29 results about "Naltrexone" patented technology

The disclosure relates to compositions comprising a phentermine and a unicyclic aminoketone and methods of use thereof. The methods of use include inducing weight loss or reducing weight gain in a human subject. The unicyclic aminoketone may be diethylpropion or bupropion. In some embodiments, the compositions further include tadalafil or naltrexone.

A single unit oral dose pharmaceutical composition for use as a medicament for separate, sequential or simultaneous administration with an agonist of a 5-hydroxytryptamine (5-HT) receptor;wherein the single unit oral dose pharmaceutical composition comprises a first active ingredient and a second active ingredient;wherein the first active ingredient is for absorption in the gastrointestinal tract from the oesophagus onwards and the second active ingredient is for absorption in the oral cavity; andwherein the first active ingredient is naltrexone in an amount of 0.01 to 10 mg and the second active ingredient is calcitriol in an amount of 80 to 200 ug.

A formulation of naltrexone that ameliorates undesirable localized reactions at the site of implantation.

Disclosed is a compound sustained release implant of naltrexone and risperidone, and a preparation method and application thereof, which belong to the technical field of implant preparation. The naltrexone compound sustained-release implant includes naltrexone, risperidone, a degradable material A, a degradable material B, an additive and a lubricant. By controlling a mass ratio of naltrexone to risperidone to be (20-30):1, a weight-average molecular weight of the degradable material A to be 10-15W, and a weight-average molecular weight of the degradable material B in risperidone microspheres to be 2W-4W, the compound sustained release implant of naltrexone and risperidone can not only effectively inhibit amphetamine type drug relapse and reduce side effects of risperidone, but also realize the synchronous release of naltrexone and risperidone.

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 application belongs to the technical field of medicine synthesis, and provides a preparation method of naltrexone, wherein norethoxy-morphinone and cyclopropylmethanol are used as raw materials, and PdCl2 (Xantphos) is used as a catalyst to perform reaction. The application has the characteristics of simple operation, mild reaction condition and the like, and the yield and purity of the obtained product are high, and the application is more suitable for industrial production.

This application relates to a method for detecting related substances in a pharmaceutical composition containing naltrexone and risperidone, comprising the following steps: preparing a test solution from the pharmaceutical composition containing naltrexone and risperidone; and detecting the test solution using high-performance liquid chromatography (HPLC), wherein the HPLC detection conditions include: (1) a chromatographic column consisting of a C18 column and a silica-bonded phenyl column arranged in series; and (2) mobile phases A, B, and C being buffer solutions, acetonitrile, and methanol at different volume percentages, respectively; each buffer solution being an aqueous solution of sodium octanesulfonate with a pH of 2.25–2.35. The detection method can effectively separate and detect multiple related substances in a pharmaceutical composition containing naltrexone and risperidone.

A recombinant microbial host cell having improved in vivo conversion of reticuline and derivatives thereof (such as thebaine and / or oripavine) to relevant downstream opioids (such as neopinone, oripavine, northebaine, nororipavine or morphinone) and related compounds (such as heroin, morphine, codeine, thebaine, oripavine, oxycodone, hydrocodone, hydromorphone, oxymorphone, buprenorphine, naltrexone, naloxone or nalbuphine), wherein the microbial (such as fungal) host cell is heterologously expressing at least one functional transporter protein capable of transporting reticuline or a derivative thereof (such as thebaine and / or oripavine) and a heterologously expressed enzyme capable of acting upon reticuline or a derivative thereof. The invention also relates to uses of the microbial host cells and methods of making an opioid compound and / or opioid precursor compound and / or opioid derivative of interest.

A combination therapy for use in treatment of substance abuse disorders, including alcohol use disorder (AUD) and opioid use disorder (OUD), includes both mitragynine (MG) and naltrexone (NTX). NTX is understood to be a mu opioid antagonist that is expected to block MG's analgesic effects. However, combining MG and NTX therefore results in a unique, unexpected, and beneficial treatment that decreases alcohol self-administration to a greater extent than either alone.

A method of treating a wound may include topically administering a statin composition including a statin selected from atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin, or combination thereof. The statin composition may be administered in an ointment, powder, or liquid format. The method may also include topically administering one or more antimicrobial drugs and / or naltrexone.

