Clevidipine butyrate fat emulsion injection and preparation process thereof

The invention relates to a technology of clevidipine butyrate and a preparation process, which is applied in the field of pharmaceutical preparations, and can solve the problems of re-precipitation and enlargement of drugs, affecting the lipid metabolism of patients, etc., and achieve the effects of reducing toxic and side effects and ensuring safety.

Inactive Publication Date: 2012-07-04
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If the proportion of clevidipine butyrate is too large, after the raw drug is dissolved in the oil for injection, when it is mixed with the water phase for emulsification, there will be a risk of re-precipitation of the drug; if the proportion of the oil for injection is too large, then During the administration process, it will virtually increase the patient's oil input, which will affect the patient's lipid metabolism to a certain extent; if the proportion of emulsifier is too large, lecithin will enter the brain and be hydrolyzed to release choline, which will generate acetylcholine under the catalysis of enzymes , so that the increase in the content of acetylcholine in the brain will increase the probability of abnormal reactions of the central nervous system (such as delirium, convulsions, auditory and visual hallucinations, etc.)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Under the protection of nitrogen, weigh 250g of soybean oil for injection and 250g of medium-chain triglycerides, mix well, heat to 80°C, add 30g of refined egg yolk lecithin, 2.5g of clevidipine butyrate, stir at high speed until completely dissolved, As the oil phase, keep it warm at 70°C; add 250g of xylitol for injection into 2500mL of water for injection, mix well, adjust the pH value to 8.5 with 1mol / L sodium hydroxide solution, and filter through a 0.22μm filter membrane as Water phase, heated and kept at 70°C; under high-speed shearing and stirring, slowly add the oil phase to the water phase, and continue high-speed shearing and stirring to make colostrum, add water for injection to 5L; Homogenize the milk under 600bar pressure until the droplet size is 50-500nm; adjust the pH value to 8.0, filter through 1μm, fill it into a 50mL glass infusion bottle, fill it with nitrogen, plug it, press the cap, and put it in a rotary water bath sterilizer Sterilize in mediu...

Embodiment 2

[0031] Under the protection of nitrogen, weigh 250g of soybean oil for injection and 250g of medium-chain triglycerides, mix well, heat to 75°C, add 30g of refined egg yolk lecithin, 5.0g of clevidipine butyrate, stir at high speed until completely dissolved, As the oil phase, keep it warm at 60°C; add 125g of glycerin for injection into 3000mL of water for injection, mix well, adjust the pH value to 10.0 with 1mol / L sodium hydroxide solution, and filter through a 0.22μm filter membrane as the water phase , heated and kept at 60°C; under high-speed shearing and stirring, slowly add the oil phase to the water phase, and continue high-speed shearing and stirring to make colostrum, add water for injection to 5L; Homogenize the milk until the droplet size is 50-500nm; adjust the pH value to 8.5, filter through 1μm, fill into a 100mL glass infusion bottle, fill with nitrogen, stopper, press the cap, and sterilize in a rotary water bath sterilizer Bacteria, after cooling promptly ob...

Embodiment 3

[0034]Under the protection of nitrogen, weigh 125g of soybean oil for injection and 125g of medium-chain triglycerides, mix well, heat to 65°C, add 15g of refined egg yolk lecithin, 2.5g of clevidipine butyrate, stir at high speed until completely dissolved, As the oil phase, keep it warm at 65°C; add 100g of glycerin for injection and 50g of xylitol into 3500mL of water for injection, mix well, adjust the pH value to 9.5 with 1mol / L sodium hydroxide solution, pass through a 0.22μm filter membrane Filtrate as the water phase, heat and keep it at 65°C; slowly add the oil phase to the water phase under high-speed shearing and stirring, and continue high-speed shearing and stirring to make colostrum, add water for injection to 5L; Under the pressure of 80MPa, homogenize the emulsion until the particle size of the emulsion is 50-500nm; adjust the pH value to 9.0, filter through 1μm, fill it into a 100mL glass infusion bottle, fill it with nitrogen, plug it, press the cap, and put i...

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PUM

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Abstract

The invention provides a clevidipine butyrate fat emulsion injection for intravenous injection. The clevidipine butyrate fat emulsion injection is prepared from an active ingredient, namely clevidipine butyrate and excipients, namely oil for injection, an emulsifier, an isoosmotic adjusting agent, a pH value regulator and water for injection. The fat emulsion injection for the intravenous injection is developed by taking the clevidipine butyrate as the active ingredient and adding some specific kinds of excipients in a specific proportion by the preparation process; and each milliliter of clevidipine butyrate fat emulsion injection contains 0.5 or 1.0mg of the clevidipine butyrate.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a fat emulsion injection of clevidipine butyrate and a preparation process thereof. Background technique [0002] Clevidipine butyrate is a dihydropyridine derivative. It is an ultra-short-acting calcium channel blocker for intravenous injection. It is highly selective for blood vessels and myocardium, and is rapidly metabolized into inactive substances in the body. Clevidipine butyrate has a strong activity of lowering the pulse rate, and also has a dilating effect on systemic blood vessels and pulmonary blood vessels. Clevidipine butyrate has a rapid onset of action and rapid elimination of effects, and can accurately control blood pressure with increasing doses. Unlike many current intravenously administered antihypertensive drugs that are metabolized by the kidney and / or the liver, it is metabolized in the blood and tissues and therefore does not accumulate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/4422A61K47/44A61P9/12
Inventor 尹东东王杏林黄汉忠张俊伟杨志强
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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