Gamma-tocotrienol-containing nano emulsion and preparation method and use thereof

A technology of tocotrienol and nanoemulsion, which is applied in the direction of medical preparations containing active ingredients, medical preparations with non-active ingredients, emulsion delivery, etc., and can solve the problem of unstable alkaline conditions and γ-tocotrienol Unsuitable, sensitive to oxygen and other problems, to achieve uniform and stable particle size, maintain the basic properties of the drug, and reduce blood vessel irritation

Inactive Publication Date: 2019-01-25
周晋
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In addition, due to the presence of triene bonds in the structure of γ-tocotrienol, alkaline conditions are unstable and sensitive to oxygen, the emulsion formula of tocopherol disclosed in the prior art and the method for preparing the emulsion are not suitable for γ-tocotrienol. suitable

Method used

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  • Gamma-tocotrienol-containing nano emulsion and preparation method and use thereof
  • Gamma-tocotrienol-containing nano emulsion and preparation method and use thereof
  • Gamma-tocotrienol-containing nano emulsion and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Preparation of γ-tocotrienol nanoemulsion

[0044] (1) Take 11g of soybean oil and medium-chain triglyceride oil (1:1), heat it in a water bath to 60°C, add 0.05g of γ-tocotrienol, 1.2g of egg yolk lecithin and 0.005g of sodium sulfite, stir to dissolve, A homogeneous mixture is formed, which is liquid A.

[0045] (2) Add 2.3 g of isotonicity regulator glycerin and sorbitol (3:1) into disodium hydrogen phosphate alkaline water at 70°C, stir to dissolve, keep warm in a water bath for later use, and fill with nitrogen throughout the process to form liquid B.

[0046] (3) Disperse liquid A before high-speed shearing, slowly add liquid B during shearing, continue shearing for 15 minutes after adding liquid B, and carry out nitrogen protection throughout the process.

[0047] (4) Colostrum is homogenized under high pressure, adjust the pressure level of the secondary homogenization to 80 bar, the pressure of the primary level to 800 bar, and homogenize 8 times.

...

Embodiment 2

[0049] Example 2 Preparation of γ-tocotrienol nanoemulsion

[0050] (1) Take 120g of soybean oil and medium-chain triglyceride oil (1:1), heat it in a water bath to 80°C, add 10g of γ-tocotrienol, 15g of soybean lecithin and 0.1g of sodium sulfite, stir to dissolve, and form a uniform The mixture is liquid A.

[0051] (2) Take 25 g of isotonic regulator glycerin and add it to disodium hydrogen phosphate alkaline water at 70°C, stir to dissolve, keep warm in a water bath for later use, and fill the whole process with nitrogen gas to become liquid B.

[0052] (3) Disperse liquid A before high-speed shearing, slowly add liquid B during shearing, continue shearing for 14 minutes after adding liquid B, and carry out nitrogen protection throughout the process.

[0053] (4) Colostrum is homogenized under high pressure, adjust the pressure level of the secondary homogenization to 80 bar, the pressure of the primary level to 800 bar, and homogenize 8 times.

[0054] (5) Adjust the pH...

Embodiment 3

[0055] Example 3 Preparation of γ-tocotrienol nanoemulsion

[0056] (1) Take 8g of soybean oil, heat it in a water bath to 60°C, add 0.1g of γ-tocotrienol, 1.1g of soybean lecithin and 0.005g of cysteine, stir and dissolve, and form a uniform mixture, which is liquid A.

[0057] (2) Add 2.1 g of isotonicity regulator glycerin and sorbitol (3:1) into disodium hydrogen phosphate alkaline water at 70°C, stir to dissolve, keep warm in a water bath for later use, and fill with nitrogen throughout the process to form liquid B.

[0058] (3) Disperse liquid A before high-speed shearing, slowly add liquid B during shearing, continue shearing for 12 minutes after adding liquid B, and carry out nitrogen protection throughout the process.

[0059] (4) Colostrum is homogenized under high pressure, adjust the pressure level of the secondary homogenization to 80 bar, and the pressure of the primary level to 800 bar, and homogenize 6 times.

[0060] (5) Adjust the pH to 7.0 with acidic solut...

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Abstract

The invention relates to a gamma-tocotrienol-containing nano emulsion and a preparation method and use thereof. The nano emulsion is composed of the following components by mass percentage: gamma-tocotrienol 0.02%- 10%, injection oil 5%- 20%, emulsify 0.5%- 2%, isoosmotic adjusting agent 1.5%- 3.0%, antioxidant 0.005%- 0.5 % and that balance is water. By using emulsifier, gamma-tocotrienol and injectable oil are made into nanoparticles with small particle size, high content of active ingredients and stable, and no need to add excipients such as Tween, Span, preservatives and the like in the preparation, and the safety is higher. The gamma-tocotrienol nanoemulsion prepared by the invention expands the dosage form for clinical application.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a nanoemulsion containing gamma-tocotrienol and a preparation method thereof. More specifically, the present invention relates to a stable and safe nanoemulsion without Tween, Span, preservatives, etc. and a preparation method thereof. Background technique [0002] In 1964, γ-tocotrienol was first discovered by Pennock et al., mainly including benzopyran ring and aliphatic unsaturated isoprene structural chain (the structure is formula I respectively). After in-depth research, it was found that the unsaturated isoprene tail in the structure of γ-tocotrienol plays an important role in the anti-tumor biological activity. Therefore, γ-tocotrienol has attracted much attention and has gradually become a research hotspot. According to reports, γ-tocotrienol is widely found in palm oil with the highest content (11.3-36.0mg / 100g oil), followed by barley oil (8.50-18.6mg / 100g ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/355A61K47/14A61K47/44A61K47/24A61P35/00A61P35/02
CPCA61K9/0019A61K9/1075A61K31/355A61K47/14A61K47/24A61K47/44A61P35/00A61P35/02
Inventor 周晋海鑫赵祎镭
Owner 周晋
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