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Nimodipine nanometer granule and its prepn. method

A nimodipine nanometer and nimodipine technology, which can be used in pharmaceutical formulations, medical preparations of non-active ingredients, cardiovascular system diseases, etc., and can solve problems that have not been reported

Inactive Publication Date: 2007-01-31
张文芳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The present invention adopts high-pressure emulsification and low-temperature curing method, uses POGC or PEGC as the carrier material, prepares nimodipine nanoparticles, and investigates its physical stability and metabolic behavior in vivo. This work has not been reported at home and abroad.

Method used

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  • Nimodipine nanometer granule and its prepn. method

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Experimental program
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Effect test

Embodiment 1

[0029] Prescription: nimodipine 0.01-1.0g, POGC 0.5-10.0g, glyceryl monostearate 1.0-6.0g, fatty acid 1.0-6.0g, lecithin 2.0-6.0g, mannitol 2.0-10.0g, injection Make up to 30ml with water.

[0030] Preparation method one:

[0031] a) Heating and melting 2.0g of glyceryl monostearate, 1.0g of fatty acid, 1.0g of lecithin, 2.0g of POGC and 1mg of nimodipine, adding the prescribed amount of water for injection (PH10-11) and 5.0g of mannitol and stirring To form colostrum, adjust the pH value to 4.5-7.0, and then use a high-pressure homogenizer to circulate and high-pressure homogenize and emulsify the colostrum system until the particle size meets the requirements.

[0032] b) The above emulsion is filtered, freeze-dried, and filled with a nitrogen pressure cap to obtain the obtained product.

[0033] Preparation method two:

[0034] a) Heat and melt 3.0g glyceryl monostearate, 1.0g fatty acid, 1.0g lecithin, 10.0g POGC and 50mg nimodipine, add prescription water for injection...

Embodiment 2

[0037] Prescription: nimodipine 0.01-1.0g, PEGC 1.0-10.0g, glyceryl monostearate 1.0-6.0g, lecithin 2.0-6.0g, mannitol 2.0-6.0g, add water for injection to 30ml.

[0038] a) Heat and melt 1.0g glyceryl monostearate, 1.0g lecithin, 3.0g PEGC and 0.0005g nimodipine, add prescription water for injection (PH10-11) and 5.0g mannitol and stir to make colostrum , adjust the pH value to 4.5-7.0, and then use a high-pressure homogenizer to circulate and high-pressure homogenize and emulsify the colostrum system until the particle size meets the requirements.

[0039]b) The above emulsion is filtered, freeze-dried, and filled with a nitrogen pressure cap to obtain the obtained product.

Embodiment 3

[0041] Composition: Nimodipine 0.01-1.0g, POGC 1.0-8.0g, glyceryl monolaurate 1.0-6.0g, lecithin 1.0-3.0g, mannitol 2.0-6.0g, low molecular weight dextran 2.0-6.0 g, add water for injection to 100ml.

[0042] Nimodipine 0.005g, POGC 0.5g, glyceryl monolaurate 2.0g and lecithin 1.0g are heated and melted, add 3.0g of mannitol in an appropriate amount of aqueous solution, stir evenly, and stir at high speed until the average particle size of milk droplets is ≤0.5 microns , adding 2.0 g of low-molecular dextran as a freeze-drying protective agent, dissolving and filtering, freeze-drying, and filling a nitrogen pressure cap to obtain the obtained product.

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Abstract

A nanoparticle of nimodipine contains nimodipine, the carrier chosen from poloxamer cholesterol ester of fatty acid and cholesterol ester of fatty acid, stabilizer and water. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to a nimodipine nanoparticle and a preparation method thereof, which is characterized in that it comprises nimodipine, a carrier, a stabilizer and water, wherein the carrier is selected from novel adjuvant fatty acid poloxamer cholesterol ester (PPGC) and fatty acid PEG cholesterol Ester (PEGP), the prepared nanoparticles have a particle size of ≤1um, which has the advantages of high drug loading and good stability. Background technique [0002] The chemical name of Nimodipine is: 1-methylethyl-2-methoxyethyl-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5 - Pyridine dicarboxylates. The molecular weight is 418.45. [0003] Nimodipine is a Ca channel blocker. Normally, the contraction of smooth muscle depends on the entry of Ca into the cell, causing the depolarization of transmembrane currents. Nimodipine achieves the purpose of relieving vasospasm by effectively preventing Ca from entering cells and inhibiting smooth muscle co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/435A61K47/34A61K47/24A61P9/10A61P9/08A61K47/28
Inventor 张文芳
Owner 张文芳
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