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Lyophilized zolmitriptan nanometer powder and preparation method thereof

A technology of nano freeze-dried powder and zolmitriptan, which is applied in the field of pharmaceuticals, can solve the problems of high equipment requirements and difficulty in industrial production, achieve good biocompatibility, avoid the problem of organic solvent residue, and increase the degree of dispersion Effect

Inactive Publication Date: 2015-07-29
徐俊 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this patent will be operated through high-speed shearing, high-pressure milk homogenization, etc., which requires high equipment, and it is generally difficult to carry out industrial production

Method used

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  • Lyophilized zolmitriptan nanometer powder and preparation method thereof
  • Lyophilized zolmitriptan nanometer powder and preparation method thereof
  • Lyophilized zolmitriptan nanometer powder and preparation method thereof

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preparation example Construction

[0027] The preparation method of zolmitriptan nano freeze-dried powder provided by the invention comprises the following steps:

[0028] (1) Add zolmitriptan and carrier materials into an organic solvent, and dissolve by ultrasonication or stirring to obtain an organic phase solution A.

[0029] (2) Add the surfactant into purified water, stir until dissolved, and obtain aqueous phase solution B.

[0030] (3) Under the condition of stirring, the organic phase solution A is slowly added dropwise to the aqueous phase solution B to obtain a mixed solution C, and the mixed solution C is continuously stirred to obtain an emulsion D.

[0031] (4) Volatilize the emulsion D in a water bath at 50-60° C. to remove the organic solvent to obtain an aqueous solution of zolmitriptan nanoparticles.

[0032] (5) Adding a protective agent to the aqueous solution of zolmitriptan nanoparticles, and then freeze-drying to obtain zolmitriptan nanometer freeze-dried powder.

[0033] The step of fr...

Embodiment 1

[0040] The present embodiment prepares raw materials and other ingredients according to the following proportions by weight:

[0041]

[0042]

[0043] Dissolving the formula amount of zolmitriptan and lecithin in an appropriate amount of ethyl acetate, and ultrasonically dissolving it to obtain an organic phase solution A; adding the formula amount of Tween 80 into an appropriate amount of purified water, stirring to dissolve it to obtain an aqueous phase solution B; Under the condition of continuous stirring, the organic phase solution A is slowly added dropwise to the aqueous phase solution B, and the mixed solution C is obtained after the dropwise addition is completed; the mixed solution C is continuously stirred for 2.5 hours to obtain the emulsion D; the emulsion D The organic phase was volatilized and removed by continuous stirring in a water bath at 57° C. to obtain an aqueous solution of zolmitriptan nanoparticles.

[0044]After testing, the obtained zolmitript...

Embodiment 2

[0048] The present embodiment prepares raw materials and other ingredients according to the following proportions by weight:

[0049]

[0050] Dissolving the formula amount of zolmitriptan and lecithin in an appropriate amount of ethyl acetate, and ultrasonically dissolving it to obtain an organic phase solution A; adding the formula amount of Tween 80 into an appropriate amount of purified water, stirring to dissolve it to obtain an aqueous phase solution B; Under the condition of continuous stirring, the organic phase solution A is slowly added dropwise to the aqueous phase solution B, and the mixed solution C is obtained after the dropwise addition; the mixed solution C is continuously stirred for 2.3 hours to obtain the emulsion D; the emulsion D The organic phase was volatilized and removed by continuous stirring in a water bath at 57° C. to obtain an aqueous solution of zolmitriptan nanoparticles.

[0051] The obtained zolmitriptan nanoparticle aqueous solution has an...

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Abstract

The invention discloses lyophilized zolmitriptan nanometer powder and a preparation method thereof. The lyophilized powder consists of the following raw materials in parts by weight: 1 part of zolmitriptan, 6-14 parts of carrier materials, and 90-130 parts of a surfactant, wherein the carrier materials adopt one or more of the following materials: lecithin, stearic acid, monoglyceride, chitosan and poloxamer. The carrier materials and the surfactant, which are selected by the lyophilized zolmitriptan nanometer powder disclosed by the invention are ideal auxiliary materials, because the biocompatibility is good, and the internal toxicity is low. Through the adoption of the method disclosed by the invention, the zolmitriptan is wrapped in solid lipid, after the wrapped zolmitriptan is lyophilized, the degree of dispersion is increased, the stability is improved, the bioavailability of zolmitriptan is improved, and the potency can be used in the level of nanometer. Organic solvents are removed, so that the residue of organic solvents can be avoided; the lyophilized zolmitriptan nanometer powder disclosed by the invention can be directly made into an oral agent of lyophilized powder, and can be further made into granules, tablets or capsules, which are used in clinical medicine.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a drug freeze-dried powder and a preparation method thereof, in particular to zolmitriptan nano freeze-dried powder and a preparation method thereof. Background technique [0002] Migraine is one of clinical common disease and frequently-occurring disease, and its incidence rate is about 10%. The incidence rate of migraine in my country ranges from 4.2% to 14.6%, and even shows an upward trend. Epidemiological surveys found that about 6% of men and 17% of women suffer from the disease, most of whom are between the ages of 25 and 55. Migraine has seriously affected the life and work of patients and brought a lot of inconvenience. The high incidence of migraine is closely related to the lack of drugs, which makes the market for this drug huge and promising. Therefore, it is very meaningful and necessary to open up effective drugs for the treatment of migraine. [0003] Zolmitriptan is a h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/422A61K47/36A61P25/06
Inventor 徐俊闫启东陈琦吴锁霞
Owner 徐俊
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