8 results about "NALMEFENE HYDROCHLORIDE" 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.

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.

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 invention relates to the Nalmefene hydrochloride dihydrate, methods of manufacturing Nalmefene hydrochloride dihydrate, a pharmaceutical composition comprising Nalmefene hydrochloride dihydrate and a method of treatment comprising administering Nalmefene hydrochloride dehydrate.

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.

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.