32 results about "Pregabalin" patented technology

The present invention relates to an orodispersible tablet manufactured by a wet granulation method comprising pregabalin or pharmaceutically acceptable salts thereof, at least one disintegrant, at least one diluent, at least one binder, at least one glidant, at least one lubricant, and one or more pharmaceutically acceptable excipients. The orodispersible tablet prepared using these excipients exhibits desirable properties such as facilitating disintegration, and dissolution of the drug for oral administration. Further, the present invention also relates to the process for preparing the said solid pharmaceutical composition.

The application discloses a sustained-release pregabalin composition and a preparation method thereof, and belongs to the technical field of medicine, and specifically relates to a sustained-release pregabalin composition and a preparation method thereof. The sustained-release pregabalin composition comprises the following components in parts by weight: 45-50 parts of pregabalin or a pharmaceutically acceptable salt thereof; 23-35 parts of a matrix forming agent; 23-30 parts of a swelling agent, wherein the swelling agent is a double-layer network structure, a first layer network provides support for a second layer network, and the two are crosslinked in a physical and chemical manner; 15-25 parts of a sustained-release agent; and 12-20 parts of a filling agent. The first layer network comprises chitosan, sodium alginate, methacrylic anhydride, a photoinitiator and zinc ions; and the second layer network comprises cyclodextrin, polyethylene glycol dimethacrylate, methacrylamide, a crosslinking agent, a photoinitiator and deionized water. The sustained-release tablet of the application is expanded to more than 13 mm after 1.5 h, and the tablet can remain intact, which is beneficial to the retention of the sustained-release pregabalin composition in the stomach, achieves the effect of sustained release, and improves the absorption of pregabalin.

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.

The invention discloses a pregabalin capsule which comprises the following raw materials in parts by weight: 7-9 parts of pregabalin, 12-21.6 parts of a filling agent, 0.5-1.5 parts of a lubricating agent and 90-110 parts of a gelatin hollow capsule, wherein the filling agent is a mixture of acetylated corn starch and lipidosome coated lactose. The pregabalin capsule is used for solving the technical problem that the stability of the pregabalin capsule is poor.

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 provides attapulgite modified gel. The attapulgite modified gel is prepared from the following raw materials: attapulgite, pregabalin, sodium alginate, carboxymethyl cellulose, calcium carbonate and D-glucolactone. The attapulgite, the sodium alginate and the carboxymethyl cellulose are mixed and cross-linked, the unique layer chain crystal structure of the attapulgite endows the gel with excellent adhesion and mechanical properties, so that the gel can be tightly attached to skin or tissues, and meanwhile, the attapulgite, the sodium alginate and the carboxymethyl cellulose have a synergistic effect to construct a stable three-dimensional network with a pore structure; the pregabalin hydrogel prepared by the preparation method disclosed by the invention is favorable for improving the continuous release performance of the gel to pregabalin, reducing the burst release phenomenon of pregabalin in application, prolonging the drug effect time of the hydrogel and meeting clinical treatment requirements.

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;

The application discloses an olefin reductase, a coding gene, a carrier, an engineering bacterium and application thereof, wherein the olefin reductase SeER mutant is obtained by single-point or multi-point site-directed mutation or site-directed saturation mutation of the 38th, 117th, 248th, 293rd and 373rd sites of the amino acid sequence shown in SEQ ID NO. 2. The application provides a series of new olefin reductase SeER mutants capable of efficiently stereocomplementary reduction of olefin compounds to prepare chiral compounds, and successfully synthesizes chiral GABA derivative drugs such as phenibut, baclofen, tolperisone and pregabalin through a chemical-enzyme coupling method. Compared with existing methods, the strain can flexibly regulate the configuration of the product, and has high stereoselectivity and conversion rate.

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.

Described herein are method of treating neuropathic pain using topical naproxen and pregabalin conjugate formulations.

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 provides hydantoinase and application thereof in preparation of pregabalin precursors and other analogues, and belongs to the technical field of medicinal chemistry. The invention provides hydantoinase PSDHP1. The amino acid sequence of the hydantoinase PSDHP1 is shown as SEQ ID NO: 1. The hydantoinase PSDHP1 is a biological chiral enzyme for synthesis of a pregabalin precursor, is resistant to high temperature and strong alkali, and still has high chiral rate, high reaction rate and enantiomer excess rate eegt under the environment of 80 DEG C and pH 10; and the reaction rate Vmax is 37.1 g product / min / mol enzyme. In addition, the hydantoinase PSDHP1 has the characteristics of low cost, environmental friendliness and no secondary pollution.

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.

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

The present invention relates to an orally disintegrating tablet comprising pregabalin or a pharmaceutically acceptable salt thereof, sucralose as a sweetener, and tomatine.

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 discloses a purification method and a new crystal form of pregabalin, and the purification method comprises the following steps: (1) enabling pregabalin and organic alkali to form a salt in a ketone solvent, dissolving the salt in the ketone solvent, then cooling the solution to 0-10 DEG C, stirring, separating out a solid, and filtering to obtain a salt wet product of pregabalin; and (2) adding the wet salt product of pregabalin into a mixed solvent composed of a ketone solvent and water, heating to completely dissolve the salt of pregabalin, dropwise adding an acid, adjusting the pH value of the solution to 2.0-5.0, cooling, stirring, and precipitating crystals, in the mixed solvent composed of the ketone solvent and water, the volume ratio of the ketone solvent to the water is 3.5: 1-1.5: 1. The pregabalin crystal obtained by the purification method of the pregabalin is high in purity and high in yield. The obtained pregabalin crystal is in a novel crystal form, is a rhombus or blocky polyhedron, has good fluidity, and is suitable for preparing tablets or capsules.

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.

An orodispersible tablet of pregabalin for oral administration comprising 15-60%w / w pregabalin or a pharmaceutically acceptable salt thereof; at least one diluent; a least one disintegrant comprising 0.1-10 %w / w; at least one lubricant comprising 0.1-5 %w / w; at least one binder comprising 0.1-10 %w / w; at least one glidant comprising 0.1-10 %w / w; and at least one or more pharmaceutically acceptable excipients; wherein the orodispersible table is disintegrated upon contact with saliva in less than 3 minutes. The diluent is preferably a combination of microcrystalline cellulose and mannitol; the disintegrant is preferably croscarmellose sodium; the binder is preferably low substituted hydroxypropyl cellulose; the glidant is preferably a combination of talc and colloidal anhydrous silica; and the lubricant is preferably magnesium stearate. The ratio of the lubricant to the diluent may be in the range of 1:70 to 1:90, preferably 1:75 to 1:85. The tablet may further comprise a sweetener, flavouring agent and / or sucralose. Methods of manufacturing the tablet via wet granulation are also provided. The tablet may release 85% of the pregabalin within 80 minutes, preferably within 60 minutes.

The present invention relates to a pharmaceutical composition comprising (a) (i) a combination of Trazodone or a salt thereof, and (ii) Gabapentin or Pregabalin or Milnacian or a salt thereof or a prodrug thereof, and (b) at least one pharmaceutically acceptable excipient, for the treatment of neuropathic pain, wherein the pharmaceutical composition comprises Trazodone:Gabapentin or Pregabalin or Milnacian in a weight ratio of between 1:40 and 1:100, preferably below 1:40 and up to 1:100.