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Beta-elemene self-microemulsion and preparation method thereof

A technology of elemene and self-microemulsion, applied in the field of β-elemene self-microemulsion and its preparation, can solve the problems of easily causing phlebitis, poor water solubility, poor absorption, etc., and achieve improved bioavailability and stability High, low energy consumption effect

Active Publication Date: 2020-05-12
QILU UNIV OF TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the high fat solubility and poor water solubility of β-elemene, the ordinary elemene emulsion has poor absorption and low bioavailability; β-elemene stimulates blood vessels and tissues when injected and administered, which is easy to cause phlebitis, leading to medication Symptoms such as pain and fever sometimes occur, so deep vein administration or direct application to abdominal lesions is often used, and patient compliance is poor.

Method used

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  • Beta-elemene self-microemulsion and preparation method thereof
  • Beta-elemene self-microemulsion and preparation method thereof
  • Beta-elemene self-microemulsion and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0035] Embodiment 1, the preparation of β-elemene self-microemulsion

[0036] Polyoxyethylene 40 hydrogenated castor oil and ethyl oleate are mixed evenly at a volume ratio of 10:6, and then mixed with β-elemene at a volume ratio of 16:3, and stirred evenly to obtain polyoxyethylene 40 hydrogenated castor oil: oil A mixture of ethyl acetate: β-elemene (10:6:3); polyethylene glycol 400 and the mixture are mixed at a volume ratio of 8:19, and then stirred evenly in a constant temperature water bath at 37°C to obtain clarification Transparent self-microemulsion of β-elemene.

Embodiment 2

[0037] Embodiment 2, the preparation of β-elemene self-microemulsion

[0038] Polyoxyethylene 40 hydrogenated castor oil and ethyl oleate are mixed evenly at a volume ratio of 10:6, and then mixed with β-elemene at a volume ratio of 16:8, and stirred evenly to obtain polyoxyethylene 40 hydrogenated castor oil: oil A mixture of ethyl acetate: β-elemene (10:6:8); after mixing polyethylene glycol 400 and the mixture at a volume ratio of 8:24, stir evenly in a constant temperature water bath at 37°C to obtain clear Transparent self-microemulsion of β-elemene.

Embodiment 3

[0039] Embodiment 3, the preparation of β-elemene self-microemulsion

[0040] Polyoxyethylene 40 hydrogenated castor oil and ethyl oleate are mixed evenly at a volume ratio of 15:6, and then mixed with β-elemene at a volume ratio of 21:8, and stirred evenly to obtain polyoxyethylene 40 hydrogenated castor oil: oil Ethyl acetate: β-elemene (15:6:8) mixed solution; after mixing polyethylene glycol 400 and the mixed solution at a volume ratio of 8:29, stir evenly in a constant temperature water bath at 37°C to obtain clarification Transparent self-microemulsion of β-elemene.

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Abstract

The invention discloses beta-elemene self-microemulsion and a preparation method thereof. The beta-elemene self-microemulsion comprises the following raw materials in parts by volume of 6 parts of ethyl oleate, 10-15 parts of surfactants, 6-10 parts of cosurfactants and 3-12 parts of beta-elemene. The preparation method comprises the following steps of (1) mixing polyoxyethylene 40 hydrogenated castor oil with the ethyl oleate to obtain mixed liquor a; (2) mixing the beta-elemene with the mixed liquor a so as to obtain mixed liquor b; and (3) stirring and mixing PEG400 with the mixed liquor b,and after complete and stable emulsifying, stopping stirring so as to obtain the beta-elemene self-microemulsion. The beta-elemene self-microemulsion produced by the method disclosed by the inventionis clear and transparent in appearance, presents uniform and baby blue opalescence and has favorable stability, the particle diameter is smaller than 50nm, and the orally-taken biological availability of a rat can be increased.

Description

technical field [0001] The invention relates to a β-elemene self-microemulsion and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] β-Elemene is extracted from Zedoary Curcumae, and it is the main active ingredient of anti-tumor, anti-thrombotic, and anti-virus, and has anti-tumor, anti-bacterial, liver-protecting, and anti-psoriasis effects. It is a candidate drug with low toxicity and high efficiency. It has no obvious damage to heart, liver and kidney function, and does not inhibit bone marrow. It has great development prospects. However, due to the high fat solubility and poor water solubility of β-elemene, the ordinary elemene emulsion has poor absorption and low bioavailability; β-elemene stimulates blood vessels and tissues when injected and administered, which is easy to cause phlebitis, leading to medication Symptoms such as pain and fever sometimes occur, so deep vein administration is oft...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/14A61K47/10A61K47/44A61K31/015A61P35/00A61P31/04A61P1/16A61P17/06
CPCA61K9/1075A61K47/14A61K47/10A61K47/44A61K31/015A61P35/00A61P31/04A61P1/16A61P17/06
Inventor 王言才郭娟闫贝贝黄璐琦
Owner QILU UNIV OF TECH