60 results about "Buprenophine" patented technology

Disclosed herein are novel buprenorphine monocarboxylic ester derivatives and dibuprenorphine dicarboxylic ester derivatives which exert a longer analgesic effect as compared to buprenorphine hydrochloride. Also disclosed are the processes for synthesizing the novel ester derivatives of buprenorphine, and long-acting analgesic pharmaceutical compositions containing a compound selected from buprenorphine base and the novel ester derivatives of buprenorphine.

Transdermal therapeutic systems for administering analgesics, preferably buprenorphine or one of its pharmaceutically acceptable salts or pro-drugs, and processes for the production of such systems.

The present invention is directed to a buprenorphine sustained release delivery system capable of delivering buprenorphine, a metabolite, or a prodrug thereof for a duration of about 14 days to about 3 months. The buprenorphine sustained release delivery system includes a flowable composition and a solid implant for the sustained release of buprenorphine, a metabolite, or a prodrug thereof. The implant is produced from the flowable composition. The buprenorphine sustained release delivery system provides in situ 1-month and 3-month release profiles characterized by an exceptionally high bioavailability and minimal risk of permanent tissue damage and typically no risk of muscle necrosis.

There is provided a method for the synthesis of norbuprenorphine, and ultimately buprenorphine, utilizing oripavine as the starting material. Conventional methods of producing buprenorphine utilize thebaine as the starting material, requiring an O-demethylation step, typically a low to moderate yield transformation. The present use of oripavine as a starting material does not require an O-demethylation step, since the oripavine molecule lacks an O-3 methyl group.

The present invention is directed to a buprenorphine sustained release delivery system capable of delivering buprenorphine, a metabolite, or a prodrug thereof for a duration of about 14 days to about 3 months. The buprenorphine sustained release delivery system includes a flowable composition and a solid implant for the sustained release of buprenorphine, a metabolite, or a prodrug thereof. The implant is produced from the flowable composition. The buprenorphine sustained release delivery system provides in situ 1-month and 3-month release profiles characterized by an exceptionally high bioavailability and minimal risk of permanent tissue damage and typically no risk of muscle necrosis.

The present invention is directed to a buprenorphine sustained release delivery system capable of delivering buprenorphine, a metabolite, or a prodrug thereof for a duration of about 14 days to about 3 months. The buprenorphine sustained release delivery system includes a flowable composition and a solid implant for the sustained release of buprenorphine, a metabolite, or a prodrug thereof. The implant is produced from the flowable composition. The buprenorphine sustained release delivery system provides in situ 1-month and 3-month release profiles characterized by an exceptionally high bioavailability and minimal risk of permanent tissue damage and typically no risk of muscle necrosis.

Disclosed are prodrugs and analogs of buprenorphine.

This disclosure relates to a buprenorphine sustained release delivery system for treatment of conditions ameliorated by buprenorphine compounds. The sustained release delivery system includes a flowable composition containing a suspension of buprenorphine, a metabolite, or a prodrug thereof.

The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R1, R2, R8, R3a, R 3b, G, X, Z and Y are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

A patch comprising an adhesive layer formed on one surface of a flexible support, wherein said adhesive layer containing a drug, an absorption enhancer and an adhesive comprising; (i) said drug is buprenorphine hydrochloride and / or buprenorphine, and (ii) said absorption enhancer is a mixture of polyoxyethylene sorbitan mono fatty acid ester having 6 to 20 of oxyethylene units and 12 to 18 of carbon number of fatty acid ester, and at least one selected from the group consisting of liquid higher fatty acid ester, 60 to 180 of molecular weight of liquid poly hydric alcohol, lactic acid and triacetin, and (iii) said adhesive is an acrylic-based adhesive.

The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II, Formula III, Formula IV, and Formula V, wherein R1, R2, R3a, R3b, R15a, R15b, X, Q, G, and Y are as defined herein.Compounds of the Invention are useful for treating pain and other conditions modulated by activity of opioid receptors.

The invention provides processes for the production of opiate alkaloids. In particular, the present invention provides processes for the formation of buprenorphine and derivatives of buprenorphine that minimizes the formation of impurities.

The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II or Formula III shown below, wherein R1, R2, R8, R3, R3a, R3b, X, Z and Y are as defined herein, R1 H3CO (I) OCH3 OCH3 (III) Compounds of the Invention are useful for treating pain and other conditions modulated by activity of opioid and ORL1 receptors.

A buprenorphine hydrochloride / naloxone hydrochloride sublingual tablets with low misuse potential , said tablets contain medicinal contents of buprenorphine hydrochloride and naloxone hydrochloride, part by weight thereof is 2:1-6:1, 1) using alcohol to dissolve regulator corrigent and bond of PH of prescription amount for use; 2) grinding main medicine buprenorphine hydrochloride / naloxone hydrochloride, filler and lubricant and sifting out thereof; 3) mixing evenly the prescription amount of buprenorphine hydrochloride / naloxone hydrochloride, filler, bond and disintegrating agent, thereafter adding contents in step 1 to prepare into soft stuff, again making into pellet, drying, sorting out, adding lubricant again, mixing evenly and pressing into tablet.

