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Microparticle preparation method for improving dragon fruit gamma-tocopherol bioavailability

A technology for the utilization of tocopherol, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, applications, etc., can solve the problems of low water solubility, low encapsulation efficiency and drug loading rate of ordinary chitosan, Poor bioavailability and other issues

Active Publication Date: 2021-11-05
CHINA JILIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low water solubility of ordinary chitosan, the encapsulation efficiency and drug loading rate are relatively low, and the bioavailability is not good

Method used

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  • Microparticle preparation method for improving dragon fruit gamma-tocopherol bioavailability
  • Microparticle preparation method for improving dragon fruit gamma-tocopherol bioavailability
  • Microparticle preparation method for improving dragon fruit gamma-tocopherol bioavailability

Examples

Experimental program
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Effect test

preparation example Construction

[0066] Case 1, the preparation method of polyethylene glycol 750 monomethyl ether grafted chitosan (mPEG750-g-CS), carries out the following steps successively:

[0067] 1) Accurately weigh 10g of polyethylene glycol 750 monomethyl ether (mPEG750) and 0.5g of succinic anhydride in a 500mL round bottom flask, add 200mL of anhydrous dichloromethane to dissolve with magnetic stirring, and then add 4-dimethyl Aminopyridine 1mol, reacted for 5h under reflux conditions;

[0068] 2), the reaction product of step 1) was spin-dried at 60°C to constant weight, cooled to 4°C and added with 100mL of saturated sodium bicarbonate solution for dissolution; then 50mL of ethyl acetate was added for extraction, and the aqueous phase located in the lower layer was collected;

[0069] 3), adjust the pH of the water phase to 2, add 500ml of dichloromethane for extraction, add anhydrous sodium sulfate (about 50g) to the obtained dichloromethane extract phase (located in the lower layer), filter and...

Embodiment 1

[0075] Embodiment 1. A method for preparing microparticles that improve the bioavailability and chemical stability of γ-tocopherol, comprising the following steps:

[0076] 1) Add 1.6g of polyethylene glycol 750 monomethyl ether grafted chitosan (mPEG750-g-CS) to a 500mL round bottom flask, add water to 80.0mL, and magnetically stir at 25°C 30-40 minutes, rotating speed 800r / min, then adjust the pH to 4.5.

[0077] 2) Accurately weigh γ-tocopherol, dissolve it in absolute ethanol, and prepare 10 mL of γ-tocopherol solution with a mass concentration of 2.0 mg / mL.

[0078] 3), drop the γ-tocopherol solution obtained in step 2) into the polyethylene glycol 750 monomethyl ether grafted chitosan (mPEG750-g-CS) solution prepared in step 1), and stir while dropping, The dropwise addition was completed in about 5 minutes.

[0079] 4) Accurately weigh the sodium polyphosphate powder, dissolve it with ultrapure water, and prepare 10 mL of an aqueous sodium polyphosphate solution with ...

Embodiment 2

[0082] In Example 1, the amount of polyethylene glycol 750 monomethyl ether grafted chitosan (mPEG750-g-CS) was changed from 1.6 g to 1.0 g, and the rest were equal to Example 1.

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Abstract

The invention discloses a particle preparation method for improving the bioavailability of dragon fruit γ-tocopherol, which comprises the following steps: preparing polyethylene glycol 750 monomethyl ether grafted chitosan solution, preparing the γ-tocopherol solution, and dissolving the γ-tocopherol Add the ‑tocopherol solution into the polyethylene glycol 750 monomethyl ether grafted chitosan solution, then add the sodium polyphosphate aqueous solution, and stir evenly to obtain a particle suspension that improves the bioavailability of the dragon fruit γ‑tocopherol. The method can prepare gamma-tocopherol microparticles with significantly increased encapsulation efficiency and stability.

Description

technical field [0001] Tocopherol is the most important natural active ingredient in dragon fruit (red heart and white heart dragon fruit), which has various pharmacological activities and health care functions. The invention relates to a method for preparing particles capable of improving the bioavailability of gamma-tocopherol in dragon fruit. Background technique [0002] The color of the pitaya peel is bright red, and the flesh is sweet and refreshing. It is a tropical fruit that is loved by everyone in my country. Dragon fruit originates in the tropics and subtropics of Central America, and is mainly distributed in Vietnam and Taiwan, my country in Asia. With the development of fruit introduction and cultivation and facility agriculture in recent years, large-scale planting has also been carried out in Guangdong, Guangxi, Hainan, Yunnan, Guizhou and Zhejiang. Pitaya seeds are seed kernels embedded in the pitaya pulp, very similar in shape to black sesame. When people...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K47/36A61K47/10A61K31/355A61P39/06A61P39/00A61P37/04A23L3/3463
CPCA23L3/3463A61K9/5031A61K9/5036A61K31/355A61P37/04A61P39/00A61P39/06
Inventor 赵进葛建
Owner CHINA JILIANG UNIV
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