45 results about "Rifaximine" patented technology

A pharmaceutical composition comprising therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s) and release controlling agent(s). Pharmaceutical composition of rifaximin comprising: at least two entities wherein one entity is an immediate release or fast release and the other is controlled release. The pharmaceutical composition in the form of multilayer tablet comprising, at least one layer comprising, therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s); said layer providing controlled release rifaximin; and at least one layer which provides increased residence time of the dosage form in the gastrointestinal tract. The pharmaceutical formulation comprising rifaximin having an in vitro dissolution profile, wherein about 70% of rifaximin is released in about 24 hours. The composition comprising therapeutically effective amount of rifaximin or pharmaceutically acceptable salt(s) or enantiomer(s) or polymorph(s) thereof, one or more release controlling agent(s) and pharmaceutically acceptable excipient(s) causing pathogenic eradication.

Amorphous rifaximin, methods of making it, and pharmaceutical compositions containing it. Also described are methods of converting amorphous rifaximin to crystalline rifaximin and vice versa.

Polyols stabilize polymorphous form of rifaximin, in particular the β form. When polyols having at least two hydroxy groups are added to rifaximin powder, polymorph β is stable and remains stable in time independently from the environment humidity. In this invention a method to prepare formulations constituted by pure and stable polymorphous forms able to give a pharmaceutical product is described.

The present invention relates to a new amorphous form of rifaximin and to methods for the preparation thereof by means of high energy milling or Spray drying. The present invention further relates to a new amorphous form for use as medicament and to the pharmaceutical compositions composing it.

A method for preventing and / or treating a functional gastrointestinal disorder, comprising administering, to a subject with the functional gastrointestinal disorder, rifaximin as an effective ingredient. The functional gastroinstestinal disorder includes a functional esophageal disorder, a functional gastroduodenal disorder (e.g., a functional dyspepsia), a functional bowel disorder (e.g., a functional bloating, a functional diarrhea), a functional abdominal pain syndrome, a functional gallbladder and Sphincter of Oddi disorder, a functional anorectal disorder (e.g., a functional fecal incontinence, a functional anorectal pain, a functional defecation disorder), a functional disorder in neonates and toddlers (e.g., an infant functional diarrhea), a functional disorder in children and adolescents (e.g., a childhood functional abdominal pain, a childhood nonretentive fecal incontinence), and other diseases.

The present invention relates to a new polymorph of Rifaximin, designated κ, and to a process for the preparation thereof. Under certain aspects, the invention also relates to pharmaceutical compositions comprising an effective amount of the polymorphic form κ of Rifaximin and a pharmaceutically acceptable carrier and its uses in the treatment of gastrointestinal conditions.

The invention discloses application of a rifamycin-quinolizidone dual-target molecule represented in a formula I in inhibition of ammonia producing floras in gastrointestinal tracts. The rifamycin-quinolizidone dual-target molecule represented in the formula I is similar to an antibacterial spectrum of rifaximin and has relatively strong antibacterial activity to common ammonia producing floras in the gastrointestinal tracts; and meanwhile, the rifamycin-quinolizidone dual-target molecule has the property of low drug resistance frequency and has application prospects in prevention and treatment of infection of hepatic encephalopathy and relevant bacterial genera (types). The formula I is as shown in the specification.

The present invention describes rifaximin powder and to a process for preparing the same. The invention relates also to a pharmaceutical composition in solid form comprising said rifaximin, pharmaceutically acceptable excipients and optionally other ingredients. The compositions according to the invention are suitable for oral administration and are characterized by producing a controlled release of rifaximin, whereby a long-lasting effect is obtained in a patient.

In alternative embodiments, the invention provides compositions and methods for treating, ameliorating and preventing various disorders and conditions in mammals, including genetically-predisposed and chronic disorders, where the microbial or bacterial flora of the bowel is at least one causative or symptom-producing factor, for example, where the microbial or bacterial flora of the bowel manufactures neurotoxins or neurotoxic agents that enter the body through the gastrointestinal (Gl) tract, e.g. the colon, and reach the systemic space, e.g., by neural streaming or via the circulation, to reach the central nervous system (CNS), including the brain, the peripheral nervous system (PNS), and other nervous systems. In alternative embodiments, methods and compositions of the invention comprise or comprise use of medications, formulations and pharmaceuticals comprising rifaximin or equivalent active agents that can suppress or eradicate the microbiota super-infection that causes various psychotropic disorders. These compositions have been found to be affective in a broad spectrum of disorders but particularly in the obsessive compulsive disorder group (OCD).

