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38 results about "Valnemulin" patented technology

Valnemulin (trade name Econor) is a pleuromutilin antibiotic used to treat swine dysentery, ileitis, colitis and pneumonia. It is also used for the prevention of intestinal infections of swine. Valnemulin has been observed to induce a rapid reduction of clinical symptoms of Mycoplasma bovis infection, and eliminate M. bovis from the lungs of calves.

Valnemulin prodrug as well as preparation method and detection method thereof

InactiveCN104927041AImprove stabilityOvercome the shortcoming that the half-life is only 1.3-2.7 hoursPharmaceutical non-active ingredientsEster active ingredientsDrug loading doseOrganic chemistry
The invention discloses a valnemulin prodrug as well as a preparation method and a detection method thereof. The provided valnemulin prodrug has good stability and overcomes the weakness that the half attenuation period of the valnemulin prodrug is only 1.3 to 2.7 hours, the prepared prodrug has a controlled-release action, and the in-vitro release experiment shows that the valnemulin prodrug can reach the maximum value in 8 hours. Since valnemulin molecules have a plurality of active reaction sites, a method for determining a reaction site for connecting the carrier and valnemulin is a method for adopting a single-molecular carrier to react with valnemulin, the obtained single-molecular prodrug is determined as the reaction site of the valnemulin by virtue of nuclear magnetic detection, and the prodrug reaction site obtained in the method is two amino acids of the valnemulin; the valnemulin prodrug with relatively high drug loading capacity can be prepared; the drug loading capacity of the prepared PEG-valnemulin prodrug is determined by adopting a UV, HPLC-UV and HPLC-ELSD combination method, so that the measured drug loading capacity is more accurate. The method is suitable for preparing and detecting the valnemulin prodrug.
Owner:HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY

Rifamycin and valnemulin hybrid antibiotic and preparation method thereof

The invention discloses a rifamycin and valnemulin hybrid antibiotic compound and a preparation method thereof. The rifamycin and valnemulin hybrid antibiotic has a structure as shown in the formula (I). The preparation method comprises the following steps: (1) adding concentrated sulfuric acid into a DMF (Dimethyl Formamide) solution of rifamycin s and sodium salt to acidize for 0.5h, and then, dropwise adding dihydroxy-tert-butylamine to react to obtain an intermediate, i.e., oxazine rifamycin II; (2) mixing the intermediate, i.e., the oxazine rifamycin II and piperazine anhydrous in a protonic solvent, and reacting to obtain an intermediate, i.e., 3-formyl rifamycin III; and (3) mixing and dissolving the 3-formyl rifamycin III and valnemulin in a solvent, stirring at the temperature of 15-30 DEG C for 2h under the protection of nitrogen gas, and cooling to obtain the rifamycin and valnemulin hybrid antibiotic. Two drug molecules with different action mechanisms are connected together, the combination way of the rifamycin and valnemulin hybrid antibiotic compound is similar to that of a prodrug with dual functions, the linking group is stable, and the rifamycin and valnemulin hybrid antibiotic compound can take a very good treating effect.
Owner:WUHAN INSTITUTE OF TECHNOLOGY

Preparation method for valnemulin liposome

The invention discloses a preparation method for a valnemulin liposome. The method comprises the following steps: 1) preparation of a NaHCO3 solution; 2) preparation of a citric acid buffer solution; 3) preparation of a blank liposome: a step of dissolving phosphatide and cholesterol in absolute ethyl alcohol in a water bath, allowing ethanol to volatilize and a film to be formed, then adding the citric acid buffer solution, carrying out complete hydration and filtering an obtained liposome solution with a millipore filter to realize whole grain filtering; 4) preparation of valnemulin fluid by dissolving raw valnemulin powder in ethanol; 5) active loading: a step of successively adding the valnemulin fluid and the NaHCO3 solution into the blank liposome and carrying out uniform mixing so as to obtain a crude liposome product; and 6) low temperature high speed centrifugation of the crude product obtained in step 5) so as to prepare the valnemulin liposome. According to the invention, through preparation of the blank liposome and active loading, the valnemulin liposome with a high entrapment rate and good clinical effects is obtained; the method is simple and easily practicable, and solubility of valnemulin in water and effective acting time, stability and targeting of valnemulin are improved.
Owner:ZHENGZHOU HOUYI PHARMA

Preparation method for valnemulin liposome

The invention discloses a preparation method for a valnemulin liposome. The method comprises the following steps: 1) preparation of a NaHCO3 solution; 2) preparation of a citric acid buffer solution; 3) preparation of a blank liposome: a step of dissolving phosphatide and cholesterol in absolute ethyl alcohol in a water bath, allowing ethanol to volatilize and a film to be formed, then adding the citric acid buffer solution, carrying out complete hydration and filtering an obtained liposome solution with a millipore filter to realize whole grain filtering; 4) preparation of valnemulin fluid by dissolving raw valnemulin powder in ethanol; 5) active loading: a step of successively adding the valnemulin fluid and the NaHCO3 solution into the blank liposome and carrying out uniform mixing so as to obtain a crude liposome product; and 6) low temperature high speed centrifugation of the crude product obtained in step 5) so as to prepare the valnemulin liposome. According to the invention, through preparation of the blank liposome and active loading, the valnemulin liposome with a high entrapment rate and good clinical effects is obtained; the method is simple and easily practicable, and solubility of valnemulin in water and effective acting time, stability and targeting of valnemulin are improved.
Owner:ZHENGZHOU HOUYI PHARMA

Method for determining content of tiamulin and valnemulin in veterinary drug preparation through solid phase extraction-high performance liquid chromatography-tandem mass spectrometry

The invention provides a method for determining the content of tiamulin and valnemulin in a veterinary drug preparation through solid phase extraction-high performance liquid chromatography-tandem mass spectrometry, and belongs to the technical field of drug detection. The invention provides a method for rapidly detecting tiamulin and valnemulin in a veterinary drug preparation through solid phase extraction/high performance liquid chromatography-tandem mass spectrometry. The method comprises the following steps: extracting a sample by using acetonitrile, purifying by using an MCX solid-phase extraction column, carrying out gradient elution on a C18 chromatographic column by using acetonitrile and a 0.1% formic acid aqueous solution as a mobile phase, and carrying out quantitative analysis in a liquid chromatography-tandem mass spectrometry MRM mode. The linear relation of the two detected compounds in the range of 1.0-100 ng/mL is good, the correlation coefficient is larger than 0.999, the detection limit of the method is 0.05 mg/kg, and the quantitation limit is 0.1 mg/kg. The method provided by the invention is simple, rapid and accurate, and can realize rapid determination of the veterinary drug preparation.
Owner:石家庄海关技术中心
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