Nalmefene injection and preparation method thereof

A nalmefene and injection technology, which can be applied to pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problem of stability of nalmefene hydrochloride injection, and cannot fully meet the quality requirements. Stability and other issues, to achieve the effect of good stability, reasonable formulation and simple process

Active Publication Date: 2011-11-16
云南龙海天然植物药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the nalmefene injection prepared with reference to the technical scheme disclosed in the instructions of CN1895251 has reduced dimers, it will produce more polar impurities after its sterilization, which still cannot fully meet the requirements of quality stability
The stability problem of nalmefene hydrochloride injection with the above specification of 0.1mg / 1ml is particularly prominent

Method used

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  • Nalmefene injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] prescription:

[0035] Nalmefene Hydrochloride 0.1g

[0036] Sodium chloride 9g

[0037] Tryptophan 0.1g

[0038] Proper amount of hydrochloric acid to pH 3.8

[0039] Sterile water for injection to 1000ml.

[0040]Preparation process: 1) Take nalmefene hydrochloride and add 60% of the total amount of water for injection, and stir until completely dissolved; 2) Add the above-mentioned amount of sodium chloride and tryptophan, stir to dissolve, and add 30% of the total amount of water for injection; 3) ) Use 1.0mol / L hydrochloric acid solution to adjust the pH, and then add the remaining 10% water for injection; 4) Add 0.05% (w / v) activated carbon activated at 115-120°C for 2 hours, and keep stirring at 80°C for 30 minutes , coarsely filtered, decarbonized, and filtered with a composite filter membrane composed of 0.45 μm and 0.22 μm until clear; 5) Filled in a glass ampoule under nitrogen-filled conditions (fill 1ml of liquid in a glass ampoule with a volume of 1ml)...

Embodiment 2

[0043] prescription:

[0044] Nalmefene Hydrochloride 0.1g

[0045] Sodium chloride 9g

[0046] Tryptophan 0.05g

[0047] Proper amount of hydrochloric acid to pH 3.8

[0048] Sterile water for injection to 1000ml.

[0049] Preparation and sterilization process: the same as in Example 1. 1ml glass ampoules are used for dispensing, and the dispensing volume is 1ml. PH value after sterilization: measuring method is the same as embodiment 1, and the result is 3.9.

Embodiment 3

[0051] prescription:

[0052] Nalmefene Hydrochloride 0.1g

[0053] Sodium chloride 9g

[0054] Tryptophan 0.025g

[0055] Proper amount of hydrochloric acid to pH 3.8

[0056] Sterile water for injection to 1000ml.

[0057] Preparation and sterilization process: the same as in Example 1. PH value after sterilization: measuring method is the same as embodiment 1, and the result is 3.9.

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Abstract

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.

Description

technical field [0001] The invention relates to a stable nalmefene hydrochloride injection and a preparation method thereof. technical background [0002] Nalmefene hydrochloride (chemical name: 4,5α-epoxy-6-methylenemorphinan-17-cyclopropylmethyl-3,14diol hydrochloride) is an opioid receptor antagonist that is 6 - Methylene-naltrexone analogs, the chemical structure of which is as follows: [0003] [0004] Nalmefene hydrochloride is white or off-white crystalline powder; easily soluble in water with a solubility of 130mg / ml; slightly soluble in chloroform with a solubility of 0.13mg / ml; pKa is 7.6. [0005] Nalmefene hydrochloride can prevent or reverse the effects of opioids including respiratory depression, sedation and hypotension. Pharmacodynamic studies have shown that the duration of action of nalmefene hydrochloride is longer than that of naloxone under the condition of full reversal dose. Nalmefene hydrochloride has no opioid receptor agonist activity. [00...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/485A61K47/16A61K47/20A61K47/22A61P11/00A61P25/20A61P9/02
Inventor 王晋张丹边玢魏淑冬任爱国
Owner 云南龙海天然植物药业有限公司
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