The present invention discloses a stable amorphous form of Rifaximin characterized by having X-ray powder diffraction pattern as given in FIG. 1, having a 2θ peaks at 7.2 and having moisture content in the range of 3% to 4% preferably, 3.4% to 3.7%. This invention also discloses a novel process for its preparation.

A pharmaceutical composition comprising therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s) and release controlling agent(s). Pharmaceutical composition of rifaximin comprising: at least two entities wherein one entity is an immediate release or fast release and the other is controlled release. The pharmaceutical composition in the form of multilayer tablet comprising, at least one layer comprising, therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s); said layer providing controlled release rifaximin; and at least one layer which provides increased residence time of the dosage form in the gastrointestinal tract. The pharmaceutical formulation comprising rifaximin having an in vitro dissolution profile, wherein about 70% of rifaximin is released in about 24 hours. The composition comprising therapeutically effective amount of rifaximin or pharmaceutically acceptable salt(s) or enantiomer(s) or polymorph(s) thereof, one or more release controlling agent(s) and pharmaceutically acceptable excipient(s) causing pathogenic eradication.

The invention discloses a rifaximin enteric-coated preparation composition and a preparation method thereof. The rifaximin enteric-coated preparation composition is mainly prepared from a rifaximin bulk drug and proper auxiliary materials. The rifaximin enteric-coated preparation provided by the invention is effective and safe for the improvement on a rifaximin preparation, and has the advantagesof less stimulations to the stomach to reduce side effects and the like compared with a common rifaximin preparation. The rifaximin enteric-coated preparation composition is particularly suitable forpatients with stomach upset diseases and can maximize the contact between an active component rifaximin and intestinal mucus. The invention provides a novel dosage form which is safer and has better curative effect; and the preparation process of the rifaximin enteric-coated preparation composition has good quality controllability and stability.

The invention discloses a rifaximin sustained-release preparation combination and a preparation method thereof. The rifaximin sustained-release preparation combination is mainly prepared from rifaximin bulk drugs, sustained-release materials and other appropriate auxiliary materials. The rifaximin sustained-release preparation provided by the invention can deaccelerate the release rate of the main drugs, reduce the frequency of administration and improve the patient compliance. The invention provides a novel form of drug having better patient compliance and having the advantages of high quality controllability and stability of the preparation process.

The present invention features an antibacterial composition comprising 1) a composition A comprising polymyxin B and trimethoprim; and 2) an antibiotic agent selected from the group consisting of rifampicin, rifabutin, rifapentine, rifaximin, pefloxacin mesylate, sparfloxacin, sarafloxacin HCl, tobramycin, lomefloxacin, besifloxacin, danofloxacin mesylate, enrofloxacin, nadifloxacin and clinafloxacin, a topical pharmaceutical thereof, and a method of treating bacterial infections using mixtures of 1 and 2.

The invention discloses a rifaximin hapten and a rifaximin artificial antigen, and a preparation method and application of the rifaximin hapten and the rifaximin artificial antigen. The rifaximin artificial antigen provided by the invention is an antigen obtained by coupling the rifaximin hapten shown as a formula I which is described in the specification with a carrier protein. The rifaximin artificial antigen provided by the invention is simple in synthesis method, high in purity and high in yield, and has important value for preparation of a rifaximin antibody and detection of rifaximin drug residues.

