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Composition comprising itraconazole for oral administration

A technology of itraconazole and a composition is applied in the field of an oral composition, which can solve the problems of itraconazole being difficult to disperse, the dissolution rate of itraconazole being low, and the like

Inactive Publication Date: 2006-11-01
SAM CHUN DANG PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are several problems: the melting method should be carried out at a temperature as high as 245-265 ° C, and it is difficult to disperse the melted itraconazole in the polymer uniformly
However, there is a problem that the disintegration of the solid dispersion does not take a long time, and the dissolution rate of itraconazole is low because an excessive amount of polyvinylpyrrolidone is used, even in simulated gastric juice. The same is true when solid preparations are subjected to dissolution tests

Method used

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  • Composition comprising itraconazole for oral administration
  • Composition comprising itraconazole for oral administration
  • Composition comprising itraconazole for oral administration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] One hundred grams of the raw material itraconazole preparation (Sigma Chemical) was dissolved in 1,000 g of dichloromethane. Then, 22.2 g of citric acid as an absorption enhancer and 100 g of hydroxypropyl methylcellulose (Dow Chemical, weight average molecular weight of 10,000 to 1,500,000) were fully dissolved in 2,000 g of dichloromethane / ethanol (1:1, v / v) In mixed solvents. A spray dryer (B-191 mini spray dryer, Buchi Co., Switzerland) was used to spray the itraconazole solution and the mixture solution of hydroxypropyl methylcellulose and citric acid to form itraconazole dispersed in A solid dispersion in hydroxypropyl methylcellulose and citric acid to produce a white amorphous powder. The weight ratio of itraconazole: hydroxypropyl methylcellulose: citric acid is 45:45:10.

Embodiment 2

[0054] The itraconazole solid dispersion prepared in Example 1 and colloidal silica were sieved through a 30-mesh sieve and thoroughly mixed. Then, other components except magnesium stearate and talc in Table 1 below were added thereto, mixed, dried and granulated, and passed through a 25-mesh sieve to obtain uniform-sized granules. Subsequently, magnesium stearate and talc were added and mixed thoroughly to form the mixture into tablets. 120 g of Opadry AMB (Colorcon) was added to 546 g of pure water and mixed thoroughly to prepare a coating liquid. Using a tablet coating machine (SFC-30FN automatic coating machine, Sejong Pharmatech, South Korea), keeping the inlet temperature at 60~70℃ and the outlet temperature at 40~43℃, apply the coating solution to the prepared tablets In addition, each tablet is coated with 20mg of coating liquid.

[0055] Itraconazole solid dispersion

Embodiment 3

[0057] The itraconazole solid dispersion prepared in Example 1 and the components in Table 2 below were used to prepare tablets. The tablets were prepared and coated in the same way as in Example 2.

[0058] Itraconazole solid dispersion

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Abstract

The present invention relates to an oral composition whose active component is itraconazole, and the composition contains 40-69.9wt% solid dispersion, 0.1-30wt% penetration inducer and 0.1-30wt% disintegrant , wherein the solid dispersion is prepared in an amorphous form by dispersing 1 part by weight of itraconazole in a mixture of 0.1 to 10 parts by weight of hydroxypropylmethylcellulose and 0.01 to 5 parts by weight of an absorption enhancer .

Description

[0001] Cross-reference of related applications [0002] This application claims the priority of Korean Patent Application No. 10-2005-0022312 filed on March 17, 2005, which is hereby incorporated by reference into this specification so that it is as if it were fully filed in this specification. Invention field [0003] The present invention relates to an oral composition which contains 40-69.9wt% (wt%) solid dispersion, 0.1-30wt% penetration inducer and 0.1-30wt% disintegrant, wherein The solid dispersion is prepared in an amorphous form by dispersing 1 part by weight of itraconazole in a mixture of 0.1-10 parts by weight of hydroxypropyl methylcellulose and 0.01-5 parts by weight of an absorption enhancer. Background technique [0004] Itraconazole, also known as (±)-cis-4-(4-(4-(4-((2-(2,4-dichlorophenyl)-2-(1H-1,2,4 -Triazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)-1-piperazinyl)-2,4-dihydro-2-(1 -Methylpropyl)-3H-1,2,...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K9/14A61P31/10
CPCA61K9/0053A61K9/2054A61K31/496
Inventor 郑炯峻文炳官李祐荣朴俊锡
Owner SAM CHUN DANG PHARM
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