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35 results about "P-Aminosalicylic Acid" patented technology

Aminosalicylic acid is rapidly degraded in acid media; the protective acid-resistant outer coating is rapidly dissolved in neutral media so a mildly acidic food such as orange, apple or tomato juice, yogurt or apple sauce should be used. Aminosalicylic acid (p-aminosalicylic acid) is 4-Amino-2-hydroxybenzoic acid.

Method for separating and determining p-aminosalicylic acid and relevant impurities in LC-MSMS method

The invention belongs to the field of pharmaceutical chemistry, and particularly relates to a method for separating and determining p-aminosalicylic acid and relevant impurities in an LC-MSMS method.A chromatographic column adopted in the method adopts octylsilane bonded silicon gel as stuffing, adopts an acetic acid aqueous solution and an acetonitrile aqueous solution as mobile phases to perform the gradient elution, and performs the detection in a tandem mass spectrum detector; and the relevant impurities comprise m-nitrobenzenesulfonic acid and m-aminobenzenesulfonic acid. The method cansimultaneously detect the content of the m-nitrobenzenesulfonic acid and m-aminobenzenesulfonic acid in the p-aminosalicylic acid, and by screening the type of the mobile phase, optimizing the gradient of the mobile phase and selecting the chromatographic column, the interference on the p-aminosalicylic acid on the m-nitrobenzenesulfonic acid and m-aminobenzenesulfonic acid can be eliminated, so that the recovery rate with limit input is greater than 95 percent, and the detection limit reaches up to 0.4 ng / ml.
Owner:CHONGQING HUABANGSHENGKAI PHARM

Method for synthesizing pasiniazide

The present invention uses water or low-grade alcohol with a certain concentration as solvent, dissolves the isoniazid in the above-mentioned solvent, then adds the p-aminosalicylic acid, and adopts the processes of heating, stirring, cooling and separation so as to obtain the invented product pasiniazide.
Owner:张之君

Preparation method for solid dispersions

A method of preparation of a solid dispersion of a polyvinyl alcohol-polyethylene glycol graft copolymer (PVA-PEG graft co-polymer), such as Kollicoat IR with a BCS Class II drug or a BCS Class IV drug, whereby the method comprises: a) dissolving the polyvinyl alcohol-polyethylene glycol graft copolymer (PVA-PEG graft co-polymer) separately in a water / first alcohol mixture; and b) dissolving the BCS Class II drug or a BCS Class IV drug, in a mixture of a second alcohol with a non alcoholic organic solvent in which the compound has an high solubility; and c) mixing the both solutions to obtain a third solution with a total amount of solved solid of 1 to 15 g per 100 ml, and optionally having an acid, including inorganic acids including hydrohalic acids, e.g. hydrochloric or hydrobromic acid; sulfuric; nitric; phosphoric and the like acids; or organic acids including acetic, propanoic, hydroxyacetic, lactic, pyruvic, oxalic, malonic, succinic, maleic, fumaric, malic, tartaric, citric, methane-sulfonic, ethanesulfonic, benzenesulfonic, p-toluenesulfonic, cyclamic, salicylic, p-aminosalicylic, palmoic and the like acids in the mixture of both the solutions to achieve an acid pH; and d) spray drying the third solution.
Owner:FORMAC PHARMA

Method for detecting anti-tuberculosis drug in serum by ultra-high performance liquid chromatography-tandem mass spectrometry technology

The invention discloses a method for detecting an anti-tuberculosis drug in serum by an ultra-high performance liquid chromatography-tandem mass spectrometry technology. The antitubercular drug comprises cycloserine (CYS), pyrazinamide (PZN), isoniazid (INZ), p-aminosalicylic acid (P-ASA), ethiisonicotinamide (ETN), ethambutol (ETB), clofazimine (CFM), bedaquiline (BDQ), rifampicin (RFP), rifbutine (RFB) and rifapentine (RFT). The method includes: detecting the content of the antituberculosis drug in the pretreated serum by adopting an ultra-high performance liquid chromatography-tandem mass spectrometry method, performing quantifying by utilizing a mass spectrometry isotope internal standard method, establishing a calibration curve by taking the concentration ratio of the standard substance to the internal standard substance as an X axis and the peak area ratio of the standard substance to the internal standard substance as a Y axis, and calculating the concentration of the target drug in the serum; the method is high in sensitivity, strong in specificity and simple in pretreatment process, separation and detection of the anti-tuberculosis drugs in serum are completed within 5 min, and a simple and rapid detection method is provided for clinical concentration monitoring of the anti-tuberculosis drugs.
Owner:南京品生医学检验实验室有限公司

