Compsns. contg. itraconazole with improved bioavailability and narrow intra-and inter-individual variation of its absorption

A technology of itraconazole and its composition, which is applied in the field of preparation of the composition, can solve problems such as the decrease of the solubility of macromolecules, and achieve the effects of improving bioavailability, improving wettability, and increasing specific surface area

Inactive Publication Date: 2003-02-19
DONG A PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] However, the above-mentioned macromolecules used in this technique suffer from the following problem: the solubility of the drug cannot be guaranteed to be large enough for the drug to be absorbed at the normal pH of gastric juice, i.e., 1-3.5, because even if it remains acidic, when Not only itraconazole itself but also the solubility of macromolecules decreased greatly as the pH shifted towards neutral

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] 100 g of hydroxypropylmethylcellulose and 7 g of poloxamer were dissolved in a mixture of ethanol and dichloromethane, and 100 g of itraconazole was added. Add 1 g of sodium chloride and 1 g of magnesium stearate to the obtained solution, and disperse to prepare a uniform spray-dried solution. The solution was spray-dried at a feed rate of 150ml / min at a pressure of 0.5kg / cm 2 The spray drying was carried out at an inlet air temperature of 190°C and an outlet air temperature of 110°C. Example 2-23: Preparation of spray-dried material 2-23

Embodiment 2-23

[0040] 100 g of hydroxypropylmethylcellulose and 7 g of poloxamer were dissolved in a mixture of ethanol and dichloromethane, and 100 g of itraconazole was added. Add 1 g of sodium chloride and 1 g of magnesium stearate to the obtained solution, and disperse to prepare a uniform spray-dried solution. The solution was spray-dried at a feed rate of 150ml / min at a pressure of 0.5kg / cm 2 The spray drying was carried out at an inlet air temperature of 190°C and an outlet air temperature of 110°C. Example 2-23: Preparation of spray-dried material 2-23

[0041] Prepare the spray-dried material according to a method similar to Example 1, wherein the amount of water-soluble macromolecules and solubilizers used per 100g itraconazole is shown in Table 1 below:

[0042] Table 1

[0043] Numbering

Drug ingredients (g)

Macromolecule (g)

Solubilizer (g)

2

Itraconazole (100)

Methylcellulose (100)

3

Itraconazol...

experiment Embodiment 2

[0052] Using appropriate excipients, the spray-dried material was made into tablets and then subjected to a dissolution test in pH 1.2 buffer. After 30 minutes, more than 90% of the itraconazole in the entire composition had been released. Experimental Example 3: Relative bioavailability of spray-dried materials containing itraconazole

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Abstract

The present invention relates to agent containing itraconazole with both improved bioavailability, due to higher water-solubility and impressively reduced difference of pH-dependent solubility, and narrow intra- and inter-individual variation of its absorption- and a manufacturing method thereof. Agent containing itraconazole of the present invention consists of itraconazole, water-soluble macromolecule of 10-100 % w/w to itracotazole, solubilizing agent of 0.1-100 % w/w to itraconazole and pharmaceutically allowed additives. Agent containing itraconazole of the present invention minimizes absorption variation by dozing time after food intake as well as is available for adults with hypoacidity, AIDS patients and normal people. In addition, the manufacturing method introduces the elementary process, the spray drying, thereby control of physical properties of particles containing drug is easier and economy/production is improved.

Description

field of invention [0001] The present invention relates to compositions containing itraconazole, which have high water solubility and little difference in solubility at different pH values, thereby providing excellent bioavailability and small intrabody absorption Variation and inter-individual (inter) variation, the present invention also relates to the preparation of compositions containing itraconazole. The composition containing itraconazole of the present invention comprises itraconazole, a water-soluble macromolecule based on itraconazole weight 10-1,000% w / w, based on itraconazole weight 0.1-100% w / w Solubilizers, and pharmaceutically acceptable additives. It is prepared by spray-drying itraconazole, water-soluble macromolecule and solubilizer. [0002] In the spray drying technique, the characteristic ordered crystal structure of itraconazole can become disordered, and the water-soluble macromolecules transform the disordered structure of the resulting particles into...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/10A61K9/12A61K9/14A61K9/16A61K9/20A61K9/30A61K9/48A61K31/4196A61K31/495A61K47/14A61K47/18A61K47/20A61K47/30A61K47/32A61K47/34A61K47/38A61P31/10
CPCA61K9/1652A61K9/1617A61K9/1635A61K31/495A61K9/1641A61K9/1611A61P31/10
Inventor 权琮远金桢薰王埙植张善瑀裴雄铎
Owner DONG A PHARMA
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