19 results about "Buprenophine" patented technology

This disclosure relates to 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 polyglycolide polymer, or a copolymer of polylactide and polyglycolide. This 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.

Disclosed herein is deuterated buprenorphine as a protective agent for fetal subjects against full-agonist opioid exposure. Use of deuterated buprenorphine prevents or reduces exposure of the fetus to opioids used by the mother. Use of deuterated buprenorphine may prevent or reduces exposure of the fetus to harmful metabolites of buprenorphine.

This disclosure provides a method for treating a disease in a subject requiring treatment, such as chronic pain or IBS-D, the method of treating the disease by orally administering i) a therapeutically effective amount of buprenorphine dimer, or ii) a pharmaceutical composition comprising a therapeutically effective amount of buprenorphine dimer, wherein the buprenorphine dimer is represented by formula (I) or a pharmaceutically acceptable salt thereof. In particular, the administered buprenorphine dimer of formula (I) is in a neutral form. A method for producing a neutral form of buprenorphine dimer is also described.

The present disclosure provides a method of treating a disease (e.g., chronic pain or IBS-D) in a subject in need thereof by oral administration: i) a therapeutically effective amount of buprenorphine dimer; or ii) a pharmaceutical composition comprising a therapeutically effective amount of the buprenorphine dimer wherein the buprenorphine dimer is represented by Formula (I): or a pharmaceutically acceptable salt thereof, in particular, the administered buprenorphine dimer of Formula (I) is in a neutral form, methods of preparing the buprenorphine dimer in neutral form are also described.

Disclosed in certain embodiments is a method of treating or preventing an opioid-induced adverse pharmacodynamic response comprising administering to a patient in need thereof an effective amount of buprenorphine.

Disclosed herein are methods that may be used for the synthesis of benzylisoquinoline alkaloids (“BIAs”) such as alkaloid morphinan. The methods disclosed can be used to produce thebaine, oripavine, codeine, morphine, oxycodone, hydrocodone, oxymorphone, hydromorphone, naltrexone, naloxone, hydroxycodeinone, neopinone, and / or buprenorphine. Compositions and organisms useful for the synthesis of BIAs, including thebaine synthesis polypeptides, purine permeases, and polynucleotides encoding the same, are provided.

The invention discloses a preparation method of a buprenorphine hydrochloride key intermediate, particularly provides an improved method for preparing 7 alpha [(S)-1-hydroxy-1, 2, 2-trimethylpropyl]-6, 14-diethylidene-6, 7, 8, 14-tetrahydrothebaine, and belongs to the technical field of medical intermediates. The compound is a key intermediate for synthesizing buprenorphine hydrochloride. The solid of the key intermediate is obtained with high yield and high purity through the method, and the method is simple and convenient to operate and suitable for industrial production.

Provided is a pharmaceutical composition including buprenorphine, a derivative thereof, or a pharmaceutically acceptable salt thereof, a stabilizer, a biocompatible solvent, and at least one compound represented by Formula (IIA), (IIB) or (IIC), wherein R1 is hydrogen, a C1-C20 alkylcarbonyl group, or a C6-C18 arylcarbonyl group, and wherein the compound of Formula (IIA), (IIB) and (IIC) each have an amount of less than 1% w / w based on the total weight of the pharmaceutical composition during a shelf life of the pharmaceutical composition. Also provided is a method for preparing the pharmaceutical composition and a method for treating opioid addiction, pain, and / or depression in a subject in need thereof by administering the pharmaceutical composition to the subject.

An injectable pharmaceutical composition comprising a solution of 3-acyl-buprenorphine or a pharmaceutical salt thereof in a biocompatible organic solvent, wherein the injectable pharmaceutical composition exhibits a sustained release profile lasting for more than one week when injected into a patient. The acyl group is an alkylcarbonyl group and an alkyl portion of the alkylcarbonyl group is straight chain, branched chain, having 1-20 carbon atoms. The biocompatible organic solvent is N-methyl-2-pyrrolidone, ethyl acetate, ethanol, butanol, 2-butanol, isobutanol, isopropanol, glycerin, benzyl benzoate, dimethyl sulfoxide, N,N-dimethylacetamide, propylene glycol, dimethyl glycol, benzyl alcohol, or a combination of two or more thereof.