Provided herein are pharmaceutical compositions, therapeutic combinations, devices and methods for treating, ameliorating, reversing, causing the remission of, and / or preventing (acting as a prophylaxis, or preventing the initiation of) an inflammatory bowel disorder (IBD) or inflammatory bowel disease (IBD), Ulcerative Colitis; Crohn's disease; J-pouch; fistulising Crohn's disease; a Colitis which can be microscopic, lymphocytic or collagenous; an eosinophilic colitis; indeterminate colitis; idiopathic colitis; diverticulosis and diverticulitis; relapsing diverticulitis; constipation associated inflammatory bowel disease and / or small intestinal bacterial overgrowth; Irritable Bowel Syndrome (IBS) with or without diarrhoea, constipation or pain predominant IBS; periodontitis; rheumatoid arthritis; respiratory infections, appendicitis, vascular disorders such as thrombophlebitis; bacteremia; osteomyelitis; septic shock; Alzheimer's disease; Lemierre syndrome (postanginal sepsis); colonic polyps or adenomas (optionally hyperplastic, adenomatous or serrated adenomas) or preventing the growth of colonic polyps or adenomas, bowl cancer, or metastases (optionally preventing the initiation or promotion of bowl cancer or metastasis); pharyngitis; otitis; sinusitis; and any disease, symptom or condition caused or exacerbated by a Fusobacteria (optionally, a F. nucleatum or F. varium) infection. In alternative embodiments, pharmaceutical compositions comprise rifaximin alone or in combination with other antibiotics or drugs.

A composition comprising rifaximin in the form of particles, wherein substantially all the particles have a particle size less than or equal to 2 micrometres.

The present invention relates to a method for treating, ameliorating, reversing and / or preventing autism or an autism spectrum disorder (ASD) via the administration of a formulation, a pharmaceuticalpreparation or a pharmaceutical composition comprising or consisting of: (a) a rifaximin (optionally a XIFAXAN, XIFAXANTA or NORMIXT), an extended intestinal release (EIR) rifaximin, a rifamycin derivative, a rifampicin (or rifampin) (optionally RIFADIN), a rifabutin (optionally MYCOBUTIN), a rifapentine (optionally PRIFTIN), a rifalazil, a bicozamycin, or a mixture or combination thereof, or (b)a rifaximin (optionally a XIFAXAN, XIFAXANTA or NORMIX) and at least one additional antimicrobial or antibiotic agent, wherein optionally the at least one additional antimicrobial or antibiotic agentcomprises a vancomycin, a metronidazole (optionally FLAGYLTM, METROTM), a tinidazole (optionally FASIGYN, SIMPLOTAN, TINDAMAX) or a combination thereof

The present invention discloses a stable amorphous form of Rifaximin characterised by having X-ray powder diffraction pattern as given in FIG. 1, having a 2θ peaks at 7.2 and having moisture content in the range of 3% to 4% preferably, 3.4% to 3.7%. This invention also discloses a novel process for its preparation.

The invention provides a synthesis process of rifaximine-D6, which comprises the following steps: 1) by using compounds I2-amino-4-methylpyridine and D2O as raw materials, reacting in the presence of5wt% palladium on carbon and under the protection of nitrogen to obtain a deuterated intermediate, i.e., a compound II 4-methyl-2-aminopyridine-D6; step 2), dissolving rifamycin S and the deuterated intermediate compound II 4-methyl-2-aminopyridine-D6 prepared in the step 1) into dichloromethane; under the protection of nitrogen, stirring at room temperature, dropwise adding a dichloromethane solution dissolved with elemental iodine, reacting at room temperature overnight for 18 hours, dropwise adding an L-ascorbic acid aqueous solution, stirring, and after the reaction is completed, washing and purifying to obtain the product rifaximin-D6. The synthesis method has the following technical effects that the synthesis method of the intermediate II of rifaximin-D6 is simple and convenient, andraw materials are easy to obtain; the steps for synthesizing rifaximin-D6 are simple and short, and the operation is easy.

The invention discloses a rifaximin enteric sustained-release preparation combination and a preparation method thereof. The rifaximin enteric sustained-release preparation combination is mainly prepared from rifaximin bulk drugs, medicinal sustained-release and enteric materials and other appropriate auxiliary materials. The rifaximin enteric sustained-release preparation provided by the invention can not only prevent rifaximin from disintegrating in the stomach and causing irritation to gastric mucosa and avoid the adverse reactions caused by the administration, such as nausea, abdominal pain, diarrhea and the like, but also deaccelerate the release rate of drugs, reduce the frequency of administration and improve the patient compliance. The invention provides a novel form of drug having higher safety and better patient compliance and having the advantages of high quality controllability and stability of the preparation process.

