17 results about "Nalmefene" patented technology

The subject matter disclosed describes a method of treating pruritus in a subject with cholestatic liver disease in need thereof, comprising administering a therapeutically effective amount of nalmefene to the subject, wherein the subject achieves an improvement in pruritus within 24 hours following administration of nalmefene.

The invention relates to the technical field of medicines, and provides a nalmefene hydrochloride injection and a preparation method thereof, every 1000 injections comprise the following components in parts by weight: 2.0 g of nalmefene hydrochloride based on nalmefene, 18g of osmotic pressure regulator, 0.05-0.1 g of meglumine, and the balance of water for injection to 2000mL. The preparation method comprises the following steps: S1, adding the osmotic pressure regulator and the meglumine in a prescription dosage into the water for injection which accounts for 90% of the total amount of the prescription dosage, stirring until the osmotic pressure regulator and the meglumine are dissolved, and regulating the pH value to 3.5-4.0 through a hydrochloric acid solution; s2, adding a prescription amount of nalmefene hydrochloride into the solution in the step S1, stirring until the nalmefene hydrochloride is dissolved, and adjusting the pH value to 3.5-3.8; and S3, adding water for injection to the total amount, uniformly stirring, filtering, canning into an ampoule bottle, sterilizing, carrying out lamp detection for leakage detection, and packaging. By adding a small amount of meglumine, the amount of the dinalmefene impurity generated by long-term placement and oxidation of the nalmefene hydrochloride injection can be reduced, adverse reactions possibly caused by a large amount of meglumine are reduced, the content of the dinalmefene impurity is maintained at a low level, and the use safety of the injection is improved.

This invention discloses a stable nalmefene hydrochloride injection and its preparation method, relating to the field of biomedical technology. The injection consists of nalmefene hydrochloride, sodium chloride, hydrochloric acid, and water for injection, and contains no metal ion chelating agents, with a pH value controlled between 3.5 and 3.6. The method includes: preparing the solution and adjusting the pH under high-purity nitrogen protection in a solution preparation system with low metal ion introduction risk; filtering the solution through a polyethersulfone membrane with low metal leaching, and then filling it into ampoules with a vulcanized inner surface. This invention, through the systematic integration of multiple measures such as source control of the solution preparation system, inert atmosphere protection, precise pH control, surface passivation of packaging materials, and the use of high-purity materials, synergistically inhibits the metal ion catalytic oxidation of the active ingredient, ensuring that the content of the key degradation impurity II (2,2'-bisnalmefene) remains stably below the quality standard during long-term storage, solving the problem of chemical stability control of products in chelator-free formulations, and combining safety and process robustness.

The presently disclosed subject matter is directed to an effective method of treating chronic kidney disease-associated pruritus. Particularly, the method comprises the transmucosal administering of nalmefene to treat chronic kidney disease-associated pruritus, as well as cholestatic pruritus and / or prurigo nodularis. The nalmefene can be configured in a single layer film comprising at least two distinct domains. The film can include a first discrete domain comprising about 50-100 weight percent polymer matrix and the second discrete domain can comprise the nalmefene or pharmaceutically acceptable nalmefene salt.

The invention discloses an application of a metabolite level detection reagent in preparation of a diagnostic kit for adenoma in a colorectal progression stage. A metabolite is selected from the group consisting of tridecane diacid, methyl 1-(methyl sulfur) propyl disulfide, histidine proline amide, termite dialdehyde, N-acetylglycine, 5-hydroxycaprin, arginyl glutamine, nalmefene and sodium alginate. The compound is selected from at least one of dialaphos and dipifolin. According to the invention, 11 kinds of differential metabolites which change continuously in the colorectal lesion progress process are screened from the serum exosome, and the 11 kinds of metabolites have good identification capability on the stage of colorectal lesion, and have good application prospects in screening and diagnosis of adenoma and colorectal cancer in the colorectal progression stage. And the method has great clinical significance in distinguishing the malignant degree of colorectal adenoma.

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.

Drug products adapted for nasal delivery, comprising a pre-primed device filled with a pharmaceutical composition comprising nalmefene are provided. Methods of treating opioid overdose with the drug products are also provided.

This application discloses nalmefene base, its preparation method, and its application, belonging to the field of pharmaceutical technology. The preparation method of nalmefene includes the following steps: mixing nalmefene hydrochloride with water to form an aqueous solution of nalmefene hydrochloride; reacting the aqueous solution of nalmefene hydrochloride with an aqueous solution of an alkaline component to form nalmefene base; the pH of the nalmefene hydrochloride is 4.0-6.5; the alkaline component includes at least one selected from sodium carbonate, sodium bicarbonate, potassium carbonate, potassium bicarbonate, sodium acetate, ammonia, and sodium dihydrogen phosphate. This application uses nalmefene hydrochloride with a pH of 4.0-6.0 to undergo a desalting reaction with an aqueous solution of a strong base-weak acid salt or a weak base, crystallizing out nalmefene base. This effectively controls the particle size and shape of nalmefene base, obtaining small-particle-size, low-content, stable, and poorly soluble tablet-shaped nalmefene base without pulverization. It is less prone to burst release, meeting the requirements for sustained-release formulations, and the reaction is mild, green, and economical.

