77 results about "Diacerein" patented technology

This invention relates to formulations in solid pharmaceutical forms containing diacereine and meloxicam. The present invention provides novel formulations comprising: (a) Diacereine, (b) Meloxicam, (c) one or more anti-adherent agents, (d) one or more disintegrating agents, (e) one or more binder agents, (f) one or more lubricants, (g) one or more diluents, (h) one or more solvents, and (i) any other additive which assists in formulation. The present invention also provides a method for treatment of osteoarthritis, rheumatoid arthritis, gout arthritis, multiple sclerosis, amyotrophic lateral sclerosis and related diseases, in addition of inflammatory processes originated from various etiologies, by administering suitable doses.

A once-daily controlled-release formulation of diacerein for treating inflammatory or autoimmune diseases or their complications, with reduced adverse side effects and methods of treating such diseases are disclosed.

The invention relates to a method for synthesizing the emodic acid which is the essential component of the traditional Chinese medicine rhubarb horsetails and duroruiyin which is antipyretic analgesic and osteoarthritis treating medicine, employing 3-nitro-ortho-phthalic anhydride as start raw material, reacting with m-cresol fuke, through reaction of reduction, diazonium salt, ring-combining to prepare intermediate compound chrysophanol, oxygenating to emodic acid, preparing duroruiyin through acetylation, the total productivity of the six reaction is 31.1%, the process is optimize through pilot-scale experiment a nd suitable for industrial production.

The invention relates to pharmaceutical compositions of rhein or diacerein, or salts or esters or prodrugs thereof which are bioequivalent to a 50 mg diacerein formulation marketed under the trade name Art 50®. The compositions exhibit no variability in fed and fasted state conditions. The compositions also result in significant reduction in side effects such as, soft stools as compared to Art 50®. The invention also relates to the methods for preparing such compositions.

Methods and compositions for treating and / or preventing hyperuricemia or metabolic disorders associated with hyperuricemia comprising administering to a patient in need a therapeutically effective amount of diacerein, rhein, or a pharmaceutically acceptable salt, an analog, a prodrug, or an active metabolite thereof.

Methods and compositions for treating and / or preventing hyperuricemia or metabolic disorders associated with hyperuricemia comprising administering to a patient in need a therapeutically effective amount of diacerein, rhein, or a pharmaceutically acceptable salt, an analog, a prodrug, or an active metabolite thereof.

The invention relates to liquid pharmaceutical compositions for oral administration comprising rhein or diacerein, or salts or esters or prodrugs thereof and processes for preparing such compositions.

The present invention provides methods of treating type II diabetes using combinations of diacerein or its derivatives with other antidiabetic agents. The methods may also allow improving glycemic control of type II diabetes patients and / or reducing side effects and / or cardiovascular risks of antidiabetic agents.

The invention provides an improved synthesis method for diacerein, comprising taking 3-nitrophthalic anhydride as the raw material, carrying out a Friedel-Crafts reaction with m-cresol, deoxidizing, cyclizing and diazotizing to obtain an intermediate chrysophanol, then acetylating, and oxidizing to obtain high-purity diacerein with a total yield of 33.7%.

The invention provides diacerein injection type thermo-sensitive gel. The diacerein injection type thermo-sensitive gel comprises diacerein, poloxamer 407, poloxamer 188 and HPMC (hydroxypropyl methylcelluloses). A concentration ratio (w / v) of the diacerein to the P-407 to the P-188 to the HPMC is 0.5%:17-22%:1-5%:0.3-1.0%. A method for preparing the diacerein injection type thermo-sensitive gelincludes preparation steps of swelling the HPMC by the aid of water at the room temperature to obtain HPMC solution; uniformly scattering the poloxamer P-407 and the poloxamer P-188 on the surface ofthe HPMC solution and carrying out overnight swelling and dissolving to obtain blank thermo-sensitive gel solution; sufficiently dissolving the diacerein by the aid of DMSO (dimethyl sulfoxide) to obtain diacerein solution and then adding the diacerein solution into the blank thermo-sensitive gel solution to obtain diacerein thermo-sensitive gel solution. The diacerein injection type thermo-sensitive gel and the method have the advantages that the diacerein injection type thermo-sensitive gel prepared by the aid of the method is prepared from water-soluble high-polymer materials, is excellentin histocompatibility and bio-adhesion, is long in detention time at medication positions, can be slowly released and is long-acting, and the purpose of reducing side effects on gastrointestinal tracts can be achieved.

