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Milk thistle silybum marianum self-emulsified micro-emulsion composition and its preparation process

A technology of silymarin and composition, which is applied in the field of silymarin self-emulsifying microemulsion composition, can solve the problems of poor bioavailability, cannot be called microemulsion, difficult silymarin and the like

Inactive Publication Date: 2005-12-28
XIAN LIJUN PHARMA CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, silymarin is insoluble in water and has poor bioavailability, resulting in reduced curative effect
Korean patent "Oral microemulsion composition of silymarin" application number is 008013195, publication number is CN1316898A, it is proposed that microemulsion with a particle size below 1 micron can be obtained, but according to the description about microemulsion in the textbook of physical chemistry and pharmacy, microemulsion A colloidal dispersion system formed by dispersing emulsion droplets with an emulsion particle size of 10 to 100 nanometers in another liquid has a transparent appearance and uniform size. Therefore, the above invention cannot be called a microemulsion.

Method used

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  • Milk thistle silybum marianum self-emulsified micro-emulsion composition and its preparation process
  • Milk thistle silybum marianum self-emulsified micro-emulsion composition and its preparation process
  • Milk thistle silybum marianum self-emulsified micro-emulsion composition and its preparation process

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Embodiment Construction

[0009] Example 1

[0010] Mix hydrogenated castor oil and absolute ethanol evenly according to the formula amount, add ethyl linoleate and ultrasonically oscillate to form a blank microemulsion concentrate, add the formula amount of silymarin, and magnetically stir at room temperature until the silymarin microemulsion concentrate is fully dissolved.

[0011] Rat isolated small intestine absorption experiment of silymarin microemulsion

[0012] when sampling

[0013] From the above results, the total absorption rate of silymarin microemulsion in 4.5 hours is 49.0%.

[0014] Absorption test of silymarin solution in isolated small intestine of rats

[0015] when sampling

[0016] From the above results, the total absorption rate of the silymarin solution in 4.0 hours was 32.2%.

[0017] From the absorption results of isolated small intestine of rats, it can be seen that microemulsification of silymarin does improve the absorption of silymarin.

...

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Abstract

The invention relates to a silymarin self-emulsifying microemulsion composition and a preparation process thereof. The invention can make the particle size of the silymarin reach the nanometer level, improve the solubility of the silymarin, and improve the absorption. A silymarin self-emulsifying microemulsion composition comprising silymarin, ethyl linoleate, hydrogenated castor oil and absolute ethanol. The surface tension of the microemulsion system of the present invention is smaller than that of simple external phase water, and each microemulsion system greatly improves the solubility of silymarin. It can be seen from the scanning electron microscope that the microemulsion particles are spherical or nearly spherical, and the particle size distribution shows that most of them are concentrated in the range of 10-50 nm, with an average particle size of 17.2 nm.

Description

technical field [0001] The invention relates to a silymarin self-emulsifying microemulsion composition and a preparation process thereof. Background technique [0002] Silymarin is a general term for a class of flavonoids extracted and isolated from the fruit of the Compositae plant, Milk Thistle. Pharmacological and toxicological studies have shown that silymarin has obvious effects of protecting and stabilizing liver cells, and is mainly used clinically for the treatment of acute and chronic hepatitis. However, silymarin is insoluble in water and has poor bioavailability, resulting in reduced curative effect. Korean Patent "Oral Microemulsion Composition of Silymarin" application number is 008013195, publication number is CN1316898A, it is proposed that microemulsions with a particle size below 1 micron can be obtained, but according to the description about microemulsions in the textbooks of physical chemistry and pharmacy, microemulsions The colloidal dispersion system...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/357A61P1/16A61P31/12
Inventor 刘艳李晓燕李馨儒赵振伟
Owner XIAN LIJUN PHARMA CO LTD
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