19 results about "Pregabalin" patented technology

The invention relates to the technical field of veterinary drugs, and particularly provides a pregabalin oral liquid and a preparation method thereof. Each 100ml of the pregabalin oral liquid comprises 10 to 35g of a pregabalin solid dispersion, 0.01 to 1g of a flavoring agent, 0.01 to 2g of a preservative, a pH regulator and water, and the pH value of the pregabalin oral liquid is 4.5 to 5.5. The pregabalin oral liquid is high in stability, strong in compliance, high in bioavailability and good in clinical effect.

This invention discloses bridged tricyclic γ-aminobutyric acid (GABA) derivatives targeting the α2δ subunit of voltage-gated calcium channels. These compounds exhibit enhanced binding affinity and improved pharmacological profiles. They aim to overcome limitations of current α2δ ligands like gabapentin and pregabalin. The new derivatives show potential for treating neuropathic pain, epilepsy, and related disorders.

Described herein are method of treating pain associated with osteoarthritis (OA) using a low dose of an oral drug conjugate of naproxen and pregabalin. Described herein are method of addressing sleep disturbance in a subject in pain using an oral drug conjugate of naproxen and pregabalin.

The present invention relates to a topical pharmaceutical composition comprising pregabalin and a reduced micellar phospholipid as an active ingredient, which results in a prolonged analgesic effect of pregabalin. The product can reduce neuropathic pain by at least 5 hours.

Compositions, kits and systems containing pregabalin haptens, immunogens and / or protein conjugates are disclosed. Methods of producing and using the pregabalin haptens, immunogens, and conjugates are also disclosed.

This invention relates to the fields of genetic engineering and protein modification technology, specifically to a lipase mutant and its application in the synthesis of a key chiral intermediate of pregabalin. This invention relates to *Thermophilus spp.* (…). Thermomyces lanuginosus Based on lipase TL, through extensive mutation screening, a lipase mutant with significantly improved catalytic efficiency for the hydrolysis of ethyl 2-carboxyethyl-3-cyano-5-methylhexanoate (CNDE) was finally obtained. Among them, the single-point mutant containing S254A has a catalytic constant... K The cat value reached 100.2, which is 45 times that of the wild type, and the enantioselectivity ee value was also higher than that of the wild type, achieving unexpected technical results. This lipase mutant has broad prospects for the efficient synthesis of key chiral intermediates of pregabalin.

The invention discloses an olefin reductase SeER mutant and application thereof in synthesis of chiral drugs, and provides a series of novel olefin reductase SeER mutants capable of efficiently and asymmetrically reducing beta-alkyl / aryl-beta-cyanoacrylate compounds, and the olefin reductase SeER mutants have high conversion rate (gt; 99% conversion rate), good enantioselectivity (gt; 99% ee), the substrate range is wide (gt; according to the present invention, the screened olefin reductase SeER mutant can be successfully synthesized into the chiral GABA derivative drugs such as pregabalin and brivaracetam through the chemical-enzyme coupling method, such that the overall reaction yield is improved, and the route is simple;

This application relates to the field of veterinary drug formulation technology, and discloses a cat anti-stress oral formulation containing pregabalin and its preparation method. The raw materials include: pregabalin-L-arginine co-ground micronized powder, isostearic acid, medium-chain triglycerides, hydrophobic fumed silica, and anhydrous yeast extract powder. The preparation method includes the following steps: weighing each raw material by mass; dissolving isostearic acid in medium-chain triglycerides by heating and stirring; starting high-speed dispersion under vacuum and constant temperature; introducing pregabalin-L-arginine co-ground micronized powder for reaction; introducing anhydrous yeast extract powder for dispersion; cooling and switching to low-speed stirring; adding hydrophobic fumed silica and running under vacuum; finally, static aging and packaging to obtain the finished product. This invention employs a technical solution of compounding pregabalin-L-arginine co-ground micronized powder, isostearic acid, and hydrophobic fumed silica in the oil phase, achieving the technical effect of thixotropic formulation and long-term static non-sedimentation.

The invention relates to a preparation method of hydrogel loaded with lidocaine hydrochloride and pregabalin and the hydrogel. The preparation method comprises the following steps: mixing hyaluronic acid, dopamine hydrochloride and pure water to prepare a solution A, and then preparing a nano cellulose suspension through an ultrasonic dispersion and magnetic stirring method; the preparation method comprises the following steps: preparing a nano-cellulose suspension, mixing and stirring lidocaine hydrochloride, pregabalin, carboxymethyl chitosan and the nano-cellulose suspension to prepare a solution B, mixing the solution A with the solution B, and carrying out step-by-step oxidation crosslinking treatment to finally obtain the hydrogel loaded with lidocaine hydrochloride and pregabalin. According to the invention, the mechanical strength and adhesion strength of the hydrogel are improved, the drug loading rate, drug loading stability and release controllability are ensured, and the synergistic treatment effect of first rapid analgesia and then long-acting nerve regulation is realized.

A veterinary tablet immediate release formulation comprising: about 25% by weight of pregabalin; from 5% to 15% by weight of a meat flavour; from 58% to 69% by weight of microcrystalline cellulose; and from 1% to 2% by weight of a lubricant such as magnesium stearate. Said composition for use in treating neuropathic pain in a non-human animal.

The invention relates to a pharmaceutical composition in the form of an orally deliverable liquid composition comprising pregabalin as an active ingredient and to the use thereof in the treatment and prevention of transportation and veterinary visit anxiety and fear in companion animals, such as cats. The composition is stable, well palatable to animals and can be easily administered by the pet owner.

