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Itraconazole hydrochloride, oral solid combination and preparation method

A technology of itraconazole hydrochloride and solid composition, which is applied in the field of oral solid composition and preparation containing itraconazole hydrochloride, can solve the problems of low heating temperature and production without industrialized setting equipment, and achieve Low energy consumption, conducive to environmental protection and large-scale industrial production, and the effect of water solubility improvement

Inactive Publication Date: 2005-08-31
SHANGHAI INST OF PHARMA IND CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the invention has a lower heating temperature than WO97 / 44014, it is produced without industrialized setting equipment

Method used

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  • Itraconazole hydrochloride, oral solid combination and preparation method
  • Itraconazole hydrochloride, oral solid combination and preparation method
  • Itraconazole hydrochloride, oral solid combination and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Preparation of itraconazole hydrochloride

[0042] Add 40 g of itraconazole and 600 ml of acetone into a 1 L reaction flask, and feed excess hydrogen chloride under reflux and stirring. After the reaction is complete, filter, wash with acetone, and dry to obtain 42 g of itraconazole hydrochloride. Yield 95%. Elemental Analysis C 35 h 38 N 8 o 4 .2 HCl: (experimental / calculated) C53.70 / 53.99, H5.20 / 5.18, N14.46 / 14.39, Cl18.20 / 18.22.

[0043] Itraconazole hydrochloride 1 HNMR data (using deuterated dimethyl sulfoxide as solvent)

[0044]

[0045] proton number

Embodiment 2

[0047] Preparation of itraconazole hydrochloride

[0048] Add 2g of itraconazole and 20ml of ethanol into a 50ml reaction bottle, heat to reflux, pass in excess hydrogen chloride under stirring, after the reaction is complete, cool to room temperature, filter, wash with ethanol, and dry to obtain itraconazole Hydrochloride 2.12g. Yield 96.4%. elemental analysis and 1 HNMR data same as above.

Embodiment 3

[0050] Preparation of capsules containing itraconazole hydrochloride (100 mg itraconazole / capsule)

[0051] 1. Prescription

[0052] Itraconazole Hydrochloride 110g

[0053] β-cyclodextrin 250g

[0054] Makes 1000 capsules

[0055] 2. Craft

[0056] 2.1 Pass itraconazole hydrochloride through a 200-mesh sieve;

[0057] 2.2 Weigh 110 grams of itraconazole hydrochloride and 250 grams of β-cyclodextrin, mix well, and pass through a 60-mesh sieve three times.

[0058] 2.3 Fill the mixed powder of 2.2 into the No. 0 capsule.

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PUM

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Abstract

An itraconazole hydrochloride and its orally taken solid composition are disclosed, which are prepared through reaction between itraconazole and hydrochloric acid to obtain itraconazole hydrochloride, and mixing it with cyclodextrin.

Description

technical field [0001] The invention relates to an itraconazole salt and its preparation, in particular to an oral solid composition containing itraconazole hydrochloride and a preparation method thereof. technical background [0002] Itraconazole is (±)-cis-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-tri Azol-1-yl-methyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro- 2-(1-Methylpropyl)-3H-1,2,4-triazol-3-one, is a broad-spectrum antifungal compound for oral, parenteral and topical use in the treatment of systemic fungi Infections include aspergillosis, candidiasis, cryptococcal meningitis, histoplasmosis, sporotrichosis, paracoccidioidomycosis, chromomycosis, blastomycosis, gynecologic vulvovaginal candidiasis, dermatology / Ophthalmic tinea versicolor, dermatophytosis, fungal keratitis and oral candidiasis and onychomycosis caused by dermatophytes and / or yeasts are disclosed in US-4,267,179. However, the bioavailability of orally administered i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496C07D405/14
CPCC07D405/14A61K31/496A61P31/10
Inventor 陶涛贺宝元顾玉兰周伟澄黄良安
Owner SHANGHAI INST OF PHARMA IND CO LTD
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