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Fluorofenidone solid dispersoid and preparation thereof

A technology of solid dispersion and flufenidone, which is applied in the field of medicine, can solve problems affecting the stable absorption of drugs, low dissolution rate, and affecting drug bioavailability, etc.

Active Publication Date: 2010-12-15
HAIKOU PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Because flufenidone is extremely fat-soluble and extremely poor in water solubility, when flufenidone is prepared into pharmaceutical preparations, the dissolution rate in the human body is relatively low, which affects the stable absorption of the drug and ultimately affects the bioavailability of the drug.

Method used

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  • Fluorofenidone solid dispersoid and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] The solid dispersion of flufenidone in this embodiment includes flufenidone, poloxamer, ethylene glycol and polymer matrix PEG4000, and the weight ratio of the four is 1:0.2:0.2:5.

[0080] Its preparation method is the melting method: first heat PEG4000 at 90°C to melt, then mix flufenidone, poloxamer and ethylene glycol, and add it to PEG4000, then rapidly cool down to 35°C within 20 minutes and cool to solidify , and finally freeze-dried into powder.

[0081] Solubility test: Take the excess of the flufenidone solid dispersion and put it in a stoppered Erlenmeyer flask, add 100ml of purified water, shake at a constant temperature of 25°C and 37°C for 48 hours, take the supernatant, filter and dilute, and then measure the concentration of flufenidone , each sample was done in triplicate. After testing, the solubility of flufenidone solid dispersion at 25°C is 51.2±1.66mg / ml, and the solubility at 37°C is 63.1±1.79mg / ml. The solubility of flufenidone raw material drug...

Embodiment 2

[0083] The preparation process is the same as in Example 1, except that the solid dispersion of flufenidone includes flufenidone, Tween-80 and PVP10000, and the weight ratio of the three is 1:0.1:4.

[0084] The solubility testing method is the same as that in Example 1. The solubility of the flufenidone solid dispersion is 53.5±1.58 mg / ml at 25°C and 78.5±1.62 mg / ml at 37°C.

Embodiment 3

[0086] The preparation process is the same as that in Example 1, except that the solid dispersion of flufenidone includes flufenidone, polyoxyethylene castor oil, glycerol and xanthan gum, each in a weight ratio of 1:0.5:0.5:10.

[0087] The solubility test method is the same as that in Example 1. The solubility of the flufenidone solid dispersion is 48.7±1.98 mg / ml at 25°C and 61.4±1.83 mg / ml at 37°C.

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Abstract

The invention provides a fluorofenidone solid dispersant, which comprises fluorofenidone, a solubilizer and a polymer matrix, wherein the weight ratio of the fluorofenidone to the solubilizer to the polymer matrix is 1: 0.1-0.5: 4-10. The invention also provides various preparations prepared by the fluorofenidone solid dispersant. The fluorofenidone solid dispersant can improve the solubility of the fluorofenidone in water, so that a product has high potency and good uniformity, and ensure the bioavailability of a final preparation. The preparations can be used for preparing medicines for treating fibrosis or rheumatoid diseases of liver, kidney and lung organs, have good curative effect on fibrotic diseases of various organs such as hepatocirrhosis, hepatofibrosis, renal fibrosis and so on, and have stronger effect than similar compounds.

Description

technical field [0001] The invention relates to a flufenidone solid dispersion and a preparation thereof, belonging to the field of medicine. Background technique [0002] Fluorofenidone (Fluorofenidone), 1-(3-fluorophenyl)-5-methyl-1H-pyridone, [0003] [0004] It belongs to pyridone compound. Pharmacological studies have shown that this drug has good curative effect on various organ fibrosis diseases such as liver cirrhosis, liver fibrosis and kidney fibrosis, and its effect is stronger than that of similar compounds. [0005] Because flufenidone is extremely fat-soluble and extremely poor in water solubility, when flufenidone is prepared into pharmaceutical preparations, the dissolution rate in the human body is relatively low, which affects the stable absorption of the drug and ultimately affects the bioavailability of the drug. As a result, it is necessary to improve the solubility of flufenidone to ensure the stable release of the drug after oral administration, s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4412A61K9/00A61P1/16A61P13/12
Inventor 吴传斌姚瑶王雪峰陶立坚胡高云王超志陈松
Owner HAIKOU PHARMA FACTORY
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