The invention provides a preparation method of a novel veterinary uterus injectant, which belongs to the field of veterinary preparations, and comprises the following steps: respectively mixing an adsorption carrier with rifaximin self-microemulsion and a growth repair factor to prepare self-microemulsion drug-loaded particles and growth repair factor drug-loaded particles; and mixing a first matrix, a second matrix and water for injection to prepare an injection matrix, mixing the injection matrix with the self-microemulsion drug-loaded particles and the growth repair factor drug-loaded particles, and freeze-drying to prepare the uterus injectant, by utilizing the cell growth promoting effect of the growth repair factor and the cell proliferation microenvironment provided by the gel matrix, the repair of endometrial epidermis cells is accelerated, the regeneration of damaged tissues is promoted, and a protective barrier is established, so that new infection in the uterus can be prevented, and the morbidity of endometritis is reduced.

Provided herein are pharmaceutical compositions that enhance the intestinal level of soluble rifaximin, formulations comprising the compositions, and their use in the treatment of one or more intestinal related disorders.

The invention relates to a rifaximin-containing preparation for preventing and treating dairy cow mastitis during the dry milk period, which comprises the main active ingredients of rifaximin and dandelion plant extracts, the auxiliary ingredients of thickening agent poloxamer 407, a viscosity modifier isopropyl myristate, an antioxidant butylated hydroxytoluene (BHT) and a solvent medical castor oil. The rifaximin-containing preparation can be used as an udder injectant for preventing and treating the dairy cow mastitis during the dry milk period, which is caused by staphylococcus aureus, staphylococcus epidermidis, streptococcus, enterococcus, corynebacterium, Escherichia coli, salmonella, shigella and bacteroides.

In alternative embodiments, provided are pharmaceutical compositions and methods for treating, ameliorating, reversing and / or preventing (acting as a prophylaxis) an Obsessive-Compulsive Disorder (OCD), with or without an accompanying autism or an autism spectrum disorder (ASD), e.g., a regressive autism. In alternative embodiments, these pharmaceutical compositions and methods are dosaged and administered to children in need thereof. In alternative embodiments, pharmaceutical compositions and methods are dosaged, formulated and dosaged as solid, liquid or aerosol preparations or formulations. In alternative embodiments, pharmaceutical compositions comprise rifaximin as the sole antibiotic, or rixafimin and other antimicrobial or antibiotic agent, for example, vancomycin, metronidazole, tinidazole, secnidazole or a combination thereof. As there are various molecular forms of rifaximins, all these are useful and used in methods and compositions as provided herein

In alternative embodiments, provided are pharmaceutical compositions and methods for treating, ameliorating, reversing and / or preventing (acting as a prophylaxis) an Obsessive-Compulsive Disorder (OCD), with or without an accompanying autism or an autism spectrum disorder (ASD), e.g., a regressive autism. In alternative embodiments, these pharmaceutical compositions and methods are dosaged and administered to children in need thereof. In alternative embodiments, pharmaceutical compositions and methods are dosaged, formulated and dosaged as solid, liquid or aerosol preparations or formulations. In alternative embodiments, pharmaceutical compositions comprise rifaximin as the sole antibiotic, or rixafimin and other antimicrobial or antibiotic agent, for example, vancomycin, metronidazole, tinidazole, secnidazole or a combination thereof. As there are various molecular forms of rifaximins, all these are useful and used in methods and compositions as provided herein

The present invention relates to a pharmaceutical composition containing a stable polymorph of rifaximin and a wicking agent as well as a method of preparing the same.

The present invention relates to an oral dosage form containing rifaximin in form beta, wherein the oral dosage form provides delayed release of the active pharmaceutical agent. Further, the invention relates to the preparation of an oral dosage form, preferably a tablet.

In alternative embodiments, provided are pharmaceutical compositions and methods for treating, ameliorating, reversing and / or preventing (acting as a prophylaxis) autism, e.g., regressive autism. In alternative embodiments, these pharmaceutical compositions and methods are dosaged and administered to children in need thereof. In alternative embodiments, pharmaceutical compositions and methods are dosaged, formulated and dosaged as solid, liquid or aerosol preparations or formulations. In alternative embodiments, pharmaceutical compositions comprise rifaximin as the sole antibiotic, or rixafimin and other antimicrobial or antibiotic agent, for example, vancomycin, metronidazole, tinidazole or a combination thereof.