Beta-asarone modified chitosan nanoparticles as well as preparation method and application thereof

A technology of chitosan nanoparticles and asarone, which is applied in non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problem of low brain permeability, etc. The effect of high controllability, improvement of BBB function, and increase of brain penetration rate

Active Publication Date: 2020-07-10
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] For the problems referred to above, the purpose of the present invention is to provide a chitosan nano-carrier modified by a good β-asarone of physical stability and its preparation method and its application in the field of pharmaceutical preparations, to solve the problems caused by the blood-brain barrier. The problem of low brain penetration caused by obstruction

Method used

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  • Beta-asarone modified chitosan nanoparticles as well as preparation method and application thereof
  • Beta-asarone modified chitosan nanoparticles as well as preparation method and application thereof
  • Beta-asarone modified chitosan nanoparticles as well as preparation method and application thereof

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Effect test

Embodiment 1

[0055] Embodiment 1: Preparation of chitosan nanoparticles modified by β-asarone

[0056] a) Modification of β-asarone onto chitosan by chemical synthesis. Specifically, 1) 2,3-dichloro-5,6-dicyano-p-benzoquinone (43.6g, 192mmoL) was added to 1,4-dioxane (250mL) and dissolved under stirring; 2) room temperature Dissolve β-asarone (20g, 96.2mmoL) in 1,4-dioxane (50mL), and then drop into the reaction solution, keeping the temperature not higher than 30°C; 3) After adding, stir at room temperature After 30 min, LC-MS detects that the raw materials disappear; 4) filter the reaction solution, concentrate the filtrate, add methyl tert-butyl ether, wash with 10% aqueous sodium hydroxide solution, wash with water, wash with saturated saline, and dry to obtain the crude product; 5) use 10mL of methanol was beaten and dried to obtain 1.8g of product, intermediate D; 6) 300mg chitosan was added to water (30mL), and 227mg of glacial acetic acid was added under stirring, and stirred unti...

Embodiment 2

[0061] Embodiment 2: Preparation of chitosan nanoparticles modified by β-asarone

[0062] a) Modification of β-asarone onto chitosan by chemical synthesis. Specifically, 1) 2,3-dichloro-5,6-dicyano-p-benzoquinone (43.6g, 192mmoL) was added to 1,4-dioxane (250mL) and dissolved under stirring; 2) room temperature Dissolve β-asarone (20g, 96.2mmoL) in 1,4-dioxane (50mL), and then drop into the reaction solution, keeping the temperature not higher than 30°C; 3) After adding, stir at room temperature After 30 min, LC-MS detects that the raw materials disappear; 4) filter the reaction solution, concentrate the filtrate, add methyl tert-butyl ether, wash with 10% aqueous sodium hydroxide solution, wash with water, wash with saturated saline, and dry to obtain the crude product; 5) use 10mL of methanol was beaten and dried to obtain 1.8g of product, intermediate D; 6) 300mg chitosan was added to water (30mL), and 227mg of glacial acetic acid was added under stirring, and stirred unti...

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Abstract

The invention relates to beta-asarone modified chitosan nanoparticles as well as a preparation method and application thereof. The beta-asarone modified chitosan nanoparticles comprise chitosan nanoparticles and beta-asarone modified on the chitosan nanoparticles.

Description

technical field [0001] The invention relates to chitosan nanoparticles modified by beta-asarone and a preparation method and application thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Acorus calamus is the dried tuber of Acorus tatarinowii Schott., a plant of the family Araceae. It has the effects of aroma rejuvenation, refreshing and intellectual development, and is a representative medicine for aroma rejuvenation. β-asarone (β-Asarone, β-Asa) is one of the main active ingredients of Shichangpu. In addition to easily entering the brain tissue through the nasal mucosa and the blood-brain barrier (BBB), it can also affect other The drug acts as a penetration enhancer, and also has the effect of improving BBB function and protecting brain tissue. [0003] Nasal administration is a non-invasive, painless, sterile-free and easy-to-operate method of administration. And administration from the nasal cavity is an effective ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/54A61K31/09A61K45/00A61P25/00
CPCA61K47/6939A61K47/54A61K31/09A61K45/00A61P25/00Y02A50/30
Inventor 刘梅胡凯莉徐晓璐余双文吴晓俊陈晓冬
Owner SHANGHAI UNIV OF T C M
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