21 results about "Naloxazone" patented technology

Described herein is a crystalline naloxone-dimethylformamide solvate and methods of making a first and a second amount thereof, as well as methods of making naloxone or a naloxone salt, involving said crystalline naloxone-dimethylformamide solvate. Further described herein is the use of dimethylformamide for preparing said crystalline naloxone-dimethylformamide solvate and the use of said crystalline naloxone-dimethylformamide solvate as a reagent for i.a. purifying naloxone. Moreover, it is described a crystalline naloxone, a use thereof and a method of making it, as well as a mixture comprising dimethylformamide and said crystalline naloxone-dimethylformamide solvate.

Provided are formulations and methods to treat ultra-potent synthetic opioid overdose with high dose Naloxone formulations comprising naloxone hydrochloride or a pharmaceutically acceptable salt thereof, one or more preservatives, one or more buffering agents, a tonicity modifier, and optionally a pH modifier.

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.

Naloxone variants that are both long lasting and responsive are disclosed. One version of the compound has a boron ester functional group and the antagonist compound is capable of a sustained release of antagonist based on reaction with hydrogen peroxide. In addition, a method of treating opioid overdose is disclosed. The method involves administering a therapeutically effective amount of the formulation described above to a patient in need thereof. Administration occurs either intranasally, sublingually or intranasally and sublingually, wherein if administration occurs intranasally and sublingually administration occurs simultaneously, sequentially or concomitantly.

The Overdose Reviver Pressurized Spray, provides two different methods to administer Narcan solution intranasally, containing enough Narcan solution, and pressurized air for at least ten one second 4 mg squirts of Narcan solution with or without a 3″ long extension air tube. To aim from the base of a nostril, depress an atomizing air release valve, administering atomized, pressurized Narcan solution into the nostrils of an unconscious, opioid overdosed person. Or to remove an air release valve, insert a pressurized air canister with Narcan solution into The Overdose Reviver Automatic Inhaler, supplying the necessary pressurized air, and Narcan solution for an Automatic Inhaler to perform its automatic reviving method. Wherein a microprocessor chip detects a life-threatening low heart rate, an Automatic Inhaler will automatically, repeatedly, administer atomized, pressurized Narcan solution into the nostrils of an unconscious opioid overdosed person once every two to three minutes and alert for help.

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.

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.

Aspects of the present invention include topical naloxone compositions for the local delivery of naloxone to the skin of a subject. The topical compositions according to certain embodiments are storage-stable, non-aqueous topical compositions comprising a free naloxone base and a non-aqueous solvent, wherein said compositions are substantially free of naloxone N-oxide. The present invention also provides methods for using said topical compositions to locally deliver naloxone to a subject, and kits containing said topical naloxone compositions.

A method of producing promorphinan, morphinan, nal-opioid, and nor-opioid alkaloid products through the increased conversion of a promorphinan alkaloid to a morphinan alkaloid. The method comprises contacting the promorphinan alkaloid with at least one enzyme. Contacting the promorphinan alkaloid with the at least one enzyme converts the promorphinan alkaloid to a morphinan alkaloid.

Described herein are compositions, devices, and methods useful for treating (reversing) and / or preventing fentanyl overdose resulting in respiratory failure or airway obstruction (FIVCC). Compositions are provided that include optimized amounts and / or ratios of two active ingredients, including: an alpha 2 adrenergic receptor agonist (e.g., lofexidine, dexmedetomidine, clonidine) and a short acting mu opioid receptor antagonist (e.g., naloxone); an alpha 2 adrenergic receptor agonist and a long acting mu opioid receptor antagonist (nalmefene); and an alpha 2 adrenergic receptor agonist and a fentanyl opioid analgesic. Methods and devices for concurrent delivery of combined active ingredients are also provided.

A method of producing promorphinan, morphinan, nal-opioid, and nor-opioid alkaloid products through the increased conversion of a promorphinan alkaloid to a morphinan alkaloid. The method comprises contacting the promorphinan alkaloid with at least one enzyme. Contacting the promorphinan alkaloid with the at least one enzyme converts the promorphinan alkaloid to a Morphinan alkaloid.

Aspects of the invention include topical naloxone compositions for topical delivery of naloxone to the skin of a subject. The topical composition according to certain embodiments is a storage stable non-aqueous topical composition comprising a naloxone free base and a non-aqueous solvent wherein the composition is substantially free of naloxone N-oxide. The invention also provides a method for locally delivering naloxone to a subject by using the external use composition, and a kit containing the external use naloxone composition.

