181 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.

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.

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 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.

An orally adminsterable pharmaceutical pellet formulation for the treatment of the intestinal tract is disclosed, which comprises a core and an enteric coating, the core including, as a pharmaceutical active compound, aminosalicylic acid or a pharmaceutically tolerable salt or a derivative thereof.

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 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 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.