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A kind of preparation method and application of cinnamon aldehyde submicroemulsion for injection

A technology of cinnamic aldehyde and sub-microemulsion, which is applied in the directions of anti-inflammatory agent, emulsion delivery, aldehyde active ingredients, etc., can solve the problems of frequent dosing, reduced anti-tumor activity, gastrointestinal adverse reactions, etc., and achieves direct cost Low cost, good formulation stability and safe use

Inactive Publication Date: 2017-01-11
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] Hydroxycamptothecin has a good curative effect on solid tumors in animals and humans. However, due to its water-insoluble and fat-insoluble properties, the anti-tumor activity of the currently commercially available hydroxycamptothecin injection is reduced, and the administration is frequent. Serious side effects limit its application to a certain extent

Method used

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  • A kind of preparation method and application of cinnamon aldehyde submicroemulsion for injection
  • A kind of preparation method and application of cinnamon aldehyde submicroemulsion for injection
  • A kind of preparation method and application of cinnamon aldehyde submicroemulsion for injection

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Experimental program
Comparison scheme
Effect test

Embodiment l

[0040] Embodiment 1: the preparation of cinnamaldehyde submicroemulsion injection

[0041] [Prescription] Cinnamaldehyde 1.0g, refined soybean oil 20.7g, egg yolk lecithin 2.4g, glycerin 5.4g, sodium oleate 0.2g, vitamin E 0.2g, add water for injection to 200ml

[0042] 【Preparation】

[0043] (1) Preparation of oil phase: heat 20.7g of refined soybean oil to 55°C, add 2.4g of egg yolk lecithin to dissolve, add 1.0g of cinnamon aldehyde, stir to dissolve;

[0044] (2) Preparation of the water phase: adding sodium oleate and glycerol into water to dissolve, and heating to 55° C.;

[0045] (3) Preparation of colostrum: Add the oil phase of step (1) into the water phase of step (2), at a temperature of 55°C, high-speed shear dispersion, a shear rate of 20,000 rpm, and a time of 10 minutes to form colostrum, and quickly cool down to 15 -30°C;

[0046] (4) High-pressure homogenization: the colostrum in step (3) is homogenized under high pressure for 3 times, the pressure is 1300 ...

Embodiment 2

[0051] Embodiment 2: Pilot scale preparation of cinnamon aldehyde submicroemulsion injection

[0052] [Prescription] Cinnamaldehyde 10.0g, refined soybean oil 200.0g, egg yolk lecithin 24.0g, glycerin 50.0g, sodium oleate 2.0g, vitamin E 2.0g, add water for injection to 2000mL

[0053] [preparation method] with embodiment 1.

Embodiment 3

[0054] Embodiment 3: the preparation of cinnamaldehyde nanoparticles

[0055] [Prescription] Cinnamaldehyde 8.0g, Tween-8064.0g, absolute ethanol 6.0g, 1,2-propanediol 4.0g, vitamin E4.0g, water for injection 120mL

[0056] [Preparation method] Prepared according to the preparation method of Ouyang Wuqing et al. (an oil-in-water type cinnamaldehyde nanoemulsion drug).

[0057] (2) Detection of physical and chemical properties of cinnamon aldehyde submicroemulsion injection and comparative study on its superiority and efficacy

[0058] 1. Physical and chemical indicators of submicroemulsion injection

[0059] (1) Stability of submicroemulsion: through the test of influencing factors, it was found that the prepared submicroemulsion injection (instructions attached) figure 1 : Finished product photo) Under the conditions of high temperature (60±2°C), high humidity (RH75±5%, 25±2°C), and strong light (4500±500LX), it is stable within 10 days.

[0060] (2) Submicroemulsion parti...

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Abstract

The invention discloses a preparation method and application of a cinnamaldehyde submicroemulsion for injection. The cinnamaldehyde submicroemulsion is prepared from the following components in percentage by weight-volume: 5.1-30.6 percent of oil, 0.5-3.0 percent of emulsifier, 1-4 percent of osmotic pressure regulator, 0.1-0.3 percent of stabilizer, 0.05-0.2 percent of antioxidant and the balance of distilled water. The submicroemulsion has excellent stability, biocompatibility and safety; the preparation method is simple, the quality is controllable, and industrial production is possible; the submicroemulsion can be used for treating tumors and other diseases.

Description

technical field [0001] The invention relates to a preparation method and application of cinnamon aldehyde submicroemulsion injection. Background technique [0002] Cinnamaldehyde (cinnamaldehyde, CA), also known as cinnamaldehyde, cinnamic aldehyde, β-phenylacrolein, 3-phenyl-2-propenal, widely exists in cinnamon oil, cinnamon oil, patchouli oil, hyacinth oil and rose oil, etc. In essential oils; at present, cinnamaldehyde can be chemically synthesized. The molecular formula of cinnamaldehyde is C 9 h 8 O, molecular weight 132.16, CAS number: 104-55-2, EINECS number: 203-213-9, FEMA: 2286; density: 1.046-1.520, melting point: -7.5°C, refractive index: 1.619-1.623, boiling point: 253 ℃. Cinnamaldehyde is a colorless or light yellow liquid at room temperature; it has a strong aroma of cinnamon oil and cinnamon oil, a mild spicy aroma, and its aroma is strong and long-lasting. Cinnamic aldehyde is insoluble in water, glycerin and petroleum ether, easily soluble in ethanol ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/11A61P35/00A61P29/00A61P9/00A61P3/00
Inventor 杨倩王四旺周暄宣周四元曹蔚谢艳华孙纪元汤海峰张云龙赵航袁佳妮
Owner FOURTH MILITARY MEDICAL UNIVERSITY