Formulations and methods are described to produce sublingual substance abuse disorder and anti-addiction lozenges. The lozenges may include troche base, ketamine, and buprenorphine. The lozenges may include 0.25 weight percent to 2.53 weight percent ketamine and 0.61 weight percent to 4.88 weight percent buprenorphine. The methods may include placing troche base into a chamber and applying heat to the chamber to melt the troche base. The methods may include adding a first ingredient into the chamber and mixing the first ingredient into the melted troche base. The first ingredient may include ketamine. The methods may include adding a second ingredient into the chamber and mixing the second ingredient into the melted troche base with the first ingredient. The second ingredient may include buprenorphine. The methods may include pouring the melted mixture into a mold. The methods may include cooling the melted mixture in the mold to form the lozenge.

The invention discloses a preparation method and intermediates of various opioid drugs. The invention provides a preparation method of various opioid drugs, and particularly provides a preparation method of a compound as shown in a formula A7 and a series of compounds as shown in a formula A6-2 and the like, the preparation method comprises the following steps: S10, under the action of a cyclization reagent, the compound as shown in the formula A6-2 is subjected to a cyclization reaction as shown in the following formula in an organic solvent, and the compound as shown in the formula A6-2 is obtained. The compound as shown in the formula A7 is obtained. A series of intermediates provided by the invention can be used for divergently synthesizing a plurality of opioid medicines, including naltrexone, nalmefene, nalbuphine, buprenorphine and the like. The preparation method provided by the invention has one or more of the following advantages: cheap and easily available raw materials, short synthesis steps, simple operation, easily amplified process and high product yield.

Disclosed herein are antibodies that specifically bind to buprenorphine and its metabolites norbuprenorphine, buprenorphine glucuronide and norbuprenorphine glucuronide analytes. Such antibodies can be used to detect a buprenorphine analyte in a sample, such as in a homogeneous enzyme immunoassay method. Hapten structures to elicit such antibodies and conjugates useful in immunoassays are also described.

The current methods and compositions provide for a novel and effective therapeutic method for treating opioid use disorder, opioid withdrawal symptoms and / or chronic pain. Accordingly, certain aspects of the disclosure relate to a method for treating opioid use disorder, opioid withdrawal symptoms and / or chronic pain in a subject, the method comprising administering at least one purified cannabinoid compound and a partial opioid agonist. In some embodiments, the method comprises administering a composition comprising cannabidiol and buprenorphine.

The disclosure provides a dosage regimen using sustained-release buprenorphine formulations to produce therapeutic levels of buprenorphine in patients for the treatment of pain or opioid use disorders.

The disclosure provides methods of treating opioid use disorder in a human by rapid induction with monthly injectable extended release buprenorphine, and to rapid induction dosage regimens for treating opioid use disorder. The methods provide increased treatment retention compared to standard of care methods.

Described herein is a method of making chemical compounds useful in pharmaceutical syntheses, e.g. chemical compounds useful as intermediates in or final products of such syntheses, and in particular a method of making chemical compounds useful for the synthesis of buprenorphine, including buprenorphine. In one preferred variant, it is described herein a method of making buprenorphine from oripavine.

Disclosed in the present invention are a preparation method for various opioids and intermediates thereof. Provided in the present invention is a preparation method for various opioids. Specifically, provided are a preparation method for a compound represented by formula A7 and a series of compounds, such as a compound represented by formula A6-2. The preparation method comprises the following step: S10: subjecting a compound represented by formula A6-2 to a cyclization reaction represented by the following formula in an organic solvent under the action of a cyclization reagent, so as to obtain a compound represented by formula A7. A series of intermediates provided by the present invention enables the divergent synthesis of various opioids, including naltrexone, nalmefene, nalbuphine, buprenorphine, etc. The preparation method provided by the present invention has one or more of the following advantages: cheap and readily available raw materials, short synthetic steps, simple operation, easy scale-up of the process, and a high product yield.