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Oxiracetam capsule and preparation method thereof

A technology of capsules and micropowdered silica gel, which is applied in the field of medicine, can solve the problems of no investigation of long-term storage stability, no mention of preparation stability, and complicated preparation process steps, and achieve excellent fluidity, simple and environmentally friendly preparation process, and high quality. good stability effect

Active Publication Date: 2014-01-08
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Chinese patent CN200410023403.4 discloses an oxiracetam dispersible tablet and its preparation method. The prescription consists of 10-90% oxiracetam, 2-90% disintegrant, and 0-20% lubricant and glidant , binder 0-20%, the preparation can quickly disintegrate into uniformly dispersed fine particles after oral administration, it is convenient to take, can be taken orally after being dispersed with water, and can also be sucked or swallowed in the mouth, but the patent No mention of formulation stability issues
This patent only tested the influence factors of high temperature and light on the oxiracetam preparation, and did not investigate its long-term storage stability
[0006] After research and analysis, it was found that the above-mentioned disclosed oxiracetam oral solid preparation product has shortcomings in terms of quality stability: the quality stability of the product is poor, and during long-term storage, the content of active ingredients is significantly reduced, and the content of impurities is significantly increased , the dissolution rate drops significantly, and the quality is not stable enough, which is not conducive to ensuring the safety of clinical medication
In addition, the preparation process steps of the oxiracetam solid preparation disclosed above are relatively complicated, and all of them need to add binders to make soft materials and granules, and the production cost is high.

Method used

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  • Oxiracetam capsule and preparation method thereof
  • Oxiracetam capsule and preparation method thereof
  • Oxiracetam capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of Oxiracetam Crystal Form

[0043] a) Take 100 g of the crude product of oxiracetam, add it to 200 ml of water, heat to dissolve it, and obtain an aqueous solution of oxiracetam;

[0044] b) Concentrate the above aqueous solution to 50ml under reduced pressure, the concentration temperature is 45-55°C, and the vacuum degree is -0.08MPa~-0.085MPa.

[0045] c) Cool the concentrated solution to 5°C, stir and crystallize for 1 hour at a stirring speed of 60 rpm, centrifuge to separate the crystals, and then vacuum-dry at a temperature of 45°C and a vacuum degree of -0.08MPa to -0.1MPa After 1 hour, 85.3 g of the finished crystal form of oxiracetam was obtained, the weight yield was 85.3%, the purity determined by HPLC was 99.89%, and the melting point was 168.2-170.0°C.

Embodiment 2

[0046] Example 2 Preparation of Oxiracetam Crystal Form

[0047] a) Take 100 g of the crude product of oxiracetam, add it to 600 ml of water, and dissolve it to obtain an aqueous solution of oxiracetam;

[0048] b) Add 5g of activated carbon to the above aqueous solution, stir and decolorize at 40-50°C for 0.5 hours, filter, and collect the filtrate;

[0049] c) Concentrate the above aqueous solution to 300ml under reduced pressure, the concentration temperature is 40-45°C, and the vacuum degree is -0.085MPa~-0.090MPa.

[0050] d) Cool the concentrated solution to 0°C, stir and crystallize for 6 hours at a stirring speed of 40 rpm, separate the crystals by filtration, and then vacuum dry at a temperature of 55°C and a vacuum degree of -0.08MPa to -0.1MPa After 4 hours, 73.5 g of the finished crystal form of oxiracetam was obtained, with a weight yield of 73.5%, a purity of 99.95% as determined by HPLC, and a melting point of 168.1-169.5°C.

Embodiment 3

[0051] Example 3 Preparation of Oxiracetam Crystal Form

[0052] a) Take 100 g of the crude product of oxiracetam, add it into 1000 ml of water, and dissolve it to obtain an aqueous solution of oxiracetam;

[0053] b) Concentrate the above aqueous solution to 200ml under reduced pressure, the concentration temperature is 35-40°C, and the vacuum degree is -0.090MPa~-0.095MPa.

[0054] c) Cool the concentrated solution to 2°C, stir and crystallize for 3 hours, and the stirring speed is 30 rpm; separate the crystals by pressure filtration, and then vacuum at a temperature of 65°C and a vacuum degree of -0.08MPa~-0.1MPa. After drying for 3 hours, 78.9 g of the finished oxiracetam crystal form was obtained, with a weight yield of 78.9%, a purity of 99.92% as determined by HPLC, and a melting point of 166.0-167.8°C.

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Abstract

The invention relates to an oral capsule preparation of oxiracetam and a preparation method thereof. The oxiracetam capsule contains 80.0-85.5% by weight of oxiracetam, 9.7-15.2% by weight of xylitol and 4.8% by weight of an emollient, wherein the oxiracetam is in a crystal form. The oxiracetam in the crystal form is a good crystal with excellent mobility. Compared with the crystal form provided in the prior art, the oxiracetam in the crystal form has higher purity, less impurity, better quality stabilizer and better crystal form stability. The quality stability of the disclosed oxiracetam capsule is improved remarkably, the preparation process is simple, and the production cost is lowered.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to an oral capsule preparation of oxiracetam and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Oxiracetam, the English name is Oxiracetam, the chemical name is 4-hydroxy-2-oxo-1-pyrrolidineacetamide, and its structural formula is shown in formula 1: [0003] [0004] Oxiracetam is a nootropic drug that can improve memory and learning functions in patients with senile dementia and memory impairment. Research results show that oxiracetam can promote the synthesis of phosphorylcholine and phosphorylethanolamine, and increase the The ratio of ATP / ADP increases the synthesis of protein and nucleic acid in the brain. At present, it is widely used clinically for the treatment of memory and intelligence disorders caused by mild to moderate vascular dementia, senile dementia, and traumatic brain injury, with definite curative effe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/4015A61K47/16A61P25/28
Inventor 王金戌高志峰张育孙鹏张文静王丽丽马园园
Owner CSPC OUYI PHARM CO LTD
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