182 results about "Aminosalicylic acid" patented technology

The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention / treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention / treatment of colon cancer.

The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention / treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention / treatment of colon cancer.

There is disclosed herein a composition for treating gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers diarrhea, chronic idiopathic nausea, IBD-associated constipation and diarrhea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux oesophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinsons disease, MS, Alzheimers Disease, Motor Neurone Disease or autism, the composition comprising: (i) at least two anti-clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or (ii) at least one anti-clostridial agent selected from the above combined with an opioid blocking agent. There is also disclosed herein a method of treating various gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers diarrhea, chronic idiopathic nausea, IBD-associated constipation and diarrhea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux oesophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinsons disease, MS, Alzheimers Disease, Motor Neurone Disease or autism, the method comprising administering orally, via enema or by suppository: (i) a composition of the invention; (ii) at least two anti-clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or (iii) at least one anti-clostridial agent selected from the above and an opioid blocking agent to a patient in need of such treatment.

An object of the present invention is to provide a medicament efficacious for an inflammatory bowel disease such as ulcerative colitis or Crohn's disease. Specifically, it provides a therapeutic agent for inflammatory bowel diseases comprising active ingredient (a) consisting of at least one compound having inflammatory inhibiting activity selected from the group consisting of an aminosalicylic acid derivative, an antiinflammatory glucocorticoid, an immunosuppressive compound, an anti-TNFα antibody, a neurohypophysial hormone and an antiinfective compound, combined with active ingredient (b) consisting of at least one compound having PPARγ agonistic activity, wherein the agent is so configured that the compound (a) and the compound (b) are used simultaneously, separately or every scheduled time.

The present invention discloses a drug sustained and controlled release microparticle preparation for treating intestinal diseases. The preparation comprises: a pill core containing the drug, wherein the pill core contains 5-aminosalicylic acid and an assistant material; an isolation layer for providing a smooth and flat surface for the microparticle and preventing the drug from penetrating into a sustained release coating layer, wherein the penetration of the drug into the sustained release coating layer can affect the release effect, the used material of the isolation layer comprises one or a plurality of materials selected from a water-soluble polymer and an anti-adhesion agent; the sustained release coating layer for slowly releasing the drug, wherein different drug release levels can be achieved through adjusting the thickness of the sustained release coating layer, the used material of the sustained release coating layer mainly adopts a sustained-release material; an enteric-coating layer, the enteric-coating layer is provided for avoiding the early release of the drug in gastric juice, reducing stimulation of the main drug to stomach, increasing the local concentration of the drug in the lesion location, the used material of the enteric-coating layer mainly adopts a polymer enteric material. The invention further discloses a preparation method for the microparticle preparation. According to the present invention, the drug and the sustained release coating material are uniformly dispersed on the surface of the pellet, such that the problem of mixing uniformity of the assistant material and the main drug can be effectively solved.

Therapeutic 5-aminosalicylic acid derivative compositions having general formula (I), wherein R is a 1-deoxy sugar residue or a poly(ethylene glycol) chain-containing residue, are provided. The compositions enable topical delivery of 5-aminosalicylic acid to the gastrointestinal tract following oral administration in pharmaceutical preparations. According to the invention, the compositions stabilize pharmaceutical compositions containing therapeutic 5-aminosalicylic acid derivatives in a manner that enhances the retention of said compositions in the intestine, decreases the cellular absorption thereof, and decreases the transfer of said compositions or the 5-aminosalicylic acid derived therefrom to the systemic circulation

The invention discloses a prescription of targeted curcumin-polylactic acid-hydroxyacetic acid copolymer (PLGA) nanoparticles for treating ulcerative colitis and a preparation process thereof. The prescription uses the targeting characteristic of the nanoparticles to an inflammatory part to reduce a medicament administration dosage and side effect and improve treatment effect. The preparation process comprises the following steps: taking a biodegradable material PLGA as a carrier material, polyvinyl alcohol as an emulsifier and 2 to 5 percent cane sugar as a freeze-drying protective agent, adding PEG 6000 into a water phase, and preparing the curcumin-PLGA nanoparticles by an emulsion-solvent volatilization method. The prescription process is optimized by taking the grain sizes of the nanoparticles and a medicament-loading rate as indexes. The prepared nanoparticles are round or elliptic and uniform in the size, have a mean grain size of 20 to 800nm and the medicament-loading rate of 10 to 20 percent, reduce dumping effect and have obviously better treatment effect on an animal pattern than a 5-aminosalicylic acid control group.

