61 results about "Rifamycins" patented technology

The invention relates to application of kelimycin in mycobacterium tuberculosis infection resistance. The application comprises the following main steps: clinical first-line antitubercular drugs isoniazide and rifamycin are used as contrast, and the antimycobacterial activity of kelimycin is detected by adopting an absolute concentration method. The result indicates that the activity of kelimycin on clinically separated mycobacterium tuberculosis including drug-resistance bacteria is remarkably superior to those of the clinical first-line contrast drugs isoniazide and rifamycin, and novel application of kelimycin is expected to be developed in treatment of tubercle bacillus infected diseases.

It has been determined that co-administration of a rifamycin and a switch-region inhibitor 1) results in synergistic antibacterial effects, enabling efficacy at low, subtoxic doses, and/or 2) results in a low spontaneous resistance frequency, enabling treatment of high-titer infections without treatment failure due to spontaneous resistance. Accordingly, certain embodiments provide composition comprising a rifamycin and a switch region inhibitor, as well as methods of use thereof.

The invention belongs to the field of veterinary medicine, and particularly relates to a compound rifaximin dry suspension for preventing and treating the endometritis of livestock and a preparation method for the same. The rifaximin and sodium new houttuyfonate dry suspension is obtained by using rifaximin and sodium new houttuyfonate as active ingredients, and preparing with pharmaceutically acceptable auxiliary materials. The preparation method comprises the following steps of: performing superfine crushing treatment on raw materials at first; uniformly mixing the treated rifaximin and sodium new houttuyfonate with right amount of filler, suspending aid, surfactant, lubricant, adsorbent and pH buffer according to an equivalent incremental mixing method; subpackaging and sterilizing for1 hour by flowing steam at 100 DEG C. Rifaximin is a novel rifamycin board-spectrum semisynthetic antibiotic medicine, with the advantages of board-spectrum antibacterium, antitoxin and the like, andcapable of preventing and treating the endometritis of dairy cow well; and sodium new houttuyfonate is antibacterial, anti-inflammatory and capable of enhancing immunity as well as resisting bacteriaand diminishing inflammation by cooperating with rifaximin, and has great effect of preventing and treating the endometritis of dairy cow.

The invention discloses a viscous soda type saline-alkali soil modifier and a process for applying the modifier to modification of saline-alkali soil. The modifier is prepared from the following materials in parts by weight: coarse sand, rifamycin fermented filter residue obtained after innocent treatment, superphosphate, ferrous sulfate, aluminum sulfate and glucosamine hydrochloride. The viscoussoda type saline-alkali soil modifier is suitable for viscous soda type saline-alkali soil, can effectively reduce the pH value and degree of alkalization of soil and improve the character of the viscous soil, and is rich in material source; crops after modification of 2-3 years can reach the level of middle-output fields; especially by using rifamycin fermented filter residue, waste is changed into wealth, so that the increasingly severe environment problem can be solved. The viscous soda type saline-alkali soil modifier fundamentally improves the character of the viscous soil by adopting the coarse sand, and can improve the porosity and permeability and increase water penetration.

A process for treating a patient with leukemia or an aplastic anemia having cells with inclusions that stain with anti-E. canis antibodies or antibodies to other Ehrlichia or Anaplasma is disclosed. That process comprises administering to the patient (i) an antibacterial amount of a rifamycin, (ii) an antibacterial amount of a quinolone, or a mixture of (i) and (ii).

The invention relates to a preparation method for a rifamycin S derivative. According to the preparation method, 3-amino-4-imine rifamycin S as shown in a formula II which is described in the specification and a 4-piperidone derivative as shown in a formula III which is described in the specification are added according to a certain feeding mode and subjected to a condensation reaction in the presence of an organic solvent, ammonium acetate and zinc dust so as to produce the rifamycin S derivative as shown in a formula I which is described in the specification. The feeding mode is that the 3-amino-4-imine rifamycin S is added into a reaction system in a final step, so 3-amino-4-imine rifamycin S is prevented from reduction and hydrolysis. The preparation method increases the utilization rate of materials and is shortened in reaction time, so high-efficiency high-yield preparation of the rifamycin S derivative is realized, and the yield and content of the rifamycin S derivative reach 80% or above and 95% or above, respectively; and the preparation method overcomes the problems of long reaction time, low yield, many impurities and high cost, and is simple to operate, highly efficient, environment friendly and beneficial for large-scale production.

