3 results about "Cefotaxime Sodium" patented technology

The application discloses a long-acting and stable drug-releasing cefotaxime sodium preparation and a preparation method and application thereof, relates to the technical field of drug synthesis, and the cefotaxime sodium preparation comprises cefotaxime sodium tablet crystals, and a slow-release carrier is coated outside the cefotaxime sodium tablet crystals; the slow-release carrier has a three-level structure, comprising a phospholipid coating layer coated on the surface of the cefotaxime sodium tablet crystals, a mesoporous silica shell layer coated on the surface of the phospholipid coating layer, and a temperature-sensitive hydrogel network layer coated on the surface of the mesoporous silica shell layer. The cefotaxime sodium preparation has the properties of rapid effect, super-long-acting and stable drug-releasing and high stability, and the preparation process flow is simple, and the control condition is mild.

The invention belongs to the technical field of chemical synthesis, and discloses a cefotaxime sodium synthesis method based on one-step salification of a mixed solvent system and sodium isooctanoate. The method comprises the following steps: by taking 7-aminocephalosporanic acid (7-ACA) and 2-(2-aminothiazole-4-yl)-2-(methoxyimino) acetoxyimino ethyl acetate (AE active ester) as raw materials, in a dichloromethane-methanol mixed solvent, completing a condensation reaction through triethylamine catalysis, directly dropwise adding a sodium isooctanoate acetone solution to realize salification in one step, and carrying out post-treatment to obtain the 7-aminocephalosporanic acid (7-ACA)-2-(methoxyimino) acetoxyimino ethyl acetate (AE active ester)-2-(methoxyimino) acetoxyimino ethyl acetate (AE active ester). The cefotaxime acid intermediate does not need to be separated; and performing low-temperature washing and accurate drying subsequently to obtain a cefotaxime sodium finished product. According to the method, the defects that in the prior art, a two-step method needs intermediate separation and a one-pot method needs alkaline degradation are overcome, the production period is shortened to be smaller than or equal to 8 h, the total yield is larger than or equal to 92%, the HPLC purity is larger than or equal to 99.6%, the wastewater COD is smaller than or equal to 2000 mg / L, solvent residues meet the ICH Q3C standard, and the method has the advantages of industrial feasibility and environmental protection.

This invention relates to the field of biomedical technology, and in particular to the application of TarA inhibitors in the preparation of antibacterial potentiators for enhancing the efficacy of β-lactam antibiotics against methicillin-resistant Staphylococcus aureus (MRSA) infections. Through virtual screening, target validation, and in vitro and in vivo pharmacodynamic experiments, this invention confirms that the natural product norzelamin is an effective TarA inhibitor and antibacterial potentiator. Experiments show that norzelamin has a synergistic effect when used in combination with various β-lactam antibiotics. In a mouse model of MRSA-infected pneumonia, the combination of norzelamin and cefotaxime sodium significantly reduced pulmonary bacterial load, alleviated systemic inflammatory response, and improved lung tissue pathological damage compared to monotherapy. This invention provides a novel synergistic treatment strategy and candidate compound for overcoming MRSA resistance in clinical practice, and has significant development value and application prospects.