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Clevidipine butyrate composition for injection and preparation method thereof

A technology of clevidipine butyrate and composition, which is applied in the field of clevidipine butyrate emulsion for injection and its preparation, can solve problems such as easy collapse, decreased drug encapsulation rate, increased drug leakage, etc. Effect of improving encapsulation rate and increasing operability

Active Publication Date: 2018-01-02
BEIJING LANDAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among the aqueous surfactants used, Tween and poloxamer are irritating to a certain extent. Moreover, after glycerol is added to the prescription, the sample is easy to collapse during the freeze-drying process, and what is more serious is that the drug is packaged after reconstitution. Decreased seal rate, leading to increased leakage of drugs

Method used

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  • Clevidipine butyrate composition for injection and preparation method thereof
  • Clevidipine butyrate composition for injection and preparation method thereof
  • Clevidipine butyrate composition for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] prescription:

[0040]

[0041] crafting process:

[0042] (1) Preparation of the water phase: add sucrose and edetate disodium into water to dissolve, heat to 65°C, and set aside;

[0043] (2) Preparation of the oil phase: heating medium-chain triglycerides to 65°C, adding egg yolk lecithin, oleic acid to dissolve, adding clevidipine butyrate, and stirring to dissolve;

[0044] (3) Preparation of colostrum: Add the oil phase of step (2) into the water phase of step (1), at a temperature of 65°C, high-speed shear dispersion, shear speed of 10,000 rpm, and time of 15 minutes, to form colostrum

[0045] (4) High-pressure homogenization: Step (3) is subjected to high-pressure homogenization by a micro-jet homogenizer twice, with a pressure of 1000 to 1200 bar;

[0046] (5) Preliminary filtration: Prefilter the refined milk in step (4) through a 0.45 μm filter membrane;

[0047] (6) Sterile filtration: the emulsion obtained in step (5) is sterilized by filtration thro...

Embodiment 2

[0051] Comparative example 1 and the comparison of embodiment 1

[0052] (1) Appearance evaluation

[0053] It is better to maintain the original volume, not collapse, not shrink, the surface is smooth, and it can fall off in one piece but not broken. For color evaluation, it is better to have uniform color, no mottle, and fine texture.

[0054] (2) Evaluation of redispersibility

[0055] Take the freeze-dried products of each prescription, add 1mL of water for injection, and shake to disperse. It is better to disperse quickly to obtain a uniform solution after shaking. The less the number of shakes, the better the redispersibility.

[0056] (3) Determination of Encapsulation Efficiency

[0057] Determination of encapsulation efficiency by ultrafiltration centrifugation

[0058] ①Choose a 10K ultrafiltration centrifuge tube and centrifuge at 3000rpm for 5 minutes to measure the particle size distribution of the viscous upper layer and whether there are particles in the s...

Embodiment 3

[0072] prescription:

[0073]

[0074] crafting process:

[0075] (1) Preparation of the water phase: add lactose and edetate disodium into water to dissolve, heat to 55°C, and set aside;

[0076] (2) Preparation of the oil phase: heating medium-chain triglycerides to 55°C, adding egg yolk lecithin, oleic acid to dissolve, adding clevidipine butyrate, and stirring to dissolve;

[0077] (3) Preparation of colostrum: Add the oil phase of step (2) into the water phase of step (1), at a temperature of 55°C, high-speed shear dispersion, shear speed of 8000rpm, and time of 30 minutes to form colostrum

[0078] (4) High-pressure homogenization: Step (3) is homogenized by a micro-jet homogenizer for 3 times at a pressure of 800 to 1000 bar;

[0079] (5) Preliminary filtration: Prefilter the refined milk in step (4) through a 0.45 μm filter membrane;

[0080] (6) Sterile filtration: the emulsion obtained in step (5) is sterilized by filtration through a 0.22 μm microporous membra...

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Abstract

The invention relates to a clevidipine butyrate composition for injection, which consists of the following raw and auxiliary materials in the weight ratio: 25-50 parts of clevidipine butyrate, 100-1000 parts of oil for injection, and 6-180 parts of egg yolk lecithin , 0.3-9 parts of oleic acid, 0.05-5 parts of edetate disodium, 50-4000 parts of lyoprotectant. The present invention removes the highly irritating water-phase surfactant and uses oil-phase auxiliary emulsifier oleic acid instead, which not only ensures the emulsification effect, but also improves safety; the glycerin is removed, the freeze-drying process is not easy to collapse, and the freeze-drying process is increased. The workability of the dry product, while, unexpectedly, the removal of glycerol improved the product's encapsulation efficiency and reduced drug leakage.

Description

technical field [0001] The invention relates to a clevidipine butyrate composition and a preparation method thereof, in particular to a clevidipine butyrate emulsion for injection and a preparation method thereof. Background technique [0002] Clevidipine belongs to dihydropyridine derivatives and is an ultra-short-acting calcium channel blocker for intravenous injection. Clevidipine has a high degree of vascular and myocardial selectivity, its onset of action is fast, and its effect is eliminated quickly, and it can accurately control blood pressure with increasing doses. [0003] The chemical name of clevidipine butyrate is (±)-4-(2',3'-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxy Acid methyl (butyryloxymethyl) ester having the formula C 21 h 23 Cl 2 NO 6 , the molecular weight is 456.3, and the structural formula is: [0004] [0005] Clevidipine butyrate is insoluble in water and needs to be made into a liquid emulsion suitable for intravenous ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/12A61K31/4422A61P9/12
Inventor 林金平其他发明人请求不公开姓名
Owner BEIJING LANDAN PHARMA TECH
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