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Pulmonary inhalation curcumin-phospholipid complex chitosan microspheres and preparation method thereof

A technology of curcumin phospholipids and chitosan microspheres, which is applied in the direction of medical preparations of non-active ingredients, drug delivery, and pharmaceutical formulations. It can solve the problems of difficult operation for patients, low drug concentration in the lungs, and low transport efficiency. Achieve the effects of good carrier biocompatibility, high drug concentration in the lungs, and simple and convenient application

Inactive Publication Date: 2016-01-20
SOUTHWEST UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Quantitative inhalation of aerosols has the following disadvantages: (1) the commonly used propellants chlorofluoroalkanes can destroy the atmospheric ozone layer and accumulate in the body with certain cardiotoxicity; Difficult to operate, low transfer efficiency
However, curcuminoids have extremely poor water solubility, extremely low oral bioavailability, and lower drug concentration in the lungs, which limit their clinical application.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: a kind of curcuminoid phospholipid complex chitosan microsphere sucked by lung, is made up of the component of following weight part:

[0029] Curcumin: 0.5g

[0030] Phospholipids: 1g

[0031] Chitosan (deacetylation degree is 92.7%, viscosity is 298mpa s): 2g

[0032] Sodium tripolyphosphate: 4g

[0033] The preparation method of the above-mentioned curcumin-like phospholipid complex chitosan microspheres is: dissolve curcumin and phospholipids in 50ml absolute ethanol, inject into 2000ml purified water after stirring (2000rpm) in a water bath at 40°C for 12h; chitosan is dissolved in 0.5 % of glacial acetic acid, mixed with a concentration of 1% solution, poured into the above-mentioned curcumin phospholipid complex aqueous dispersion, mixed uniformly, dripped 0.2% sodium tripolyphosphate solution 2000ml under stirring conditions (1500rpm); Liquid spray drying, collecting microspheres, spray drying conditions are: inlet temperature: 120°C, injection ...

Embodiment 2

[0035] Embodiment 2: a kind of curcuminoid phospholipid complex chitosan microsphere sucked by lung, is divided into and forms by the composition of following parts by weight:

[0036] Curcumin: 0.5g

[0037] Phospholipids: 1g

[0038] Chitosan (deacetylation degree is 91.3%, viscosity is 196mpa·s): 3g

[0039] Sodium tripolyphosphate: 3g

[0040] The preparation method of above-mentioned curcuminoid phospholipid complex chitosan microsphere is: with curcumin and phospholipid, be dissolved in 50ml dehydrated alcohol, inject into 3000ml purified water after stirring (1500rpm) 5h in 50 ℃ of water baths; Chitosan is dissolved in 1% glacial acetic acid, mixed with a concentration of 2% solution, poured into the above-mentioned curcumin phospholipid complex aqueous dispersion, mixed uniformly, and added dropwise 1% sodium tripolyphosphate solution 300ml under stirring (2000rpm); The obtained liquid was spray-dried, and the microspheres were collected. The spray-drying conditions...

Embodiment 3

[0042] Embodiment 3: a kind of curcuminoid phospholipid complex chitosan microsphere sucked by lung, is divided into and forms by the composition of following parts by weight:

[0043] Curcumin: 0.5g

[0044] Phospholipids: 2g

[0045] Chitosan (deacetylation degree is 93.20%, viscosity is 112mpa·s): 8g

[0046] Sodium tripolyphosphate: 4g

[0047] The preparation method of above-mentioned curcuminoid phospholipid complex chitosan microsphere is: dissolve curcumin and phospholipid in 50ml dehydrated alcohol, pour into 5000ml purified water after stirring (1000rpm) 3h in 60 ℃ of water baths, chitosan is dissolved in 2 % glacial acetic acid, be mixed with a concentration of 3% solution, pour into the above-mentioned curcumin phospholipid complex aqueous dispersion, mix uniformly, drip 3% sodium tripolyphosphate solution 133ml under stirring condition (2500rpm); Liquid spray drying, collecting microspheres, spray drying conditions: inlet temperature: 160 ° C, injection speed: ...

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Abstract

The present invention discloses pulmonary inhalation curcumin-phospholipid complex chitosan microspheres and a preparation method thereof, wherein the pulmonary inhalation curcumin-phospholipid complex chitosan microspheres comprise, by weight, 1 part of a curcumin compound, 2-4 parts of phospholipid, and 4-10 parts of chitosan, and are prepared by using a spray-drying method. According to the present invention, the microspheres have good dispersion property, do not have significant aggregation and other phenomena, have the particle size of 1-10 [mu]m, and are suitable for the dry powder inhalation agent so as to achieve the pulmonary administration purpose, wherein the effective site deposition rate determined by a two-stage glass impactor is 20-60%.

Description

technical field [0001] The invention relates to a microsphere preparation for lung inhalation, in particular to a curcumin-phospholipid complex chitosan microsphere and a preparation method thereof. [0002] The invention belongs to the technical field of pharmaceutical preparations. Background technique [0003] The pulmonary route of drug delivery has been used for thousands of years. Pulmonary administration can directly deliver the drug to the site of action, reducing the distribution of the drug in other tissues; the lung has a large absorption area, rich blood flow, rapid drug absorption, and no liver first-pass effect, making pulmonary administration more effective Improve drug bioavailability and drug concentration in the lungs, reduce drug dosage, reduce or avoid adverse drug reactions, etc., and become an effective drug delivery route for the treatment of pneumonia, bronchial asthma, tuberculosis and other lung diseases. [0004] At present, the commonly used pul...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K47/48A61K31/12
Inventor 张继芬徐晓玉
Owner SOUTHWEST UNIVERSITY
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