2 results about "Cinoxacine" patented technology

The invention discloses a preparation method of a moxifloxacin hydrochloride intermediate with high yield, high purity and low cost, and aims to overcome the technical defects of low resolution yield, need of additional acid addition, single solvent system, complex resolution agent recovery process and limited salifying efficiency in the prior art. According to the method, cis-8-benzyl-7, 9-dioxo-2, 8-diazabicyclo [4.3. 0] nonane (a compound as shown in a formula I) is taken as a raw material, N-acetylphenylalanine (including L-type and D-type) is taken as a resolving agent, acid does not need to be additionally added in a water-alcohol-ester ternary solvent system, efficient resolution of the enantiomer is directly realized through a salt forming reaction, and the yield of the enantiomer is increased. And the high-purity diazabicyclo compounds shown in the formulas IIIa and IIIb can be obtained without a refining step. The resolution yield can reach 90% or above, the recovery process of the resolving agent is simple and efficient, the recovery rate is larger than or equal to 95%, the resolving agent can be stably and circularly applied for five times or above, the resolution yield is still larger than or equal to 90% after the resolving agent is applied, the comprehensive production cost is reduced by 40%-60% compared with the prior art, and the method has outstanding industrial application advantages.

The present application relates to the field of ophthalmic drugs, and particularly relates to an ophthalmic composition, a preparation method and application thereof, the ophthalmic composition comprising a compound as shown in formula I, an osmotic pressure regulator, a pH regulator and water for injection; the pH value of the ophthalmic composition is 4.0-6.0; the concentration of the compound as shown in formula I is 0.1-3.0% w / v, and the concentration of the osmotic pressure regulator is 0.3-10.0% w / v; the antibacterial activity against Streptococcus pneumoniae, Staphylococcus aureus and Staphylococcus epidermidis is 2-8 times that of levofloxacin and moxifloxacin hydrochloride; the antibacterial activity against Haemophilus influenzae, Moraxella catarrhalis, Escherichia coli and Pseudomonas aeruginosa is also strong, and is equivalent to that of levofloxacin and moxifloxacin hydrochloride; the irritation is small, the light stability and high-temperature stability are good, the quality and drug safety are guaranteed, and the application value is good.