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Lipid nanosuspension containing clevidipine butyrate, and freeze-drying preparation of lipid nanosuspension

A technology of clevidipine butyrate and nanosuspension, which is applied in the field of preparation of lipid nanosuspension and freeze-dried preparations thereof, can solve the problems of low solubility of clevidipine butyrate, increase safety and the like, and achieve no The effect of drug leakage, increased safety, and low toxicity and side effects

Inactive Publication Date: 2014-01-01
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] For above-mentioned prior art, the present invention provides a kind of lipid nanosuspension containing clevidipine butyrate and freeze-dried preparation thereof, improved the content of clevidipine butyrate in the preparation, solved the problem of clevidipine butyrate The problem of low solubility in water; the preparation does not contain medium and long-chain triglycerides, which increases the safety of the drug; the freeze-dried preparation is prepared by the freeze-drying method, which improves the stability of the preparation and is suitable for large-scale industrial production.

Method used

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  • Lipid nanosuspension containing clevidipine butyrate, and freeze-drying preparation of lipid nanosuspension
  • Lipid nanosuspension containing clevidipine butyrate, and freeze-drying preparation of lipid nanosuspension
  • Lipid nanosuspension containing clevidipine butyrate, and freeze-drying preparation of lipid nanosuspension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Accurately weigh 1.5 g of soybean lecithin and 2.0 g of glycerin, add to 100 ml of distilled water and dissolve to form a dispersion medium (solution A). Add 50 mg of clevidipine butyrate to solution A, and ultrasonically disperse to obtain suspension B. Continue to use a high-speed shearing machine at 20000r / min for 3min and 30000r / min for 2min to obtain colostrum C. Colostrum C was subjected to a high-pressure homogenization method and circulated 10 times at 200 bar, 10 times at 500 bar, and 20 times at 800 bar to prepare clevidipine butyrate lipid nanosuspension.

[0040] Add 5.0 g of mannitol to the above-prepared suspension to fully disperse, divide into vials (2ml / bottle), and pre-freeze in a -80°C refrigerator for 24 hours. The pre-frozen sample was placed in a freeze dryer at -40°C and 0.5mbar for 48 hours to freeze-dry for 48 hours to finally obtain a white and loose clevidipine butyrate lipid nanosuspension freeze-dried preparation, such as figure 1 shown. ...

Embodiment 2

[0044] Accurately weigh 1 g of soybean lecithin, add it to 100 ml of distilled water and dissolve it to form a dispersion medium (solution A). Add 50 mg of clevidipine butyrate to solution A, and ultrasonically disperse to obtain suspension B. Continue to use a high-speed shearing machine at 20000r / min for 3min and 30000r / min for 2min to obtain colostrum C. Colostrum C was subjected to a high-pressure homogenization method and circulated 10 times at 200 bar, 10 times at 500 bar, and 20 times at 800 bar to prepare clevidipine butyrate lipid nanosuspension.

[0045] Add 2.0 g of mannitol to the above-prepared suspension to fully disperse, dispense into vials (2 ml / bottle), and pre-freeze in a -80°C refrigerator for 24 hours. The pre-frozen sample was placed in a freeze dryer at -40°C and 0.5 mbar for 48 hours to obtain a white and loose clevidipine butyrate lipid nanosuspension freeze-dried preparation. The lyophilized preparation can be completely reconstituted within 1 min b...

Embodiment 3

[0048] Accurately weigh 1.5 g of soybean lecithin, add it to 100 ml of distilled water and dissolve it to form a dispersion medium (solution A). Add 40mg of clevidipine butyrate to solution A, and ultrasonically disperse evenly to obtain suspension B. Continue to use a high-speed shearing machine at 20000r / min for 3min and 30000r / min for 2min to obtain colostrum C. Colostrum C was subjected to a high-pressure homogenization method and circulated 10 times at 200 bar, 10 times at 500 bar, and 20 times at 800 bar to prepare clevidipine butyrate lipid nanosuspension.

[0049] Add 2.0 g of mannitol to the above-prepared suspension to fully disperse, dispense into vials (2 ml / bottle), and pre-freeze in a -80°C refrigerator for 24 hours. The pre-frozen sample was placed in a freeze dryer at -40°C and 0.5 mbar for 48 hours to obtain a white and loose clevidipine butyrate lipid nanosuspension freeze-dried preparation. The lyophilized preparation can be completely reconstituted within...

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Abstract

The invention discloses a lipid nanosuspension containing clevidipine butyrate, and a freeze-drying preparation of the lipid nanosuspension. A preparation method comprises the following steps that (1) a surfactant is dispersed in an aqueous solution to form a solution A; (2) the clevidipine butyrate is dispersed in the solution A obtained in Step (1) to form a suspension solution B; (3) the suspension solution B is cut for 1-5min at a high speed to form a first emulsion C; (4) the first emulsion C is subjected to high-pressure homogenization treatment, and the clevidipine butyrate lipid nanosuspension is obtained; (5) a freeze-drying protective agent is added to the nanosuspension, and filtration and sterilization are performed; (6) freeze-drying is performed, moisture is removed, and the freeze-drying preparation of the clevidipine butyrate lipid nanosuspension is obtained. The lipid nanosuspension and the freeze-drying preparation are free of any organic solvent and long chain triglyceride or medium chain triglyceride, high in safety, low in toxic and side effects, high in drug loading capacity, good in stability and free from drug leakage; and meanwhile, a preparation technology is simple, and the repeatability is good, and the industrial production can be realized.

Description

technical field [0001] The invention relates to a preparation method of a lipid nanosuspension containing clevidipine butyrate and a freeze-dried preparation thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Hypertension is a common and multiple cardiovascular and cerebrovascular disease, and is an important risk factor for coronary heart disease and stroke. In recent years, the incidence of hypertension in my country has been increasing year by year, and it has become one of the main killers threatening human health. Therefore, research on hypertension has become a hot issue in the field of cardiovascular research. [0003] At present, the main way to treat hypertension is to rely on antihypertensive drugs. The drugs commonly used in clinical treatment of hypertension are mainly diuretic and antihypertensive drugs, β receptor blockers, angiotensin converting enzyme inhibitors and angiotensin II receptors. Body antagonis...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/19A61K31/4422A61P9/12
Inventor 张娜刘毅孔俊杰冯立霞
Owner SHANDONG UNIV
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