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Moxifloxacin hydrochloride monohydrate crystal form and preparation method thereof

A technology of moxifloxacin hydrochloride and monohydrate, which is applied in the field of pharmacy, can solve the problems that affect the dosage accuracy, instability, moisture absorption and other problems of preparations, and achieve the effect of remarkable drug effect, low cost and improved solubility

Active Publication Date: 2013-09-18
CHINA RESOURCES SAIKE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Crystal form I is the anhydrous crystal form of moxifloxacin hydrochloride, but it has strong hygroscopicity, is unstable under conventional storage and preparation conditions, and is easy to absorb moisture, which directly affects the accuracy of dosage and the quality of preparations, so Not a good medicinal form of moxifloxacin hydrochloride

Method used

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  • Moxifloxacin hydrochloride monohydrate crystal form and preparation method thereof
  • Moxifloxacin hydrochloride monohydrate crystal form and preparation method thereof
  • Moxifloxacin hydrochloride monohydrate crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: the preparation of moxifloxacin

[0041] Add 50g of moxifloxacin hydrochloride to a mixed solution of 205mL of water and 250mL of dichloromethane, adjust the pH to 7.5-8.5 with saturated aqueous sodium hydroxide solution at room temperature, let the layers stand, separate the organic layer, evaporate the solvent to obtain moxifloxacin Xishaxing.

Embodiment 2

[0042] Example 2: Preparation of new crystal form of moxifloxacin hydrochloride monohydrate

[0043] Add 5 g of moxifloxacin to a mixed solution of 30 mL of acetone and 1 mL of water, heat to reflux, adjust the pH to 1-2 with concentrated hydrochloric acid, stir at the same temperature for 30 min, stop heating, cool to room temperature, filter, and wash the filter cake with a small amount of acetone , and air-dried at 40°C for 6 hours to obtain a new crystal form of moxifloxacin hydrochloride monohydrate. see Attachment

Embodiment 3

[0044] Example 3: Preparation of new crystal form of moxifloxacin hydrochloride monohydrate

[0045] Add 5g of moxifloxacin to a mixed solution of 30mL of dioxane and 1mL of water, heat to reflux, adjust pH=1-2 with concentrated hydrochloric acid, stir at the same temperature for 30min, stop heating, cool to room temperature, filter, and filter cake A small amount of dioxane was washed, and air-dried at 40°C for 6 hours to obtain a new crystal form of moxifloxacin hydrochloride monohydrate. See attached figure 2 .

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Abstract

The invention relates to a moxifloxacin hydrochloride monohydrate crystal form, wherein characteristic spectrum areas are in an X-diffractogram where 2theta=31.58, 45.32, 56.34, 66.08+-0.2. The invention also provides a preparation method of the novel crystal form. The method comprises steps that: anhydrous moxifloxacin hydrochloride or moxifloxacin hydrochloride hydrate or a mixture of the two is added to a mixed solution of an organic solvent and water; the mixture is heated to an appropriate temperature; the pH value of the mixture is regulated by using hydrochloric acid; heating is stopped, and the mixture is cooled, such that crystals are precipitated, and the novel moxifloxacin hydrochloride monohydrate crystal form is obtained.

Description

Technical field: [0001] The invention belongs to the field of pharmacy, and relates to a new crystal form of moxifloxacin hydrochloride monohydrate and a preparation method thereof. Background technique: [0002] Moxifloxacin hydrochloride, namely 1-cyclopropyl-7-(S,S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-8-methoxy- 4-oxo-1,4-dihydro-3-quinoline carboxylic acid hydrochloride is a new generation of fluoroquinolone broad-spectrum antibacterial drugs, developed by Bayer (Bayer) in Germany, and it is reported in the patent US5607953, And it was first listed in Germany in 1999. This product has broad-spectrum antibacterial activity against Gram-positive bacteria, Gram-negative bacteria, Legionella, anaerobic bacteria, acid-fast bacteria and atypical microorganisms. It is mainly used for acute exacerbation of chronic bronchitis, chronic obstructive pneumonia, social Acquired pneumonia, acute acquired sinusitis, and uncomplicated skin and skin and soft tissue infections. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/04A61K31/4709A61P31/04A61P11/00A61P29/00A61P17/00
Inventor 张益坤邹江刘蕴秀杨琰王文峰
Owner CHINA RESOURCES SAIKE PHARMA