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Valnemulin hydrochloride diluent and preparation method thereof

A technology of warnemulin hydrochloride and diluent, which is applied in the direction of pharmaceutical formulas, medical preparations of non-active ingredients, non-effective ingredients of polymer compounds, etc., can solve problems such as unstable aqueous solution, difficulty in injection, easy swelling, etc., and achieve The clinical effect is stable, the acupuncture is good, and the stability is good

Pending Publication Date: 2020-12-29
HENAN SOAR VETERINARY PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor solubility of warnemulin hydrochloride, the aqueous solution is unstable, and when water or saline is used as a dilution carrier, there are problems such as difficulty in injection, easy swelling, compounding with oil seedlings and delamination, and unstable clinical effects.

Method used

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  • Valnemulin hydrochloride diluent and preparation method thereof
  • Valnemulin hydrochloride diluent and preparation method thereof
  • Valnemulin hydrochloride diluent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] A diluent of warnemulin hydrochloride, which consists of 88% by weight of water for injection, 2% of 2,2-dimethylol butyric acid, 3% of water-soluble β-cyclodextrin polymer, copovidone S630 1 %, chelating agent 2%, emulsifier 2%, stabilizer 2%; wherein, the water for injection is deionized water; the emulsifier is polyethylene glycol cetostearyl ether 20; the chelating agent is Potassium sodium tartrate; The stabilizer is adenine.

[0025] Preparation method, the steps are as follows:

[0026] (a) Put 2,2-dimethylolbutyric acid, water-soluble β-cyclodextrin polymer, copovidone S630 and 40 wt% water for injection into the reaction kettle in sequence, and close the reaction The door of the kettle is sealed tightly;

[0027] (b) Thoroughly stir the mixed liquid obtained in step (a) through the stirring mechanism in the reactor, the rotating speed is 5000rpm, and the time is 15 minutes;

[0028] (c) While stirring, pressurize and heat the inside of the reactor, raise the...

Embodiment 2

[0032] A diluent of warnemulin hydrochloride, which consists of 85% by weight of water for injection, 3% of 2,2-dimethylol butyric acid, 3% of water-soluble β-cyclodextrin polymer, copovidone S630 2 %, chelating agent 2%, emulsifier 2%, stabilizer 3%; wherein, the water for injection is distilled water; the emulsifier is vitamin E polyethylene glycol succinate; the chelating agent is ammonium citrate ; The stabilizer is polypropylene glycol.

[0033] Preparation method, the steps are as follows:

[0034] (a) Put 2,2-dimethylolbutyric acid, water-soluble β-cyclodextrin polymer, copovidone S630 and water for injection with 50 wt% total water for injection into the reactor in turn, and close the reaction The door of the kettle is sealed tightly;

[0035] (b) Thoroughly stir the mixed solution obtained in step (a) through the stirring mechanism in the reactor, the rotating speed is 8000rpm, and the time is 10 min;

[0036] (c) While stirring, pressurize and heat the inside of t...

Embodiment 3

[0040] A diluent of warnemulin hydrochloride, which is composed of 90% water for injection, 1% 2,2-dimethylol butyric acid, 2% water-soluble β-cyclodextrin polymer, copovidone S630 1 %, chelating agent 1%, emulsifier 3%, stabilizer 2%; wherein, the water for injection is deionized water; the emulsifier is castor oil polyoxylate 35; the chelating agent is ethylenediaminetetra In acetic acid; the stabilizer is adenine.

[0041] Preparation method, the steps are as follows:

[0042] (a) Put 2,2-dimethylolbutyric acid, water-soluble β-cyclodextrin polymer, copovidone S630 and 60 wt% water for injection into the reaction kettle in sequence, and close the reaction The door of the kettle is sealed tightly;

[0043] (b) Thoroughly stir the mixed liquid obtained in step (a) through the stirring mechanism in the reactor, the rotating speed is 6000rpm, and the time is 12 minutes;

[0044] (c) While stirring, pressurize and heat the inside of the reactor, raise the temperature inside t...

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Abstract

The invention belongs to the technical field of veterinary drugs, and discloses a valnemulin hydrochloride diluent and a preparation method thereof. The valnemulin hydrochloride diluent is prepared from the following raw materials in percentage by weight: 85 to 90 percent of water for injection, 1 to 3 percent of 2, 2-dimethylolbutanoic acid, 1 to 3 percent of water-soluble beta cyclodextrin polymer, 1 to 2 percent of copovidone S630, 1 to 2 percent of chelating agent, 1 to 3 percent of emulsifier and 2 to 3 percent of stabilizer. The preparation method comprises the following steps of: putting the 2, 2-dimethylolbutanoic acid, the water-soluble beta cyclodextrin polymer, the copovidone S630 and part of the water for injection into a reaction kettle, and sealing; stirring a mixed solution,pressurizing and heating the reaction kettle to 50 to 70 DEG C and 2 to 6MPa while stirring, keeping for 5 to 10 minutes, and then releasing pressure; adding the chelating agent, the emulsifier and the stabilizer into the mixed solution, stirring, and adding the rest of the water for injection into the mixed solution while stirring; and taking out the mixed solution, filtering and sterilizing toobtain the diluent. The valnemulin hydrochloride prepared by the diluent disclosed by the invention has the advantages of good needle cleaning property, no bulge at an injection part, good stability and stable clinical effect.

Description

technical field [0001] The invention belongs to the technical field of veterinary medicine, and in particular relates to a diluent of warnemulin hydrochloride and a preparation method thereof. Background technique [0002] Valnemulin hydrochloride (Valnemulin) is a new generation of pleuromutilin semi-synthetic antibiotics, which belongs to diterpenes and is the same drug as tiamulin. In 1984, Swiss Sandoz company Bemer et al took the lead in successfully synthesizing pleuromutilin. In 1999, the Swiss company Norvatis made it into a premix, trade name Econor, which is now on the market in many countries, mainly used to prevent and treat mycoplasma and intestinal spirochete infection in livestock and poultry. Due to its safety, high efficiency, low toxicity, and low resistance to drug resistance, warnemulin hydrochloride has been widely used in many countries. However, the solubility of varnimulin is low, the stability is relatively poor, and it is inconvenient for veterina...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/12A61K47/40A61K47/32A61K47/18A61K47/10A61K47/22A61K47/44A61K31/22A61P31/04
CPCA61K47/12A61K47/40A61K47/32A61K47/183A61K47/10A61K47/22A61K47/44A61K9/0019A61K31/22A61P31/04
Inventor 胡帅李凌峰郑泽中吕明霞孙娅莉常磊
Owner HENAN SOAR VETERINARY PHARMA