49 results about "Gabapentin enacarbil" patented technology

The invention discloses a nitrilase mutant and an application thereof in preparation of an anti-epileptic drug intermediate. The mutant is obtained by mutating one or more of 151th amino acid, 223th amino acid and 250th amino acid of an amino acid sequence shown in SEQ ID No.2. The thermal stability of the nitrilase mutant AcN-T151V / C223A / C250G is improved by 1.73 times, 1M 1-cyanocyclohexyl acetonitrile is hydrolyzed by use of recombinant escherichia coli containing the nitrilase mutant at the temperature of 35 DEG C to generate 1-cyanocyclohexylacetic acid, and the yield of a final product reaches 95%. When 1.2 M 1-cyanocyclohexyl acetonitrile is hydrolyzed at the temperature of 35 DEG C, the final yield reaches 97%. Gabapentin is synthesized by use of the nitrilase mutant, and the yieldof the final product reaches 80%.

A complex comprised of gabapentin or pregabalin and a transport moiety, such as an alkyl sulfate, is described. The complex has an enhanced absorption in the gastrointestinal tract, particularly the lower gastrointestinal tract. The complex, and compositions and dosage forms prepared using the complex, provide for absorption by the body of the drug through a period of ten to twenty-four hours, thus enabling a once-daily dosage form for gabapentin or pregabalin.

The present invention is generally directed to methods for preparing stable gabapentin tablets by wet granulation. A wet granulation method for preparing gabapentin tablets includes forming a mixture by dry mixing of a first portion of a binder with the gabapentin, one or more excipients, or a combination of the gabapentin and the one or more excipients; and adding a second portion of the binder to the mixture, wherein the second portion of the binder is in the form of a solution or dispersion.

The present invention relates to sustained release oral dosage forms of gabapentin and at least one rate controlling polymer, and a process for the preparation of the sustained release oral dosage forms, and a process for the preparation thereof. The sustained release tablet includes gabapentin or a pharmaceutically acceptable salt or hydrates thereof and at least one rate-controlling polymer such that the tablet provides therapeutically effective plasma levels of gabapentin for a period of up to about 12 hours.

Gabapentin enacarbil was prepared and purified from intermediates such as 1-haloalkyl carbamate or carbonate and diacid acetal skeleton. For example, a 1-haloalkyl carbonate or carbamate was prepared by combining a C1 to C10 alcohol or C1 to C10 primary amine, a solvent selected from the group consisting of: acetonitrile, C3 to C7 ketone, C5 to C10 ether, C2 to C7 ester, C5 to C10 hydrocarbon and a combination thereof; a 1-haloalkyl haloformate of the following formula:wherein each X is independently selected from Br, I, or Cl; R1 is alkyl or H; and a C6 to C21 tertiary amine.

The invention discloses a method for directly synthesizing gabapentin by virtue of 1-cyanocyclohexyl acetic acid. The method comprises the following steps: dispersing immobilized cells of nitrilase genetically engineered bacteria into deionized water, adding 1-cyanocyclohexyl acetonitrile, stirring the completely react at 20-50 DEG C and 10rpm-350rpm, and carrying out suction filtration, so as to obtain filtrate a; adding the filtrate a into a hydrogenation reaction kettle, adding a catalyst and an aid, introducing nitrogen to completely react at 20-150 DEG C and 300rpm-1100rpm, and separating and purifying reaction liquid, so as to obtain gabapentin. By adding the aid and changing a heating strategy, the reaction is carried out for one batch under the optimal condition, and then the yield of gabapentin reaches 53.3%; 1-cyanocyclohexyl acetic acid is recycled and hydrogenated for five cycles, the yield of gabapentin reaches above 80% and is increased by 20% than that of a reported chemical process.

This invention relates to synergistic combinations of non-steroidal anti not inflammatory drugs, particularly carprofen, with alpha-2-delta ligands, such as gabapentin or pregabalin, for veterinary treatment of pain and / or inflammation, particularly in dogs, cats and horses.

The invention discloses nitrilase mutant and application thereof. The mutant is obtained by carrying out mutation one or more of the sits including 201 site, 339 site and 343 site of an amino acid sequence as shown in SEQ ID No.2. By modification of protein molecules, the thermal stability of nitrilase AcN pure enzyme is improved by 14 times to a maximum extent, recombinant escherichia coli which contains the nitrilase mutant is used for hydrolyzing 1-cyanocyclohexane acetonitrile at the high temperature (45 DEG C), and the reaction time is shortened to be one third of the original reaction time. Therefore, the acquired mutant has good application prospect in efficient catalysis of the 1-cyanocyclohexane acetonitrile to synthesize 1-cyanocyclohexane acetic acid as a gabapentin intermediate.

The present invention relates to a solid veterinary pharmaceutical composition, of oral administration comprising: a) a drug selected from gabapentin and / or fluoxetine or a pharmaceutically acceptable salt thereof, preferably gabapentin or an acceptable salt thereof in a concentration from 10 to 1000 mg; b) from 10% to 80% of the composition total weight of at least one silicon salt selected preferably from silicon dioxide, colloidal silicon dioxide, calcium silicate, magnesium silicate or combinations thereof; c) from 1% to 20% of the composition total weight of at least one polyoxyethylenated sorbitan ester, preferably selected from sorbitan monolaurate, sorbitan monooleate and sorbitan trioleate, or combinations thereof; and d) one or more pharmaceutically acceptable excipients; such that it is optimally prepared as a veterinary pharmaceutical product that exhibits safety and efficacy in mammalian animals, preferably in companion animals.

The present invention relates to a pharmaceutical composition comprising a combination of trazodone or a salt thereof, and gabapentin or a salt or prodrug thereof, said combination having a synergistic effect in the treatment of pain.