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Clevidipine butyrate intralipid and preparation method thereof

A technology of clevidipine butyrate and fat emulsion, which is applied in the directions of oil/fat/wax inactive ingredients, pharmaceutical formulations, emulsion delivery, etc. Thermodynamic instability and other problems, to achieve the effects of low preparation cost, low biological toxicity, and improved physical stability

Active Publication Date: 2013-07-24
SHANGHAI ACEBRIGHT PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, fat emulsion is a submicron emulsion drug delivery system, which is a thermodynamically unstable system with a tendency of spontaneous polymerization, which can easily affect the chemical stability of clevidipine butyrate, resulting in impurities, side effects and drug safety.

Method used

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  • Clevidipine butyrate intralipid and preparation method thereof
  • Clevidipine butyrate intralipid and preparation method thereof
  • Clevidipine butyrate intralipid and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0033] a) Prepare the oil phase: dissolve and disperse 0.05g of clevidipine butyrate active ingredient, 1.2g of lecithin, 0.1g of distearoylphosphatidylglycerol (DSPG), and 0.1g of vitamin E in 20g of medium-chain triglycerides (MCT ), heated to 60°C for use;

[0034] b) Preparation of water phase: Dissolve and disperse 2.3g glycerin and 0.005g EDTA-2Na in 60mL water for injection, heat to 60°C for use;

[0035] c) mixing and shearing the prepared oil phase and water phase to form colostrum;

[0036] d) dilute the volume of colostrum to 100mL with water for injection, and then circulate and homogenize 6 times under a pressure of 800bar to obtain end milk;

[0037] e) adding NaOH to adjust pH=8.0;

[0038] f) After filtering with a microporous membrane with a pore size of 0.8 μm, fill with nitrogen, and sterilize to obtain the clevidipine butyrate fat emulsion.

Embodiment 2

[0046] a) Prepare the oil phase: Dissolve and disperse 0.05g clevidipine butyrate active ingredient, 1.2g lecithin, 0.5g distearoylphosphatidylglycerol (DSPG) in 20g medium chain triglycerides (MCT), heat to 80°C for use;

[0047] b) Prepare the water phase: dissolve and disperse 2.3g of glycerin in 60mL of water for injection, heat to 80°C for use;

[0048] c) mixing and shearing the prepared oil phase and water phase to form colostrum;

[0049] d) dilute the volume of colostrum to 100mL with water for injection, and then circulate and homogenize 8 times under a pressure of 600bar to obtain end milk;

[0050] e) adding NaOH to adjust pH=8.0;

[0051] f) After filtering with a microporous membrane with a pore size of 0.8 μm, fill with nitrogen, and sterilize to obtain the clevidipine butyrate fat emulsion.

Embodiment 3

[0058] a) Prepare the oil phase: dissolve and disperse 0.05g of clevidipine butyrate active ingredient, 1.2g of lecithin, and 1.0g of distearoylphosphatidylglycerol (DSPG) in 20g of medium-chain triglycerides (MCT), and heat to 70°C for use;

[0059] b) Prepare the water phase: dissolve and disperse 2.3g of glycerin in 60mL of water for injection, heat to 70°C for use;

[0060] c) mixing and shearing the prepared oil phase and water phase to form colostrum;

[0061] d) dilute the volume of colostrum to 100mL with water for injection, and then circulate and homogenize it 4 times under a pressure of 1000bar to obtain end milk;

[0062] e) adding NaOH to adjust pH=8.0;

[0063] f) After filtering with a microporous membrane with a pore size of 0.8 μm, fill with nitrogen, and sterilize to obtain the clevidipine butyrate fat emulsion.

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Abstract

The invention discloses a clevidipine butyrate intralipid and a preparation method thereof. The intralipid comprises clevidipine butyrate active components, injection oil, an emulsifier, an isoosmotic adjusting agent, a pH adjusting agent and injection water, and also comprises a stabilizer, and the stabilizer is an electronegative phosphatide compound. The preparation method of the intralipid comprises the following steps: preparing an oil phase, preparing a water phase, mixing the prepared oil phase with the prepared water phase, shearing to form an crude intralipid, adding water to a constant volume, carrying out high pressure homogenization to obtain a finished intralipid, adjusting the pH value, filtering, carrying out nitrogen loading, and disinfecting. The addition of the electronegative phosphatide compound as the stabilizer in the invention improves the stability of the clevidipine butyrate intralipid, reduces the toxic side effects, ensures the use safety of the clevidipine butyrate intralipid, and has practical values.

Description

technical field [0001] The invention relates to a clevidipine butyrate fat emulsion and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Clevidipine Butyrate (Clevidipine Butyrate) is a third-generation dihydropyridine L-type calcium antagonist, which selectively acts on vascular smooth muscle, has no effect on heart rate and myocardial contractility, and has no effect on myocardium and sinoatrial node. During intravenous infusion, it reaches a steady state within 2 minutes, and can reduce blood pressure by 4 to 5% in 2 to 3 minutes. This product is hydrolyzed and metabolized in the blood and tissues, with a half-life of only 1.6 minutes, and the blood pressure can be restored within 15 minutes after stopping the infusion. It can precisely control the blood pressure by controlling the infusion speed without accumulating toxicity. It is a new type of emergency drug for hypertension and is suitable fo...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/4422A61K47/24A61K47/26A61K47/44A61P9/12
Inventor 安晓霞牛国琴陈香夏秦何桃斌杜晓敏
Owner SHANGHAI ACEBRIGHT PHARMA CO LTD
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