The invention relates to an aminosalicylic acid derivative. The structure of the aminosalicylic acid derivative accords with the following general formula (I). At least one of R1, R2, R3 and R5 is -OH; when R1, R2, R3 and R5 are not -OH, R1, R2, R3 and R5 are -H, -OCH3, -F, -Cl, -Br, -CF3 or -NO3; R4 is -OCH3, -F, -Cl, -Br, -CF3 or -NO3; R6 and R7 are -COOH or -OH. When R6 is -COOH, R7 is -OH; when R6 is -OH, R7 is -COOH. In the invention, target compounds have strong protection function on PC12 cell injuries caused by glutamate. And the target compounds block the coupling between PSD-95 and nNOS by specificity to develop the pharmacological action.

The present invention is related to a novel process for the preparation of amisulpride (I) which involves: methylation of 4-amino-salicylic-acid (VI) with dimethyl sulphate and base, optionally in presence of TBAB to obtain 4-amino-2-methoxy methyl benzoate (VII) and (ii) oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) or 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) with oxidizing agent in the presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV) or 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) respectively.

The invention belongs to the technical field of fluorescence detection materials and discloses an enhanced fluorescent probe and a preparation method and application thereof. The fluorescent probe is 5-{4-[3-(2-{2-[2-(toluene-4-sulfamine)-ethyl]-1H-benzo(de)isoquinoline-1,3(2 H)-diketone-6-amino}-ethylamino)-propoxy]-phenylazo}-2-hydroxybenzoic acid and has a molecular structural formula shown in a formula (1). The probe compound is prepared from visible light excited and emitted fluorescent chromophore naphthalimides and an azo reductase recognition group 5-aminosalicylic acid azobenzene derivative. The probe compound not only has better water solubility, but also is high in accuracy when being used for azo reductase detection, is convenient to use and can simultaneously trace release of anti-inflammatory drugs such as 5-aminosalicylic acid and provide a supplementary means for diagnosis and treatment of colitis.

Inflammatory bowel diseases are represented by two idiopathic disorders, which include ulcerative colitis and Crohn's disease. Ulcerative colitis is restricted to the colon and involves uncertain and inflammation of the lining (mucosa) of the large intestine. Crohn's disease, on the other hand, can involve the mucosa of the small and / or large intestine and may involve deeper layers of the bowel wall. The present invention is a combination of 5-aminosalicylic acid and one or more antioxidants (e.g., N-acetylcysteine) for treating such inflammatory bowel diseases.

The invention discloses preparation and application of a heavy metal ion adsorption fiber with a wide pH application range. The method comprises the following steps: soaking a polypropylene fiber in a solvent containing a double-bond carboxylic acid monomer, a polymerization inhibitor and a catalyst, introducing nitrogen and swelling; irradiating through high-power electron beams, taking out homopolymer of which the fiber surface is cleaned, and drying to obtain a carboxylic-acid-grafted polypropylene fiber; and putting the polypropylene fiber into a sodium hydroxide solution in which 5-aminosalicylic acid is dissolved, introducing nitrogen for protection, heating for 2-10 hours, taking out and cleaning, thus obtaining a 5-aminosalicylic acid modified heavy metal ion adsorption fiber. The pH hardly has influence on heavy metal ions adsorbed by the fiber, so that wide pH application range can be realized. The adsorption speed is high, and the adsorption equilibrium can be achieved within 3 minutes; the fiber can be made into various shapes, is convenient to use and recycle, has wide application prospects in treatment of wastewater in metal smelting and petrochemical engineering and is particularly suitable for adsorption of the heavy metal ions in open water.

Methods of treating patients suffering from Crohn's disease or ulcerative colitis who did not experience a clinical response to previous thiopurine administration, or suffered side effects from previous thiopurine administration, by administering a delayed release pharmaceutical composition comprising 6-mercaptopurine are disclosed. Methods of treating patients suffering from Crohn's disease or ulcerative colitis who are also being administered a steroid, 5-aminosalicylic acid, or an antibiotic by adjunctively administering a delayed release pharmaceutical composition comprising 6-mercaptopurine are also disclosed.

The invention discloses a preparation method of a theophylline molecular surface printing material, and relates to a molecular printing polymer. The preparation method comprises the following steps of: activating silica gel microparticles; connecting surface chemical bonds of silica gel microparticles with sulfydryl containing silane coupling agents; chemically grafting polyglycidyl methacrylate on surfaces of silica gel microparticles; modifying by 5-aminosalicylic acid; and preparing the surface molecular printing polymer of silica gel microparticles. According to the invention, high performance molecular printing polymer is prepared through a method of graft polymerization and crosslinking printing sequentially. The molecular surface printing material has special identifying selection and excellent combining affinity to theophylline.

