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Stable S-oxiracetam preparation for injection and preparation method of same

A technology for injection and preparation, applied in the field of medicine, can solve the problems such as loss of pharmacological activity advantage of S-oxiracetam

Inactive Publication Date: 2012-09-19
FUKANGREN BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the inventors have found that, like other L- or D-structural compounds, S-oxiracetam is prone to racemization if the prescription and production process parameters of the S-oxiracetam injection preparation are not well controlled. , forming a racemate, which leads to the loss of the pharmacological activity advantage of S-oxiracetam

Method used

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  • Stable S-oxiracetam preparation for injection and preparation method of same
  • Stable S-oxiracetam preparation for injection and preparation method of same
  • Stable S-oxiracetam preparation for injection and preparation method of same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1 S-oxiracetam drug solution pH screening

[0018] Take 5g of S-oxiracetam, add 100mL of water to dissolve, measure the pH to be about 1.8, add EDTA sodium calcium to dissolve in an appropriate amount, divide the solution into several equal parts, and use sodium hydroxide / hydrochloric acid to adjust the pH of the solution to 4.5, 4.8, 5.1, 5.4, 5.7, 6.0, 6.3, 6.6, 6.9, and 7.2, after being adsorbed by activated carbon, decarbonized by filtration, sealed in ampoules. The color appearance, content, related substances and isomer purity of S-oxiracetam were investigated respectively at the initial stage, under high temperature (℃) and under accelerated light conditions for 30 days. The content is based on the relative content of the initial result. The result obtained is as follows:

[0019]

[0020] The above results suggest that within the investigated pH range, the content of S-oxiracetam has no significant change, suggesting that no hydrolysis or other degr...

Embodiment 2

[0021] Example 2 Effect of heat exposure on racemization of S-oxiracetam

[0022] Take 100g of S-oxiracetam, add 10000mL of water to dissolve it, add an appropriate amount of EDTA sodium calcium to dissolve, and adjust the pH of the solution to 6.0 with sodium hydroxide / hydrochloric acid, absorb it with activated carbon, filter and decarbonize, and seal it in 100ml infusion inside the bottle. The sterility, content, related substances, and Isomeric purity of S-oxiracetam. The content is based on the relative content of the initial result. The result obtained is as follows:

[0023]

[0024] The above obtained results suggest that: due to the rapid and uniform temperature rise of the material in the rotary sterilization process, it can achieve the purpose of sterilization in a short time (within 15 minutes), and at this time the effect on the racemization of S-oxiracetam The impact is minimal, therefore, during the production of injections, the method of rotary steriliza...

Embodiment 3

[0025] Example 3 Effect of pH of S-oxiracetam drug preparation solution on long-term stability of drug preparation (purity of L-isomer)

[0026] Take 50g of S-oxiracetam, add 250mL of water to dissolve it, add an appropriate amount of sodium calcium EDTA to dissolve it, and adjust the pH of the solution to 4.5, 6.0 and 7.2 with sodium hydroxide / hydrochloric acid, after adsorption by activated carbon and decarbonization by filtration, One part was filled in ampoules and freeze-dried; the other part was sealed in ampoules, rotatable (121°C, 15 minutes), and stored at room temperature for 1, 3, 6, 12 and 18 months. Oxiracetam appearance (powder or solution), content, related substances, isomer purity of S-oxiracetam. The content is measured in absolute content. The results obtained are shown below.

[0027] Long-term stability of S-oxiracetam lyophilized preparation

[0028]

[0029] Long-term stability of S-oxiracetam injection

[0030]

[0031] As shown in the results...

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Abstract

The invention relates to a stable preparation for injection by taking S-oxiracetam as active ingredient. The preparation is a composition for injection, and is formed by the S-oxiracetam or salts thereof serving as active ingredient and pharmaceutically acceptable auxiliary material. To restrain the racemization of the S-oxiracetam, when the powder injection with the active ingredient is prepared, and only the pH value of the S-oxiracetam medicament solution ranges from 4.5 to 7.0, the pH value is between 5.4 to 6.6 preferably, so that the S-oxiracetam medicament solution can be produced, and the final freeze-dried product has acceptable long stability; and moreover, when injection is produced, a rotary steam sterilization method needs to be adopted, terminal rotating sterilization is performed for 15 to 45 minutes under the temperature of 121 DEG C, and the terminal rotating sterilization is performed for 15 to 20 minutes preferably, so that the S-oxiracetam injection with high purity can be obtained and has acceptable long stability.

Description

technical field [0001] The invention relates to an injection preparation with S-oxiracetam or its salt as an active ingredient and a stable configuration, including powder injection, large-volume injection (above 50ml), and small-volume injection (below 20ml). It belongs to the field of medical technology. Background technique [0002] Oxiracetam is a new type of central nervous system drug that promotes learning and enhances memory. The active ingredient is a synthetic cyclic derivative of hydroxyaminobutyric acid (BABOB), which only acts on the central nervous system and is mainly distributed in the cerebral cortex and hippocampus. It can activate, protect or promote the functional recovery of nerve cells and improve mental retardation. The memory and learning function of the patient, while the drug itself has no direct vasoactive activity and no central excitatory effect, the effect on the learning and memory ability is a lasting promotion effect. Mechanism research res...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/19A61K31/4015A61P25/28
Inventor 刘露其他发明人请求不公开姓名
Owner FUKANGREN BIO PHARMA
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