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: 2009-06-24
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 fluorofenidone in this embodiment includes fluorofenidone, poloxamer, ethylene glycol and a polymer matrix PEG4000, and the weight ratio of the four is 1:0.2:0.2:5.

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

[0081] Solubility test: Take an excess of the solid dispersion of fluorofenidone into a stoppered Erlenmeyer flask, add 100ml of purified water, and shake at 25°C and 37°C for 48 hours. Take the supernatant, filter and dilute, and detect the concentration of fluorofenidone. , Make three copies of each sample in parallel. After testing, the solubility of fluorofenidone 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 fluorofenidone bulk drug in water is ...

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 test method is the same as in Example 1. The solubility of the fluorofenidone solid dispersion at 25°C is 53.5±1.58 mg / ml, and the solubility at 37°C is 78.5±1.62 mg / ml.

Embodiment 3

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

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

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

Claims

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Application Information

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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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