The invention discloses application of a biomarker for preparing a medicine for predicting feedback response of 5-aminosalicylic acid in treatment of ulcerative colitis. The biomarker determined in the invention is the basis of a target biomarker associated with gender difference response when 5-aminosalicylic acid (5-ASA) is used to treat ulcerative colitis (UC). The biomarker comprises a group of protein biomarkers which can differentiate response difference for treatment by 5-ASA between different genders and determine the curative effect by using 5-ASA under different UC conditions. Meanwhile, a novel drug target for a UC novel curative method is effectively determined and verified by using the biomarker with specificity for genders and disease focus parts, novel diagnostic reagents, medicines, methods and diagnostic standards are developed, and the application is used for establishing a UC treatment policy.

Disclosed are pharmaceutical compositions comprising immediate release and sustained release formulations of 5-aminosalicylic acid, or a pharmaceutically acceptable salt or ester thereof, and / or N-acetylcysteine, or a pharmaceutically acceptable salt or ester thereof, for release in the lower gastrointestinal tract.

The invention discloses a cobalt complex and a preparation method thereof, and the cobalt complex is characterized by having good electrocatalytic activity on hydrogen peroxide, the molecular formula of the cobalt complex is C26H26N4O10Co, the crystal system is orthorhombic, the space group is Pbcn, the cell parameters alpha, gamma and beta satisfy: a=15.928Angstrom, b=10.602Angstrom, c=15.596Angstrom, alpha is equal to gamma, is equal to beta and is equal to 90 degrees. The cobalt complex prepared in the invention is obtained by a mixing reaction of a cobalt salt and a derivative of 5-aminosalicylic acid, namely, 5-((2-pyridyl) methylene amino)-2-hydroxybenzoic acid according to a certain proportion, the cobalt complex has a specific spatial structure and an accurate molecular formula, the synthesis steps are simple, the yield can reach 45-70%, and the cobalt complex has good electrocatalytic activity, thereby being capable of being used as an electrocatalytic active material having a potential application prospect.

It is an object of the present invention to inhibit browning of a 5-aminosalicylic acid solid preparation, and to maintain for an extended period the properties of the 5-aminosalicylic acid solid preparation the same as they were at the time of the manufacturing the preparation. The present invention provides a solid preparation obtained by formulating 5-aminosalicylic acid or a salt thereof and a discoloration inhibitor into a drug product, wherein this solid preparation exhibits a color difference in a CIELAB color space being 10.5 or less before and after storage at 80° C. for one week. The above-mentioned discoloration inhibitor contains at least one selected from the group consisting of a thiol compound, a sulfide compound, an acid anhydride, and a hygroscopic compound.

The invention relates to aminosalicylic acid derivative lysine complex salt, a preparation method and application thereof. The structure of the aminosalicylic acid derivative lysine complex salt conforms to the following general formula (I), R1 stands for -H, -Cl or -Br; R2 stands for -F, -Cl or -Br; one of R3 and R4 stands for COO-, and the other one stands for -OH or -OCOCH3. A target compound of the aminosalicylic acid derivative lysine complex salt has the pharmacological action of treating neuropathic pain.

The invention provides mesalazine sustained-release pellets, a preparation method thereof and a mesalazine sustained-release capsule. The preparation method comprises the steps that 5-aminosalicylic acid, microcrystalline cellulose and a binding agent are mixed, and cores with pills are obtained through an extrusion rolling technology; materials comprising ethyecellulose are adopted, and cores with the pills are coated with sustained-release coating layers; the sustained-release coating layers are coated with enteric coating layers by the adoption of enteric materials and a processing aid, and mesalazine sustained-release pellets are obtained; the enteric materials are methacrylic acid and ethyl acrylate copolymer. PH dependent form and time dependent form drug release mechanisms are combined to achieve an ideal drug release curve, and the drug release position accuracy is improved. The mesalazine sustained-release capsule comprises the mesalazine sustained-release pellets, can be better released in the gastrointestinal tract and is beneficial to treatment on ulcerative colitis and Crohn's disease.

