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Preparation method and application of cinnamaldehyde submicroemulsion for injection

A technology of cinnamon aldehyde and submicron emulsion, which is applied in anti-inflammatory agents, emulsion delivery, active ingredients of aldehydes, etc. It can solve the problems of reduced anti-tumor activity, adverse reactions in the gastrointestinal tract, frequent administration, etc., and achieve stable preparations Good performance, low direct cost, and safe use

Inactive Publication Date: 2014-10-01
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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  • Preparation method and application of cinnamaldehyde submicroemulsion for injection
  • Preparation method and application of cinnamaldehyde submicroemulsion for injection
  • Preparation method and application of cinnamaldehyde submicroemulsion for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment l

[0041] Example 1: Preparation of cinnamon aldehyde submicroemulsion injection

[0042] [Prescription] 1.0g cinnamaldehyde, 20.7g refined soybean oil, 2.4g egg yolk lecithin, 5.4g glycerol, 0.2g sodium oleate, 0.2g vitamin E, water for injection to 200ml

[0043] 【Preparation】

[0044] (1) Preparation of oil phase: heat 20.7 g of refined soybean oil to 55°C, add 2.4 g of egg yolk lecithin to dissolve, add 1.0 g of cinnamaldehyde, and stir to dissolve;

[0045] (2) Preparation of water phase: add sodium oleate and glycerol to dissolve in water, and heat to 55°C;

[0046] (3) Preparation of colostrum: add step (1) oil phase to step (2) water phase, temperature 55℃, high-speed shear dispersion, shear speed 20,000 rpm, time 10 minutes, form colostrum, and quickly cool down to 15 -30℃;

[0047] (4) High pressure homogenization: Step (3) colostrum is homogenized 3 times by high pressure, the pressure is 1300 bar, and the temperature is controlled at 20°C;

[0048] (5) Filling: Filling and seali...

Embodiment 2

[0052] Example 2: Pilot-scale preparation of cinnamon aldehyde submicroemulsion injection

[0053] [Prescription] Cinnamaldehyde 10.0g, refined soybean oil 200.0g, egg yolk lecithin 24.0g, glycerol 50.0g, sodium oleate 2.0g, vitamin E 2.0g, water for injection to 2000mL

[0054] [Preparation method] Same as Example 1.

Embodiment 3

[0055] Example 3: Preparation of cinnamaldehyde nanoparticles

[0056] [Prescription] Cinnamaldehyde 8.0g, Tween-8064.0g, Absolute Ethanol 6.0g, 1,2-Propanediol 4.0g, Vitamin E4.0g, Water for Injection 120mL

[0057] [Preparation method] According to the preparation method of Ouyang Wuqing et al. (an oil-in-water cinnamaldehyde nanoemulsion drug).

[0058] (2) The physical and chemical properties of cinnamon aldehyde submicroemulsion injection and the comparative study on its superiority characteristics

[0059] 1. Physical and chemical indexes of submicroemulsion injection

[0060] (1) The stability of the submicroemulsion: After the influencing factor test, it is found that the prepared submicroemulsion injection (instruction attached figure 1 : Finished product photo) Under high temperature (60±2℃), high humidity (RH75±5%, 25±2℃), strong light irradiation (4500±500LX), it is stable for 10 days.

[0061] (2) Particle size of submicron emulsion: Take this product, dilute it with distill...

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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 (CA) is also known as cinnamaldehyde, cinnamic aldehyde, β-phenylacrolein, 3-phenyl-2-propenal, and is widely found in cinnamon oil, cinnamon oil, ageratum oil, hyacinth oil, rose oil, etc. In essential oils; 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; its 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 lasting. Cinnamaldehyde is difficult to dissolve in water, glycerin and petroleum ether, and is easily soluble in ethanol and ether, and c...

Claims

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Application Information

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Patent Type & Authority Applications(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
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