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Artemisinin derivatives freeze-dried preparation and preparation method

A technology for freeze-dried preparations and derivatives, which is applied in the field of freeze-dried preparations and preparations of artemisinin derivatives, which can solve problems such as microbial contamination and organic solvent residues, and achieve the effects of short production cycle, fast dissolution speed and simple process

Active Publication Date: 2008-02-20
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to overcome the safety problems such as organic solvent residues and microbial contamination in the prior art, and provide a brand-new Artemisia annua with stable drug composition, easily soluble in water, fast dissolution speed, and stable compatibility with commonly used clinical infusions. Freeze-dried preparation and preparation method of steroid derivatives

Method used

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  • Artemisinin derivatives freeze-dried preparation and preparation method
  • Artemisinin derivatives freeze-dried preparation and preparation method
  • Artemisinin derivatives freeze-dried preparation and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] formula:

[0029] Artemether (conventional refined powder, particle size greater than 315μm) 60g

[0030] Hydroxypropyl-β-cyclodextrin 2350g

[0031]

[0032] Made 1000 pieces

[0033] Weigh the hydroxypropyl-β-cyclodextrin of the prescribed amount, first take 1600g and dissolve it in 4000ml water for injection to make a concentration of 40%, heat it to 70°C-90°C, add the prescribed amount of artemether (particle size greater than 315 μm), stir, then add the remaining hydroxypropyl-β-cyclodextrin, stir to dissolve, add water for injection to 5000ml, fill, freeze-dry to obtain the finished product.

Embodiment 2

[0035] formula:

[0036] Artemether (fine powder 1.0μm~10μm) 60g

[0037] Hydroxypropyl-β-cyclodextrin 2200g

[0038]

[0039] Made 1000 pieces

[0040] The artemether is pulverized by a low-temperature pulverizer (0° C. to 10° C.) to obtain artemether with a particle size of 1.0 μm to 10 μm. Separately weigh the prescribed amount of hydroxypropyl-β-cyclodextrin, firstly take 1800g and dissolve it in 4000ml water for injection to make a concentration of 45%, heat it to 50°C-60°C, add the prescribed amount of artemether, stir, Then add the remaining hydroxypropyl-β-cyclodextrin, stir to dissolve, add water for injection to 5000ml, fill and freeze-dry to obtain the finished product.

Embodiment 3

[0042] formula:

[0043] Artemether (fine powder 1.0μm~20μm) 80g

[0044] Sulfobutyl ether-β-cyclodextrin 440

[0045] Methyl-β-cyclodextrin 2000

[0046]

[0047] Made 1000 pieces

[0048] The artemether is pulverized by a low-temperature pulverizer (0° C. to 10° C.) to obtain artemether with a particle size of 1.0 μm to 20 μm. In addition, take the sulfobutyl ether-β-cyclodextrin and methyl-β-cyclodextrin of prescription quantity, first get the methyl-β-cyclodextrin of 1200g and be dissolved in 4000ml water, make the concentration of 30%, add Warm to 50 ℃ ~ 60 ℃, add the prescribed amount of artemether, stir, then add the remaining methyl-β-cyclodextrin and sulfobutyl ether-β-cyclodextrin, stir to dissolve, add water for injection to 5000ml, filled and freeze-dried to get the finished product.

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Abstract

The present invention relates to a frozen dry preparation of drug artemisinin derivatives and the preparation method. The present invention is composed of artemisinin derivatives and water-soluble cyclodextrin derivatives, the weight ratio of the artemisinin derivatives and water-soluble cyclodextrin derivatives is 1: 30 to 70, the smashed artemisinin derivatives are added into the water solution of the water-soluble cyclodextrin derivatives at 50 DEG C to 90 DEG C for agitating and dissolving, then the frozen dry preparation is prepared by the conventional process of the injection and the frozen drying. The low-temperature micro-powder technology of the present invention has the advantages that the technology can ensure the physical and chemical properties of the artemisinin derivatives to be consistent before and after the smashing, the process is relatively simple compared with the prior art, the equipments make use of the existing production equipments of the company, thus saving the investment and shorten the production cycle; the dispensing solvent is the water for injection, without the organic solvents, surfactants and cosolvents, so as to improve the safety; the present invention is easy to be dissolved in water, and has fast dissolution speed and the infinite dilution stability, thus avoiding the secondary pollution caused in the other methods which firstly prepare the artemisinin derivatives into the inclusions by using the organic solvents and then sub-package the inclusions thereof.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a freeze-dried preparation of artemisinin derivatives for intravenous injection and a preparation method thereof. Background technique [0002] The well-known antimalarial drug artemisinin derivatives, due to their unique chemical structure, have good clinical curative effect and less toxic and side effects. Artemisinin drugs are clinically recommended by WHO for the prevention and treatment of malaria. Recent literature reports that artemisinin drugs also have anti-tumor effects, but the solubility of artemisinin drugs in water is very low, and they are insoluble drugs. Vegetable oil is used as a solvent for the preparation of injections, and they can only be administered intramuscularly in clinical practice. Long-term use can easily cause muscle agglomeration and necrosis at the injection site, so it is of clinical significance to develop a new preparation that can be adminis...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/365A61K31/366A61K31/357A61K47/48A61K47/40A61P35/00A61P33/06A61K47/61
CPCY02A50/30
Inventor 陈云建黄照昌张嗣昆吴宏宾
Owner KPC PHARM INC
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