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1, 8-cineole emulsion and preparation method thereof

A technology of eucalyptol and emulsion, which is applied in the direction of pharmaceutical formula, emulsion delivery, oil/fat/wax non-active ingredients, etc., can solve the problems of strong volatility, limited application, low safe concentration range, etc., and achieve toxic and side effects Reduce, improve the effect of the drug, and be easily absorbed

Active Publication Date: 2021-07-02
GUIZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The existing traditional preparations targeting cardiovascular inflammatory factor delivery systems are difficult to obtain suitable clinical application methods due to their immiscibility with water and strong volatility, which greatly limits their clinical application
Since 1,8-CNL controls the nuclear translocation of NF-κB p65 through a potential anti-inflammatory mechanism such as the induction of IkBa, resulting in the reduction of NF-κB activity and thus improving the dysfunction of endothelial cells, it can effectively regulate NF-κB activation-related inflammation response, so the applicant has studied the 1,8-cineole self-microemulsion drug delivery system in the early stage, but the 1,8-cineole self-microemulsion drug delivery system has a lower safe concentration range, 1 , the efficacy of 8-cineole can not be fully exerted

Method used

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  • 1, 8-cineole emulsion and preparation method thereof
  • 1, 8-cineole emulsion and preparation method thereof
  • 1, 8-cineole emulsion and preparation method thereof

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Embodiment 1

[0075] When preparing 1,8-cineole lipid microsphere delivery emulsion, 1,8-CNL-LM emulsion, the average particle size (D 50 ) and centrifugal stability constant (Ke) were used as the investigation indexes for experimental optimization. Determine the best prescription of 1,8-CNL-LM, in terms of parts by mass: 50 parts of 1,8-CNL, 50 parts of soybean oil, 153 parts of HS, 9 parts of soybean lecithin, 25 parts of glycerin, 5 parts of oleic acid, and the rest The amount is distilled water, and the add-on of distilled water is the add-on amount that makes solution from turbidity to the critical point when clarification.

[0076] The preparation method of above-mentioned 1,8-CNL-LM is:

[0077] Step 1. Take the raw materials corresponding to the above proportions, heat HS15, glycerin and distilled water to 60°C and mix them evenly. After cooling down to room temperature, cool in an ice bath to 0-15°C to obtain the water phase;

[0078] Step 2. Mix soybean oil, oleic acid and soybe...

Embodiment 2

[0109] When preparing 1,8-cineole sustained-release lipid microsphere delivery emulsion, 1,8-CNL-SRLM emulsion, the average particle size (D 50 ) and centrifugal stability constant (Ke) were used as the investigation indexes for experimental optimization. Determine the best prescription of 1,8-CNL-SRLM, in parts by mass: 40 parts of 1,8-cineole, 20 parts of MCT, 40 parts of soybean oil, 154 parts of HS, 8 parts of soybean lecithin, 25 parts of glycerin , 3 parts of oleic acid, 3 parts of sodium oleate, 0.5 part of stearic acid, and the remainder is distilled water, and the add-on of distilled water is the add-on of critical point when making solution from turbid to clarification.

[0110] The preparation method of the above-mentioned 1,8-CNL-SRLM is:

[0111] Step 1. Take the raw materials corresponding to the above proportions, heat HS15, glycerin and distilled water to 60°C and mix them evenly. After cooling down to room temperature, cool in an ice bath to 0-10°C to obtain ...

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Abstract

The invention discloses a 1, 8-cineole emulsion and a preparation method thereof. The 1, 8-cineole emulsion is prepared from, by mass, 80-120 parts of a mixed oil phase, 10-15 parts of an emulsifier, 20-30 parts of a co-emulsifier, 5-10 parts of a stabilizer and the balance distilled water; the mixed oil phase comprises 1, 8-cineole and other oil phases, wherein the mass ratio of the 1, 8-cineole to other oil phases is (1: 10)-(10: 1), and the mass ratio of the 1, 8-cineole to the mixed emulsifier is (1: 10)-(10: 1); wherein the addition amount of the distilled water is the addition amount of a critical point when the solution is changed from turbid to clear. The 1, 8-cineole emulsion disclosed by the invention has the characteristics of expanding the safe concentration range of the 1, 8-cineole emulsion, improving the drug absorption rate of the 1, 8-cineole and improving the drug effect of the 1, 8-cineole.

Description

technical field [0001] The invention relates to a preparation of 1,8-cineole, in particular to a 1,8-cineole emulsion and a preparation method thereof. Background technique [0002] The incidence of cardiovascular disease has been at the forefront of major diseases for many years, and it is on the rise and younger. The death and disability rate caused by cardiovascular events is extremely high, the disease cycle is long, and the patient's compliance with long-term high-frequency drug treatment is poor. , and high nursing costs etc. have brought great pain and heavy burden to individuals, families and society. [0003] Vascular endothelial cells (VEC), also known as endothelial cells, usually refer to the single-layer squamous epithelium lining the inner surface of the heart, blood vessels and lymphatic vessels, forming the inner wall of blood vessels, between blood flow and blood vessel wall tissue, and have the ability to phagocytose Foreign matter, bacteria, necrotic and ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/35A61K47/44A61K47/24A61K47/10A61K47/12A61P9/00
CPCA61K9/107A61K31/35A61K47/44A61K47/24A61K47/10A61K47/12A61P9/00Y02P20/54
Inventor 沈祥春陶玲张敏吴林菁肖婷周雪姜丰陈英
Owner GUIZHOU MEDICAL UNIV
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