Sustained/controlled release microsphere of biological extract Genipin cross-linked chitosan coated stilbene compound and preparation method thereof

Abstract

The invention discloses a sustained/controlled release microsphere of a chitosan coated stilbene compound using a biological extract Genipin as a cross-linking agent and a preparation method thereof. In the microsphere, a cross-linked condensation compound layer of the chitosan and the Genipin serves as a capsule shell and is used for coating a medicament 3,5-dihydroxyl-4-isopropyl stilbene, resveratrol, pterostilbene, oxidized resveratrol or piceatannol; the medicament stability of the product is improved; the sustained/controlled release of the medicament is realized; and the released Genipin after in vivo metabolism of the capsule shell has the characteristics of biocompatibility, no cytotoxicity and the like. The invention is applicable to the sustained/controlled release microspheresof Genipin cross-linked chitosan coated 3,5-dihydroxyl-4-isopropyl stilbene, resveratrol, pterostilbene, oxidized resveratrol, piceatannol and other stilbene compounds and a preparation method thereof. The preparation method is low in requirements on the control condition and easy to operate. In the microspheres, the quality is uniform; the grain size is 0.1 to 100 mu m; the surface of the microsphere has a multiporous structure; and the entrapment rate of the capsule shell to the medicament is 30 to 90 percent.

Description

Technical field [0001] The invention belongs to the field of chemical medicine preparation, and specifically relates to a biological extract genipin crosslinked chitosan coated stilbene compound sustained and controlled release microspheres and a preparation method thereof. Background technique [0002] Stilbene compounds 3,5-dihydroxy-4-isopropyl stilbene, resveratrol (3,4',5-trihydroxystilbene), pterostilbene (3,5-dimethoxy -4'-hydroxystilbene), resveratrol oxide (2,4,3',5'-tetrahydroxystilbene), paclitaxel (3,4,3',5'-tetra Hydroxystilbene), etc., belong to the active non-flavonoid polyphenols, which are widely found in natural foods or plants. A large number of studies have shown that they have anti-inflammatory, anti-oxidant, anti-bacterial, anti-free radicals, inhibition of platelet aggregation, and anti-thrombosis. , Anti-hyperlipidemia, can be used for the prevention and treatment of fungi, eczema, arteriosclerosis, coronary heart disease, viral hepatitis, AIDS, cancer an...

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Problems solved by technology

In this patent, the strength of the microspheres prepared by using glutaraldehyde as a crosslinking agent is moderate, but because glutaraldehyde is toxic to human cells, although the microspheres were thoroughly cleaned during the preparation process to remove the residual glutaraldehyde on the surface of the microspheres , but after the microsphere enters the human body and is metabolized by enzymes, it will still release glutaraldehyde, which is harmful to the human body, so its application is subject to certain restrictions

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