Non-crystalline vancomycin hydrochloride, its preparation method and use, and its pharmaceutical composition

A technology of vancomycin hydrochloride and vancomycin, which is applied in the direction of drug combination, anti-infective drugs, glycopeptide components, etc., can solve the problems of large capsule particles and difficulty in taking, and achieve the improvement of effective components, appearance and color change, and impurities Reduced effect

Active Publication Date: 2016-08-17
ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, the vancomycin hydrochloride used clinically is to use freeze-dried powder as raw material to prepare oral and injection dosage forms. In the capsule dosage form of oral dosage form, because the density of the freeze-dried powder is relatively small, the prepared capsule particles are relatively large and difficult to take.

Method used

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  • Non-crystalline vancomycin hydrochloride, its preparation method and use, and its pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Preparation of crude vancomycin

[0035] The vancomycin fermentation broth was filtered under alkaline conditions, and the obtained clarified filtrate was passed through the macroporous adsorption resin XAD-1600. Vancomycin was adsorbed on the resin. After the resin was washed with water, it was eluted with an acidic aqueous solution of 40% ethanol. After elution, the eluate containing vancomycin was added to activated carbon for decolorization, the filtrate obtained by filtration was concentrated to obtain an aqueous solution of vancomycin hydrochloride, and then NH was added. 4 HCO 3 Precipitation was carried out to obtain crude vancomycin. The vancomycin B content in the crude vancomycin product was 86.8%, and the titer was 599u / mg.

[0036] Take 2500g of this crude product, add 20.0L of purified water, add NaOH solution to adjust the pH to 10.0, use 0.2M 2 The 0.5μm pore size ceramic membrane was filtered to obtain 25.0L vancomycin filtrate, the soluti...

Embodiment 2

[0037] Example 2: Precipitation of Vancomycin Hydrochloride

[0038] Take 500 mL of the concentrated solution in Example 1, filter it through 0.45 μm and 0.2 μm filters, and add 25 g of NaHCO while stirring. 3 , Vancomycin was precipitated from it to form a slurry, add HCl aqueous solution to adjust the pH to 2.80, continue to stir for 60min to make it evenly mixed, stop stirring and let stand for 38 hours, the process temperature is controlled at 14 ~ 15 ℃. The mixture was separated by filtration and firstly washed with 200 mL of 90% ethanol. After the top washing, the conductivity of the top washing liquid was 385us / cm, and then top washed with 200 mL of absolute ethanol to obtain 99.7 g of vancomycin hydrochloride wet product. After removing the residual ethanol by drying, 72.5 g of the intermediate was obtained, and then 63.2 g of finished vancomycin hydrochloride was obtained after drying in high vacuum. The moisture content of the finished product was 3.4%. g / ml. The n...

Embodiment 3

[0039] Example 3: Precipitation of Vancomycin Hydrochloride

[0040] Take 500 mL of the concentrated solution in Example 1, filter it through 0.45 μm and 0.2 μm filters, and add 15 g of NaHCO while stirring. 3 , Vancomycin was precipitated from it to form a slurry, add HCl aqueous solution to adjust the pH to 3.50, continue to stir for 30min to make it evenly mixed, stop stirring and let stand for 48 hours, the process temperature is controlled at 5 ~ 6 ℃. The mixture was separated by filtration and firstly washed with 200 mL of 90% ethanol. After the top washing, the conductivity of the top washing liquid was 293 us / cm, and then top washed with 200 mL of absolute ethanol to obtain 92.3 g of vancomycin hydrochloride wet product, wet product. The product is dried to remove residual ethanol to obtain 68.5g of intermediate, and then dried in high vacuum to obtain 58.6g of finished vancomycin hydrochloride, the moisture content of the finished product is 3.1%, the bulk density of ...

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Abstract

The invention provides a high-density amorphous vancomycin hydrochloride, a preparation method thereof, an application of the vancomycin hydrochloride for oral administration or injection administration and a pharmaceutical composition containing the vancomycin hydrochloride. The vancomycin hydrochloride in an amorphous state has the characteristics similar to the diffraction pattern of an X-ray powdery crystal shown in the attached drawing 1. The effective components of vancomycin hydrochloride prepared by the preparation method are enhanced greatly, other impurities are reduced to a large extent, the purity is high, and the chromatographic purity can reach more than 95 percent. The amorphous vancomycin hydrochloride not only can be used as injections, but also can be used as capsules and other solid preparations. Meantime, the appearance and the color of products are improved obviously, and the products are suitable for oral administration or injection administration.

Description

technical field [0001] The present invention relates to a kind of vancomycin hydrochloride, in particular, to a kind of high-density non-crystalline vancomycin hydrochloride and its preparation method, and the use of the vancomycin hydrochloride for oral administration or injection administration, and containing The pharmaceutical composition of vancomycin hydrochloride. Background technique [0002] Vancomycin hydrochloride is an amphoteric glycopeptide antibiotic produced by Nocardia orientalis under controlled fermentation conditions, its chemical formula is C 66 H 75 C 12 N 9 O 24 HCl with a molecular weight of 1,486. The preparation of vancomycin by fermentation of the microorganism Amycolatopis orientalis (formerly Nocardia orientalis) has been described in more detail in US Pat. No. 3,067,099 (filed 1955) and WO 91 / 08,300. The lyophilized powder of vancomycin hydrochloride is off-white, its aqueous solution is a transparent solution, and its pH is 2.5-4.5. [0...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K9/00A61K38/14A61P31/00
Inventor 王小勇张国钧劳学军孙新强
Owner ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
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