42 results about "Gabapentin enacarbil" patented technology

Methods are provided for use in treating humans suffering from irritable bowel syndrome. In the subject methods, an effective amount of a nerve-acting agent, e.g., lidocaine, topiramate, mexiletine and gabapentin, etc., is administered to a human suffering from irritable bowel syndrome. Also provided are pharmaceutical compositions and kits for use in practicing the subject methods.

The invention relates to application of 7-O-beta-D-acetylation sugar-coumarin compounds in treating chronic neuropathic pains. The 7-O-beta-D-acetylation sugar-coumarin compounds comprise a pharmaceutically acceptable salt, ester or a solvate thereof, and the application relates to the application of the salt, the ester or the solvate in preparing medicaments for treating the chronic neuropathic pains, wherein a glycosyl part is arbitrary pyranose or furanose, the hydroxy of which is totally acetylated; a representative compound is 7-O-beta-D-acetylation glucose-coumarin; and the structural formula is disclosed in the specification. On a classical sciatic nerve chronic compression injury (CCI) model, through single intragastric administration and continuous intragastric administration for 7 days, the compound shows definite treatment effect of resisting nervous pains. At a dose point appointed by an experiment, the compound can obviously improve the mechanical stimulus pain threshold, the nervous pain resistant efficacy is equivalent to that of Gabapentin which is a contrast medicament, and the duration is superior to that of the Gabapentin. Proved by research results, the compound can be used for treating the chronic neuropathic pains.

The present invention relates to new processes for the preparation of gabapentin by the desilylation of a silylated gabapentin or by the silylation-desilylation of an acid addition salt of gabapentin with a silylating agent.

The invention relates to the technical field of medicine synthesis, in particular to a preparation method of cyano reductase and gabapentin. The method comprises the following steps: by taking sodium hydride as a catalyst, carrying out condensation reaction on cyclohexyl methyl cyanide and 2-ethyl bromoacetate to generate 2-cyano-2-cyclohexyl ethyl acetate; under an alkaline condition, carrying out hydrolysis reaction on 2-cyano-2-cyclohexyl ethyl acetate to obtain 2-cyano-2-cyclohexyl acetic acid; and converting the 2-cyano-2-cyclohexyl acetic acid into gabapentin under the action of the cyano reductase. Aiming at the defects (the problem of traditional chemical preparation of gabapentin) of a literature scheme, cyano reductase is introduced, and a route is systematically optimized, so that reaction steps are reduced, and meanwhile, reaction conditions are milder and more environment-friendly. According to the route, the overall yield of gabapentin can be remarkably increased, and meanwhile, the gabapentin better meets the requirements of current green production.

The invention belongs to the field of medicine preparation and relates to a gabapentin tablet which is prepared by wet granulation and prepared mainly from the following raw materials by weight percentage: 80.0% or more of gabapentin, 4.0-17.0% of low-substituted hydroxypropyl cellulose, 0.5-2.5% of adhesive, 0.1-2.5% of stabilizer and 0.5-1.5% of lubricant. The invention further provides a preparation method of the gabapentin tablet. The gabapentin raw material adopted in the invention has good formability and high physical strength after being crushed. Besides, the gabapentin raw material can be prepared by adopting an ordinary wet granulation method and has the characteristics of simple preparation and low cost. The gabapentin tablet provided by the invention has the advantages of very high dissolution in vitro, high content of gabapentin, less application auxiliary materials and high convenience for use, thus meeting modern medicine's requirements of 'small in three aspects' and 'convenient in three aspects', and can be prepared by adopting an ordinary wet granulation method and has the characteristics of simple preparation and low cost.

The instant invention is a route to stereospecific 3-substituted 5-membered ring isomers of Formula (A). The final products are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), inflammation especially arthritis, sleep disorders, premenstrual syndrome, and hot flashes. The invention provides novel routes to synthesize stereoselectively analogs of gabapentin (Neurontin3) of Formulas (I), (II), (III) and (IV) wherein R is C1-C10 alkyl or C3-C10 cycloalkyl and pharmaceutically acceptable salts thereof.

The invention provides a gabapentin soft chewable tablet preparation, and a preparation method and application thereof. The gabapentin soft chewable tablet preparation comprises gabapentin, a phagostimulant, a filler and a wetting agent, the wetting agent is a mixture of glycerol and polyethylene glycol, the content of polyethylene glycol is 20-40 wt%, the phagostimulant is selected from chicken liver powder, beef powder or chicken powder and the like, and the filler comprises common auxiliary materials such as microcrystalline cellulose, corn starch, potato starch or pregelatinized starch. The preparation method comprises the following steps: mixing gabapentin, the phagostimulant and the filler in a wet type granulator, then dropwise adding the wetting agent into the wet type granulator, and carrying out granulation, granule finishing and tabletting. According to the invention, feeding and administration are convenient, and the subjective initiative of pet eating can be improved by adding the phagostimulant; and soft tablets chewable in the mouth can be prepared through the high viscosity property of a moisturizer such as glycerin, and meanwhile the moisturizer such as glycerin can just play a role of a stabilizer for gabapentin.