The invention provides naloxone-loaded adhesive hydrogel as well as a preparation method and application thereof, and relates to the technical field of adhesive hydrogel. The naloxone-carrying adhesive hydrogel is obtained by cross-linking boric acid oxidized chondroitin sulfate and methacrylated gelatin; and naloxone and hectorite nano particles are loaded in the naloxone carrying adhesive hydrogel. The naloxone-loaded hydrogel constructed by the invention is used for repairing damage of bone and nervous tissues, naloxone is used as a small molecule drug, has more stable physical and chemical properties, is easier to store, and also has the functions of promoting osteogenesis and neurogenesis, so that the combined use of various bioactive factors is reduced; and the naloxone-carrying adhesive hydrogel has adhesive performance, can effectively fill a bone defect area and form a stable repair microenvironment, and accelerates the bone and nervous tissue regeneration efficiency.

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.

To provide a method for producing an antibody or a functional fragment thereof that can specifically bind to naloxone and naltrexone.SOLUTION: The method comprises the steps of: immunizing a non-human animal with a conjugate comprising the structure of Formula III, thereby inducing B cells that produce an antibody binding to the conjugate (A is -O-, -N-, or -S-; B is -CO-, a lower alkyl, -CONH-, -SO2-, or the like; C is a carrier protein; and R2 is an allyl or cyclopropyl group); and obtaining an antibody or a functional fragment thereof produced by the B cells.SELECTED DRAWING: Figure 1

Bivalent ligands which bind to MOR-CCR5 heterodimers are provided. The bivalent ligands comprise two discrete pharmacophores, naltrexone and maraviroc, linked by a spacer and bind to MOR-CCR5 heterodimers, e.g. at the surface of a cell. The bivalent ligands are useful in assays to detect MOR-CCR5 heterodimers, as therapeutic agents to prevent and / or treat diseases characterized by the presence of MOR-CCR5 heterodimers.

Disclosed are method for predicting naltrexone response in subjects with AUD. In some embodiments, the methods include performing or having performed one or more methylation assays on a genomic DNA sample isolated from the subject to determine the methylation status of one or more regions of the isolated genomic DNA, wherein the one or more regions are subsequences of a gene selected from a mu opioid receptor (OPRM1) gene, a catechol-O-methyltransferase (COMT) gene, and a dopamine transporter (SLC6A3) gene, wherein the methylation status of the one or more regions of the isolated genomic DNA determined is predictive of naltrexone response in the subject. Also provided are method for treating patients diagnosed with AUD with the medication naltrexone based on a methylation status of a combination of specific methylation sites located associated with an OPRM1 gene, a COMT gene, and / or an SLC6A3 gene in obtained from each AUD patient.

To provide antibodies or functional fragments thereof which can specifically bind to naloxone and / or naltrexone, and methods of production thereof.SOLUTION: The invention provides: antibodies or functional fragments thereof which include heavy chain variable regions CDR1, CDR2, and CDR3 each having a specific amino acid sequence and light chain variable regions CDR1, CDR2, and CDR3 each having a specific amino acid sequence; methods of production of the antibodies or functional fragments thereof; and compositions comprising the antibodies or functional fragments thereof and detectable labels attached thereto.SELECTED DRAWING: Figure 1

The invention relates to a method for monitoring the treatment of a subject undergoing therapy with an active that is naltrexone or a metabolite or analogue thereof, comprising:measuring the gene expression profile of any of the genes listed in Table 1 or Table 2, in a sample of CD3+ cells obtained from the subject undergoing treatment;wherein if the expression of any of the genes in Table 1 is increased compared to a control, or if any of the genes listed in Table 2 is decreased compared to a control the active is being administered at an effective level.

There is disclosed a liquid resin extended-release oral naltrexone formulation suspension comprising from, about 1,0 mg / ml to about 10.0 mg / ml naltrexone in a resin, wherein no more than 30% of the total naltrexone dose administered is released within one hour and wherein no more than 60% of the total naltrexone dose administered is released within two hours. Specifically, there is disclosed a method for treating a child with an autism- type disorder with approximately a teaspoon (about 5 ml) of a liquid resin extended-release oral naltrexone formulation suspension comprising from about 1.0 mg / ml to about 10.0 mg / ml naltrexone in a resin, wherein no more than 30% of the total naltrexone dose administered is released within one hour and wherein no more than 60% of the total naltrexone dose administered is released within two hours.

Described are pharmaceutical formulations comprising naltrexone and / or bupropion. Such pharmaceutical formulations can comprise extended-release, multilayer beads. Also described are methods of administering such formulations, such as for the treatment of overweight or obesity.