The invention discloses a method for the preparation of diacerein having a structure represented by the formula (II), comprising the steps of: feeding rhein having the structure presented by the formula (I), a catalyst and acetic anhydride into a reaction vessel, heating up to 50 to 140 DEG C under a stirring state for reaction for 0.5-8 hours, tracing the reaction progress by means of TLC, detecting the amount of the diacerein to measure a reaction endpoint, upon completion of the reaction, cooling the temperature of reaction solution to room temperature, separating out solid for filtering, and recrystallizing filter cakes with acetic acid to obtain the diacerein; the catalyst is metal triflates, the amount of substances in the catalyst is 0.1%-10% of the amount of substances in rhein. The invention only needs the catalytic amount of the metal triflates to complete acylation reaction and the catalyst can be recycled, therefore, the invention greatly lowers the production cost, has higher yield and purity, simple post-treatment and simple production period, and is a preparation method for diacerein having favorable popularization and application prospect.

A process for obtaining diacerein with an aloe-emodine content lower than 100 ppm, preferably of 0-5 ppm, is herein disclosed. The process comprises subjecting an an aqueous-organic solution of a diacerein salt with a weak base to extraction with a water immiscible or sparingly water-miscible solvent, such as toluene, acetates of C2-C4 alcohols, halohydrocarbons and the like.

The invention relates to a diacerein composition with good leaching property, and preparation and a use thereof. The diacerein composition consists of diacerein and pharmaceutically acceptable adjuvants. The pharmaceutically acceptable adjuvants are selected from one or more from starch, microcrystalline cellulose, lactose, a disintegrating agent, a lubricant, an edulcorant and an adhesive. The diacerein composition quickly enters a blood circulation system more easily than an imported diacerein capsule, has better storage stability and is suitable for application to preparing drugs for preventing and treating arthritis, nephritis, glomerulonephritis and psoriasis as well as an interleukin-1 inhibitor.

A once-daily controlted-release formulation of diacerein for treating inflammatory or autoimmune diseases or their complications, with reduced adverse side effects and methods of treating such diseases are disclosed.

The invention provides a method capable of efficiently obtaining high-purity diacerein, wherein the high-purity compound can be obtained by washing a diacerein solvate; at the same time, a crystalline morphology of the diacerein solvate and a preparation method for the crystalline morphology are provided.

The invention relates to the field of compound medical preparations, and especially relates to applications of a compound preparation of diacerein and berberine in the medicine field. The invention discloses an oral pharmaceutical composition, which is composed of pharmaceutical active components and pharmaceutical auxiliary materials; wherein the pharmaceutical active components are composed of berberine / pharmaceutically-acceptable salts of berberine and diacerein / pharmaceutically-acceptable salts of diacerein, and the pharmaceutically-acceptable salts can be hydrochloride or sulfate. The pharmaceutical composition can be made into common tablets, dual-layer tablets, enteric coated tablets, capsules, particles, and powder. The pharmaceutical composition can reduce the blood sugar and blood fat, and prevent / treat diabetic complication, especially diabetic nephropathy.

