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Stabilized nalmefene hydrochloride injection and its preparation

A technology for injection and nalmefene, applied in the field of nalmefene injection and its preparation, can solve the problems of cumbersome clinical use, increase production cost and the like, and achieve the effects of reasonable formulation, good stability and simple process

Active Publication Date: 2009-09-09
西藏易明西雅医药科技股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although freeze-dried powder injection can improve the stability of the preparation, the freeze-drying process of more than 30 hours has greatly increased the production cost, and nalmefene is mainly used for first aid, and the powder injection needs to be dissolved in water for injection during clinical use. use, making clinical use more cumbersome

Method used

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  • Stabilized nalmefene hydrochloride injection and its preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] prescription:

[0023] Nalmefene Hydrochloride 0.1g

[0024] Sodium chloride 9g

[0025] Proper amount of hydrochloric acid to pH3.6

[0026] Process: 1) Take 1000ml of water for injection and put it in the liquid mixing tank, add the full amount of sodium chloride prescribed, and stir until dissolved; 2) Add the prescribed amount of nalmefene hydrochloride, stir until dissolved; then use a 0.22 μm microporous filter membrane Fine filtration until clarity; 3) filling in a glass ampoule (filling 1ml of liquid in a glass ampoule with a volume of 2ml); 4) melting and sealing. 5) Sterilize at 115°C for 20 minutes. 5) Capping, labeling, packaging, and the finished product after passing the inspection. PH value after sterilization: Take 10 sticks of this product, combine them, and measure according to the law (Appendix VI H of Part Two of the Chinese Pharmacopoeia Edition in 2000), and the pH value is 3.9.

Embodiment 2

[0028] prescription:

[0029] Nalmefene Hydrochloride 1g

[0030] Sodium chloride 9g

[0031] Proper amount of hydrochloric acid to pH3.8

[0032] Technology: with embodiment 1. 2ml glass ampoules are used for dispensing, and the dispensing volume is 2ml.

[0033] PH value: measuring method is the same as embodiment 1, gets the solution in 5 ampoules to merge, and the result of measuring pH value is 3.9.

Embodiment 3

[0035] prescription:

[0036] Nalmefene Hydrochloride 1g

[0037] Sodium chloride 9g

[0038] Proper amount of hydrochloric acid to pH3.8

[0039] Technology: with embodiment 1. 5ml glass ampoules are used for dispensing, and the dispensing volume is 4ml.

[0040] PH value: measuring method is the same as embodiment 1, gets the solution in 3 ampoules to merge, and the result of measuring pH value is 3.9.

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Abstract

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.

Description

Technical field: [0001] The invention relates to a nalmefene injection and a preparation method thereof, belonging to the technical field of medicines. technical background: [0002] Nalmefene hydrochloride was designed and developed on the basis of transforming and optimizing the structure of the parent compound during the in-depth study of naloxone and naltrexone in the 1970s to address the shortcomings of existing opioid receptor antagonists. new compound. Nalmefene hydrochloride completely retains the characteristics of naloxone and naltrexone as a pure antagonist, has no agonistic effect on opioid receptors, and does not produce dependence. Compared with naloxone and naltrexone, it has the advantages of long action time, high oral bioavailability, small dosage, and wide safety range. Therefore, nalmefene hydrochloride has the characteristics of high efficiency and low toxicity, and has become a new generation of opioid recipients. It is the species with the most poten...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/485A61P25/36A61P39/02
Inventor 王家权董红梅于晓军徐小虎王晋吕俊耀
Owner 西藏易明西雅医药科技股份有限公司
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