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Method for preparing clevidipine fat emulsion injection

A technology of clevidipine and fat emulsion, which is applied in the field of pharmaceutical preparations, can solve problems such as poor stability, difficulty in shearing and dissolving phospholipid oil phase, and impurities in the finished product are easy to exceed the standard, and achieve the effect of small changes in product impurities

Inactive Publication Date: 2016-08-17
JIANGSU CHIA TAI FENGHAI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The present invention aims at the poor stability of the clevidipine raw material in the prior art (it is easily hydrolyzed into CLP-4 in alkaline water, easily hydrolyzed into CLP-B in acid hydrolysis, and easily produces CLP-A, CLP-C under high temperature conditions) And phospholipids are difficult to shear and dissolve in the oil phase, and the impurities in the finished product are easy to exceed the standard. Provide a method for the preparation of fat emulsion that can be used for clinical use with stable and high-quality products.

Method used

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  • Method for preparing clevidipine fat emulsion injection
  • Method for preparing clevidipine fat emulsion injection
  • Method for preparing clevidipine fat emulsion injection

Examples

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Effect test

Embodiment 1

[0028]

[0029] Preparation Process:

[0030] (1) Preparation of the oil phase: under the protection of nitrogen, weigh the prescription amount of soybean oil and medium and long-chain triglycerides, heat to 60°C, add the prescription amount of clevidipine into the oil for injection, and stir at high speed to make it Dissolved as the oil phase; keep warm at about 70°C.

[0031] (2) Preparation of the water phase: Dissolve the prescription amount of edetate disodium and glycerol in water, adjust the pH to 8 with 1N sodium hydroxide solution, add lecithin and oleic acid to stir and disperse evenly, heat the water phase and keep it warm At around 70°C.

[0032] (3) Under high-speed shearing and stirring, mix the oil phase and the water phase at a ratio of 1:3 to 1:4, shear and stir to make colostrum, add water for injection to the prescribed amount, and shear at high speed for 1 to 2 hours.

[0033] (4) Homogenization: Homogenize the colostrum under high pressure at 500-800 ...

Embodiment 2

[0042]

[0043]

[0044] Preparation Process:

[0045] (1) Preparation of the oil phase: under the protection of nitrogen, weigh the prescribed amount of soybean oil, heat it to 60°C, add the prescribed amount of clevidipine into the oil for injection, and dissolve it with high-speed shearing and stirring, and use it as the oil phase; 70 Keep warm at about ℃.

[0046] (2) Preparation of the water phase: Dissolve the prescription amount of disodium edetate and glycerol in water, adjust the pH to 9 with 1N sodium hydroxide solution, add lecithin and sodium oleate to stir and disperse evenly, heat the water phase and Keep warm at around 70°C.

[0047] (3) Under high-speed shearing and stirring, mix the oil phase and the water phase at a ratio of 1:3 to 1:4, shear and stir to make colostrum, add water for injection to the prescribed amount, and shear at high speed for 1 to 2 hours.

[0048] (4) Homogenization: Homogenize the colostrum under high pressure at 500-800bar to a...

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Abstract

The invention relates to a method for preparing a clevidipine fat emulsion injection. The method comprises the following steps: preparing an oil phase for dissolving clevidipine in oil used for injection; preparing a water phase for dissolving a metal ion chelating agent edetate disodium and an osmotic pressure regulator in water and adjusting a pH value to an optimal value and then adding an emulsifier and a stabilizing agent; and mixing the oil phase and the water phase. The clevidipine fat emulsion injection has the advantages of high stability, little change of impurity content, and low cost, accords with the injection drug administration requirements, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations and relates to a preparation method of clevidipine fat emulsion injection. Background technique [0002] Clevidipine is a short-term acting dihydropyridine calcium channel blocker with high selectivity for blood vessels and myocardium. It is rapidly metabolized into active substances in the body and has a strong activity of reducing pulse rate. Pulmonary blood vessels also have a dilating effect. Unlike many current antihypertensive drugs that are metabolized by the kidney and / or liver through intravenous injection, it is metabolized in the blood and tissues, so it does not accumulate in the body, has a fast onset of action, and quickly eliminates the effect, and can accurately control blood pressure with increasing doses . [0003] Clevidipine fat emulsion injection was approved by FDA in August 2008. It is prepared from 20% soybean oil, 1.2% refined egg yolk phospholipid, 2.25% glyce...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/4422A61P9/12
Inventor 唐云刘双朱永强
Owner JIANGSU CHIA TAI FENGHAI PHARMA
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