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Nalmefene hydrochloride injection medicine composition and preparation method

A composition and technology of nalmefene, applied in the field of medicine, can solve problems such as increased impurity content and non-compliance with pharmacopoeia regulations

Active Publication Date: 2015-09-23
成都天台山制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the Chinese patent CN101406474B, the antioxidant tert-butylhydroxyanisole in CN101658489B is replaced with tryptophan, and nalmefene hydrochloride, a chelating agent, and an osmotic pressure regulator are added to adjust the pH to 3.7 to 4.1 after dissolving, and then use 0.05% ( W / V) activated carbon was activated at a temperature of 115°C to 120°C for 2 hours. After 24 months of storage of nalmefene hydrochloride injection obtained by the above method, the content of dinalmefene had exceeded the pharmacopoeia regulations; after 30 months , the content reaches 2.45%, which does not meet the requirements of the Pharmacopoeia
[0011] From the investigation of the degraded impurity dinalmefene, it is found that adding auxiliary materials such as specific antioxidants, chelating agents or pH buffers in the nalmefene hydrochloride injection can indeed improve the long-term storage stability of the finished product of the injection. The above-mentioned prior art prescription Although the binalmefene content of the produced products was all lower than 1.0% at day 0, the impurity content increased as the storage time increased, especially after the storage reached 30 months, the binalmefene content was all above 2.0%, all Does not meet Pharmacopoeia regulations

Method used

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  • Nalmefene hydrochloride injection medicine composition and preparation method
  • Nalmefene hydrochloride injection medicine composition and preparation method
  • Nalmefene hydrochloride injection medicine composition and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Embodiment 1: prepare nalmefene hydrochloride injection pharmaceutical composition

[0077] formula:

[0078] Nalmefene Hydrochloride 0.1mg,

[0079] Sodium chloride 0.9 mg,

[0080] Water for injection, add appropriate amount to 1ml,

[0081] Injection target pH value = 3.8;

[0082] Preparation method:

[0083] (a) Weigh the nalmefene hydrochloride and solid excipients of the prescribed amount, add an appropriate amount (about 70%) of water for injection to dissolve, then add activated carbon (0.05%, the same below), stir, and filter for decarbonization;

[0084] (b) add water for injection to the full amount, stir evenly, measure the pH value of the solution and optionally determine the active ingredient content, adjust to the specified pH value with an acid-base regulator;

[0085] (c) The obtained solution is carefully filtered, filled into an ampoule bottle, and sterilized by autoclaving at 115° C. for 30 minutes to obtain a pharmaceutical composition for in...

Embodiment 2

[0086] Embodiment 2: prepare nalmefene hydrochloride injection pharmaceutical composition

[0087] formula:

[0088] Nalmefene Hydrochloride 0.1mg,

[0089] Sodium chloride 0.75mg,

[0090] Water for injection, add appropriate amount to 1ml,

[0091] Injection target pH value = 3.5;

[0092] Preparation method:

[0093] (a) Take nalmefene hydrochloride and solid excipients of the prescribed amount, add appropriate amount (about 70%) of water for injection to dissolve, then add activated carbon, stir, filter and decarbonize;

[0094] (b) add water for injection to the full amount, stir evenly, measure the pH value of the solution and optionally determine the active ingredient content, adjust to the specified pH value with an acid-base regulator;

[0095] (c) The obtained solution is carefully filtered, filled into an ampoule bottle, and sterilized by autoclaving at 115° C. for 30 minutes to obtain a pharmaceutical composition for injection.

Embodiment 3

[0096] Embodiment 3: prepare nalmefene hydrochloride injection pharmaceutical composition

[0097] formula:

[0098] Nalmefene Hydrochloride 0.1mg,

[0099] Sodium chloride 1.5 mg,

[0100] Water for injection, add appropriate amount to 1ml,

[0101] Injection target pH value = 4.0;

[0102] Preparation method:

[0103] (a) Take nalmefene hydrochloride and solid excipients of the prescribed amount, add appropriate amount (about 70%) of water for injection to dissolve, then add activated carbon, stir, filter and decarbonize;

[0104] (b) add water for injection to the full amount, stir evenly, measure the pH value of the solution and optionally determine the active ingredient content, adjust to the specified pH value with an acid-base regulator;

[0105] (c) The obtained solution is carefully filtered, filled into an ampoule bottle, and sterilized by autoclaving at 115° C. for 30 minutes to obtain a pharmaceutical composition for injection.

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Abstract

The invention belongs to the technical field of medicine, and relates to a nalmefene hydrochloride injection medicine composition and a preparation method, and particularly relates to a nalmefene hydrochloride injection medicine composition. The medicine composition comprises nalmefene hydrochloride. Particularly the medicine composition comprises the nalmefene hydrochloride, inorganic salt and injection water. The nalmefene hydrochloride in the medicine composition is added into the composition in a form of 17-(cyclopropyl)-4, 5alpha-epoxyl-6-methylene morphinan-3, 14-diol hydrochloride. Sugar is selected from one or more of mannitol, glucitol, lactose, maltose, maltitol, glycine, trehalose, glucose, dextran and the like. The medicine composition is an opiates receptor antagonist and is mainly clinically used for completely or partially inverting the effects of opiates drugs, including the respiratory depression caused by natural or synthetic opiates drugs. The injection is good in pharmaceutical properties such as excellent chemical stability and physical stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a pharmaceutical composition of nalmefene hydrochloride, in particular to the pharmaceutical composition of nalmefene hydrochloride for injection, and to a preparation method of the pharmaceutical composition. Background technique [0002] Nalmefene hydrochloride, an opioid receptor antagonist, is a 6-methylene analog of naltrexone. The English name of nalmefene hydrochloride is Nalmefene Hydrochloride, which is the hydrochloride salt of nalmefene base, molecular formula: C21H25NO3·HCl, molecular weight: 375.9, CAS#58895-64-0, chemical name: 17-(cyclopropyl)- 4,5α-epoxy-6-methylenemorphinan-3,14-diol hydrochloride, its chemical structure is: [0003] [0004] Nalmefene hydrochloride is white to off-white powder, easily soluble in water with a solubility of 130mg / mL; slightly soluble in chloroform with a solubility of 0.13mg / mL. The pK of Nalmefene Hydrochloride a is 7.6. ...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/485A61P11/00A61P25/20A61P9/02A61P39/02A61P25/36
Inventor 陈娟左伟伍隆霞龙成全姚波苟治君赵东明
Owner 成都天台山制药股份有限公司
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