The present application relates to compositions comprising flumazenil and naltrexone and methods of use thereof. In particular, the present invention relates to a pharmaceutical composition comprising a microdose of flumazenil and a microdose of naltrexone, or a pharmaceutically acceptable salt thereof, where the flumazenil and naltrexone are present in a weight ratio of about 25: 1 to about 10: 1, where the composition is in the form of a single dose unit, and wherein the single dose unit comprises flumazenil in an amount that provides a daily microdose in the range of about 250 to about 7,500 micrograms and naltrexone in an amount that provides a daily microdose in the range of about 25 to about 1,000 micrograms. The present invention also relates to methods of treating depression and / or anxiety and / or post traumatic stress disorder (PTSD) using a combination of flumazenil and naltrexone.

A method of treating a wound may include topically administering a statin composition including a statin selected from atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin, or combination thereof. The statin composition may be administered in an ointment, powder, or liquid format. The method may also include topically administering one or more antimicrobial drugs and / or naltrexone.

The present invention discloses a responsive full-cyanine small molecule near-infrared fluorescent probe targeting MOR, its synthesis method and application. The fluorescent probe is a compound with the structural formula shown in (I) or a pharmaceutically acceptable salt thereof. The fluorescent probe constructed by the present invention is based on a full-cyanine fluorescent dye and the MOR antagonist naltrexone, with low synthesis cost and simple operation. It can specifically identify MOR and produce a considerable fluorescent signal after binding to the hydrophobic region of MOR, avoiding washing operations and detecting MOR with high sensitivity. The fluorescent probe described in the present invention has a stable skeleton structure and is suitable for real-time monitoring of MOR on the cell membrane of living cells under a confocal microscope. The fluorescent probe described in the present invention plays an important role in the study of the binding kinetics of MOR and various ligands, and can also be used for screening ligands that specifically bind to MOR receptors. #imgabs0#

Antibodies that specifically bind naloxone and / or naltrexone are disclosed. Also disclosed are conjugates used in the production of the antibodies, as well as methods of producing the antibodies. Also disclosed are methods of using the antibodies in direct assays for naloxone and / or naltrexone. Further disclosed are methods of reducing naloxone and / or naltrexone interference in opiate assays using the antibodies.

The invention discloses a (+)-naltrexone derivative and an application of the (+)-naltrexone derivative in treatment of amphetamine drug addiction. Compared with the (+)-naltrexone, the (+)-naltrexone derivative has the advantages that the anti-neuroinflammatory activity is obviously improved, the anti-inflammatory activity of most of the derivatives is improved by 1000 times or more, and the anti-inflammatory activity of the derivative with the highest activity is even improved by 10000 times or more.

The present invention provides an agent that increases the expression of BAD, for use in the treatment of cancer in conjunction with a chemotherapeutic agent wherein the agent is selected from the list consisting of 6-β-naltrexol, naloxone, methyl naltrexone, or pharmaceutically acceptable salts thereof.

Antibodies that specifically bind naloxone or naltrexone are disclosed. Also disclosed are conjugates used in the production of the antibodies, as well as methods of producing the antibodies. Also disclosed are methods of using the antibodies in direct assays for naloxone or naltrexone. Further disclosed are methods of reducing naloxone or naltrexone interference in opiate assays using the antibodies.

The invention belongs to the technical field of medical intermediates, and provides a preparation method of a samidoprofen intermediate 3-formamide naltrexone. The preparation method comprises the following steps: mixing naltrexone, ethylene glycol, p-toluenesulfonic acid and toluene, and carrying out a reflux reaction to obtain a compound A; mixing the compound A, organic alkali and dichloromethane to obtain a mixed solution, dropwise adding trifluoromethanesulfonic anhydride into the mixed solution, and reacting to obtain a compound B; mixing the compound B, amine and N, N-dimethylformamide, and introducing carbon monoxide for reaction under the condition of a palladium catalyst to obtain a compound C; and adding the compound C into acid for hydrolysis reaction. According to the preparation method, highly toxic zinc cyanide does not need to be used, carbon monoxide is adopted as a carbonyl donor, and raw materials are easy to obtain; the reaction pressure is 0.1-0.5 MPa, the reaction conditions are mild, and industrial production is facilitated; the total molar yield of the 1, 3-formamide naltrexone reaches 71% or above, and the purity reaches 98.0% or above.

A formulation of naltrexone that ameliorates undesirable localized reactions at the site of implantation.

Described are pharmaceutical formulations comprising naltrexone and / or bupropion. Such pharmaceutical formulations can comprise extended-release, multilayer beads. Also described are methods of administering such formulations, such as for the treatment of overweight or obesity.