The invention provides a preparation method of high-purity rifapentine, which is characterized by comprising the following steps: 1. carrying out a cyclization reaction on rifamycin S acid, acid and dimethyloltert-butylamine in an N, N-dimethylformamide solvent; 2, pouring the reaction solution into acid water, standing, and filtering to obtain a rifaxizine filter cake; 3, adding urea, n-butyl alcohol, Vc and sodium carbonate into the rifaxizine filter cake for a ring-opening reaction; 4, after the reaction is completed, increasing the purity to 1-amino-4-cyclopentylpiperazine for a condensation reaction until the reaction is completed so as to obtain a rifapentine reaction solution; and step 5, dropwise adding acid water into the rifapentine reaction solution, stirring, stopping heating after crystallization, lowering the rotating speed after turning red, cooling after dropwise adding is finished, filtering to obtain the filter cake, and carrying out secondary recrystallization on thefilter cake. According to the preparation method of the high-purity rifapentine, provided by the invention, the maximum single impurity of the rifapentine can be controlled within 0.1%, and the residual n-butyl alcohol and the residual ethanol can be controlled within 0.5%.

The invention belongs to the field of analytical chemistry, and particularly relates to a method for separating and determining 3-amino-4-imino rifamycin S and related impurities. A chromatographic column adopted in the method takes octadecylsilane chemically bonded silica as a filler, a mobile phase A and a mobile phase B are adopted for gradient elution, and a detector is entered for detection; the related impurities comprise one or more of 3-amino rifamycin S, 3-bromo rifamycin S, rifamycin S, an impurity A, an impurity B, an impurity C and an impurity D; the mobile phase A is acetonitrile and methanol; and the mobile phase B is a phosphate buffer solution. According to the method disclosed by the invention, the 3-amino rifamycin S, the 3-bromo rifamycin S, the rifamycin S, the impurity A, the impurity B, the impurity C and the impurity D can be simultaneously separated and determined; and the quality of the 3-amino-4-imino rifamycin S bulk drug can be accurately controlled, and the safety and effectiveness of the product are finally ensured.

The invention discloses a method for continuously preparing benzoxazine rifamycin. The method comprises the following steps: 1) dissolving rifamycin S into an organic solvent, performing filtering soas to obtain a homogeneous solution of rifamycin S; 2) dissolving dihydroxymethyl tert-butylamine into an organic solvent, and performing sufficient mixing so as to obtain a homogeneous solution of dihydroxymethyl tert-butylamine; 3) continuously pumping the two homogeneous solutions obtained in steps 1) and 2) into a micro-reactor for mixing, enabling the mixed materials to react in a second reactor of the micro-reactor so as to obtain a product benzoxazine rifamycin; and 4) performing aftertreatment on samples, and performing external standard quantitative analysis on the samples by using ahigh performance liquid chromatography method, so as to obtain the content of benzoxazine rifamycin in the samples. By adopting the method disclosed by the invention, the characteristics of efficientmass transfer and heat transfer of the micro-reactor are utilized, and with optimized reaction parameters, the reaction time can be shortened to 30 minutes, and the product yield is 95% or greater.

The invention relates to a process method for synthesizing rifampicin, wherein the process method mainly comprises the steps: by using rifamycin S as a raw material, carrying out cyclization reactionto obtain a rifamycin oxazine-containing solution, and carrying out solventing-out crystallization on the rifamycin oxazine-containing solution to obtain a rifamycin oxazine crude product; carrying out condensation reaction on the crude rifamycin oxazine product and 1-amino-4-methylpiperazine to obtain a reaction solution containing rifampicin; and cooling and crystallizing the reaction solution containing rifampicin to obtain a rifampicin product. Compared with the prior art, the method has the advantages that the reaction steps are few, the product yield is high, the reaction raw material cost is low, meanwhile, the production is more environmentally friendly, the consumption of raw materials is reduced by 30% (the consumption of dimethylol tert-butylamine required by every 1 kg of rifamycin S is reduced by about 28%, and the consumption of 1-amino-4-methylpiperazine is reduced by about 30%). The method overcomes the defect that a large amount of sewage is generated in production byadopting an elution method, and reduces the influence of impure reaction products on the yield due to the fact that rifamycin S-Na is used as a raw material.

The present invention relates to novel pyrido-imidazo rifamycins, characterized by a highly selective antibacterial activity and low absorption by oral route.