The invention relates to a salt of gabapentin and 2, 6-pyridine dicarboxylic acid as well as a preparation method and application thereof. The salt of gabapentin and 2, 6-pyridine dicarboxylic acid has the advantages of being high in purity, small in hygroscopicity, simple in preparation method and good in reproducibility, the chemical stability is remarkably improved, the production process of amedicine is optimized, and the druggability of the medicine is improved.

The present invention provides a stabilized composition comprising a non-crystalline gabapentin enacarbil and at least one crystallization-inhibiting compound. In particular, the present invention provides a stabilized composition of gabapentin enacarbil, wherein the gabapentin enacarbil is maintained in a non-crystalline form by the composition, for example, as an amorphous form. The invention also provides, among other things, methods of making the stabilized composition, or use of the stabilized composition for making a medicament.

The disclosure provides methods of treating pain in a patient who will be subjected to a surgical procedure, comprising administering meloxicam to the patient prior to start of the surgical procedure.In some embodiments, meloxicam is nanocrystalline meloxicam. The disclosure further provides methods of treating pain in a patient in need thereof, comprising administering meloxicam intravenously tothe patient in combination with acetaminophen and/or gabapentin.

The invention belongs to the technical field of medicines, and particularly relates to a pharmaceutical composition with a synergistic analgesic effect, and the pharmaceutical composition comprises resveratrol and one of gabapentin and duloxetine. According to the invention, resveratrol and gabapentin or duloxetine are combined for medication, a large number of experimental studies show that the combined medication can generate a very obvious synergistic analgesic effect, and experiments show that the dose combination does not affect the movement balance ability and muscle coordination of an acting object. Therefore, the analgesic effect of the combination of the resveratrol and the gabapentin or duloxetine is superior to that of the gabapentin or duloxetine which is independently used, so that the pharmaceutical composition has a better application prospect; in addition, the use dosage of gabapentin or duloxetine can be greatly reduced through pharmaceutical composition, guarantee is provided for compliance and tolerance of clinical medication, and adverse reactions of gabapentin or duloxetine are reduced or avoided.

This invention refers to a pharmaceutical composition that comprises the synergic combination of a NSAID, such as the active ingredient: S-ketorolac of tromethamine and a GABA derivative agent, such as the active ingredient: gabapentin, which are formulated with pharmaceutically acceptable excipients in a single dosing unit to be administered by oral, parenteral, topical, transdermal means or with the use of transdermal, oral or nasal inhalation devices, which is indicated for the treatment of neuropathic and/or nociceptive pain caused by different etiologies.

A process for producing Gabapentin, (1-(anminomethyl)-1-cyclohexaneacetic acid) from Gabapentin hydrochloride salt. In the process the Gabapentin hydrochloride is converted to Gabapentin using inorganic base such as Barium hydroxide. Gabapentin hydrochloride is converted to Gabapentin sulfate which in turn is converted to free base using Barium hydroxide. The process is directed to improvement in the manufacture of Gabapentin which would be industrially feasible and effective Gabapentin obtained following the process of the invention is suitable as a drug especially in the treatment of cerebral diseases such as epilepsy. The above process involves simple steps and avoid the problems of the known art. In particular the process avoids severe conditions and/or complexities and can be readily adopted for industrial application. The process provides for good yield and does not involve lengthy extended process steps. It is cost-effective and can be carried out involving simple ingredients and steps of manufacture.

The instant invention is a route to stereospecific 3-substituted 5-membered ring isomers of Formula (A). The final products are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), inflammation especially arthritis, sleep disorders, premenstrual syndrome, and hot flashes. The invention provides novel routes to synthesize steroselectively analogs of gabapentin (Neurontin®) of Formulas (I), (II), (III) and (IV) wherein R is C₁-C₁₀ alkyl or C₃-C₁₀ cycloalkyl and pharmaceutically acceptable salts thereof.

The invention provides a gabapentin and pregabalin compound capsule and a preparation method thereof.The preparation method comprises the steps that pregabalin, polyglycerol fatty acid ester, an adhesive and an ethanol solution are stirred and mixed to prepare a drug-loaded suspension, gabapentin is added, stirring and dispersing are conducted, pelleting is conducted, and drug-loaded pellets are obtained; and finally, coating the surfaces of the drug-loaded pellets soaked and dispersed in a film solution by adopting the film solution containing sericin to form an isolation film layer, so as to obtain film drug-loaded pellets, and filling the film drug-loaded pellets into capsules, so as to obtain the gabapentin and pregabalin compound capsules. The gabapentin and pregabalin compound capsule prepared by the invention not only effectively improves the drug loading capacity of the drug-loaded pellet, but also has excellent in-vitro dissolution rate and release rate, and greatly reduces adverse reactions caused by gabapentin, especially headache, insomnia, edema and ataxia; meanwhile, the gabapentin and pregabalin compound capsule is stable in quality, and the combination of gabapentin and pregabalin raw material medicines is effectively realized.