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Scutelloside colon targeted medicine preparation and preparation method thereof

A technology of baicalin colon and pharmaceutical preparation, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of small drug loading, poor targeting, incomplete drug release, etc., and achieves improved solubility and reduced preparation volume. , good for dissolution and absorption

Active Publication Date: 2016-06-01
石家庄市度智医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to provide a baicalin colon-targeted drug preparation and a preparation method thereof, to solve the problems of the existing baicalin dosage forms such as small drug loading, poor targeting, and incomplete drug release, so as to treat and treat colon cancer clinically. Prevention Offers More Medication Options

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1 Preparation of baicalin-β-cyclodextrin inclusion compound

[0048] Get 1000g of ethanol aqueous solution (mass percentage concentration is 50%) that 250gβ-cyclodextrin is dissolved in; Place in constant temperature magnetic stirrer, keep temperature 40 ℃, add 600g dehydrated ethanol solution containing baicalin (baicalin 100g, 500g of absolute ethanol), stirring while adding, after 2 hours of clathrate, put the suspension containing the inclusion compound in the refrigerator for 24 hours, then filter with suction, wash the solid with absolute ethanol, and obtain the inclusion compound at 40°C Dry under reduced pressure to obtain baicalin-β-cyclodextrin inclusion compound.

Embodiment 2

[0049] Example 2 Preparation of baicalin-hydroxypropyl β-cyclodextrin inclusion compound

[0050] Dissolve 250g of hydroxypropyl β-cyclodextrin in 1000mL of water, place it in a constant temperature magnetic stirrer, add 1100g of acetone solution containing baicalin (100g of baicalin, 1000g of acetone) while stirring at 40°C, stir for 2h, 0.45 Filter through a μm microporous membrane, and spray-dry the filtrate to obtain the inclusion compound of baicalin-hydroxypropyl β-cyclodextrin.

Embodiment 3

[0051] Example 3 Preparation of baicalin-α-cyclodextrin inclusion compound

[0052] Dissolve 300g of α-cyclodextrin in 2000mL of water, place it in a constant temperature magnetic stirrer, add 900g of baicalin-containing propylene glycol solution (100g of baicalin, 800g of propylene glycol) while stirring at 40°C, stir for 2h, 0.45μm Filter through a porous membrane, and freeze-dry the filtrate for 24 hours to obtain the inclusion compound of baicalin-α-cyclodextrin.

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Abstract

The invention discloses a scutelloside colon targeted medicine preparation, which comprises scutelloside and cyclodextrin inclusion compounds, natural polysaccharide colon targeted materials and enteric coating materials at a specific proportion. Meanwhile, the invention also discloses a preparation method of the scutelloside colon targeted medicine preparation. The method comprises the following steps that scutelloside and cyclodextrin are proportionally prepared into the scutelloside and cyclodextrin inclusion compounds; the scutelloside and cyclodextrin inclusion compounds and the natural polysaccharide colon targeted materials are proportionally crosslinked and solidified; filtering, washing and drying are performed; scutelloside colon targeted protomeres are obtained; the scutelloside colon targeted protomeres are coated by a solution of the enteric coating materials, and the scutelloside colon targeted medicine preparation is obtained. The scutelloside colon targeted medicine preparation is invented by a specific method; the defect of low water solubility of the scutelloside is overcome; medicine can be located and released in the colon position; a colon targeted goal is achieved; the process is simple; the popularization and the application are easy.

Description

technical field [0001] The invention relates to a traditional Chinese medicine preparation and a preparation method thereof, in particular to a baicalin colon-targeting preparation and a preparation method thereof. Background technique [0002] Colon cancer is one of the main malignant tumors of human beings. Since the 1970s, with the progress of our society, the improvement of living conditions and the gradual westernization of people's lifestyles, the incidence of colon cancer in my country has risen rapidly, and it has become the most common cancer in my country. It is one of the five common malignant tumors and seriously endangers human health. Inflammatory bowel diseases such as ulcerative colitis and Crohn's disease are also related to the occurrence of colon cancer, and both are considered to be precancerous lesions of colon cancer. [0003] Oral colon-targeted drug delivery system is a class of pharmaceutical preparations that deliver drugs to the colon for localized...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/36A61K9/50A61K31/7048A61P35/00
CPCA61K9/0002A61K9/5026A61K9/5036A61K9/5042A61K31/7048A61K47/36
Inventor 杜青曹德英党云洁齐晓丹王静敦洁宁方瑜向柏
Owner 石家庄市度智医药科技有限公司
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