The invention discloses an application of traditional Chinese medicine composition in preparation of a drug for treating osteoarthritis. The traditional Chinese medicine composition comprises traditional Chinese medicines in parts by weight as follows: 600 parts of rhizoma cibotii, 192 parts of fructus rosae fruit, 360 parts of caulis spatholobi, 144 parts of philippine flemingia roots, 360 parts of kadsura coccinea, 240 parts of beautiful millettia roots, 30 parts of glossy privet fruit, 180 parts of mistletoe, 30 parts of semen cuscutae, 26 parts of rhizoma corydalis, 26 parts of radix zanthoxyli, 12 parts of mastic and 20 parts of myrrh. Research demonstrates that the traditional Chinese medicine composition has anti-inflammatory and analgesic effects, has a good inhibiting effect on inflammatory factors causing the osteoarthritis, and is definite in curative effect compared with indometacin and diacerein used clinically. The traditional Chinese medicine composition is used as a traditional Chinese patent medicine and has no adverse effect during decades of clinical use, so that the high-efficiency and low-toxicity treatment drug is provided for patients with the osteoarthritis, and the significant progress is achieved.

The present invention relates to a combined pharmaceutical formulation having therapeutic anti-inflammatory, analgesic, antipyretic and osteoarthritis activities. From another perspective, the present invention relates to a new solid oral dosage form comprising a pharmaceutically effective amount of NSAID and a pharmaceutically effective amount of diacerein and the solid oral dosage form according to the present invention is preferably in the form of tablet and more preferably in the form of multi-layer tablet.

The present invention provides methods of treating type II diabetes using combinations of diacerein or its derivatives with other antidiabetic agents. The methods may also allow improving glycemic control of type II diabetes patients and / or reducing side effects and / or cardiovascular risks of antidiabetic agents.

The invention relates to the field of pharmaceutical preparations, in particular to a diacerein solid dispersion preparation and a preparation method thereof. The diacerein solid dispersion preparation is prepared from diacerein, povidone, a specific lubricating agent, a specific disintegrating agent and a diluent. The dissolution effect, bioavailability and stability of the diacerein solid dispersion preparation are beneficial to the industrial production of the diacerein solid dispersion preparation.

The invention discloses a diacerein quick-release pellet preparation and a preparation method, and relates to the field of pharmaceutical preparations and application. A drug-delivery way of the quick-release pellet preparation is oral medication, a core pellet is utilized as a carrier, and diacerein water solution containing a cosolvent and adhesive serves as a medicine applying solution. The diacerein quick-release pellet preparation has the characteristics of high medicine applying rate, good content evenness, quick drug release, quick effect in abirritation and the like. Meanwhile, the quick-release pellet preparation has the characteristics of good clinical use adaptability, high safety and the like. In addition, a fluidized bed medicine applying method of the core pellet is suitable for preparing extremely-low-standard diacerein oral preparation.

The present invention relates to compositions comprising: a) a Vitis vinifera extract in free form or in the form of a complex with phospholipids, or a Punica granatum extract; and b) a lipophilic extract of Zingiber officinale; and c) a lipophilic extract obtained from plants containing polyunsaturated fatty acid isobutylamides selected from the group consisting of Echinacea spp. extract or Zanthoxylum spp. extract or Acmella oleracea (or Spilanthes oleracea) extract; and d) an unsaponifiable fraction of olive oil and / or corn oil; or e) N-acetyl glucosamine; or f) diacerein; and their use in the prevention and / or treatment of osteoarticular inflammation and pain, and cartilage damage.

The invention discloses a microporous membrane-coated controlled-release trelagliptin succinate pellet and a preparation method thereof. The microporous membrane-coated controlled-release trelagliptin succinate pellet sequentially comprises a drug-containing pellet core and a controlled-release coating layer from inside to outside, wherein the drug-containing pellet core is prepared from a primary material and an auxiliary material at the ratio of (5%-20%):(80%-95%). According to the microporous membrane-coated controlled-release trelagliptin succinate pellet, a bitter taste can be coated, the effective ingredients can be dissolved out, constant long-acting plasma concentration is ensured, and the defect that a drug is discharged along with excrement before not completely released is avoided.

