Nimodipine lyophilized emulsion for injection and preparing method thereof

A technology of nimodipine and freeze-dried emulsion, which is applied in the field of medicine to achieve the effects of improving stability, reducing toxic and side effects, and avoiding stimulation and injury

Inactive Publication Date: 2008-06-18
YAOPHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no relevant bibliographical report about nimodipine freeze-dried emulsion and preparation method thereof in the prior art

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  • Nimodipine lyophilized emulsion for injection and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] 1. Dissolve 10 mg of the main drug nimodipine in 5 g of olive oil as the oil phase;

[0034] 2. Disperse 1.0g of soybean lecithin in water, and add 5g of glycerin and 1g of Vc as the water phase;

[0035] 3. Add the oil phase to the water phase under stirring, stir at 20°C at high speed to make it colostrum, and adjust the pH to 8.0 with 0.1mol / L NaOH solution to obtain colostrum;

[0036] 4. The colostrum is homogenized by an APV2000 homogenizer to obtain a uniform emulsion I, and 400g of sucrose is dissolved to obtain a solution II;

[0037] 5. Mix solution I and solution II, dilute the solution to 1000ml, and remove water by freeze-drying to obtain dry nimodipine freeze-dried emulsion. The above processes are all completed under the condition of nitrogen filling.

Embodiment 2

[0039] 1. Dissolve 500mg of the main drug nimodipine in 100g of soybean oil as the oil phase;

[0040] 2. Disperse 20g of egg yolk phospholipids in water, and add 2g of glycerin as the water phase;

[0041] 3. Add the oil phase to the water phase under stirring, stir at 40°C at high speed to make it colostrum, and adjust the pH to 7.5 with 0.1mol / L sodium citrate buffer to obtain colostrum;

[0042] 4. The colostrum is homogenized by an APV2000 homogenizer to obtain a uniform emulsion I, and 100g of glucose is dissolved to obtain a solution II;

[0043] 5. Mix solution I and solution II, dilute the solution to 1000ml, and remove water by freeze-drying to obtain dry nimodipine freeze-dried emulsion. The above processes are all completed under the condition of nitrogen filling.

Embodiment 3

[0045] 1. Dissolve 2.0g of the main drug nimodipine and 25g of egg yolk phospholipid in 300g of soybean oil for injection as the oil phase;

[0046] 2. Disperse 25g of soybean lecithin in water, then add 2.0g of sodium chloride and 1g of sodium oleate as the water phase;

[0047] 3. Add the water phase to the oil phase under stirring, stir at 90°C at high speed to make it colostrum, and adjust the pH to 8.0 with 0.5mol / L citric acid buffer to obtain colostrum;

[0048] 4. The colostrum is homogenized by an APV2000 homogenizer to obtain a uniform emulsion I, and 200g of maltose is dissolved to obtain a solution II;

[0049] 5. Mix solution I and solution II, dilute the solution to 1000ml, and remove water by freeze-drying to obtain dry nimodipine freeze-dried emulsion. The above processes are all completed under the condition of nitrogen filling.

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Abstract

The invention relates to nimodipine lyophilization dry emulsion for injection. Before freeze-dried or reconstituted, according to percentage concentration per 1000 ml of fat emulsion, the lyophilization dry emulsion contains 0.001 percent to 0.2 percent of nimodipine, 0.5 percent to 30 percent of oiliness solvent, 0.1 percent to 5 percent of emulsifier, 5 percent to 40 percent of the freeze-drying protective agent and 0.1 percent to 10 percent of isotonic regulator. The invention also relates to a preparation method of nimodipine lyophilization dry emulsion. The invention has the advantages that ethanol is avoided to decrease irritation; the product can be mixed with any proportion of water for injection, sodium chloride solution, glucose solution, blank fat emulsion or other aqueous solution without phenomena of precipitation or crystallization; in addition, compared with the fat emulsion, the lyophilization dry emulsion is more helpful to improve the stability of nimodipine and excipient of the nimodipine, thereby lowering the requirements of production, transportation and storage conditions and prolonging the period of validity.

Description

Technical field: [0001] The invention relates to the technical field of medicine, specifically, it is a nimodipine freeze-dried emulsion for injection and a preparation method thereof, and the emulsion can be used for cerebral vasospasm and acute cerebral vascular spasm after subarachnoid hemorrhage caused by various reasons. Improved blood circulation during convalescence. technical background: [0002] Nimodipine (nimodipine, NIM), chemical name: 1-methylethyl-2-methoxyethyl-1,4-dihydro-2,6-dimethyl-4-(3-nitrobenzene base)-3,5-pyridine dicarboxylate, molecular formula: C 21 h 26 N 2 o 7 , molecular weight 418.5. [0003] Nimodipine is a 1,4-dihydropyridine calcium ion antagonist widely used clinically, and is currently a commonly used cardiovascular and cerebrovascular drug. Normally, the contraction of smooth muscle depends on Ca 2+ Enters the cell, causing depolarization of the transmembrane current. Nimodipine effectively blocks Ca 2+ Enter the cell, inhibit th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4422A61K9/107A61K9/19A61K47/44A61K47/34A61K47/24A61P9/10A61K47/10A61K47/14A61K47/22A61K47/26A61K47/28
Inventor 熊迎新柴莉
Owner YAOPHARMA CO LTD
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