77 results about "Codeine" patented technology

A one-pot process for preparing opioid analgesics such as hydrocodone, hydromorphone, and analogues thereof by reacting codeine, morphine, and analogues thereof with hydrogen in a solvent system of benzophenone and neutral solvent in the presence of a metal catalyst followed by oxidation in the presence of potassium tert-alkylate.

A method for the catalytic conversion of codeine, morphine or analogs thereof into hydrocodone, hydromorphone or analogs thereof utilizing a transition metal complex of a tertiary phosphine halide as catalyst.

A method for the catalytic conversion of codeine, morphine or analogs thereof into hydrocodone, hydromorphone or analogs thereof utilizing a transition metal catalyst of the formula [M(PR3R4R5)nXm]p; wherein R1 is H, alkyl, aryl or acyl; M is a Group VIII transition metal; R3, R4 and R5 are selected from the group consisting of alkyl, aryl, alkoxyl, phenoxyl and combinations thereof; X is a halide or an anion; n is 1, 2, 3 or 4; m is 1 or 2; and p is at least 1.

The invention consists of a new formulation of ibuprofen and codeine in the form of a tablet, which comprises L-leucine in a concentration ranging between 4%-15% as a lubricant, in order to prevent the formulation mixture from adhering to the punches and to other elements of the compression machine during the compression process. The new formulation additionally comprises talc (0.5%-5.0%) and silicified microcrystalline cellulose (30%-80%). The formulation is preferably arranged in the form of a core that comprises the active principles and, amongst others, the L-leucine, part of the talc and the silicified microcrystalline cellulose; this core is coated with a composition that contains a copolymer of methacrylic acid and ethyl acrylate. The tablets of the invention do not exhibit flaking problems, have an adequate hardness with a convenient attrition to allow for subsequent coating, offer disintegration values of less than 5 minutes, with dissolution values for both active principles in accordance with those specified for rapid-release tablets.

A morphine component, e.g., a concentrate of poppy straw, is converted into codeine in high yield and high purity and in a highly controlled manner. The conversion process involves the following steps: (a) providing a solution or suspension of a morphine component in an inert solvent or a mixture of solvents; (b) methylating the resultant solution or suspension with a methylating agent in the presence of an alkaline ingredient; and (c) recovering the resultant codeine as the free base or as a salt.

The invention discloses an asarum total lignan extract and a preparation method and application thereof, belonging to the technical field of medicines. The preparation method comprises the following steps: extracting the root and / or tuber of asarum with a polar solvent and then carrying out concentration and drying so as to obtain an asarum total extract; and dissolving the asarum total extract with water, injecting the dissolved asarum total extract into a macroporous adsorption resin, carrying out gradient elution by using an aqueous ethanol solution, collecting eluate, recovering the solvent and carrying out drying so as to obtain the asarum total lignan extract with a content of 60 to 80 wt%, wherein yield of the asarum total lignan extract is 8.4 wt%. Through a great number of pharmacodynamic tests, it is proved for the first time that the asarum total lignan extract has substantial cough-inhibiting and cough reflex sensitivity-lowering effects which are close to the effects of codeine, and it is found out that the asarum total lignan extract has effects on inhibiting airway inflammations, reducing coughing frequencies and prolonging the incubation period of cough, exerts good prevention and treatment effects on a variety of coughs and can be used for preparation of drugs used for treating diseases related to cough. The asarum total lignan extract has the advantages of definite activity, usage of original plants as experimental materials and low cost.

A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine base, oxidation of the dienolsilyl ether congener using peracetic acid, and hydrogenation of the resulting 14-hydroxycodeinone product.

The invention consists of a new formulation of ibuprofen and codeine in the form of a tablet, which comprises L-leucine in a concentration ranging between 4%-15% as a lubricant, in order to prevent the formulation mixture from adhering to the punches and to other elements of the compression machine during the compression process. The new formulation additionally comprises talc (0.5%-5.0%) and silicified microcrystalline cellulose (30%-80%). The formulation is preferably arranged in the form of a core that comprises the active principles and, amongst others, the L-leucine, part of the talc and the silicified microcrystalline cellulose; this core is coated with a composition that contains a copolymer of methacrylic acid and ethyl acrylate. The tablets of the invention do not exhibit flaking problems, have an adequate hardness with a convenient attrition to allow for subsequent coating, offer disintegration values of less than 5 minutes, with dissolution values for both active principles in accordance with those specified for rapid-release tablets.

The invention discloses a column switching LC-MS / MS (Liquid Chromatography-Mass Spectrometry / Mass Spectrometry) analytical method for detecting morphine alkaloid in urine, comprising the following steps of: (1) configuring a double-pump transfusion system and a high-pressure flow path selecting valve system; (2) analyzing a sample according to the set LC-MS / MS condition; and (3) analyzing a result. The limit of detection of the method for morphine, O6-monoacetylmorphine, codeine and acetylcodeine in the urine sample is 0.3-1ng.mL-1, the related coefficient gamma is above 0.9991, and the linear relation is favorable. Meanwhile, the urine sample can be directly injected and analyzed without pretreatment so that the experimental step is simplified, and the cost is saved. The method has the advantages of rapidity, sensitivity, simplicity and reliability and can be widely applied to actual case analysis.

The present disclosure relates to novel methods of treating pain comprising administering to a human in need thereof an effective amount of (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, in free and / or pharmaceutically acceptable salt form, substantially free of the corresponding (−) enantiomer, wherein the human is a heavy drinker and / or binge drinker and / or wherein the human has compromised liver function and / or wherein the human is a codeine non-responder. The present disclosure also relates to a method of treating pain comprising concurrently or sequentially administering to a patient in need thereof an effective amount of (a) (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, in free and / or pharmaceutically acceptable salt form, and (b) acetaminophen. The present disclosure also relates to a method of treating pain comprising simultaneously or sequentially administering to a patient in need thereof an effective amount of (a) (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, in free and / or pharmaceutically acceptable salt form, and (b) a non-steroidal anti-inflammatory drug.