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Voriconazole aerosol inhalant and application thereof

A voriconazole and inhalation technology, applied in the field of antifungal drugs, can solve problems such as instability of voriconazole

Active Publication Date: 2022-06-17
奥信阳光(北京)药业科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The voriconazole-cyclodextrin inclusion compound is prepared in the form of freeze-dried powder by freeze-drying technology, which solves the defect of voriconazole instability in the water phase; through the form of nebulized inhalation, the active ingredient is inhaled and administered directly to the lung lesions, It has a very good therapeutic effect on patients with fungal infections in the lungs

Method used

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  • Voriconazole aerosol inhalant and application thereof
  • Voriconazole aerosol inhalant and application thereof
  • Voriconazole aerosol inhalant and application thereof

Examples

Experimental program
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Effect test

preparation example 1

[0030] (S1) dissolve 0.04 part of polyoxyethylene hydrogenated castor oil and 0.01 part of pentaerythritol monostearate in 15 parts of acetic acid aqueous solution with pH 3, stir evenly, slowly add 1 part of voriconazole original drug, continue to stir until voriconazole is completely dissolved . The obtained acetic acid solution of voriconazole was added to a saturated aqueous solution containing 10 parts of sodium sulfobutyl-β-cyclodextrin, stirred at 30 ° C for 4 h, the inclusion was complete, and the pH was adjusted to 6.5 with 6.5 wt % aqueous sodium carbonate solution , adding 0.1 wt % of activated carbon in the solution, stirring for 0.5 h, and filtering with a 0.22 μm microporous membrane to obtain a clear and transparent solution, which is used for the next step of freeze-drying.

[0031] (S2) Pre-freeze the mixture of the inclusion compounds obtained in (S1) at -30°C for 5h, vacuumize, heat up to -10°C at 5Pa, keep the temperature for 30h, and then slowly heat up to...

preparation example 2

[0038] Other conditions and operations are the same as in Preparation Example 1, except that the solubilizer in step (S1) is 0.05 part of polyoxyethylene hydrogenated castor oil, that is, no pentaerythritol monostearate is added. After testing, the inclusion rate of the voriconazole-cyclodextrin inclusion complex freeze-dried powder obtained in Preparation Example 2 was 96.4%, and in a phosphate buffer solution with pH=7 and a saturated solution at 25°C, the dissolved concentration of voriconazole reached 18.6 mg / mL.

preparation example 3

[0040] Other conditions and operations are the same as in Preparation Example 1, except that the solubilizer in step (S1) is 0.05 part of pentaerythritol monostearate, that is, no polyoxyethylene hydrogenated castor oil is added. After testing, the inclusion rate of the voriconazole-cyclodextrin inclusion complex freeze-dried powder obtained in Preparation Example 3 was 93.2%, and in a phosphate buffer solution with pH=7 and a saturated solution at 25°C, the dissolved concentration of voriconazole reached 18.0 mg / mL.

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Abstract

The invention relates to a voriconazole aerosol inhalant, which is prepared from the following raw materials in parts by mass: 8 to 13 parts of voriconazole-cyclodextrin inclusion compound freeze-dried powder and 100 parts of water for injection, the voriconazole-cyclodextrin inclusion compound freeze-dried powder is prepared by the following steps: preparing an inclusion compound solution from voriconazole, polyoxyethylene hydrogenated castor oil, an organic weak acid solution of pentaerythritol monostearate and a cyclodextrin aqueous solution, and freeze-drying. The compound of polyoxyethylene hydrogenated castor oil and pentaerythritol monostearate is used as a solubilizer, so that voriconazole can be smoothly solubilized in organic weak acid to complete inclusion with cyclodextrin, and the plasma concentration of the aerosol inhalant prepared from the inclusion compound and redissolved in freeze-dried powder is stable after inhalation; the adverse reaction caused by high blood concentration of voriconazole is reduced, and the use safety of voriconazole is improved.

Description

technical field [0001] The invention relates to the field of antifungal drugs, in particular to a voriconazole atomized inhaler and its application. Background technique [0002] Voriconazole, a derivative of fluconazole, is a triazole antifungal drug with broad-spectrum antibacterial activity, especially against Aspergillus. The therapeutic mechanism of voriconazole is to inhibit the demethylation of 14α-sterol mediated by cytochrome 450, thereby inhibiting the conversion of lanosterol to ergosterol, and the loss of ergosterol destroys the integrity of fungal cells, which leads to the apoptosis of fungi. The dosage forms that have been developed include intravenous injection and oral administration. At present, clinical applications and researches are mostly oral pharmaceuticals, including tablets, capsules, and dry suspensions. And for critically ill patients, elderly and young children and other patients with weak autonomy, oral preparations have the disadvantage of bei...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K31/506A61K47/14A61K47/44A61K47/69A61P11/00A61P31/10A61K9/19
CPCA61K31/506A61K47/6951A61K9/0078A61K47/44A61K47/14A61P31/10A61P11/00A61K9/19
Inventor 孔小轶李金花王蕾
Owner 奥信阳光(北京)药业科技有限公司
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