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Self-microemulsion composition, microemulsion and preparation methods thereof

A composition and self-microemulsion technology, which can be used in pharmaceutical combinations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., and can solve the problem of low solubility of oleanolic acid, poor bioavailability of oral preparations, etc. problems, to increase blood circulation time, improve bioavailability, and facilitate industrial production.

Active Publication Date: 2011-03-30
KAIHUI SCI & TECH DEV SHANGHAI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved by the present invention is to overcome the defects of the extremely low solubility of oleanolic acid in water and the poor bioavailability of its oral preparations, and provide a self-microemulsion composition that can dissolve oleanolic acid well Or its water-insoluble or water-insoluble derivatives, and the self-microemulsion composition can be mixed with water in any proportion to spontaneously form a transparent or translucent microemulsion, thereby greatly improving the solubility and dispersion of oleanolic acid in water At the same time, the particle size of the microemulsion is nano-scale, which is much smaller than the traditional emulsion (micron-scale), so it has higher bioavailability and better thermodynamic stability, which can increase the half-life of oleanolic acid and blood Circulation time, improving drug efficacy and reducing toxicity

Method used

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  • Self-microemulsion composition, microemulsion and preparation methods thereof
  • Self-microemulsion composition, microemulsion and preparation methods thereof
  • Self-microemulsion composition, microemulsion and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Dissolve oleanolic acid 10g (2.2mg / ml) in polyethylene glycol-2001000ml (22.2%), add polyoxyethylene castor oil (Cremophor EL) 1000ml (22.2%), isopropyl myristate 2500ml ( 55.6%), mixed to obtain a colorless and transparent self-microemulsion composition.

[0047] The obtained self-microemulsion composition is diluted 2 times with water to obtain microemulsion (light blue opalescent liquid), and the particle size is measured with Nicomp™ 380ZLS particle size analyzer, see figure 1 . The average particle diameter of the microemulsion is 21.9nm, and the standard deviation is 4.1nm.

Embodiment 2

[0049] Dissolve 2 g (0.44 mg / ml) of oleanolic acid in 1000 ml (22.2%) of propylene glycol, add 1000 ml (22.2%) of polyoxyethylene castor oil (Cremophor EL), 2500 ml (55.6%) of isopropyl myristate, Mix well to obtain a colorless and transparent self-microemulsion composition.

[0050] The obtained self-microemulsion composition is diluted 5 times with water to obtain microemulsion (light blue opalescent liquid), and the particle size is measured with Nicomp™ 380ZLS particle size analyzer, see figure 2 . The average particle diameter of the microemulsion is 18.8nm, and the standard deviation is 3.7nm.

Embodiment 3

[0052] Dissolve oleanolic acid 2g (0.5mg / ml) in 1000ml (25%) of glycerin, add 500ml (Labrasol) caprylic acid macrogol glyceride (Labrasol), Tween-80500ml (12.5%), caprylic acid Capric triglyceride 1000ml (25%), linoleic acid glyceride 1000ml (25%), mix well to obtain colorless transparent self-microemulsion composition.

[0053] The obtained self-microemulsion composition is diluted 10 times with water to obtain microemulsion, and the particle size is measured with Nicomp™ 380ZLS particle size analyzer, see image 3 . The average particle diameter of the microemulsion is 21.2nm, and the standard deviation is 4.4nm.

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Abstract

The invention provides a self-microemulsion composition which comprises one kind or multiple kinds of materials in oleanolic acid, water-insoluble oleanolic acid and difficultly water-soluble oleanolic acid derivant. The self-microemulsion composition also comprises an oil phase, a surface active agent and a cosurfactant, and the self-microemulsion composition does not contain water. The invention overcomes the defect that the solubility of the oleanolic acid in water is very low, provides the self-microemulsion composition capable of being diluted into the microemulsion with the nanometer level grain diameters by water or water solution, and also provides the microemulsion which obviously improves the dispersivity and the solubility of the oleanolic acid, the water-insoluble oleanolic acid and the difficultly water-soluble oleanolic acid derivant in water, so the bioavailability is improved, the half-life and the blood circulation time of the oleanolic acid can be prolonged, in addition, the microemulsion can be targeted to the tumor because of the nanometer grain diameter of the microemulsion, the curative effect of the medicine can be improved, the medicine toxin can be reduced, and in addition, filtration and sterilization can be realized, and the needle applicability of the injection can be improved. The invention also provides preparation methods of the self-microemulsion composition and the microemulsion.

Description

technical field [0001] The invention relates to a self-microemulsion composition and a microemulsion, and their preparation methods. Background technique [0002] Oleanolic acid is clinically used in the adjuvant treatment of acute and chronic hepatitis. It has a certain protective effect on liver injury, can reduce the elevated serum alanine aminotransferase, promote liver cell regeneration, and accelerate the repair of necrotic tissue. Modern pharmacological studies have shown that in addition to protecting the liver, oleanolic acid also has the functions of lowering fat, lowering blood sugar, anti-tumor, and two-way immune regulation. At present, the development and utilization of oleanolic acid other than liver protection are still rare, and its clinical preparations mainly include tablets and capsules. [0003] In terms of physical and chemical properties, oleanolic acid is an alkane-type pentacyclic triterpenoid compound, and its powder is white crystal, odorless, ta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/14A61K9/48A61K9/70A61K31/56A61K47/34A61K47/44A61K47/14A61P1/16A61P3/06A61P3/10A61P35/00A61P37/02
Inventor 施斌焦艳张志明李原强
Owner KAIHUI SCI & TECH DEV SHANGHAI
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