The invention relates to transdermal therapeutic system for the transdermal administration of buprenorphine, comprising a buprenorphine-containing self-adhesive layer structure comprising A) a buprenorphine-impermeable backing layer, and B) a buprenorphine-containing pressure-sensitive adhesive layer on said buprenorphine-impermeable backing layer, the adhesive layer comprising a) at least one polymer-based pressure-sensitive adhesive, b) an analgesically effective amount of buprenorphine base or a pharmaceutically acceptable salt thereof, c) a viscosity-increasing substance in an amount of about 0.1% to about 8% of said buprenorphine-containing pressure-sensitive adhesive layer, and d) a carboxylic acid selected from the group consisting of oleic acid, linoleic acid, linolenic acid, levulinic acid and mixtures thereof, in an amount sufficient so that said analgesically effective amount of buprenorphine is solubilized therein to form a mixture including said viscosity-increasing substance, and wherein the carboxylic acid-, buprenorphine- and viscosity-increasing substance-containing mixture forms dispersed deposits in the said pressure-sensitive adhesive, and wherein said buprenorphine-containing pressure-sensitive adhesive layer is the skin contact layer.

The present invention provides compound having the structure and pharmaceutically acceptable salts or derivatives thereof, as well as compositions including such compounds. The invention also provides methods of (1) preventing pain, (2) treating pain, (3) inducing sedation, (4) treating opiate addiction, (5) treating opiate withdrawal (abstinence syndrome) and / or (6) treating cough in a patient in need thereof by administering a compound or composition of the invention.

The present invention is directed to oral pharmaceutical compositions of buprenorphine and it pharmaceutically acceptable salts and the use thereof.

There is provided an efficient industrial process for the preparation of 21-cyclopropyl-7α-(2-hydroxy-3,3-dimethyl-2-butyl)-6,14-endo-ethano-6,7,8,14-tetrahydro-oripavine, i.e. buprenorphine of Formula-I in high yield and purity, with enhanced safety and eco-friendly norms. The invention further relates to an improved process for preparation of intermediates thereof in high yield and purity.

Formulation comprising buprenorphine or a pharmaceutically acceptable salt thereof as the sole active ingredient, a viscosity enhancer, and a buffering agent in an amount to provide a pH of from 5.0 to 7.0 are useful for treating opioid withdrawal syndrome.

A method of treating postoperative pain in a patient undergoing a surgery is described. The method is based on preoperative administration of a buprenorphine-containing transdermal dosage form. The dosage form can be administered to the patient, for example, 1-4 days prior to surgery. Alternative embodiments of the invention include subsequent transdermal dosage forms to treat the postoperative pain.

The invention relates to an improved method of preparing buprenorphine, a salt thereof, analogues of buprenorphine and their salts. In particular, the invention relates to a method of preparing buprenorphine and related products and salts in economic and ecologic ways having increased yields.

The invention relates to transdermal therapeutic system for the transdermal administration of buprenorphine, comprising a buprenorphine-containing self-adhesive layer structure comprisingA) a buprenorphine-impermeable backing layer, andB) a buprenorphine-containing pressure-sensitive adhesive layer on said buprenorphine-impermeable backing layer, the adhesive layer comprisinga) at least one polymer-based pressure-sensitive adhesive,b) an analgesically effective amount of buprenorphine base or a pharmaceutically acceptable salt thereof, andc) a carboxylic acid selected from the group consisting of oleic acid, linoleic acid and linolenic acid, levulinic acid and mixtures thereof, in an amount sufficient so that said analgesically effective amount of buprenorphine is solubilized therein to form a mixture, and the carboxylic acid buprenorphine mixture forms dispersed deposits in the said pressure-sensitive adhesive,wherein said buprenorphine-containing pressure-sensitive adhesive layer is the skin contact layer.

Described is a transdermal device comprising a backing layer; a single layer adhesive matrix comprising buprenorphine or a salt thereof, a pressure sensitive adhesive including a silicone-type adhesive blended with an acrylate-type adhesive, a solubilizer, a permeation enhancer, and a crystallization inhibitor; and a release layer. Also described is a method of relieving pain and a method of preparing a transdermal delivery system.

Disclosed are crystalline forms of 3-acyl-buprenorphine derivatives and sustained release injectable pharmaceutical compositions for treatment of opioid dependence, pain or depression, including an aqueous suspension of crystalline 3-acyl-buprenoprhine, or a pharmaceutically acceptable salt thereof, wherein the composition does not include an organic solvent, a polylactide polymer, a polyglycolidepolymer, or a copolymer of polylactide and polyglycolide. The disclosure also includes 3-acyl-buprenoprhine or a pharmaceutically acceptable salt thereof prepared in a controlled release matrix, including poly (lactide-co-glycolide), sucrose acetoisobutyrate, lecithin, diolein and a combination of two or more thereof.

Ester derivatives of the phenolic hydroxyl group of buprenorphine are described that can be used in the treatment of opiate dependency and / or moderate to severe pain. The esters have an enhanced bioavailability, an enhanced duration of action, and a reduced abuse potential.

There is provided an efficient industrial process for the preparation of 21-cyclopropyl-7α-(2-hydroxy-3,3-dimethyl-2-butyl)-6,14-endo-ethano-6,7,8,14-tetrahydro-oripavine, i.e. buprenorphine of Formula-I in high yield and purity, with enhanced safety and eco-friendly norms. The invention further relates to an improved process for preparation of intermediates thereof in high yield and purity.

Formulations comprising buprenorphine are useful for treating opioid withdrawal syndrome.