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Clevidipine lipid microsphere injection and preparation method thereof

A technology of clevidipine and dipine lipid, which is applied in the field of clevidipine lipid microsphere injection and preparation thereof, can solve the problems of consumption of medical and social resources, heavy burden on the country, and high fatality rate, and achieve the effect of improving quality and improving biological utilization. The effect of narrow size and particle size distribution

Inactive Publication Date: 2017-11-14
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main complications of elevated blood pressure include stroke, myocardial infarction, heart failure, and chronic kidney disease, which not only cause disability and high mortality, but also seriously consume medical and social resources, causing a heavy burden on the family and the country

Method used

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  • Clevidipine lipid microsphere injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] (1) Weigh 500mg of clevidipine, 12.3g of lecithin, 4.8g of creatinine and 38.5g of soybean oil, add them into a container, use a high-speed shearing machine to disperse until dissolved, and form an oil phase, and heat to 50-60°C for later use;

[0023] (2) Take 2.6g of sodium metabisulfite and 1.4g of hydroxypropyl butyl ester into the water for injection, adjust the pH value of the aqueous phase to 9.2 with sodium hydroxide, mix well and heat to a temperature of 50-60°C for later use;

[0024] (3) Under the protection of nitrogen, slowly drop the water phase obtained above into the oil phase under the condition of stirring, the dropping speed is 5-10ml / min, stir for 25 minutes after dropping, and then transfer to a high-speed homogenizer for high-speed stirring 3-5 times, 5-10min each time, to obtain a uniform white emulsion;

[0025] (4) Add 1,000ml of water for injection at 50-60°C to the white emulsion obtained in (3), mix it evenly, and transfer it to a high-pressu...

Embodiment 2

[0028] (1) Weigh 500mg of clevidipine, 11.6g of lecithin, 4.5g of creatinine and 45g of soybean oil, add them into a container, use a high-speed shearing machine to disperse until dissolved, and form an oil phase, and heat to 50-60°C for later use;

[0029] (2) Take 2.3g of sodium metabisulfite and 1g of hydroxypropyl butyl ester into the water for injection, adjust the pH value of the aqueous phase to 9.2 with sodium hydroxide, mix well and heat to a temperature of 50-60°C for later use;

[0030] (3) Under the protection of nitrogen, slowly drop the water phase obtained above into the oil phase under the condition of stirring, the dropping speed is 5-10ml / min, stir for 25 minutes after dropping, and then transfer to a high-speed homogenizer for high-speed stirring 3-5 times, 5-10min each time, to obtain a uniform white emulsion;

[0031] (4) Add 1,000ml of water for injection at 50-60°C to the white emulsion obtained in (3), mix it evenly, and transfer it to a high-pressure m...

Embodiment 3

[0034] (1) Weigh 500mg of clevidipine, 12.9g of lecithin, 5.1g of creatinine and 34g of soybean oil, add them into a container, use a high-speed shearing machine to disperse until dissolved, and form an oil phase, and heat to 50-60°C for later use;

[0035] (2) Take 3.1g of sodium metabisulfite and 1.5g of hydroxypropyl butyl ester into the water for injection, adjust the pH value of the aqueous phase to 9.2 with sodium hydroxide, mix well and heat to a temperature of 50-60°C for later use;

[0036] (3) Under the protection of nitrogen, slowly drop the water phase obtained above into the oil phase under the condition of stirring, the dropping speed is 5-10ml / min, stir for 25 minutes after dropping, and then transfer to a high-speed homogenizer for high-speed stirring 3-5 times, 5-10min each time, to obtain a uniform white emulsion;

[0037] (4) Add 1,000ml of water for injection at 50-60°C to the white emulsion obtained in (3), mix it evenly, and transfer it to a high-pressure...

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Abstract

The invention relates to a clevidipine lipid microsphere injection, which comprises the following 1 part of clevidipine, 68-90 parts of soybean oil, 23.1-25.7 parts of lecithin, 8.9-10.2 parts of creatinine, 4.5-6.2 parts of sodium metabisulfite, 2-3.1 parts Parts of hydroxypropyl butyl and water for injection. The lipid microsphere injection greatly increases the stability of clevidipine, has simple preparation process, high yield and good reconstitution.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a safe and stable clevidipine lipid microsphere injection and a preparation method thereof. Background technique [0002] Hypertension is the most common chronic disease in my country and the main risk factor for cardiovascular and cerebrovascular diseases. The main complications of elevated blood pressure include stroke, myocardial infarction, heart failure, and chronic kidney disease, which not only cause disability and high mortality, but also consume medical and social resources, and impose a heavy burden on the family and the country. Over the years, practice at home and abroad has proved that hypertension is a disease that can be prevented and controlled. Reducing the blood pressure level of hypertensive patients can significantly reduce stroke and heart disease events, significantly improve the quality of life of patients, and effectively reduce the b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/44A61K47/24A61K47/22A61K31/4422A61P9/12
CPCA61K9/1075A61K9/0002A61K9/0019A61K31/4422A61K47/22A61K47/24A61K47/44
Inventor 严洁王志凤
Owner TIANJIN HANKANG PHARMA BIOTECH
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