The invention discloses application of diacerein in preparation of antiviral drugs and treatment of virus infection, and belongs to new application of diacerein. The experimental results prove that diacerein can be used for effectively inhibiting hepatophilic DNA viruses, retroviruses, enteroviruses, orthomyxoviruses, fibroviruses, reoviruses, arenavirus, hepatitis E viruses, astroviruses, circoviruses, coronaviruses, parvoviruses, adenoviruses, polyomaviruses, herpes viruses, poxviruses, human papillomaviruses, paramyxoviruses, flaviviruses, herpes viruses, alphaviruses and rhabdoviruses.

The invention provides a diacerein composition and a preparing method thereof. The diacerein composition is characterized by being prepared from the following raw materials in parts by weight: 1 part of diacerein, 0.01-0.1 part of poloxamer, 0.001-0.1 part of sodium benzoate, 0.3-6 parts of a filler, 0-0.5 part of a disintegrant, 0.01-0.5 part of an adhesive, 0-0.8 part of a moistening agent and 0.01-0.5 part of a lubricant. The diacerein composition not only can improve the solubility and the bioavailability of medicine, but also can reduce side effect generated when a patient takes the medicine.

The invention relates to the field of compound medical preparations, and especially relates to applications of a compound preparation of diacerein and berberine in the medicine field. The invention discloses an oral pharmaceutical composition, which is composed of pharmaceutical active components and pharmaceutical auxiliary materials; wherein the pharmaceutical active components are composed of berberine / pharmaceutically-acceptable salts of berberine and diacerein / pharmaceutically-acceptable salts of diacerein, and the pharmaceutically-acceptable salts can be hydrochloride or sulfate. The pharmaceutical composition can be made into common tablets, dual-layer tablets, enteric coated tablets, capsules, particles, and powder. The pharmaceutical composition can reduce the blood sugar and blood fat, and prevent / treat diabetic complication, especially diabetic nephropathy.

Methods and compositions for inhibiting expression of ASC, expression of NLRP3, and / or formation of NLRP3 inflammasome complex by using diacerein or its analogs are provided. Also provided are methods and compositions for the treatment and / or prevention of a disorder mediated by ASC and / or NLRP3, and / or by formation of NLRP3 inflammasome complex by using diacerein or its analogs.

The invention discloses a synthetic process for diacerein. The process comprises the steps of oxidizing aloe-emodin to produce chrysophanic acid under double combination effects of a catalyst and hydrogen peroxide, keeping a temperature of 80 DEG C to the refluxing temperature of a solvent, and reacting for 1-5 hours; and performing an acetylation reaction on the chrysophanic acid to form the diacerein. In the process, a chromium-containing oxidant used by a conventional process is avoided; an inexpensive and easily available, environment-friendly and mild-reaction oxidant is employed; the process is easy to control; and the obtained product quality is greatly improved, so that the process is particularly suitable for industrialized large-scale production.

The invention discloses a method for the preparation of rhein having a structure represented by the formula (II), comprising the steps of: adding into a reaction vessel aloe emodin represented by the formula (I) and aqueous solution of inorganic acids, stirring until solids are completely dissolved, feeding an oxidant at the temperature ranging from 20 to 50 DEG C, with amount ratio of the oxidant to the aloe emodin of 0.5-10:1, after feeding the oxidant, heating up to 50 to 90 DEG C for reaction, tracing the reaction progress by means of TLC, detecting the amount of the diacerein to measure a reaction endpoint, upon finish of the reaction, pouring reaction solution into icy water to separate out solid, filtering, washing filter cake with water until the filtrate is neutral, and then obtaining the rhein via recrystalliation by glacial acetic acid, filtering and drying; the amount ratio of the aloe emodin to organic acid feeding substances is 1:1-20. The invention has the advantages of great availability of raw material, simple processes, small use amount of solvent, higher yield and purity of the obtained products and no residues of harmful metal ions, and is a preparation method for the rhein having favorable popularization and application prospect.