Method for preparing nalmefene hydrochloride injection and prepared nalmefene hydrochloride injection

A nalmefene and injection technology, applied in the field of nalmefene hydrochloride injection, can solve the problems of inability to achieve stable effects, poor drug stability, safety, and effectiveness risks, and achieve easy control and effective ingredient content. Stabilization, effects related to the stabilization of substances

Inactive Publication Date: 2013-07-17
ANHUI HEALSTAR PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Chinese patent document CN1895251 discloses a stable nalmefene hydrochloride injection and its preparation method. The preparation is composed of a pharmaceutically effective amount of nalmefene hydrochloride and an appropriate amount of pharmaceutical carrier, and its core is the addition of hydrogen sulfite to the prescription. Inorganic antioxidants such as sodium, sodium sulfite, pyrosulfite, vitamin C, and a certain amount of antioxidant synergist disodium ethylenediaminetetraacetate were added, but the results of the stability test according to this prescription showed that it could not reach its The stabilizing effect in the instructions, the relevant substances also changed significantly during the investigation period (increased from 0.7% to 1.4%), and the pH value also changed significantly (increased from 3.9 to 5.3). Although the results did not exceed the standard, they were close to the upper limit. There are certain risks in the safety and effectiveness of the drug
[0005] Several nalmefene hydrochloride injections currently on the market are valid for 12 to 18 months, indicating that the stability of the drug is not good, which brings certain risks to the clinical use and drug safety of the drug

Method used

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  • Method for preparing nalmefene hydrochloride injection and prepared nalmefene hydrochloride injection
  • Method for preparing nalmefene hydrochloride injection and prepared nalmefene hydrochloride injection
  • Method for preparing nalmefene hydrochloride injection and prepared nalmefene hydrochloride injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] This example prepares 1000 nalmefene hydrochloride injections (specification: 1ml: 0.1mg)

[0020] Material name Feed amount

[0021] Nalmefene hydrochloride 0.1108g (equivalent to nalmefene 0.1g)

[0022] Sodium chloride 9g

[0023] Add water for injection to 1000ml,

[0024] Preparation steps: (1) Take 9g of sodium chloride in the prescribed amount, add 500ml of water for injection to dissolve, add 0.05% (W / V) activated carbon and stir for 15 minutes, filter and decarbonize and cool to room temperature;

[0025] (2) Under the protection of nitrogen, add 0.1108g of nalmefene hydrochloride (equivalent to 0.1g of nalmefene) in the prescribed amount, stir to dissolve, add water for injection at room temperature to the full amount of 1000ml, mix well, and add 1mol / L hydrochloric acid Adjust the pH value of the solution to 3.5-4.5;

[0026] (3) After filtering with 0.45 μm and 0.22 μm filters, subpackage, fill with nitrogen, seal, and sterilize at 116°C / 40 minutes to ob...

Embodiment 2

[0028] This example prepares 1000 nalmefene hydrochloride injections (specification: 1ml: 0.1mg)

[0029]

[0030] Preparation steps: (1) Take 9g of sodium chloride and 10g of citric acid as prescribed, add 500ml of water for injection to dissolve, add 0.05% (W / V) activated carbon and stir for 15 minutes, filter and decarbonize and cool to room temperature;

[0031] (2) Under the protection of nitrogen, add 0.1108g of nalmefene hydrochloride (equivalent to 0.1g of nalmefene) in the prescribed amount, stir to dissolve, add water for injection at room temperature to the full amount of 1000ml, mix well, and use 1mol / L hydrogen The sodium oxide solution adjusts the pH value to 3.5-4.5;

[0032] (3) After filtering with 0.45 μm and 0.22 μm filters, subpackage, fill with nitrogen, seal, and sterilize at 116°C / 40 minutes to obtain Nalmefene Hydrochloride Injection.

Embodiment 3

[0034] This example prepares 1000 nalmefene hydrochloride injections (specification: 1ml: 0.1mg)

[0035]

[0036] Preparation steps: (1) Take 9g of sodium chloride and 1g of sodium metabisulfite in the prescribed amount, add 500ml of water for injection to dissolve, add 0.05% (W / V) activated carbon and stir for 15 minutes, filter and decarbonize and cool to room temperature;

[0037] (2) Under the protection of nitrogen, add 0.1108g of nalmefene hydrochloride (equivalent to 0.1g of nalmefene) in the prescribed amount, stir to dissolve, add water for injection at room temperature to the full amount of 1000ml, mix well, and add 1mol / L hydrochloric acid Adjust the pH value of the solution to 3.5-4.5;

[0038] (3) After filtering with 0.45 μm and 0.22 μm filters, subpackage, fill with nitrogen, seal, and sterilize at 116°C / 40 minutes to obtain Nalmefene Hydrochloride Injection.

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Abstract

The invention discloses a method for preparing nalmefene hydrochloride injection. The method comprises the steps of adding a certain amount of citric acid or citrate auxiliary material to the preparation when the nalmefene hydrochloride injection is prepared according to a common method, wherein the adding amount is 5-15g of citric acid or citrate added to each liter of injection; firstly, taking the prescribed auxiliary material in preparation, adding injection water to dissolve, adding active carbon to agitate and adsorb, filtering and removing impurities; adding the prescribed nalmefene hydrochloride under the protection of nitrogen, fully dissolving and sizing to an appointed constant volume by water, adjusting the pH value to 3.5-4.5; and finally conducting split charging, charging nitrogen, sealing and sterilizing after filtering by a filter. By adopting the method disclosed by the invention, the validity period of the nalmefene hydrochloride injection can be obviously prolonged; a specific citric acid pH value stabilizer is adopted; and the nalmefene hydrochloride injection has good stability, and stable sample appearance, pH value, effective ingredient content and related substances, and the like. Therefore, the safety of medication is ensured.

Description

technical field [0001] The invention relates to a pharmaceutical dosage form, in particular to a preparation method of nalmefene hydrochloride injection and the prepared nalmefene hydrochloride injection. Background technique [0002] Nalmefene hydrochloride was synthesized in 1975. It is a new generation of pure opioid receptor antagonist synthesized after naloxone and naltrexone. It has no agonistic effect on opioid receptors and does not produce dependence. Compared with naltrexone, it has the advantages of long action time, high oral bioavailability, small dosage, and wide safety range. [0003] Chinese patent document CN1813739 discloses a nalmefene hydrochloride injection, wherein the content of nalmefene hydrochloride in each unit dose ranges from 0.1 to 4.5 mg; the pharmaceutical carrier can be mannitol, glucose, β-cyclodextrin, chloride One or more of sodium, dextran, fructose, sorbitol, etc., preferably mannitol and glucose, whose content in the preparation ranges...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/485A61K47/12
Inventor 刘经星夏源丁玉娟余启丽司艳君李娟赵蕾
Owner ANHUI HEALSTAR PHARM CO LTD
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