42 results about "Naloxazone" patented technology

Aspects of the invention include topical naloxone compositions for locally delivering naloxone to the skin of a subject. Topical compositions according to certain embodiments are storage stable non-aqueous topical compositions that include naloxone free base and a non-aqueous vehicle, wherein the compositions are substantially free of naloxone N-oxide. Also provided are methods of using the topical compositions to locally deliver naloxone to a subject, as well as kits containing the topical naloxone compositions.

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.

The present disclosure provides a naloxone film product for treatment and prevention of opioid overdoses. Also provided is a method of making the film product. The film product comprises a naloxone composition and at least one polymer.

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 invention presented is a remedial opioid overdose mixture that includes a therapeutically effective dose of an opioid receptor antagonist; and, a therapeutically effective dose of an opioid receptor agonist. In one embodiment, the opioid receptor antagonist is naloxone while the opioid receptor agonist is nalbuphine. One specific naloxone derivative is NX-90 and a specific nalbuphine derivative is NB-33. The mixture can be administered intranasally, intravenously and by autoinjector. In some dose mixtures, reversal time is about three minutes.

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.

Aspects of the invention include topical naloxone compositions for locally delivering naloxone to the skin of a subject. Topical compositions according to certain embodiments are storage stable non-aqueous topical compositions that include naloxone free base and a non-aqueous vehicle, wherein the compositions are substantially free of naloxone N-oxide. Also provided are methods of using the topical compositions to locally deliver naloxone to a subject, as well as kits containing the topical naloxone compositions.

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.

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.

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.

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

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.

Naloxone is commonly used to treat opioid overdose. The present invention presents a combination of naloxone with atipamezole. The invention presents various dosage forms to be administered parenterally, orally or topically. The formulations may also contain a chelating agent such as disodium EDTA. These combination formulations can be used to treat drug addicts.

Provided herein are methods of treating alcohol use disorder (AUD), opioid use disorder (OUD), and other substance use disorders (SUDs) in a subject, for example by administering an oral transmucosal dosage form of esketamine, such as an oral thin film (OTF) form of esketamine, sublingually or buccally. Disclosed methods may combine one or more therapy modalities provided before, during, and / or after drug administration. In some aspects, the methods comprise administering a dose of esketamine that is sufficient to produce dissociative effects in a subject. In some further aspects, the methods comprise the use of specific therapy modalities or ketamine-assisted psychotherapy (KAP) protocols, including manualized relapse prevention cognitive behavioral therapy (CBT). In yet further aspects, the methods comprise ongoing support, including additional psychotherapy and / or adjunct medication, such as naltrexone, buprenorphine, buprenorphine-naloxone, disulfiram, naloxone, and others.

To provide topical naloxone compositions for locally delivering naloxone to the skin of a subject.SOLUTION: A topical composition is a storage stable non-aqueous topical composition comprising naloxone free base and a non-aqueous vehicle, and is substantially free of naloxone N-oxide. The non-aqueous vehicle comprises two or more different polyethylene glycols having different average molecular weights. Also provided are methods of using the topical composition to locally deliver naloxone to a subject, as well as kits containing the topical naloxone compositions.SELECTED DRAWING: None

The present invention relates to a formulation delivery system designed to deliver formulations through a removable cartridge that houses an atomizer and wick assembly. The system is adaptable for multiple medications and environments, including wearable devices such as masks, helmets, and protective suits. The removable cartridge ensures controlled, consistent delivery of medications, including solutions, suspensions, and emulsions. Key features include air-tight seals, sensor technology for cartridge detection and dosage control, and a modular design that allows easy replacement or refilling. This system addresses the challenges of traditional nebulizers by improving portability, ease of use, and precision. It is particularly suited for patients with chronic respiratory conditions or emergency situations where rapid medication delivery, such as naloxone for opioid overdoses, is crucial. The system is also integrated with modern technologies, offering real-time monitoring and feedback to ensure user safety and compliance.

The present invention discloses a morphinone reductase mutant, as well as polynucleotides, expression vectors, host cells, and production methods related to the morphinone reductase mutant. The morphinone reductase mutant provided by the present invention, or cells expressing the morphinone reductase mutant, can convert 7,8-didehydronaloxone into naloxone through a specific bioconversion reaction, effectively removing impurities while increasing naloxone production.

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.

Described herein are syringe devices comprising a syringe including a therapeutic dose of at least one drug to be used in a drug or substance overdose. Also provided herein are compositions and methods of treating opioid overdose using high dose naloxone.

The invention belongs to the technical field of pharmacy, and particularly relates to a naloxone hydrochloride injection and a preparation method thereof. The injection takes water as a solvent and comprises the following components: 1 mg / mL of naloxone hydrochloride, 0.01 mg / mL to 0.05 mg / mL of polyacrylamide, 6 mg / mL to 10 mg / mL of sodium chloride and 0.02 mg / mL to 0.05 mg / mL of sodium thiosulfate. The polyacrylamide in the injection can be combined with naloxone hydrochloride through a chemical bond or a physical effect, so that the interaction between molecules is enhanced, the thermal stability of drug molecules is improved, meanwhile, a stable compound can be formed, and direct exposure of the drug molecules is reduced, so that the degradation rate of the drug molecules at high temperature is reduced; the sodium thiosulfate can form a stable complex with metal ions to remove free radicals in a solution and prevent the free radicals from attacking phenolic groups in naloxone molecules, so that oxidation reaction is reduced, and the product can tolerate an end sterilization process.