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Oxiracetam for injection and preparation method thereof

A water for injection and prescription technology, which is applied in the field of pharmaceutical preparations, can solve the problems of long freeze-drying cycle, difficulty in reconstitution, product shrinkage, etc., and achieve the effects of short freeze-drying cycle, avoiding side effects, and shortening the time

Active Publication Date: 2014-10-01
YAOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, for freeze-dried products with excessive solute concentration (greater than 20% (W / V)), it is easy to accumulate solutes in the surface frozen layer during the freezing process, forming a hard shell, which is not conducive to later drying, and it is easy to cause the product to shrink, melt and burn. A series of problems such as difficult reconstitution
Oxiracetam injection has been listed with a specification of 1.0 / bottle, filled with 5ml, and its solute concentration is 20%. Freeze-drying is carried out in different ways, and the drying is slow due to the formation of a freeze-concentrated layer on the surface. As a result, the freeze-drying cycle is very long, and a hard film is formed on the surface of the product, and it needs to be shaken vigorously to dissolve completely when reconstituted.

Method used

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  • Oxiracetam for injection and preparation method thereof
  • Oxiracetam for injection and preparation method thereof
  • Oxiracetam for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Prepare oxiracetam solution at a concentration of 50%, add ethanol of 0%, 1.0%, 1.2%, 1.4%, 1.6%, 1.8%, 2.0% and 2.2% (V / V) of the total volume respectively, observe the oxiracetam Dissolution of Piracetam. The results are shown in Table 1:

[0052] Ethanol concentration (V / V) 0.0% 1.0% 1.2% 1.4% 1.6% 1.8% 2.0% 2.2% Dissolution of Oxiracetam completely dissolved completely dissolved completely dissolved completely dissolved completely dissolved completely dissolved completely dissolved partially insoluble

[0053] From the above experimental results, it can be seen that when the amount of ethanol is greater than 2.0%, oxiracetam cannot be completely dissolved, and its solubility decreases. Therefore, during the preparation of this product, the amount of ethanol should not exceed 2.0%.

Embodiment 2

[0055] On the basis of Example 1, store the completely dissolved drug solution at 60°C for 24 hours, and take a sample at the specified time to detect the amount of impurity (oxiracetam acid). The results are shown in Table 2:

[0056] Table 2 The impurity levels of oxiracetam in solutions containing different amounts of ethanol

[0057]

[0058] From the above experimental results, it can be seen that the amount of oxiracetam acid increases with time, and the amount of increase is related to the amount of ethanol in the solution. The more the amount of ethanol, the less the amount of increase. When the amount of ethanol is greater than or equal to 1.4%, the amount of increase is the least, and oxiracetam is the most stable.

Embodiment 3

[0060] On the basis of Example 1, carry out terminal filtration and sterilization of the completely dissolved medicinal liquid through a 0.22 μm microporous membrane to obtain a filtrate, fill the filtrate into a control bottle at 5.0 ml / bottle, stopper, and use ordinary pre-freezing Freeze-drying is carried out after the method, and the freeze-drying program is shown in Table 3:

[0061] pre-freeze Place the sample on the shelf, cool the plate temperature to -30°C at a rate of 1°C / min, and keep the temperature at -30°C for 8 hours. once dry The temperature of the plate is raised to -10°C within 10 hours, kept at a constant temperature for 12 hours, and the vacuum degree is not higher than 100Pa. secondary drying The plate temperature was raised to 40°C within 5 hours and kept at a constant temperature for 10 hours.

[0062] Statistically obtain the ratio of frozen concentrated layer samples in each batch of samples, the results are shown in Table ...

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Abstract

The invention discloses oxiracetam freeze-dried powder injection and a preparation method thereof; and the oxiracetam freeze-dried powder injection disclosed by the invention is prepared by comprising the following steps: dissolving oxiracetam in water for injection, adding ethanol which is 1.2-2.0% (V / V) of the total volume, preparing into a 200-500 mg / ml oxiracetam solution, and freeze-drying. The oxiracetam freeze-dried powder injection disclosed by the invention is prepared by adopting a proper amount of ethanol with the help of the special freeze-drying process, particularly a special pre-freezing manner; pre-freezing process parameters are established, therefore, the surface of the solution is crystallized at first; the solute on the surface is prevented from being accumulated; and the oxiracetam freeze-dried powder injection prepared by the invention is basically free from accessories, rapid to re-dissolve, good in quality and steady for storage.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, more specifically, to an oxiracetam for injection and a preparation method thereof. Background technique [0002] Oxiracetam, the chemical name is: 4-hydroxy-2-oxo-1-pyrrolidineacetamide, the structural formula is: [0003] [0004] Oxiracetam is a pyrrolidone derivative first synthesized by the Italian ISF company, and it is a new generation of brain metabolism improving drug. This product can promote the synthesis of phosphorylcholine and phosphorylethanolamine, increase the utilization of oxygen and glucose in the brain and the ratio of ATP / ADP, increase the synthesis of protein and nucleic acid in the brain; act on glutamate-promoting receptors, Prevent neurotoxicity caused by glutamate; can improve memory and learning functions of patients with memory and intellectual disabilities. This product is suitable for memory and intelligence disorders caused by mild to moderate vascul...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/4015A61P25/28
Inventor 喻義王小霞
Owner YAOPHARMA CO LTD
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