Silymarin solubilized particles as well as preparation method and application thereof

A technology for silymarin and granules, which is applied to the field of silymarin solubilization granules and their preparation, can solve the problems of low bioavailability and an absolute bioavailability of only 0.98%, and achieve the effects of low-cost medication, good fluidity and dispersion, and low toxicity.

Inactive Publication Date: 2018-09-07
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to overcome the deficiencies of existing silymarin preparations, and provide a simple production process that can effectively improve the solubility of silymarin, increase oral absorption, increase bioavailability and blood drug concentration, reduce the dosage of silymarin, and reduce the dosage of silymarin. A silymarin solubilized granule with low cost and good palatability for animal medicine, which overcomes the shortcomings of existing silymarin preparations such as poor water solubility, poor oral absorption, low bioavailability, and absolute bioavailability of only 0.98%.

Method used

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  • Silymarin solubilized particles as well as preparation method and application thereof
  • Silymarin solubilized particles as well as preparation method and application thereof
  • Silymarin solubilized particles as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 Preparation of silymarin solubilized granules

[0045] Prepare silymarin solubilized granules as follows:

[0046] (1) Weigh 2% silymarin API, 25% hydroxypropyl-β-cyclodextrin, 35% poloxamer 188, 28% polyethylene monostearate and 10% peppermint oil according to the proportion; Measured poloxamer 188 and hydroxypropyl-β-cyclodextrin were heated and melted at 90°C to obtain mixture A;

[0047] (2) After dissolving the weighed silymarin raw material in ethanol, add the weighed polyethylene monostearate in step (1), fully oscillate and mix evenly to obtain mixture B;

[0048] (3) Add mixture B obtained in step (2) to mixture A obtained in step (1), and stir evenly to combine silymarin molecules with the carrier to obtain mixture C;

[0049] (4) Add the weighed peppermint oil into the mixture C obtained in step (3), and stir evenly at a temperature of 60°C to obtain the mixture D;

[0050] (5) Cool the mixture D obtained in step (4) to 50-80°C, and then spray an...

Embodiment 2

[0052] Example 2 Preparation of silymarin solubilized granules

[0053] Prepare silymarin solubilized granules as follows:

[0054] (1) Weigh 2.5% silymarin API, 20% phospholipids, 30% D-α-tocopherol, 40% polyoxyethylene castor oil and 7.5% clove oil; weigh the phospholipids and D-α- Tocopherol was heated and melted at 90°C to obtain mixture A;

[0055] (2) After dissolving the weighed silymarin raw material in ethanol, add the weighed polyoxyethylene castor oil in step (1), shake and mix well to obtain mixture B;

[0056] (3) Add mixture B obtained in step (2) to mixture A obtained in step (1), and stir evenly to combine silymarin molecules with the carrier to obtain mixture C;

[0057] (4) Add the weighed clove oil into the mixture C obtained in step (3), and stir evenly at a temperature of 60°C to obtain the mixture D;

[0058] (5) Cool the mixture D obtained in step (4) to 50-80°C, and then spray and granulate through a fluidized bed; wherein the temperature of the flui...

Embodiment 3

[0060] Example 3 Preparation of silymarin solubilized granules

[0061] Prepare silymarin solubilized granules as follows:

[0062] (1) Weigh 3% silymarin API, 40% polyethylene glycol 6000, 20% hydroxypropyl-β-cyclodextrin, 30% Tween-80 and 7% sorbitol according to the proportion; Polyethylene glycol 6000 and hydroxypropyl-β-cyclodextrin were heated and melted at 90°C to obtain mixture A;

[0063] (2) After dissolving the weighed silymarin raw material in ethanol, add the weighed Tween-80 in step (1), shake and mix well to obtain mixture B;

[0064] (3) Add mixture B obtained in step (2) to mixture A obtained in step (1), and stir evenly to combine silymarin molecules with the carrier to obtain mixture C;

[0065] (4) Add the weighed sorbitol to the mixture C obtained in step (3), and stir evenly under the condition of 60°C heat preservation temperature to obtain the mixture D;

[0066] (5) Cool the mixture D obtained in step (4) to 50-80°C, and then spray and granulate thr...

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Abstract

The invention discloses silymarin solubilized particles as well as a preparation method and application thereof. The silymarin solubilized particles are prepared from the following components in percentage by mass: 1 percent to 6 percent of silymarin raw material, 20 percent to 80 percent of water-soluble carrier, 10 percent to 65 percent of solubilizing agent and 4 percent to 10 percent of aromatic flavoring agent. The invention provides a brand-new solubilizing preparation formula for the silymarin; the technical blank of the field is filled up; a matching ratio of the water-soluble carrier,the solubilizing agent, the aromatic flavoring agent and the silymarin raw material is scientifically determined, the solubility and peak concentration of the slightly-soluble silymarin are remarkably improved and the bioavailability is obviously higher than that a common preparation; the plasma drug concentration is high and the dosage is reduced; meanwhile, the silymarin solubilized particles have good palatability, good flowability and dispersity, stable properties and easiness for storage; a preparation technology is simple and the operation of medication feeding is simple; an efficient,low-toxicity and low-cost medication target of the silymarin in the aspect of medical health care of veterinary medicine is successfully realized.

Description

technical field [0001] The invention belongs to the technical field of preparation of animal medicines. More specifically, it relates to a silymarin solubilized granule and its preparation method and application. Background technique [0002] Milk thistle is native to the Kashmir mountains of India and Pakistan. China introduced milk thistle from the UK in 1952. At present, milk thistle grown as a medicinal material was imported from Germany in 1972 by Tianjin Native Products Branch of China Native Products and Animal Products Import and Export Corporation. Introduced, it has been widely promoted and planted in China. [0003] Milk thistle is a newly developed variety of medicinal materials in China in recent decades. There are domestic pharmaceutical companies to make medicinal materials for treating liver diseases. In Europe, milk thistle has been used for thousands of years to treat liver diseases. The main effective active ingredient silymarin extracted from the seed ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/357A61K47/10A61K47/44A61K47/40A61K47/24A61K47/28A61K47/38A61K47/22A61K47/32A61P1/16A61P35/00A61P29/00A61P3/06A61P9/00A61P25/00
CPCA61K9/1641A61K9/1617A61K9/1623A61K9/1635A61K9/1652A61K31/357A61P1/16A61P3/06A61P9/00A61P25/00A61P29/00A61P35/00
Inventor 黄显会李洁
Owner SOUTH CHINA AGRI UNIV
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