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Pharmaceutical composition containing nalmefene hydrochloride for injection

A technology of nalmefene and water for injection, which is applied in the direction of drug combination, medical preparations containing active ingredients, drug delivery, etc., and can solve the problems of high dinalmefene content, high production cost, and low industrial application value

Active Publication Date: 2014-04-09
CHENGDU GUOHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In order to overcome the problems of high content of degraded impurity dinalmefene after long-term storage in nalmefene hydrochloride injection produced by the prior art, short validity period, and complicated existing prescriptions, which lead to high production cost and low industrial application value, etc., provide A kind of nalmefene hydrochloride injection and its preparation process that can obtain low impurity content, long shelf life, and simple prescription, simple process flow, suitable for large-scale industrial production, the present invention provides the following technical scheme:

Method used

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  • Pharmaceutical composition containing nalmefene hydrochloride for injection
  • Pharmaceutical composition containing nalmefene hydrochloride for injection
  • Pharmaceutical composition containing nalmefene hydrochloride for injection

Examples

Experimental program
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Effect test

Embodiment 1

[0167] prescription:

[0168] Nalmefene hydrochloride 0.1g (calculated as nalmefene)

[0169] Sodium chloride 4.5g

[0170] L-arginine hydrochloride 0.5g

[0171] Hydrochloric acid Adjust pH to 3.2

[0172] Add water for injection to 1000ml.

[0173] Process: Take the full amount of sodium chloride and L-arginine hydrochloride in the prescription tank, add water for injection, stir to dissolve, adjust the pH to 3.2-3.5 with 0.2mol / L hydrochloric acid solution, and then add the prescription The full amount of nalmefene hydrochloride, stir to dissolve, then add water for injection to the full amount, after coarse filtration, fine filter with a 0.22μm microporous membrane until it is clear, and carry out semi-finished product inspection, the control content is 0.45mg / ml~0.55mg / ml ml, pH=3.2, after passing the inspection, fill it under the protection of nitrogen, steam sterilize at 115°C for 30 minutes, check for leaks, light inspection, label and pack, and make...

Embodiment 2

[0175] prescription:

[0176] Nalmefene hydrochloride 2.0g (calculated as nalmefene)

[0177] Sodium chloride 22.5g

[0178] L-arginine hydrochloride 4.5g

[0179] Hydrochloric acid Adjust pH to 4.5

[0180] Add water for injection to 1000ml.

[0181] Process: Take the full amount of sodium chloride and L-arginine hydrochloride in the prescription tank, add water for injection, stir to dissolve, adjust the pH to 4.5-4.8 with 0.1mol / L hydrochloric acid solution, and then add the prescription The full amount of nalmefene hydrochloride, stirred to dissolve, and then add water for injection to the full amount, after coarse filtration, fine filter with a 0.22μm microporous membrane until it is clear, and carry out semi-finished product inspection, the control content is 2.45mg / ml~2.55mg / ml ml, pH=4.5, after passing the inspection, fill it under the protection of nitrogen, steam sterilize at 120°C for 15 minutes, check for leaks, light inspection, label and pack, ...

Embodiment 3

[0183] prescription:

[0184] Nalmefene hydrochloride 0.1g (calculated as nalmefene)

[0185] Sodium chloride 22.5g

[0186] L-arginine hydrochloride 0.5g

[0187] Hydrochloric acid Adjust pH to 3.2

[0188] Add water for injection to 1000ml.

[0189] Process: Take the full amount of L-arginine hydrochloride and sodium chloride in the prescription and add it to the water for injection. After dissolving, adjust the pH to 3.2 with hydrochloric acid, add water for injection to 1000ml, add 1.0g of activated carbon, and decolorize at room temperature for 30 minutes. After decolorization is completed Filtrate with a 0.22 μm filter membrane, add the full amount of nalmefene hydrochloride to the filtrate, stir to dissolve, filter with a 0.22 μm filter membrane, fill with nitrogen, fill and seal, sterilize with damp heat at 121°C for 12 minutes, check for leaks, light inspection, labeling, Packed and made into 1000 samples.

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Abstract

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.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing nalmefene hydrochloride for injection and a preparation method thereof. Background technique [0002] Nalmefene hydrochloride is a new generation of pure opioid receptor antagonist synthesized after naloxone and naltrexone. It was developed by Ivax / Ohmeda company in the United States and was first approved by the FDA in 1995. The marketed dosage form is injection. At present, nalmefene hydrochloride has become a substitute for naloxone. Compared with naloxone and naltrexone, it has the advantages of long action time, high oral bioavailability, small dosage, and wide safety range. Nalmefene hydrochloride has a wide range of clinical uses, and has been used to antagonize the symptoms of respiratory depression, sedation and hypotension caused by narcotic analgesics, and has been used in the treatment of alcoholism and heroin dependen...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/18A61K47/04A61K47/26A61K31/485A61P11/16A61P25/26A61P9/02A61P39/02A61P25/36
Inventor 汪飞郭礼新郭晖
Owner CHENGDU GUOHONG PHARMA
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