Construction method and application of recombinant drug-resistant BCG strain

The invention discloses a construction method and application of a recombinant drug-resistant BCG strain, M.bovis BCG is used as an original bacterium to construct a drug-resistant BCG strain with resistance to at least one of streptomycin, levofloxacin, ethambutol, protionamide, p-aminosalicylic acid and amikacin; and sequence fragments capable of expressing related antigens Ag85b and Rv2628 causing immune response can be further inserted to construct a recombinant drug-resistant BCG strain. The recombinant drug-resistant BCG strain can compete with Mtb in growth to accelerate death of the Mtb, and when the recombinant drug-resistant BCG strain is combined with a drug for treating tuberculosis, the treatment effect on Mtb (sensitive Mtb and drug-resistant Mtb) can be further enhanced, re-infection of a patient can be avoided, and an important medical prospect is achieved.
Owner:GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI

P-aminosalicylic acid fluoroquinolone derivative as well as intermediate, preparation method and application thereof

The invention discloses a p-aminosalicylic acid fluoroquinolone derivative and an intermediate, a preparation method and application thereof, and belongs to the technical field of drug synthesis. Thestructural formula of the p-aminosalicylic acid fluoroquinolone derivative is shown in the specification. In-vitro activity determination results show that part of fluoroquinolone aminosalicylate derivatives (compounds for short) and intermediates have inhibition effects on mycobacterium smegmatis; the compounds and intermediates have good inhibition activity on common pathogenic bacteria as a whole; most compounds and intermediates have better antibacterial activity on pichia pastoris as a whole; part of the compounds have good inhibitory activity on citrus canker pathogens. The p-aminosalicylic acid fluoroquinolone derivative and the intermediate thereof have potential application prospects in the fields of tuberculosis resistance, bacteria resistance, fungus resistance and citrus pathogen resistance.
Owner:SOUTHWEST UNIVERSITY

Preparation method of 4-amino-2-sulfonic benzoic acid

The invention discloses a preparation method of 4-amino-2-sulfonic benzoic acid, and belongs to the preparation technology of aromatic sulfonic acid. The process of the method comprises the following steps: dissolving raw materials of p-nitrotoluene o-sodium sulfonate, 4-nitro-2- sodium sulfonate benzaldehyde, 4,4'-dinitro diphenylethane-2,2'-disodium disulfonate or 4,4'-dinitro diphenylethene-2,2'-disodium disulfonate in a sodium hydroxide solution, performing oxidation with pressurized air, performing reduction with iron powder, performing filtration and crystallization to obtain 4-amino-2-sulfonic benzoic acid. The invention has a simple process, high yield and purity, and the product 4-amino-2-sulfonic benzoic acid can be prepared into p-aminosalicylic acid through simple alkali fusion technology with high yield and high product purity.
Owner:TIANJIN UNIV +1

Medicine used for treating recurrent pulmonary tuberculosis

InactiveCN103006673AShorten the duration of treatmentHigh cure rateAntibacterial agentsOrganic active ingredientsRifabutinPyrazine
The invention provides a medicine used for treating recurrent pulmonary tuberculosis. The medicine comprises, by weight, 5-12 parts of moxifloxacin, 18-24 parts of p-aminobenzoic isoniazid salicylate, 5-12 parts of rifabutin, 36-45 parts of pyrazinamide, and 18-24 parts of ethambutol. As a result of clinical verification, with the recurrent pulmonary tuberculosis medicine provided by the invention, recurrent pulmonary tuberculosis treatment period can be shortened, and a cure rate can be greatly improved.
Owner:SHANGHAI PULMONARY HOSPITAL

Novel crystal form of p-aminosalicylic acid as well as preparation method and applications thereof

