4 results about "NALMEFENE HYDROCHLORIDE" patented technology

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.