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Cinepazide maleate injection and preparation method thereof

A technology of cinepazide maleate and injection, which is applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problem of cinepazide maleate injection. problems such as stability, increased content, and greater impact on drug safety, to achieve the effects of reducing production costs, reducing content, and reducing dosage

Inactive Publication Date: 2009-07-08
北京康瑞达彤科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, cinepazide maleate injection is unstable, and after long-term storage, the content of the cis-isomer of cinepazide maleate, which is more toxic, increases significantly, which has a great impact on drug safety.

Method used

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  • Cinepazide maleate injection and preparation method thereof
  • Cinepazide maleate injection and preparation method thereof
  • Cinepazide maleate injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0025] Sample 1: Operate in dark place, weigh 2.54g of D-sorbitol and add it to 80ml water for injection, stir to dissolve; then weigh 4.05g of cinepazide maleate and add to the above solution, stir to dissolve; use 4% hydrogen phosphate Adjust the pH of the disodium solution to 4.15, and add water for injection to 100ml. A solution of cinepazide maleate was prepared.

[0026] Sample 2: Avoid light, weigh 2.54g of mannitol and add it to 80ml water for injection, stir and dissolve; then weigh 4.08g of cinepazide maleate and add it to the above solution, stir and dissolve; use 4% disodium hydrogen phosphate Adjust the pH of the solution to 4.12, and add water for injection to 100ml. A solution of cinepazide maleate was prepared.

[0027] Table 1 Comparative experiment

[0028]

[0029] As can be seen from the data in Table 1, the content of the two samples has no significant change, and mannitol is selected as the cinepazide maleate cis isomer and other impurities of the s...

preparation example 2

[0033] Sample 3: Weigh 0.25g of mannitol and add it to 40ml of water for injection, stir and dissolve; then weigh 2.03g of cinepazide maleate and add it to the above solution, stir and dissolve; use 4% disodium hydrogen phosphate solution to adjust the pH value When it is 4.05, add water for injection to 50ml, filter, and seal.

[0034] Sample 4: Weigh 1.08g of mannitol and add it to 40ml of water for injection, stir and dissolve; then weigh 2.04g of cinepazide maleate and add it to the above solution, stir and dissolve; use 4% disodium hydrogen phosphate solution to adjust the pH value When it is 4.01, add water for injection to 50ml, filter, and seal.

[0035] Sample 5: Weigh 1.26g of mannitol and add it to 40ml of water for injection, stir and dissolve; then weigh 2.06g of cinepazide maleate and add it to the above solution, stir and dissolve; use 4% disodium hydrogen phosphate solution to adjust the pH value When it is 4.08, add water for injection to 50ml, filter, and se...

Embodiment 1

[0054] 1. Prescription:

[0055]

[0056] 2. The preparation process, the following steps are all operated in the dark:

[0057] (1) Weigh the prescribed amount of mannitol and add it to 1600ml water for injection, stir to dissolve.

[0058] (2) Add the prescribed amount of cinepazide maleate into the above solution, and stir to dissolve.

[0059] (3) 4% disodium hydrogen phosphate solution to adjust the pH value to 4.15.

[0060] (4) Add water for injection to 2000ml, add 2g of activated carbon, keep stirring at 50°C for 20min, and decarbonize by filtration.

[0061] (5) Intermediate product detection: pH value and content of cinepazide maleate.

[0062] (6) After the intermediate product is qualified, it is filtered with a 0.22 μm microporous membrane, and then potted.

[0063] (7) Sterilize at 121°C for 15 minutes with high temperature and damp heat.

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Abstract

The invention relates to a cinepazide maleate injection and a preparation method thereof. Every 1000ml injection contains 30-45g of cinepazide maleate, 5-23g of mannite, 0.5g-1.5g of disodium hydrogen phosphate used for regulating the pH value, and the rest of water used for injection. The preparation method comprises: under the condition of keeping out of the sun, the mannite is added to and dissolved in the water which accounts for 80% of the total quantity, the cinepazide maleate is then added into the mannite aqueous solution to be stirred and dissolved, the pH value of the mixed solution is regulated by the solution with 4% of the disodium hydrogen phosphate, and the water used for injection is added until the total quantity is achieved. The invention selects the mannite with high safety as stabilizing agent, and the operation which is kept out of the sun is adopted in the preparation process of the product, so that the content of the cis isomer of the cinepazide maleate is more effectively reduced, and the stability as well as the safety of clinical medication can be improved.

Description

technical field [0001] The invention relates to pharmaceutical preparations, in particular to a cinepazide maleate injection and a preparation method thereof. Background technique [0002] Cinepazide maleate, chemical name: (E)-1-{4-[(3',4',5'-trimethoxycinnamoyl)]1-1piperazine}acetylpyrrolidine cis-butyl Elenate, molecular formula: C 22 h 31 N 3 o 5 ·C 4 h 4 o 4 . Cinepazide maleate has calcium ion antagonism mechanism and unique endogenous adenosine synergistic effect. Cinepazide maleate injection is used clinically to treat cardiovascular, cerebrovascular and peripheral vascular diseases. However, the cinepazide maleate injection is unstable, and after long-term storage, the content of the cis-isomer of cinepazide maleate, which has greater toxicity, increases significantly, which has a greater impact on the safety of the drug. [0003] The Chinese invention patent application with the publication number CN101204372A discloses a kind of cinepazide maleate injecti...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/10A61K47/02A61K31/496A61K31/194A61P9/00
Inventor 罗军
Owner 北京康瑞达彤科技有限公司
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