The invention relates to the field of pharmaceutical chemistry, in particular to a novel crystal form of p-aminosalicylic acid and a preparation method thereof. A crystal in the novel crystal form is subjected to X-ray powder diffraction, diffraction peak positions 2theta are used as spectrogram characteristic parameters, and 2theta are 7.36+ / -0.2, 14.61+ / -0.2, 17.01+ / -0.2, 21.91+ / -0.2 and 29.28+ / -0.2 sequentially. The preparation of the crystal comprises steps of mixing p-aminosalicylic acid and an organic solvent, then utilizing a temperature differential method for crystallization, carrying out solid-liquid separation, drying solid, and obtaining the crystal in the novel crystal form. The invention further relates to preparations or compositions containing the novel crystal form, and applications of the novel crystal form to preparations of drugs for treating tuberculosis. The novel crystal form of p-aminosalicylic acid is good in stability, and not only has storage and transportation advantages, but also greatly facilitates industrial production.
Owner:CHONGQING HUAPONT PHARMA

Preparation method of modified lignin-sulfonate aliphatic water reducer

The invention discloses a preparation method of a modified lignin-sulfonate aliphatic water reducer. The preparation method comprises the steps that certain pH and temperature of black liquor are controlled, and an oxidizing agent and a catalyst are added to prepare alkali lignin; a mixture of water, the alkali lignin, a ketone compound and p-aminosalicylic acid and 3-carboxyl sodium benzenesulfonate are added into a reaction container, a pH value is controlled, and then a aldehyde compound is added in a dropwise way to prepare the modified lignin-sulfonate aliphatic water reducer. The produced water reducer has the advantages of being low in water reducing rate, obvious in concrete reinforcement effect, small in slumping loss, good in dispersion adhesiveness, freezing resistance, seepageresistance and heat resistance, free of crystals at low temperature and not prone to steel bar corrosion when being used with concrete, the operation method is simple, the reaction time is short, andthe production efficiency is high.
Owner:王颖皓

Preparation method of ethopabate

InactiveCN107540568ALow costReduce transit lossOrganic compound preparationCarboxylic acid amides preparationSodium acetatePara-aminosalicylic acid
The invention discloses a preparation method of ethopabate. Initially, para-aminosalicylic acid and p-toluene sulfonic acid are dissolved in methanol to form a mixed solution, the mixed solution is put in a reaction bottle, evenly stirred and heated, and a thermal insulation reaction is carried out; sodium acetate is added into a methyl p-aminosalicylate reaction liquid, the pH and temperature ofthe reaction liquid are controlled, acetylase is added, and a reaction is carried out to obtain methyl p-acetaminosalicylate; methyl p-acetaminosalicylate is added into acetone, heating is carried out, diethyl sulfate is added dropwisely, and after adding dropwisely is completed, a reaction is carried out to obtain ethopabate. The method has the advantages that industrial production can be achieved, resource conservation and environmental protection can be achieved, the cost can be better saved, the product quality is stable, the yield is high, and the method is suitable for large-scale industrial stable production.
Owner:XUCHANG HENGSHENG PHARMA

Industrial production method of m-phthalic acid derivatives

The invention discloses an industrial production method of a compound represented by the formula I. The method comprises the following steps: taking p-aminosalicylic acid, potassium salts, and carbon dioxide as the raw materials, and carrying out reactions in melted potassium formate so as to introduce carboxyl groups into a multi-substituted benzene ring under mild conditions. Compared to the prior art, the provided method is carried out under a normal pressure, thus the production operation is safe, furthermore, pricy high-pressure reactor is not required, and the cost is reduced. While the reaction pressure is reduced, the reaction time is not increased, and the reaction time is greatly reduced instead.
Owner:CHONGQING HUAPONT PHARMA

