Compositions containing itraconazole and their preparation methods

Abstract

The present invention relates to compositions containing itraconazole with a greatly increased bioavailability and their preparation methods. More specifically, the present invention relates to compositions containing itraconazole which is a sparingly-soluble drug, fatty acid or fatty alcohol and surfactant and their preparation methods. Compositions according to the present invention act as Self-MicroEmulsifying Drug Delivery System(SMEDDS) wherein itraconazole which is a sparingly-soluble drug is dissolved and dispersed to form a mocoidal phase, and the mocoidal phase is dissolved in water to form microemulsion. And because of increased dissolution property and increased bioavailability, compositions according to the present invention show equal efficacy using less amount than commercial pharmaceutical preparations such as sporanox capsule and are cheaper rather than the commercial pharmaceutical preparations such as sporanox capsule.

Description

technical field [0001] The present invention relates to compositions comprising itraconazole having significantly improved bioavailability, more particularly, pharmaceutical compositions comprising almost water-insoluble itraconazole, fatty acids or aliphatic alcohols, and surfactants. Furthermore, the invention relates to a process for the preparation of the composition. Background technique [0002] Itraconazole is a C 35 h 30 C 12 N 8 o 4 The molecular formula and the molecular weight of 705.64 are pyrrole antifungal agents. Itraconazole, which exists as a pale yellow powder, is almost insoluble in water and slightly soluble in ethanol, showing solubility of ≤1 μg / ml and 300 μg / ml, respectively, while it is easily soluble in dichloromethane, showing a solubility of 239 mg / ml. In addition, itraconazole, as a weak base (pKa=3.7), is almost completely ionized at low pH values ​​such as in gastric juice, and has high fat solubility. Itraconazole is known to exhibit bro...

AI Technical Summary

Problems solved by technology

This method does not use organic solvents, but has disadvantages because the vacuum melting step is performed at about 160-180°C, at which temperature water-soluble sugars can be denatured, resulting in a high priced product, and additionally does not achieve the dosing that can be achieved by improving the drug dissolution rate reduction of

Furthermore, there is no detailed information on the bioavailability in humans, thus making its practical use difficult

[0015] As mentioned above, in order to achieve the improved dissolution rate and dissolution rate of almost water-insoluble itraconazole, solid dispersions containing itraconazole can be prepared using various techniques including vacuum melt extrusion, spray drying and solution evaporation, But all these techniques have the obvious disadvantages of being inefficient, complex, uneconomical and harmful due to the use of organic solvents

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