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Itraconazole mesylate and its composition and preparation method

A technology of itraconazole mesylate and composition, applied in the field of itraconazole salt and preparation thereof, can solve the problems of unfavorable drying, surface layer becoming pasty, and high equipment requirements

Inactive Publication Date: 2007-05-30
SHANGHAI SEANPHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This preparation method has higher requirements on equipment, and it is also unfavorable to consider the use of hydrogen chloride gas from the perspective of environmental safety.
[0014] 2. In the final stage of preparing itraconazole hydrochloride, when it is formed into salt and filtered, itraconazole hydrochloride is very easy to absorb moisture, and the surface layer becomes paste after absorbing moisture, which is not conducive to drying
[0015] 3. Itraconazole hydrochloride is easy to generate hydrogen chloride gas during storage, and it is easy to corrode the packaging. This phenomenon is more likely to occur in non-solution preparations

Method used

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  • Itraconazole mesylate and its composition and preparation method
  • Itraconazole mesylate and its composition and preparation method
  • Itraconazole mesylate and its composition and preparation method

Examples

Experimental program
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Effect test

preparation example Construction

[0055] These pharmaceutical compositions can be prepared by mixing with suitable pharmaceutical additives such as excipients, disintegrants, binders, lubricants, diluents, buffers or by diluting and dissolving in suitable additives , isotonic agent, preservative, wetting agent, emulsifier, dispersant, stabilizer, solubilizer, etc., and prepare the pharmaceutical composition according to conventional methods.

[0056] When the pharmaceutical composition of the present invention is used for actual treatment, the dose of the compound represented by the above general formula as the active ingredient can be appropriately determined according to the age, sex, body weight, symptoms and degree of treatment of each patient. The dose is approximately 0.1-1,000 mg per adult per day, and the dose is approximately 0.01-500 mg per adult per day for parenteral administration, and the daily dose can be divided into one or several times a day and administered at an appropriate time .

[0057]...

Embodiment 1

[0065] Preparation of itraconazole dimesylate

[0066] Add 50g of itraconazole and 600ml of acetone into a 1L reaction flask, add excess methanesulfonic acid under reflux and stirring, after the reaction is complete, filter with suction, wash with acetone, and dry at 60°C to obtain itraconazole methanesulfonic acid Salt 60.3g, yield 95%.

[0067] Elemental Analysis C 35 h 38 N 8 o 4 .2CH 3 SO 3 H: (exp. / calc.) C 49.33 / 49.49, H 5.18 / 5.16, N 12.56 / 12.48, Cl 7.83 / 7.90, S 7.19 / 7.14.

[0068] Itraconazole mesylate 1 H-NMR data (using deuterated dimethyl sulfoxide as solvent)

[0069]

[0070] 1 Information about H-NMR spectrum

[0071] proton number

Embodiment 2

[0073] Preparation of itraconazole dimesylate

[0074] Add 2g of itraconazole and 20ml of ethanol into a 50ml reaction bottle, heat to reflux, add excess methanesulfonic acid under stirring, after the reaction is complete, cool to room temperature, filter, wash with ethanol, and dry to obtain itraconazole Azole mesylate 2.36g. Yield 93%.

[0075] elemental analysis and 1 The HNMR data were the same as shown in Example 1, indicating the formation of itraconazole dimesylate.

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Abstract

The invention discloses an eosin constantan methanesulfonic acid salt and component and making method, wherein the eosin constantan methanesulfonic acid salt possesses chemical structural formula (n=1-2), which possesses excellent solubility and stability; the component of eosin constantan methanesulfonic acid salt consists of eosin constantan methanesulfonic acid salt and acceptable carrier, which can prepare kinds of liquid, freeze-drying and film or skin give drug.

Description

technical field [0001] The invention relates to an itraconazole (itraconazole) salt and a preparation thereof, in particular to itraconazole mesylate, a composition and a preparation method thereof. Background technique [0002] Itraconazole is (±)-cis-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1 H -1,2,4-triazol-1-yl-methyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl] -2,4-dihydro-2-(1-methylpropyl)-3 H -1,2,4-Triazol-3-one, is a broad-spectrum antifungal compound for oral, parenteral and topical administration, which can be used for the treatment of systemic fungal infections including aspergillosis, candidiasis, cryptococcal Meningitis, histoplasmosis, sporotrichosis, paracoccidioidomycosis, chromomycosis, blastomycosis, gynecological vulvovaginal candidiasis, dermatology / ophthalmology tinea versicolor, dermatophytosis, fungal cornea Inflammation and oral candidiasis and onychomycosis caused by dermatophytes and / or yeasts are disclosed in US-4,267,179. However...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/14A61K31/4196A61K9/48A61K9/20A61K9/46A61K9/14A61K9/02A61K9/08A61K9/19A61K9/06A61K9/107A61K47/40A61K47/38A61K47/36
Inventor 徐学明
Owner SHANGHAI SEANPHARM
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