The invention relates to the technical field of gene engineering and protein modification, in particular to a lipase mutant and application thereof in synthesis of a pregabalin key chiral intermediate. According to the invention, on the basis of thermomyces lanuginosus lipase TL, a large amount of mutation screening is carried out, so that the lipase mutant of which the catalytic efficiency of hydrolysis of 2-carboxyethyl-3-cyano-5-methyl ethyl hexanoate (CNDE) is remarkably improved is finally obtained. Wherein the catalytic constant Kcat of the single-point mutant containing S254A reaches 100.2 and is 45 times of that of a wild type, the enantiomer selectivity ee value of the single-point mutant containing S254A is also higher than that of the wild type, and an unexpected technical effect is achieved. The lipase mutant can be applied to efficient synthesis of a pregabalin key chiral intermediate, and has a wide prospect.

The present application relates to the technical field of biology, in particular to a method for synthesizing a pregabalin intermediate by using immobilized hydantoinase. The pregabalin intermediate with an optical purity of more than 99.9% is obtained by catalyzing the reaction of a substrate 3-isobutyl succinimide under the action of immobilized enzyme; wherein the amino acid sequence of the immobilized enzyme is shown in SEQ ID No. 1. The present application is immobilized by using specific enzyme under specific conditions, and the stability and purity of the enzyme are improved after the treatment, the optical purity of the product is more than 99.9%, and 50 batches of stable application are realized.

The invention discloses a pregabalin liquid composition. The pregabalin liquid composition is prepared from pregabalin, a solvent and an optional surfactant, the solvent is selected from soybean oil, sesame oil, corn oil, mineral oil, propylene carbonate, glycerol formaldehyde or a combination thereof. The pregabalin liquid composition provided by the invention is suitable for oral administration, stable at room temperature, convenient for administration, short in onset time and small in side effect, and can be used for preparing medicines for treating and / or preventing feline transportation and treatment anxiety disorder.

The invention belongs to the technical field of medicine preparation, and particularly relates to a perampanel sustained release microsphere, a pharmaceutical preparation and a preparation method based on membrane emulsification. The invention firstly provides a preparation method which comprises the following steps: (1) dissolving perampanel and a polylactic acid-glycolic acid copolymer in an organic solvent to prepare an oil phase; (2) preparing a water phase; (3) adding the oil phase into the water phase to prepare a pre-emulsion; (4) adding the pre-emulsion into a membrane emulsifier, and dispersing to obtain an emulsion; and (5) curing to obtain the drug microspheres. By strictly controlling the membrane emulsification process, the drug microspheres with uniform size and stable quality are obtained.

The present invention relates to a method for purifying pregabalin, comprising the following steps: 1) heating a reaction solution, maintaining the temperature and removing impurities; and 2) adding an acid into the reaction solution in step 1) to adjust the pH value, crystallizing and centrifugally drying the solution to obtain high-purity pregabalin. The pregabalin prepared and obtained by employing the purification method of the present invention has a product purity that reaches 99.8% or above, a product yield of 90% or above, an impurity X and impurity Y content that is ≤0.05%, and has no detected impurity peak the relative retention time of which is 1.3.

The invention belongs to the field of medicine synthesis, and relates to (2E, 4E)-N-cyclopropyldecyl-2, 4-dienamide as well as a preparation method and application of the (2E, 4E)-N-cyclopropyldecyl-2, 4-dienamide. The structure of the (2E, 4E)-N-cyclopropyldeca-2, 4-dienamide is shown as a formula I. The preparation method comprises the following steps: carrying out oxidation reaction on (2E, 4E)-2, 4-decadienal (compound II) to obtain a compound III, carrying out condensation reaction on the compound III and cyclopropylamine (compound IV) to obtain (2E, 4E)-N-cyclopropyldeca-2, 4-dienamide (compound I), and carrying out condensation reaction on the (2E, 4E)-N-cyclopropyldeca-2, 4-dienamide (compound I) and (2E, 4E)-N-cyclopropyldeca-2, 4-dienamide (compound II) to obtain the (2E, 4E)-N-cyclopropyldeca-2, 4-dienamide. The 2, 4-dienamide has the effect of preventing or treating nervous system related diseases, and in a pharmacodynamic test of a mouse neuralgia model, in a similar pain value range, the required dosage of the compound I is smaller than that of a contrast drug pregabalin.

The application discloses a method for determining degradation impurities and excipients in Pregabalin oral solution by HPLC, selects octadecylsilane bonded silica gel as a stationary phase, and uses a mixed solvent of an organic phase and a buffer as a mobile phase for gradient elution. The method can separate the degradation impurities and excipients in the Pregabalin oral solution under the same chromatographic condition, and the separation is fast and efficient, so that the detection result of the related substances of the product is exclusive and reliable, and the quality of the preparation can be effectively controlled. The detection method has strong specificity, high precision, good accuracy and convenient operation, and can effectively control the quality of the medicine.

The application discloses a small-molecule twin drug compound with synergistic analgesic effect, a pharmaceutical composition, a preparation method and application thereof. The twin drug molecule is formed by covalently connecting a drug A and a drug B, wherein the drug A is nefopam, and the drug B is gamma-aminobutyric acid (GABA) and an analogue thereof, including gabapentin, pregabalin, GABA, methoxycarbonyl-gamma-aminobutyric acid (MGB), and cligabalin. The analgesic efficacy of the twin drug molecule is superior to that of combined administration and single drug, the twin drug molecule can obviously improve various acute and chronic inflammatory pains and relieve peripheral neuropathic pain induced by paclitaxel, has higher anti-inflammatory activity than that of combined administration and single drug, and thus has the potential to treat pain, inflammation and inflammation-related diseases, and can effectively reduce the interaction between drugs and increase the medication compliance of patients.