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Nimodipine emulsion injection liquid and method for preparing the same

A technology of nimodipine milk and nimodipine, which is applied in the direction of emulsion delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of hindering blood coagulation, prolonging the time of crystallization, general effect, etc., and achieve storage and Ease of use, enhanced solubility, stable content

Inactive Publication Date: 2006-02-15
SHANGHAI INST OF PHARMA IND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When this preparation is used clinically, there is mainly the problem that the concentration is low (0.2mg / ml), crystals are easily precipitated when diluted, and non-aqueous solvents stimulate blood vessels to cause phlebitis. In addition, when used clinically, when using 5% glucose injection 2 to 3 hours after dilution, needle-like or columnar nimodipine crystals will appear, and the content will drop rapidly, which will directly affect the safety and effectiveness of the drug.
In order to prevent crystallization after dilution, foreign products are infused immediately after infusion three-way valve is used online, and the infusion speed and dosage are not easy to control
Some domestic products use polyvinylpyrrolidone (PVP) to prolong the crystallization time, but the effect is average, and because PVP enters the body, it will hinder blood coagulation, so it has been restricted by the State Food and Drug Administration (SFDA)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Under nitrogen protection, weigh 50 g of soybean oil for injection and heat it to 70 ° C. Under high-speed stirring, add 5 g of egg yolk lecithin, 0.1 g of nimodipine, and 0.5 g of benzyl alcohol, and stir evenly as the oil phase; 10 g of glycerin for injection Add to 600ml of water for injection, mix well and filter with a 0.45μm membrane as the water phase. Add the oil phase to the water phase under high speed stirring to make colostrum. Measure the pH value to 6.0, add water for injection to 1000ml, homogenize repeatedly through a high-pressure homogenizer, and check the size of the milk particles. The particle size of all particles is less than 1 μm. After the emulsion is filtered, it is filled with nitrogen, sealed, and sterilized by rotary steam. After cooling, nimodipine milk injection is obtained after passing the inspection.

Embodiment 2

[0072] Under the protection of nitrogen, weigh 300g of soybean oil for injection and heat it to 80°C. Under high-speed stirring, add 30g of egg yolk lecithin, 3g of nimodipine, and 50g of benzyl alcohol, and stir evenly as the oil phase; add 50g of glycerin for injection into 500ml In water for injection, mix well and filter with a 0.45 μm filter membrane as the water phase. Add the oil phase to the water phase under high speed stirring to make colostrum. Measure the pH value to be 8.0, add water for injection to 1000ml, homogenize repeatedly through a high-pressure homogenizer, and check the size of the milk particles. The particle size of all particles is less than 1 μm. After the emulsion is filtered, it is filled with nitrogen, sealed, and sterilized by rotary steam. After cooling, nimodipine milk injection is obtained.

Embodiment 3

[0074] Under nitrogen protection, weigh 100g of soybean oil for injection and heat it to 75°C. Under high-speed stirring, add 12g of egg yolk lecithin, 1g of nimodipine, and 10g of benzyl alcohol, and stir evenly as the oil phase; add 22.5g of glycerin for injection 600ml water for injection, mix well and filter with a 0.45μm filter membrane as the water phase. Add the oil phase to the water phase under high speed stirring to make colostrum. Measure the pH value to 7.0, add water for injection to 1000ml, homogenize repeatedly through a high-pressure homogenizer, and check the size of the milk particles. The particle size of all particles is less than 1 μm. After the emulsion is filtered, it is filled with nitrogen, sealed, and sterilized by rotary steam. After cooling, nimodipine milk injection is obtained.

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Abstract

The invention provides a high concentration nimodipine emulsion injection for intravenous injection, which is prepared from active component of nimodipine and auxiliary materials including oil for injection, emulsifying agent, auxiliary solvent, isotonic conditioning agent and water for injection.

Description

technical field [0001] The invention relates to nimodipine emulsion injection for intravenous injection and a preparation method thereof. Background technique [0002] Nimodipine (Nimodipine) is a second-generation calcium antagonist. The drug acts preferentially on small arteries and selectively acts on cerebral blood vessels. It can significantly reduce cerebral hemorrhage damage and promote the recovery of nerve function. It is clinically used for ischemic The treatment of cerebrovascular disease, migraine, sudden deafness, subarachnoid cerebral hemorrhage and hypertension has achieved good therapeutic effect. [0003] Nimodipine is a poorly soluble drug that is soluble in ethanol, ether and other organic solvents but insoluble in water. Nimodipine injections currently on the market are made into non-aqueous solvent injections, which contain a large amount of ethanol (20-25%) and polyethylene glycol (17-20%) as solvents. When this preparation is used clinically, there i...

Claims

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Application Information

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IPC IPC(8): A61K31/4422A61K9/107A61P9/10A61P25/06A61P9/12
Inventor 谢保源张锡昌陆敏张喜全陈允发张来芳张兵王林晏彩霞蔡紫阳
Owner SHANGHAI INST OF PHARMA IND
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