol and dichloromethane, and the obtained crystals were vacuum-dried to obtain basic micron-sized CD-MOFs (average particle size 1~ 10 μm), the pH is about 11-13, and the yield is about 80%.

[0068] Dissolve 3.26g of γ-CD and 1.12g of KOH in 100mL of water, pre-add 60mL of methanol to the mixed solution of γ-CD and KOH, seal it, and heat at 50°C for 2h. After reacting for a certain period of time, add an equal volume of methanol, and then add 1.28g of polyethylene glycol 20000. After standing at room temperature for a period of time, wash with ethanol an...

Embodiment 2

[0075] Specific surface area investigation of acidified CD-MOFs-VAP composites with different particle sizes

[0076] According to the method of Example 1, the mass ratio of CD-MOFs and vitamin A palmitate was adjusted to prepare respectively: acidified nanoscale CD-MOFs, unwashed acidified nanoscale CD-MOFs-VAP composite (VAP content is 14.11 wt%), acidified micron-sized CD-MOFs, unwashed acidified micron-sized CD-MOFs-VAP composite (VAP content of 9.77wt%) and unwashed acidified micron-sized CD-MOFs-VAP composite (VAP content of 5.42 wt%).

[0077] Carry out gas adsorption test on the above six samples respectively. The specific test process is: weigh 100-200mg of the sample to be tested, degas the sample at 50°C for 4-5h before gas adsorption, and measure the CD- MOF vs. N 2 Adsorption effect. The gas adsorption results are as figure 2 as shown, figure 2 It is the gas adsorption curve of acidified CD-MOFs before and after drug loading provided by Example 2 of the pre...

Embodiment 3

[0079] Preparation of acidified micron-sized CD-MOFs-VAP complexes at different dosage concentrations

[0080] Dissolve 3.26g of γ-CD and 1.12g of KOH in 100mL of water, pre-add 60mL of methanol to the mixed solution of γ-CD and KOH, seal it, and heat it at 50°C for 2h. After reacting for a certain period of time, 1.28g of polyethylene glycol 20000 was added, and after standing at room temperature for a period of time, it was washed with ethanol and dichloromethane, and the obtained crystals were vacuum-dried to obtain basic micron-sized CD-MOFs (average particle size 1~ 10 μm), the yield was about 80%.

[0081] Weigh a certain amount of basic micron-sized CD-MOFs prepared above, disperse them in absolute ethanol containing glacial acetic acid (the volume ratio of glacial acetic acid to absolute ethanol is 1:10), and place them in a shaker at 25 °C After shaking and incubating for 2 h, the solids were washed with ethanol and dried in vacuum to obtain acidified micron-sized CD...

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Abstract

The invention belongs to the field of composite materials, and particularly relates to a cyclodextrin-metal organic framework complex loading vitamin A and a derivative thereof, and a deep processing method of the vitamin A and the derivative thereof. The cyclodextrin-metal organic framework complex is prepared from a cyclodextrin-metal organic framework, and vitamin, wherein the vitamin is loaded on the framework, and is vitamin A and / or the derivative thereof. The cyclodextrin-metal organic framework complex has the advantages that the cyclodextrin-metal organic framework is used as solid medicine reservoirs, the safety is high, and the biocompatibility is good; the vitamin fills the cyclodextrin-metal organic framework, and the stability is higher; experiment results show that the degrading amount is less than or equal to 40% after heat treatment is performed on the complex for 10 days at the temperature of 60 DEG C, and is less than or equal to 20% after the complex is placed for 90 days at the temperature of 40 DEG C, and the heat stability is better than that of of Basf vitamin A powder.

Description

technical field [0001] The invention belongs to the field of composite materials, and in particular relates to a cyclodextrin-metal organic framework compound loaded with vitamin A and its derivatives and a deep processing method of vitamin A and its derivatives. Background technique [0002] Vitamin A (Vitamin A) is an important, easily deficient, fat-soluble vitamin necessary for the body to maintain normal metabolism and function. It was first discovered by American scientists Elmer McCollum and Margaret Davis between 1912 and 1914. Margaret Davis et al. extracted a yellow viscous liquid-vitamin A from the liver of sturgeon. Vitamin A in the narrow sense is retinol, vitamin A in the broad sense also includes retinol derivatives including retinal, retinoic acid, retinyl acetate and retinyl palmitate, etc., currently commercially available vitamin A Mainly vitamin A acetate and vitamin A palmitate. Vitamin A has many physiological functions, and plays an important role in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/40A61K31/07A61P3/02
CPCA61K9/146A61K31/07
Inventor 钱蔚孟凡月彭辉郭桢肖健伍丽张旭光张继稳
Owner BY HEALTH CO LTD
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