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Preparation technology and application of paeoniflorin wheat gliadin nanoparticles

The invention relates to a wheat prolamin and a preparation process technology, which can be applied to medical preparations containing active ingredients, antipyretics, drug combinations, etc., and can solve the problems of weak transmembrane absorption, low bioavailability, weak lipophilicity, and the like, Achieve the effect of improving bioavailability, simple production process, and easy access to materials

Inactive Publication Date: 2017-01-04
苏州承瑞健康科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Paeoniflorin is the main active ingredient of traditional Chinese medicine Radix Paeoniae Rubra and Radix Paeoniae Alba. It has biological activities such as anti-inflammatory, analgesic, and tranquilizing. Anti-inflammatory and immunomodulatory drugs for rheumatoid arthritis, which have a certain curative effect and few adverse reactions in the treatment of RA, but the onset of effect is slow
Due to the strong hydrophilicity of paeoniflorin, weak lipophilicity, and weak transmembrane absorption capacity, it is difficult to absorb paeoniflorin in the small intestine, and the bioavailability is low, only 3%-4%.
Oral absorption of paeoniflorin is poor, which not only wastes a lot of drug resources, but also increases the amount of drugs taken by patients. It is difficult for ordinary preparations to exert their good biological activity in the body through oral administration.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0011] The material for preparing nanoparticles preferably has a ratio of wheat prolamin: paeoniflorin of 85-95: 5-15; the aqueous phase dispersant is selected from 0.1%-1.0% Pluronic F 68 Or PVA-0486 aqueous solution; the paeoniflorin wheat prolamin nanoparticle scaffolding agent uses 1-5% trehalose.

[0012] The particle size range of the drug-loaded wheat prolamin nanoparticles prepared by adopting an optimized process is 150-250nm, the encapsulation efficiency of the paeoniflorin wheat prolamin nanoparticles is not less than 70%, and the drug-loading capacity is 4.0-6.0%.

Embodiment 1

[0014] Weigh gluten powder, add 5 times the volume percentage of petroleum ether to degrease twice, add 8 times the amount of 65% ethanol to the defatted gluten, ultrasonically extract for 2 hours, centrifuge, concentrate the supernatant until it has no alcohol smell, and carry out water dialysis for 24 hours to the concentrated solution. Without sour taste, the dialyzate was pre-frozen at -20°C for 24 hours, and then freeze-dried for 24 hours to obtain wheat prolamin; weigh the prescribed amount of wheat prolamin: paeoniflorin (90:10). Add 2 times the volume percentage of 65% ethanol, and ultrasonically dissolve it completely. Under the condition of mechanical stirring, inject the obtained ethanol mixture solution into 3 times the volume of 0.3% PVA-0486 aqueous solution, stir for 15 minutes, then add 2% trehalose, stir for 20 minutes, pre-freeze at 20°C for 24 hours, and freeze-dry for 24 hours , to get paeoniflorin wheat prolamin nanoparticles. The particle diameter range ...

experiment example 2

[0016] Weigh the gluten powder, add 6 times the volume percentage of petroleum ether to degrease twice, add 7 times the amount of 80% ethanol to the defatted gluten, ultrasonically extract for 3 hours, centrifuge, concentrate the supernatant until it has no alcohol smell, and carry out water dialysis for 24 hours to the concentrated solution. Without sour taste, the dialyzate was pre-frozen at -20°C for 24 hours, and then freeze-dried for 24 hours to obtain wheat prolamin; weigh the prescribed amount of wheat prolamin: paeoniflorin (85:15). Add 2 times the volume percentage of 85% ethanol, and ultrasonically dissolve it completely. Under the condition of mechanical stirring, inject the obtained ethanol mixture solution into 4 times the volume of 0.5% Pluronic F 68 In the aqueous solution, stir for 10 minutes, then add 4% trehalose, stir for 10 minutes, pre-freeze at 20° C. for 24 hours, and then freeze-dry for 24 hours to obtain paeoniflorin wheat prolamin nanoparticles. The ...

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Abstract

The invention discloses a preparation technology and application of paeoniflorin wheat gliadin nanoparticles. After gluten flour is subjected to degreasing, ethyl alcohol is added for extraction, an extracting solution is concentrated, and freeze drying is performed to obtain wheat gliadin; the wheat gliadin and paeoniflorin of the formula are weighed, ethyl alcohol is added for dissolution, the ethyl alcohol mixture solution is injected into a pluronic F68 or PVA-0486 solution, stirring is performed to obtain a colloid dispersion solution, and then freeze drying is performed to obtain paeoniflorin wheat gliadin nanoparticles. A nano-carrier is edible wheat gliadin and is free of toxicity, easy to obtain and low in production cost. The prepared paeoniflorin wheat gliadin nanoparticles can be independently used or be compatible with other medicines to prepare a preparation, absorption of paeoniflorin inside a human body is improved, the defect that the biological availability of paeoniflorin is poor is overcome, the medicine effect of paeoniflorin can be greatly improved, and the dosage is reduced.

Description

technical field [0001] The invention relates to a preparation method and application of paeoniflorin wheat prolamin nanoparticles. [0002] technical background [0003] Paeoniflorin is the main active ingredient of traditional Chinese medicine Radix Paeoniae Rubra and Radix Paeoniae Alba. It has biological activities such as anti-inflammatory, analgesic, and tranquilizing. Anti-inflammatory and immunomodulatory drugs for rheumatoid arthritis have positive curative effect and few adverse reactions in the treatment of RA, but the onset of effect is slow. Due to the strong hydrophilicity of paeoniflorin, weak lipophilicity and weak transmembrane absorption capacity, it is difficult to absorb paeoniflorin in the small intestine, and the bioavailability is low, only 3%-4%. Oral absorption of paeoniflorin is poor, which not only wastes a lot of drug resources, but also increases the dosage of drugs taken by patients. It is difficult for ordinary preparations to exert their good b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/7048A61K47/42A61P29/00A61P25/20A61K9/19
CPCA61K9/19A61K9/5169A61K31/7048
Inventor 田景奎宫明华李守信李卫国
Owner 苏州承瑞健康科技有限公司
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