This disclosure provides devices, delivery systems, medicaments, and methods for use to rescue a subject identified in need thereof from opioid overdose. In certain embodiments, the device is an injection device (such as, an autoinjector) for intramuscular or subcutaneous administration of a medicament comprising a therapeutically effective amount of nalmefene or a pharmaceutically acceptable salt thereof.

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.

The application is directed to an efficient process for crystallizing nalmefene hydrochloride in a hydrated form from an aqueous hydrochloric acid solution (or a mixture) with a high yield.

The present disclosure provides a method for using nalfurafine or nalmefene for activating JNK / PRDX6 to stimulate localized peroxide production that causes G-protein depalmitoylation and deactivation of kappa opioid receptors (KORs) in a subject; a method for using nalfurafine or nalmefene for inactivating kappa opioid receptors responsible for dysphoria during mu-opioid withdrawal in a subject; a method for using nalfurafine or nalmefene for promoting stress resilience in a subject recovering from polysubstance withdrawal; a method for using nalfurafine or nalmefene for inactivating kappa opioid receptor responsible for the dysphoria and psychotomimetic effects of kappa opioid agonists administered to a subject for the treatment of pruritus or for the promotion of diuresis; and a method for using nalfurafine or nalmefene in combination with a kappa opioid agonist for the treatment of neuropathic pain in a subject.

The invention provides an in-situ gel composition containing xenomeline. The in-situ gel composition containing xenomeline is prepared from 1 to 30 percent of xenomeline, 25 to 50 percent of a slow-release carrier material and 30 to 70 percent of a solvent. The slow-release carrier material is selected from one or more of sucrose acetate isobutyrate (SAIB), polyorthoester (POE) and poly (lactic-co-glycolic acid) (PLGA). The composition can be applied by injection, forms a gelatinized medicine storage cavern at an administration part, continuously delivers medicines, and has a remarkable long-acting slow-release effect and good stability and safety.

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.

The present invention relates to the field of pharmaceutical preparations, and in particular to a composition of a nalmefene hydrochloride nasal preparation and a preparation method therefor. The nalmefene hydrochloride nasal preparation comprises: nalmefene hydrochloride or a hydrate thereof and dodecylphosphorylcholine. A product of the nalmefene hydrochloride nasal preparation is absorbed by the nasal cavity rapidly, so that the problems of inconvenient administration and slow onset of existing preparations are solved, and the technical effect of providing safe, effective, and convenient clinical use is realized.

To provide a method and device for treating pruritus associated with chronic kidney disease. [Solution] The subject matter of this disclosure relates to an effective method for treating pruritus associated with chronic kidney disease. Specifically, the method comprises administering nalmefene transmucosally to treat pruritus associated with chronic kidney disease, as well as cholestatic pruritus and / or nodular prurigo. The nalmefene is disposed on a monolayer film comprising at least two distinct domains. The film may contain a first distinct domain comprising about 50–100 weight percent of a polymer matrix, and the second distinct domain may contain nalmefene or a pharmaceutically acceptable nalmefene salt.

The present invention relates to the field of pharmaceutical technology and provides a nalmefene hydrochloride injection and a preparation method thereof. Each 1,000 injections comprise the following components in parts by weight: 2.0 g of nalmefene hydrochloride, 18 g of an osmotic pressure regulator, and 0.05 to 0.1 g of meglumine, with water for injection added to 2,000 mL. The preparation method comprises the following steps: S1. adding the prescribed amount of the osmotic pressure regulator and meglumine to 90% of the total amount of water for injection, stirring until dissolved, and adjusting the pH to 3.5 to 4.0 with a hydrochloric acid solution; S2. adding the prescribed amount of nalmefene hydrochloride to the solution in step S1, stirring until dissolved, and adjusting the pH to 3.5 to 3.8; S3. adding water for injection to the full amount, stirring thoroughly, filtering, sealing in an ampoule, sterilizing, inspecting for leaks with a light source, and packaging. By adding a small amount of meglumine, the amount of dinalmefene impurities produced by oxidation of nalmefene hydrochloride injection during long-term storage can be reduced, the adverse reactions that may be caused by the use of a large amount of meglumine can be reduced, and the content of dinalmefene impurities can be maintained at a low level, thereby improving the safety of the injection.