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Dimethylcurcumin solid dispersoid as well as preparation method and application thereof

A technology of dimethyl curcumin and solid dispersion, which is applied in the field of dimethyl curcumin solid dispersion and its preparation, and can solve the problems of poor water solubility of dimethyl curcumin, limitation of preparation development and utilization, and slow oral release speed, etc. , to achieve the effect of low price, high bioavailability and high dissolution rate

Inactive Publication Date: 2018-11-16
CHANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, there is no report about dimethyl curcumin solid dispersion in China
Dimethyl curcumin has poor water solubility, resulting in slow oral release, rapid metabolism in the body, and low bioavailability, which limits the development and utilization of its preparations

Method used

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  • Dimethylcurcumin solid dispersoid as well as preparation method and application thereof
  • Dimethylcurcumin solid dispersoid as well as preparation method and application thereof
  • Dimethylcurcumin solid dispersoid as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] A solid dispersion of dimethyl curcumin, consisting of dimethyl curcumin and PEG4000, using a melting method, heating 2 g of PEG4000 in a water bath at 60 to 80 ° C to melt, and under constant stirring, 1 g of dimethyl curcumin Add the ingredients in batches, continue to stir for 30 minutes, pour the molten material onto a glass container and spread it into a thin layer, cool it quickly, dry it in a desiccator for 24 hours, crush it, and pass it through a 100-mesh sieve to obtain dimethyl curcumin / PEG4000 solid Dispersion, in vitro dissolution test results show that: 5min dissolution rate is 51.07%, 2h dissolution rate is 71.15%, it can be seen that the solid dispersion prepared with PEG4000 as carrier can effectively improve the dissolution behavior of dimethyl curcumin.

Embodiment 2

[0043] A solid dispersion of dimethyl curcumin, consisting of dimethyl curcumin and PEG4000, using a melting method, heating 10 g of PEG4000 in a water bath at 60 to 80 ° C to melt, and under constant stirring, 1 g of dimethyl curcumin Add the ingredients in batches, continue to stir for 30 minutes, pour the molten material onto a glass container and spread it into a thin layer, cool it quickly, dry it in a desiccator for 24 hours, crush it, and pass it through a 100-mesh sieve to obtain dimethyl curcumin / PEG4000 solid Dispersion, in vitro dissolution test results show that: 5min dissolution rate is 50.08%, 2h dissolution rate is 73.51%, it can be seen that the solid dispersion prepared with PEG4000 as carrier can effectively improve the dissolution behavior of dimethyl curcumin.

Embodiment 3

[0045]A solid dispersion of dimethyl curcumin, which is composed of dimethyl curcumin and PEG4000, using a melting method, heating 4 g of PEG4000 in a water bath at 60 to 80 ° C to melt, and under constant stirring, 1 g of dimethyl curcumin Add the ingredients in batches, continue to stir for 30 minutes, pour the molten material onto a glass container and spread it into a thin layer, cool it quickly, dry it in a desiccator for 24 hours, crush it, and pass it through a 100-mesh sieve to obtain dimethyl curcumin / PEG4000 solid Dispersion, in vitro dissolution test results show that: 5min dissolution rate is 51.07%, 2h dissolution rate is 71.15%, it can be seen that the solid dispersion prepared with PEG4000 as carrier can effectively improve the dissolution behavior of dimethyl curcumin.

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Abstract

The invention discloses a dimethylcurcumin solid dispersoid as well as a preparation method and application thereof, and relates to the field of pharmaceutic preparations. The dimethylcurcumin solid dispersoid is formed by dimethylcurcumin and a water-soluble carrier material, wherein the water-soluble carrier material comprises PEG4000, PEG6000, polyvinylpyrrolidone (PVP K30), and poloxamer 188.The dimethylcurcumin solid dispersoid is prepared by using a melting method or a solvent method. An indissoluble drug of the dimethylcurcumin is prepared as the solid dispersoid. A dissolution rate, dispersity, solubility and bioavailability of the drug are improved. The solid dispersoid can be further prepared as solid preparations of a tablet, a capsule and the like. The dimethylcurcumin solid dispersoid is simple in preparation process, cheap in price, and easy to industrialization.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a dimethyl curcumin solid dispersion and a preparation method and application thereof. Background technique [0002] Dimethoxycurcumin (ASC-J9) chemical name: 5-hydroxy-1,7-bis(3,4-dimethoxyphenyl)-1,4,6-heptattrien-3-one molecular formula: C 23 h 24 o 6 , molecular weight: 396, the structure is shown in the following formula [0003] [0004] It is a compound obtained by modifying the structure of curcumin, and it shows higher pharmacological activity than curcumin in androgen receptor-related diseases. [0005] Dimethyl curcumin is a new type of androgen receptor (Androgen Receptor, AR) drug invented by the laboratory of professor chawnshang Chang, University of Rochester, USA, which can degrade the androgen receptor and its androgen receptor coactivator (ARA55 or ARA70) ), inhibit the function of androgen receptor, and is used for the treatment of androgen rec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/10A61K47/32A61K31/12A61P35/00A61P17/14A61P21/00
CPCA61K9/146A61K31/12A61P17/14A61P21/00A61P35/00
Inventor 徐德锋刘亚林
Owner CHANGZHOU UNIV
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