Preparation method of p-aminosalicylic acid

A preparation method of p-aminosalicylic acid comprises the following steps: adding sodium p-aminosalicylate dihydrate into a mixed phase of water and an organic solvent, wherein the organic solvent comprises lower alcohol; and adding an antioxidant and a complexing agent, stirring, adding an acid solution to adjust the pH value to 2.5-4.0, filtering, washing and drying. According to the preparation method of the p-aminosalicylic acid, the sodium p-aminosalicylate dihydrate is taken as a raw material, the sodium salt is converted into organic acid by adding acid, and the water and the mixed organic solvent are taken as solvents, so that a high-density crystal habit and high-purity product is favorably generated, the suction filtration and drying time of the product is shortened, and the preparation efficiency of the product is improved; the p-aminosalicylic acid is prepared by a one-step method, the process steps are few, and the yield is high; and heating is not needed in the whole process to avoid heating oxidation of the p-aminosalicylic acid to generate impurities.
Owner:广药白云山化学制药(珠海)有限公司 +1

P-aminosalicylic acid dihydroartemisinin derivative as well as preparation method and application thereof

The invention discloses a p-aminosalicylic acid dihydroartemisinin derivative as well as a preparation method and application thereof, and belongs to the technical field of drug synthesis. The structural formula of the p-aminosalicylic acid dihydroartemisinin derivative is shown in the specification. An in-vitro antibacterial activity determination result shows that the overall antibacterial activity of the target compound is relatively good; an in-vitro antifungal activity determination result shows that the target compound has good antibacterial activity on pichia pastoris as a whole; citruspathogen resistance activity determination results show that the compound has inhibitory activity on colletotrichum gloeosporioides, citrus brown blotch bacteria and citrus canker pathogens; the anti-mycobacterium smegmatis activity determination result shows that the inhibition activity of the intermediates IM1'and IM2 'is very good. Therefore, it is proved that the p-aminosalicylic acid dihydroartemisinin derivative and the intermediate thereof have potential application prospects in the fields of bacterium resistance, fungus resistance, citrus pathogen resistance and tuberculosis resistance.
Owner:SOUTHWEST UNIVERSITY

A kind of preparation method of isoniazid p-aminosalicylate

The invention relates to a preparation method of isoniazid para-aminosalicylate. The preparation method of isoniazid para-aminosalicylate comprises the following steps: (1) respectively weighting water and an organic solvent, mixing, adding para-aminosalicylic acid and isoniazid to a solvent of the water and the organic solvent, heating and stirring; (2) cooling and growing grains, and filtering to obtain isoniazid para-aminosalicylate, wherein the organic solvent is an organic ester with the carbon number of less than or equal to 6. By using the preparation method, the preparation of isoniazid para-aminosalicylate is realized at low cost and high efficiency in a water and ester two-phase solvent system under a simple, convenient and feasible technological condition. The content of isoniazid para-aminosalicylate prepared by the method is higher than 99%. Isoniazid para-aminosalicylate has good appearance crystal form, standard color and luster and good stability. The preparation method has the advantages of few reaction operating units, simple technological process, short time consumption, low production cost, environmental friendliness, simple operation and easiness for control on the implementation process and is suitable for the industrial production of isoniazid para-aminosalicylate.
Owner:GUANGZHOU BAIYUNSHAN PHARM CO LTD

Method for separating and determining pasiniazide and related impurities thereof by HPLC method

The invention belongs to the field of analytical chemistry and particularly relates to a method for separating and determining pasiniazide and related impurities thereof by an HPLC method. According to the method, an adopted chromatographic column takes octadecylsilane chemically bonded silica as filler, a mobile phase A and a mobile phase B are adopted to carry out gradient elution, and detectionis carried out in a detector; related substances comprise isoniazide, p-aminosalicylic acid and related impurities; the related impurities are one or more of A to E; the mobile phase A is a phosphatebuffer solution, and the mobile phase B is methanol. The method provided by the invention can be used for simultaneously separating and determining the isoniazide, the p-aminosalicylic acid and the related impurities A to E in the pasiniazide, and the efficiency of separation detection is increased compared with the prior art; the controllable quality of pasiniazide raw pharmaceutical materials and preparations thereof can be more accurately ensured, and the product can be safe and effective finally.
Owner:CHONGQING HUAPONT PHARMA

P-aminosalicylic acid azole derivatives and preparation method and application thereof