Belonging to the field of medicinal preparations, the invention relates to an orally taken colon-targeted preparation for treatment of inflammatory bowel diseases, particularly to an Eudragit S100 wrapped 5-aminosalicylic acid nanoparticle and its preparation method. In the invention, 5-aminosalicylic acid is taken as a model drug, and a pH sensitive Eudragit S100 is employed as a coating material to prepare the Eudragit S100 wrapped 5-aminosalicylic acid nanoparticle with a particle size of 70-400nm. The prepared nanoparticle can protect a 1, 5-aminosalicylic acid drug from being damaged by the digestive juice in a gastrointestinal tract until the drug reaches a colon region with pH greater than 7. The preparation method provided in the invention is simple to operate, and the prepared colon-targeted nanoparticle has the characteristics of small particle size and narrow distribution, as well as low solvent residue. The orally taken colon-targeted preparation can be used as a novel preparation of 5-aminosalicylic acid in treatment of inflammatory bowel diseases.

The subject invention pertains to materials and methods for the prevention and treatment of disease conditions associated with oxidative stress or a compromised reducing environment, including inflammatory bowel diseases such as Crohn's disease and ulcerative colitis. Therapeutic compositions of the invention include compositions that can neutralize hydrogen peroxide, such as reducing agents and oxidizing agents. In one embodiment, a composition includes dihydrolipoic acid as a first reducing agent, an aminosalicylic acid, and a mast cell stabilizer. In another embodiment, the composition further includes a second reducing agent. Methods of the invention include administration of compounds or compositions of the invention. In one embodiment, compounds or compositions of the invention are rectally instilled in a patient.

The invention relates to a synthesis method of an Azasetron intermediate, comprising the following steps of: reducing 5-chlorine-3 nitrosalicylic acid methyl ester in a glacial acetic acid medium to obtain 5-chlorine-3 aminosalicylic acid methyl ester through iron powder, processing the 5-chlorine-3 aminosalicylic acid methyl ester to obtain a solution containing the 5-chlorine-3 aminosalicylic acid methyl ester, and then directly reacting the solution with chloroacetic chloride to generate 3-(2-chloroacetic amido)-5 chlorosalicylic acid methyl ester with better purity and higher yield. The method has thorough reduction, solves the problem that the obtained 3-(2-chloroacetic amido)-5 chlorosalicylic acid methyl ester can not be refined when charging to next step due to the incomplete reduction and the poor product purity of the 5-chlorine-3 nitrosalicylic acid methyl ester in heterogeneous systems comprising toluene, hydrochloric acid / ammonium chloride and the like.

The invention discloses a transpiration regulator for planting stocks in hilly lands. The transpiration regulator comprises the following raw materials by weight in 1 L of water: 50 to 150 mg of fulvic acid, 50 to 100 mg of sodium thiosulfate, 50 to 100 mg of sodium bisulfite, 50 to 80 mg of para-aminosalicylic acid, 200 to 300 mg of nitrogen, phosphorus and potassium compound fertilizer, 200 to 400 mg of trace elements, and 50 to 100 mg of citric acid. The transpiration regulator for planting stocks in hilly lands can effectively solve the problem that the planting stocks in the hilly lands are lack of water and dry, can promote the growth of root systems of the planting stocks in the hilly lands, improves the survival rate of planting stock transplantation, effectively decreases the opening degree of air holes of the planting stocks in the small hilly lands, inhibits transpiration, improves the water content of leaves, improves the content of free proline and the content of chlorophyl, and greatly improves the survival rate and the drought resistance of transplanted planting stocks. The invention further discloses a preparation method of the transpiration regulator for planting stocks in hilly lands.

The invention relates to a para-aminosalicylate colon positioning drug delivery system which is a pellet or a particle. The inner part of the system is a kernel which contains the following components according to the mass percent: 50-98 percent of para-aminosalicylate, 1-30 percent of adhesive and 1-20 percent of skeleton material; and the surface of the kernel is coated with a layer of coatings which is 1 percent-40 percent of the mass of the whole pellet or the particle and contains film forming agent, sticking resistant agent and plasticizer. The invention also discloses a method for preparing the formulation, which comprises a sugar coating pot method, an extrusion-rolling method and a fluidized bed preparation method. Compared with the prior common tablet and a colon positioning tablet, the formulation has the better colon positioning effect, has the characteristics of increased specific surface area and good dissolving effect, is beneficial to absorbing and can reduce the poison and side effect caused by fast drug release by an individual difference of the formulation with a large dose, such as tablets, and the like.

A medicine targeting to colon for treating colitis is prepared through dispersing 5-aminosalicylic acid in chitosan solution, adding the oil-phase substance containing surfactant, stirring, adding the aqueous solution of ammonium sulfate, stirring, depositing, separating, washing and vacuum drying.