41 results about "Gamithromycin" patented technology

The invention discloses a gamithromycin injection and a preparation method thereof. The gamithromycin injection is prepared from the components including gamithromycin, a cosolvent, an antioxidant and water for injection, and is characterized by comprising 5-35 g of gamithromycin, 1-15 ml of the cosolvent, 0.1-0.5 g of the antioxidant and the balance of water for injection in every 100 ml injection. The preparation method comprises the steps as follows: dissolving the cosolvent in the water for injection, continuously adding gamithromycin and stirring to enable the gamithromycin to be dissolved, then adding the antioxidant to adjust pH to be 4.0-6.0, filtering and sterilizing, so that the gamithromycin injection is obtained. The gamithromycin injection is stable in properties, fast in absorption, remarkable in effect and simple in the preparation method, has less irritation to an injection part, effectively solves the problem that the gamithromycin is indissolvable in water, and meets the requirement of mass industrial production.

The present invention relates to methods for synthesizing macrolide compounds which are known to have antibacterial activity, and are useful in the therapy of bacterial infections in mammals. More specifically, the invention relates to methods for synthesizing the macrolide antibiotic, gamithromycin utilizing a novel configuration of catalysts, chemical structures, and / or methods. An embodiment of the present invention may include allowing multiple chemical reactions to proceed without the isolation of chemical intermediates. Thus, multiple reactions may occur in one reaction vessel allowing for a considerable decrease in the cycle-time. The present invention also provides a novel method for inhibiting degradation while isolating a structure of a pharmaceutical composition.

The present invention relates to a preparation method of a gamithromycin intermediate, which uses 9-deoxy-6-deoxy-6,9-imino ether-(8a-aza-8a)-erythromycin A as a raw material, Dissolve in an organic solvent, adjust the pH to 3~6 with an acid, and use potassium borohydride or sodium borohydride as a reducing agent to perform a reduction reaction; then add an organic sugar acid to perform a hydrolysis reaction to obtain 9‑deoxy‑8a‑aza ‑8a‑homotype erythromycin A, because the organic sugar acid contains hydroxyl group, which is beneficial to the hydrolysis of gamimycin borate intermediate, the acid degradation products are reduced, and it can effectively reduce 9‑deoxy‑6‑deoxy‑6,9‑sub Amino ether-(8a-aza-8a)-erythromycin A was hydrolyzed, which increased the yield of the target product and significantly reduced the 9-deoxy-8a-aza-8a-homoerythromycin A The preparation cost is convenient for industrialized production.

The invention discloses a gamithromycin composition lyophilized powder for injection. The gamithromycin composition lyophilized powder contains gamithromycin serving as an active ingredient and pharmaceutical excipients, the pharmaceutical excipients are at least one of citric acid, L-malic acid, tartaric acid and succinic acid, the weight ratio of the active ingredient and the pharmaceutical excipients is 1:0.27-0.65, and the pH value of a solution is adjusted to be 5.5-6.0 by using sodium hydroxide before lyophilizing. The invention further provides a preparation method of the gamithromycin composition lyophilized powder for injection. By the method, sterile gamithromycin composition lyophilized powder can be prepared; during clinic use, the gamithromycin composition lyophilized powder is dissolved in sterile normal saline, the solution is small in viscosity, easy for suction and easy for injection, and the gamithromycin composition lyophilized powder is simple and convenient in clinic use and small in irritancy to animals. Consequently, stability, safety and convenience in use of gamithromycin for injection are improved.

The invention discloses a hybridoma cell line secreting gamimycin monoclonal antibody and its application, belonging to the field of food safety immunoassay. The hybridoma cell line ABC11 secreting gamimycin monoclonal antibody of the present invention has been deposited in the General Microbiology Center CGMCC of the China Microbiological Culture Collection Management Committee, with a storage date of November 28, 2019, and a storage number of CGMCC No.19167. The gamimycin monoclonal antibody secreted by the strain is used for the analysis and detection of gamimycin residues in food safety testing. The garamimycin monoclonal antibody cell line obtained by the present invention can be used for immunoassay detection, and it has better detection sensitivity and specificity (IC 50 The value is 0.82ng / mL, less than 10% crossover to gamithromycin analogues, crossover rate=(IC of gamithromycin 50 / analogue IC 50 )×100%).

The invention discloses a preparation method of gamithromycin or a 13-descladinosylation compound serving as a precursor of gamithromycin, belonging to the field of chemical synthesis. The method comprises the steps of adding a reaction substrate and a solvent into a high-pressure kettle, wherein the reaction substrate is gamithromycin or the precursor thereof, and the solvent is low-grade amide, low-grade ketone or low-grade alcohol; adding acid, and controlling the pH value of a reaction system at 0.5-5; introducing nitrogen gas to the high-pressure kettle, and keeping the pressure at 0.1-0.8Mpa; and controlling the reaction temperature at 0-35 DEG C and stirring for 1-12 hours. The preparation method is simple in process and high in selectivity, and the yield of gamithromycin or the 13-descladinosylation compound serving as the precursor of gamithromycin is high. Gamithromycin or the precursor thereof contains hydroxyls, ester groups and a plurality of ether bonds; and the reaction substrate of gamithromycin and the precursor thereof in the method disclosed by the invention selectively breaks the ether bonds at the juncture of cladinose and a matrix under an acid condition, but the hydroxyls and the ester groups are unchanged under the reaction condition, so that the selectivity is high.

The invention discloses a gamimycin injection and a preparation method thereof. The gamimycin injection is composed of gamimycin, vitamin C and water for injection, wherein every 100ml of the solution contains 5-35 g of gamimycin , vitamin C 1~10g, all the other are water for injection; Gamithromycin injection of the present invention uses vitamin C to improve the dissolving speed of gamimycin bulk drug, has increased the solubility of gamimycin bulk drug, and vitamin C not only It has a good solubilizing effect, and also has anti-oxidation effect, which can improve the stability of the product; the gamimycin injection of the present invention is a weakly acidic aqueous phase injection, which can be used in compatibility with most drugs, greatly increasing the Gamithromycin has stable properties after long-term storage, has little irritation to the injection site, fast absorption, remarkable effect, high safety, simple prescription, convenient quality control of raw and auxiliary materials, cost saving, and is suitable for industrial production.

The invention discloses a method for synthesizing gamithromycin, which uses 9-deoxy-8a-aza-8a-homoerythromycin A as a raw material, and diaces with propionaldehyde in a protic solvent under the catalysis of an organic acid. Alcohol reaction forms propyral 9-deoxy-8a-aza-8a-homoerythromycin A, then reduces through boron reducing agent, removes protecting group under acidic conditions, obtains gamithromycin; preparation process of the present invention The yield of the obtained gamithromycin product can reach more than 92.0% before post-treatment, after recrystallization treatment, its purity can reach more than 99.0%, the overall yield can reach more than 90.0%, and the reaction process is mild, Able to realize industrialized mass production.