The invention discloses p-aminosalicylic acid azole derivatives, a preparation method and application thereof, and belongs to the technical field of drug synthesis. The structural formula of the p-aminosalicylic acid azole derivatives is as follows. The antibacterial activity assay results show that the p-aminosalicylic acid azole derivatives of the present invention have good overall inhibitory activity against common pathogens, and the antibacterial activity of some molecules against Pichia pastoris is stronger than or equivalent to the positive drug fluconazole , all the molecules have good inhibitory activity against C. citrus anthracnose, some molecules have comparable or stronger inhibitory activity to the positive control prochloraz, and most of the molecules have good inhibitory effect on C. citrus canker. The anti-tumor cell activity assay results show that the p-aminosalicylic acid azole derivatives of the present invention have inhibitory effects on three tumor cells. The p-aminosalicylic acid azole derivatives of the present invention have potential application prospects in the fields of antibacterial, antifungal, anti-citrus pathogen and antitumor.
Owner:SOUTHWEST UNIV

Licorzinc solution composition, preparation process thereof and licorzinc preparation

The present invention relates to a licorzinc solution composition, including licorzinc, solvent and cosolvent, the zinc content in the licorzinc is 4.0-20.0%, the solvent is water or oil, and the cosolvent is one of the following substances: citric acid and its potassium salt, sodium salt and iron salt, tartaric acid and its potassium salt, sodium salt and iron salt; glucose and its potassium salt, sodium salt and iron salt and P-aminosalicylic acid and its potassium salt, sodium salt and iron salt, and the ratio of licorzinc and cosolvent is 1:0.4-1:1.5, and the concentration of said licorzinc solution is 0.01%-10%. Said invention can be made into several dosage forms, and can raise its biological utilization rate.
Owner:XIAN LIJUN PHARMA CO LTD

A kind of construction method and application of recombinant drug-resistant bcg strain

The invention discloses a method for constructing a recombinant drug-resistant BCG strain and its application. Using M.bovis BCG as the original bacterium, a strain containing streptomycin, levofloxacin, ethambutol, prothionamide, and p-aminosalicylic acid is constructed. and amikacin at least one resistant drug-resistant BCG strain; further insert the sequence fragments that can express the related antigens Ag85b and Rv2628 that can cause immune responses to construct a recombinant drug-resistant BCG strain; the recombinant drug-resistant BCG strain can be combined with Mtb competes for growth, thereby accelerating its death. Combined with drugs for the treatment of tuberculosis, it can further strengthen the therapeutic effect on Mtb (sensitive Mtb and drug-resistant Mtb), and can also prevent patients from reinfection, which has important medical prospects.
Owner:GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI

Aminosalicylic acid resistance diagnostic markers of Mycobacterium tuberculosis and its application

The invention discloses a diagnostic marker for drug resistance to aminosalicylic acid of Mycobacterium tuberculosis, which consists of Rv3890c, Rv2002, Rv1886c, Rv3824c, and Rv3825c. When the expression level is higher, it can be judged that Mycobacterium tuberculosis is resistant to p-aminosalicylic acid. The invention discloses a diagnostic marker for drug resistance to aminosalicylic acid of Mycobacterium tuberculosis, which can realize rapid clinical detection of whether Mycobacterium tuberculosis is resistant to aminosalicylic acid, and provides a method for treating drug resistance to aminosalicylic acid. potential target.
Owner:周琳

Graphene composite rubber for durable automobile wiper blade and preparation method for graphene composite rubber

The invention belongs to the field of new materials, and provides graphene composite rubber for a durable automobile wiper blade and a preparation method for the graphene composite rubber. The methodcomprises the following steps that p-aminosalicylic acid is added into a phosphate buffer solution, graphene oxide and a AlCl3 catalyst are added, ultrasonic treatment is carried out for 4 hours, heating is carried out to reach 60 DEG C, then an ascorbic acid reducing agent is added, ultrasonic treatment is carried out on low-molecular epoxy resin liquid for 30 minutes, cooling is carried out to reach room temperature so as to obtain a functionalized graphene / low molecular epoxy resin mixed solution, natural rubber (NR) is put into an open mill, and stearic acid, the prepared functionalized graphene / low molecular epoxy resin mixed solution, molybdenum disulfide, aromatic hydrocarbon oil, an accelerant TMTD and a cross-linking agent DCP and rest auxiliary agents are sequentially added, areuniformly mixed and then are taken out so as to obtain the graphene composite rubber.
Owner:CHENDU NEW KELI CHEM SCI CO LTD

