Proanthocyanidin sustained release nano-micro spheres, as well as preparation method and application thereof

A technology of proanthocyanidins and nano-microspheres, which is applied in the direction of pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve the problems that proanthocyanidins are easily damaged by the outside world, and improve bioavailability Stabilization, the effect of reducing the dose

Active Publication Date: 2015-02-25
WEIFANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is to provide a slow-release nano-microsphere of proanthocyanidins to overcome the defect that proanthocyanidins are easily damaged by the outside world in the prior art. Insufficient technology, good powder properties and slow release

Method used

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  • Proanthocyanidin sustained release nano-micro spheres, as well as preparation method and application thereof
  • Proanthocyanidin sustained release nano-micro spheres, as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Embodiment 1, a proanthocyanidin slow-release nano-microsphere, mainly composed of proanthocyanidin and a carrier material with a slow-release effect, including proanthocyanidin and chitosan, phospholipid or its derivatives with a molar ratio of 1:1:1:1, Excipient; chitosan molecular weight is 1125kDa, deacetylation degree is 65%; phospholipid or its derivative is dipalmitoylphosphatidylcholine; excipient is mannitol.

[0049] The preparation method of proanthocyanidin sustained-release nano microspheres comprises the following steps:

[0050] (1) Take each component according to the above ratio, add it into the acidic solution to prepare a mixed solution, and the mass percentage concentration of the mixed solution is 0.1%;

[0051] The solute part in the acidic solution is citric acid; the solvent part includes methanol, ethanol, acetonitrile and purified water with a volume ratio of 1:1:1:1; the pH of the acidic solution is 6.5;

[0052] (2) Filtrating the mixed solu...

Embodiment 2

[0056] Embodiment 2, a proanthocyanidin slow-release nano-microsphere, mainly composed of proanthocyanidin and a carrier material with a slow-release effect, including proanthocyanidin and chitosan, phospholipid or its derivatives with a molar ratio of 5:12:12:10, Excipients; chitosan molecular weight is 1350kDa, deacetylation degree is 95%; phospholipid or its derivatives include dipalmitoylphosphatidylcholine and dipalmitoylphosphatidylglycerol (sodium salt) with a molar ratio of 3:1; The excipient is trehalose.

[0057] The preparation method of proanthocyanidin sustained-release nano microspheres comprises the following steps:

[0058] (1) Take each component according to the above ratio, add it into the acidic solution to prepare a mixed solution, and the mass percentage concentration of the mixed solution is 2.5%;

[0059] The solute part in the acidic solution is hydrochloric acid; the solvent part includes ethanol, acetonitrile and purified water with a volume ratio o...

Embodiment 3

[0064] Embodiment 3, a proanthocyanidin slow-release nano-microsphere, mainly composed of proanthocyanidin and a carrier material with a slow-release effect, including proanthocyanidin, chitosan quaternary ammonium salt, phospholipid or its molar ratio of 1:12:1:10 Derivatives, excipients; chitosan quaternary ammonium salt has a molecular weight of 1210kDa, a degree of deacetylation of 95%, and a degree of substitution of 65%; phospholipids or their derivatives include dipalmitoylphosphatidylcholine with a molar ratio of 2:1:2 base (DPPC), dipalmitoylphosphatidylglycerol (sodium salt) (DPPG), and di(eicosyl)lecithin (DAPC); excipient is lactose.

[0065] The preparation method of proanthocyanidin sustained-release nano microspheres comprises the following steps:

[0066] (1) Take each component according to the above ratio, add it into the acidic solution to prepare a mixed solution, and the mass percentage concentration of the mixed solution is 0.15%;

[0067] The solute par...

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Abstract

The invention relates to proanthocyanidin sustained release nano-micro spheres. The proanthocyanidin sustained release nano-micro spheres comprise 1-5 parts of proanthocyanidin, 1-12 parts of chitosan or derivatives thereof, 1-12 parts of phospholipid or derivatives thereof and 1-10 parts of excipients, wherein the chitosan and the derivatives thereof are one or more of high, medium and low-molecular weight chitosan, chitosan oligosaccharide, chitosan quaternary ammonium salt and carboxymethyl chitosan. The particle size of the proanthocyanidin sustained release nano-micro spheres is 10nm-0.3 mu m; the proanthocyanidin is prepared into the powder sustained release nano-micro spheres, and the proanthocyanidin sustained release nano-micro spheres can directly play a role in the lung as a pulmonary inhalation medicine-carrying formulation, improve the bioavailability of the proanthocyanidin and reduce the dosage by sustained release; the proanthocyanidin nano-micro spheres can also be applied as an oral sustained release formulation; the proanthocyanidin nano-micro spheres have appropriate particle size and morphology and other powder properties, as well as sustained release; furthermore, the preparation method has the advantages of simplicity and convenience in operation, stable process and easiness in industrial production.

Description

technical field [0001] The invention relates to a sustained-release nano-microsphere, in particular to a proanthocyanidin sustained-release nano-microsphere and its preparation method and application, and belongs to the technical field of biomedicine-carrying dosage forms. Background technique [0002] Oligomeric Proantho Cyanidins (OPC), a bioflavonoid with a special molecular structure, is internationally recognized as the most effective natural antioxidant for removing free radicals in the human body. The anti-free radical oxidation ability of OPC is 50 times that of vitamin E and 20 times that of vitamin C, and it can be absorbed quickly and completely. It can reach the highest blood level in 20 minutes after oral administration, and its metabolic half-life can reach 7 hours. Proanthocyanidins have the functions of protecting cardiovascular, preventing and treating cancer, protecting skin, anti-allergy, anti-inflammation, treating eye diseases, and protecting teeth. How...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/72A61K9/14A61K31/353A61K47/36A61P39/06A61P35/00A61P17/00A61P37/08A61P29/00A61P27/02A61P1/02
Inventor 张维芬郑增娟冯占芹商洪才
Owner WEIFANG MEDICAL UNIV
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