54 results about "NALMEFENE HYDROCHLORIDE" patented technology

A high-stability nalmefene hydrochloride injection is prepared from nalmefene hydrochloride (0.005-0.2 W / v %) and the medicinal carrier chosen from sodium chloride, glucose, beta-cyclodextrin, dextran, pectose, sorbitol, etc. Its preparing process is also disclosed.

The invention relates to a stable nalmefene injection and a method for preparing the same. The nalmefene hydrochloride injection has the advantages of reasonable formulation, simple process, and good stability. After a test of keeping stand the injection under high temperature condition for 10 days and a test of accelerating at the temperature of 40 DEG C for 6 months, the appearance property, the pH value, the content of active components, the related substances and the like of a sample are not changed obviously.

The invention relates to a nalmefene hydrochloride injection for injection. The preparation is composed of an effective amount of nalmefene hydrochloride and an appropriate amount of pharmaceutical carrier, wherein the concentration of nalmefene hydrochloride in the preparation can be 0.005%-0.2%. (w / v), its content range in each unit preparation is generally 0.1-4mg; the pharmaceutical carrier can be one of sodium chloride, glucose, β-cyclodextrin, dextran, fructose, sorbitol, etc. Or several, preferably sodium chloride and glucose, its content range in each unit preparation can be 4.5mg~90mg, or glucose can be 25mg~400mg; Sodium bisulfite can be 0.005mg~0.5mg; Disodium amine tetraacetate can be 0.001mg ~ 0.5mg; appropriate amount of hydrochloric acid or acetic acid, adjust the pH value of the solution before dispensing this product to 3.5 ~ 5.5. The preparation process of nalmefene hydrochloride injection adopts a nitrogen filling process, and the sterilization conditions can be sterilized at 105°C for 45 minutes or autoclaved at 115°C for 20 minutes or autoclaved at 121°C for 15 minutes. It is preferably autoclaved at 115°C for 20 minutes. The appearance, clarity, pH value, content and related substances of nalmefene hydrochloride injection had no obvious changes after 10 days of strong light irradiation and high temperature storage and 6 months after accelerated test.

Method for producing nalmefene hydrochloride from naltrexone, which method is particular well adapted for large-scale industrial application, and has been found to be efficient, to give a high yield and to afford highly pure nalmefene hydrochloride salt.

The invention discloses a nalmefene hydrochloride injection, which is solution prepared from nalmefene hydrochloride and usable pharmaceutical excipients dissolved in injection water. The pharmaceutical excipients comprise an antioxidant and an osmotic pressure modifier. The nalmefene hydrochloride injection is characterized in that: the weight ratio of nalmefene to the antioxidant in the nalmefene hydrochloride is 1:0.1-1.0; and the antioxidant is mixed by one or more of tertiary butyl hydroxy anisole, 2,6-di-tert-butyl-4-methyl-phenol and rosemary. The injection is stable in property and ensures medication safety.

The invention discloses a formula of a pharmaceutical composition containing nalmefene hydrochloride for injection. The pharmaceutical composition is characterized in that an injection does not contain a chelating agent, and comprises effective dose of nalmefene hydrochloride and a defined amount of pharmaceutical carrier, wherein the concentration of the nalmefene hydrochloride in the injection can be 0.01-0.2 percent (w / v), the content of the nalmefene hydrochloride in each unit of injection is 0.1-2.0mg; an osmotic pressure regulator can be sodium chloride or glucose, preferably, sodium chloride, the content of the osmotic pressure regulator in each unit of injection is 4.5-22.5mg; the pH value of the injection is regulated to be 3.2-4.5 by using hydrochloric acid. The invention further discloses a preparation method of the formula of the injection. The preparation method comprises the steps of in a blending process, regulating the pH value of a solution to be 6.0-9.0 by using alkaline in first time, and after adsorbing by using active carbon, regulating the pH value of the solution to be 3.2-4.5 by using acid in second time. The formula of the injection containing the nalmefene hydrochloride is simple, and is stable in quality; the preparation method is simple in process, simple and convenient to operate, and more suitable for industrialized production.

The invention belongs to a technical field of medicines. Specifically, the invention relates to a nalmefene hydrochloride compound and a preparation method thereof. Nalmefene hydrochloride is a derivative of water-soluble naltrexone, and due to the chemical structure of 6-bit methylene of the nalmefene hydrochloride, the nalmefene hydrochloride has the characteristics of long action time, more medication ways, high bioavailability, less side effects, stronger physiological activity, easier biofilm penetration and the like, has different degrees of effects on keeping the normal functions of breathing, circulation, digestion, endocrine and nervous systems, and is applied to the antagonism of respiratory depression of narcotic analgesics, the treatment of heart failure and shock, the treatment of alcoholism and addiction, weight loss and the like. According to the invention, the drug stability is improved, and the medication safety is ensured.

The invention provides a nalmefene preparation to be administered through nasal cavity, which comprises nalmefene, namefene free alkali or other pharmaceutically acceptable medicinal salt of nalmefene and absorption promoting agent, a large number of tests have shown that, the nasal cavity administered medicinal preparation by the invention can make the medicament absorbed through the path of nasal mucosa, and enter into blood circulation for actions. The advantages of the preparation include stabilized performance, controlled quality and non-stimulation to nasal cavity.

The invention relates to a nalmefene hydrochloride preparation method, nalmefene hydrochloride preparation process is improved, the new process is easier to operate and easier to control, the production cycle is shortened, and the environment pollution is reduced, so that the new technology is more safe and reliable to meet the requirement of large scale production.

The invention provides a nalmefene preparation to be administered through nasal cavity, which comprises nalmefene, namefene free alkali or other pharmaceutically acceptable medicinal salt of nalmefene and absorption promoting agent, a large number of tests have shown that, the nasal cavity administered medicinal preparation by the invention can make the medicament absorbed through the path of nasal mucosa, and enter into blood circulation for actions. The advantages of the preparation include stabilized performance, controlled quality and non-stimulation to nasal cavity.

The present invention relates to an improved process for recovery of nalmefene hydrochloride [17-(cyclopropylmethyl)-4,5- alpha-epoxy-6-methylenemorphinan-3,14-diol hydrochloride] from an aqueous composition containing nalmefene and certain impurities.

The invention relates to a pharmaceutical composition containing a nalmefene hydrochloride compound. For every 1000 injections, the pharmaceutical composition comprises the following components: 100mg of nalmefene hydrochloride, 1-2g of Tween 80, 1-3g of EDTA (Ethylene Diamine Tetraacetic Acid) calcium, 1-2g of vitamin C, 1000ml of sodium hydrogencitrate and trisodium citrate buffer liquor with molar ratio of 1:4, and the balance of water for injection.