Preparation method of 4-amino-2-sulfonic benzoic acid

The invention discloses a preparation method of 4-amino-2-sulfonic benzoic acid, and belongs to the preparation technology of aromatic sulfonic acid. The process of the method comprises the following steps: dissolving raw materials of p-nitrotoluene o-sodium sulfonate, 4-nitro-2- sodium sulfonate benzaldehyde, 4,4'-dinitro diphenylethane-2,2'-disodium disulfonate or 4,4'-dinitro diphenylethene-2,2'-disodium disulfonate in a sodium hydroxide solution, performing oxidation with pressurized air, performing reduction with iron powder, performing filtration and crystallization to obtain 4-amino-2-sulfonic benzoic acid. The invention has a simple process, high yield and purity, and the product 4-amino-2-sulfonic benzoic acid can be prepared into p-aminosalicylic acid through simple alkali fusion technology with high yield and high product purity.
Owner:TIANJIN UNIV +1

Preparation method of p-vinylsalicylic acid

The invention discloses a p-vinylsalicylic acid preparation method, which comprises: (1) carrying out a diazotization reaction on p-aminosalicylic acid and nitrous acid in water to generate a diazotization intermediate, and adding a metal iodide to carry out an iodination reaction to generate p-iodosalicylic acid; (2) reacting p-iodosalicylic acid with the compound shown in the formula (a) in a mixed solution of methanol and water to generate p-vinylsalicylic acid, wherein in the formula (a), R1, R2 and R3 are independently selected from C1-6 alkyl, C1-6 alkoxy, phenoxy, CH3 (CH2) mO (CH2) nO-, m is 0, 1, 2, 3, 4, 5 or 6, and n is 1, 2, 3, 4, 5 or 6; according to the method, ideal yield and purity can be obtained under mild and simple reaction conditions, side reactions are reduced, meanwhile, adopted reagent raw materials are cheaper and easier to obtain, and the method is safe, environmentally friendly and suitable for industrial large-scale production.
Owner:江苏美迪克化学品有限公司

Trimolecular conjugate taking p-aminosalicylic acid as mother nucleus, intermediate, preparation method and application

The invention discloses a trimolecular conjugate taking p-aminosalicylic acid (PAS) as a mother nucleus, which is shown in a formula I, wherein the trimolecular conjugate is formed by conjugating three structural units, namely PAS, isonicotinic acid and fluoroquinolone; anti-human pathogenic bacterium activity tests prove that the trimolecular conjugate synthesized by the invention has certain antibacterial activity, especially has a plurality of molecules with high antibacterial activity on mycobacterium tuberculosis, salmonella, pseudomonas aeruginosa and staphylococcus aureus, and meanwhile, hemolytic tests verify the safety of the molecules, so that the trimolecular conjugate can be used for preparing the antibacterial peptide. The polypeptide has the potential of further developing and researching antibacterial drugs, especially antituberculosis drugs.
Owner:SOUTHWEST UNIVERSITY

Para-aminosalicylic acid azole derivative as well as preparation method and application thereof

The invention discloses a para-aminosalicylic acid azole derivative as well as a preparation method and application thereof, and belongs to the technical field of drug synthesis. The structural formula of the para-aminosalicylic acid azole derivative is shown in the specifications. An antibacterial activity determination result shows that the para-aminosalicylic acid azole derivative disclosed bythe invention has good inhibition activity on common pathogenic bacteria as a whole, and the antibacterial activity of part of molecules on pichia pastoris is stronger than or equal to that of a positive drug, fluconazole; all the molecules have good inhibitory activity on colletotrichum gloeosporioides, part of the molecules have the inhibitory activity equal to or higher than that of positive control prochloraz, and most of the molecules have a good inhibitory effect on citrus canker pathogens. An anti-tumor cell activity determination result shows that the para-aminosalicylic acid azole derivative disclosed by the invention has an inhibition effect on the three kinds of tumor cells. The para-aminosalicylic acid azole derivative disclosed by the invention has a potential application prospect in the fields of bacterium resistance, fungus resistance, citrus pathogen resistance and tumor resistance.
Owner:SOUTHWEST UNIV
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