A pharmaceutical composition in the form of droplets for oral administration is disclosed. The pharmaceutical composition is an aqueous solution comprising sodium chloride in an amount of 0.6% to 3% by weight per volume, at least one active ingredient selected from naloxone, yohimbine, albuterol, epinephrine, buprenorphine, and exosomes in an amount of 0.01% to 25% by weight per volume, and having a pH from 3 to 7.5. The composition is converted into droplets with diameters of 0.5 to 5 microns using an atomizer with a vibrating mesh membrane undergoing piezoelectric vibration at a frequency of 25 to 400 kilohertz. The process involves providing the composition in a capsule, inserting the capsule into the atomizer, and activating the atomizer to produce droplets. This system provides precise, efficient, and patient-friendly oral delivery of medications.

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a morphine naloxone pharmaceutical composition and application thereof.The morphine naloxone pharmaceutical composition comprises morphine sulfate and naloxone hydrochloride as active ingredients, and the weight ratio of morphine sulfate to naloxone hydrochloride is 1: 1-6: 1; the invention also provides an application of the morphinaloxone pharmaceutical composition in preparation of a medicine for treating pain. The pharmaceutical composition is good in dissolution property and good in stability, and the technical problem of misuse of morphine sulfate can be avoided.

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 first selective SuFEx antagonists to μ-opioid receptors (MOR) were developed by functionalizing an opioid scaffold with an SO2—F warhead. Our model, based on a MOR structure with antagonist β-FNA, indicates the naloxone carbonyl as an advantageous point for derivatization as it is chemically accessible and is not involved in interaction with receptors. Of the three accessible Tyr residues in MOR pocket, Tyr77, Tyr130 and Tyr150, Tyr150 in proximity to the carbonyl of the docked naloxone was selected as a target, which resulted in the development of highly potent antagonists.

Provided herein are drug products adapted for nasal delivery comprising a device and a pharmaceutical composition comprising an opioid receptor antagonist, wherein the claimed invention provides a unit dose of an aqueous pharmaceutical solution, or aqueous pharmaceutical composition, housed in a device configured for intranasal administration to a patient, wherein the aqueous pharmaceutical solution consists of, or the aqueous pharmaceutical composition consists essentially of: (i) naloxone hydrochloride in an amount of about 9% by weight based on the total weight of the aqueous pharmaceutical solution; (ii) glycerin in an amount of about 1.4% by weight based on the total weight of the aqueous pharmaceutical solution; (iii) a citrate buffer system adjusted by hydrochloric acid and / or sodium hydroxide; and (iv) United States Pharmacopeia (USP)-grade Purified Water; wherein the pH of the aqueous pharmaceutical solution is from about 3.5 to about 4.7; and wherein the hydrochloric acid and the sodium hydroxide may each be independently present in the aqueous pharmaceutical solution, as required, to achieve the pH from about 3.5 to about 4.7.

The present invention relates to an intranasal pharmaceutical dosage form comprising a dosing unit comprising naloxone or a pharmaceutically acceptable salt thereof in an amount of equivalent to ≥0.5 mg naloxone HCl dissolved in an application fluid of a volume of ≤250 μl. Furthermore, the present invention relates to such an intranasal pharmaceutical dosage form for use in the treatment of opioid overdosing and / or at least one symptom thereof.

Methods for treating stimulant-induced agitation include administering naloxone (NLX) and dexmedetomidine (DEXMED) to a subject in need thereof. Treatment can be directed to a subject having concurrent opioid intoxication and stimulant intoxication. Administration of NLX and DEXMED can include co-administration of NLX and DEXMED or separate administration of NLX and DEXMED to the subject. Administration of DEXMED to the subject can occur at a time when the subject exhibits one or more signs of opioid intoxication and / or at a time when the subject does not exhibit excessive restlessness and movement. Pharmaceutical compositions which include NLX and DEXMED in an amount sufficient to treat concurrent opioid intoxication and stimulant intoxication are also provided.

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.

Described herein are i) sequestering agents and ii) central nervous system (CNS) active agents for the treatment of intoxication due to toxic agents such as drugs of abuse, and associated symptoms. Also disclosed herein, are a cucurbituril and naloxone for use in the treatment of opioid overdoses through sequestering and excretion of the bound molecule of interest through the urine. Also provided herein, are kits and methods of treatment of the disclosure.