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Intestine-protecting and detoxifying micro pellets and use thereof

A micro-pill and detoxification technology, which is applied in the direction of medical formula, medical preparations containing active ingredients, bulk delivery, etc., can solve the problem of low bioavailability of the colon, achieve the elimination of intestinal endotoxins, protect the intestinal barrier, relieve damage effect

Active Publication Date: 2013-05-08
THE AFFILIATED HOSPITAL OF SHANDONG UNIV OF TCM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After oral administration of conventional preparations of traditional Chinese medicine, the drug is absorbed through the gastrointestinal tract and enters the systemic circulation before reaching the colon, and the bioavailability of the colon is not high
Colon-targeted drug delivery not only makes the active ingredients of the drug less likely to be destroyed by digestive juices, but also enables the drug to reach the disease directly. Therapeutic method with higher use value; but the conventional drug enema in the prior art is only limited to the rectum and sigmoid colon, and is restricted by the inconvenience of enema in patients with anorectal disease, etc.
At present, there are no research reports on the clearance of gut-derived endotoxin by colon-targeted drug delivery

Method used

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  • Intestine-protecting and detoxifying micro pellets and use thereof
  • Intestine-protecting and detoxifying micro pellets and use thereof
  • Intestine-protecting and detoxifying micro pellets and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Study on the preparation process of Huchangqingdu pellets

[0030] 1. Instruments and reagents

[0031] Spray dryer (Wuxi Qianzhou Dryer Complete Equipment Factory), extrusion-spheronizing pelletizing machine (Chemical Machinery Research Institute, East China University of Science and Technology), ultrafine pulverizer (Jinan Beili Powder Technology Engineering Co., Ltd.), 78X-2 Tablet four-purpose tester (Shanghai Huanghai Drug Inspection Instrument Factory).

[0032] Microcrystalline cellulose (MCC101, Taiwan Mingtai Company, batch number: 80920), anhydrous calcium chloride (Tianjin Bodi Chemical Co., Ltd., batch number: 80329014), paeoniflorin reference substance (China Institute for the Control of Pharmaceutical and Biological Products, 110736- 200629) medicinal powder (prepared by fine powder after extraction and drying), low-fat pectin (Henan Zhengzhou Yongkang Food Factory; batch number: 090123), absolute ethanol.

[0033] 2. Methods and results

[00...

Embodiment 2

[0059] Example 2 Physicochemical properties and in vitro release research of Huchang Qingdu pellets

[0060] In this part of the experiment, the in vitro release law of the above-mentioned pellets was explored, which provided a theoretical basis for further in-depth research on the in vivo process of Huchang Qingdu pellets.

[0061] 1. Instruments and reagents

[0062] ER-182A electronic balance (Japan); 85B-2 magnetic heating stirrer (Nantong Scientific Instrument Factory); ultrasonic cleaner (Shanghai Kedao Ultrasonic Instrument Co., Ltd.); D800C intelligent drug dissolution apparatus (Tianjin University Radio Factory). Biofuge Stratos all-round desktop high-speed refrigerated centrifuge (Heraeus, Germany); Waters600 high-performance liquid chromatography (Waters, USA), Waters 2996 diode array detector (Waters, USA), MicrofLudizer (MicrofLudics, USA); JEM-100SX electronic Transmission microscope (Japan Electronics Co.); MASTERSIZER-2000 laser scattering particle size analyz...

Embodiment 3

[0088] Example 3 Pharmacokinetic study of colon-targeted Huchang Qingdu pellets in rats

[0089] The traditional Chinese medicine powder of the present invention is made of ten traditional Chinese medicines such as rhubarb, comfrey, red peony, etc., and has complex chemical components, and the general slow and controlled release preparation technology is not suitable for the dosage form modification of the medicine. Therefore, according to the physiological conditions of the human body, acrylic resin (Eudragit) dissolved under different pH conditions was used as the coating material to prepare sustained-release pellets for colon-targeted drug delivery. The main active ingredient of ) is an investigation index, investigate the drug concentration of the micropills in the colon contents of rats after oral administration; measure the blood drug concentration of the drug-loaded micropills and coated micropills after oral administration in rats.

[0090] 1. Instruments and reagents ...

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Abstract

The invention discloses intestine-protecting and detoxifying micro pellets and use thereof, which are used to clear enterogenous endotoxin through colon-targeted administration. The micro pellets consist of Chinese medicine powder, coating material and other common auxiliary materials used in pharmaceutics, wherein the Chinese medicine powder is prepared by the following raw material medicines in part by weight: 6 to 12 parts of rhubarb, 6 to 12 parts of sinkiang arnebia root, 25 to 35 parts of tuckahoe, 25 to 35 parts of coix seed, 10 to 20 parts of common bletilla pseudobulb, 20 to 30 partsof root of common peony, 10 to 20 parts of baical skullcap root, 10 to 15 parts of common andrographis herb, 6 to 12 parts of cutch and 2 to 5 parts of liquoric root. The preparation method of the intestine-protecting and detoxifying micro pellets comprises: mixing the medicine powder and the common auxiliary materials used in pharmaceutics to prepare a soft material, pelletting the mixture, drying and obtaining pellet cores; adding water into calcium pectinate to prepare suspension; adding the common auxiliary materials used in pharmaceutics to prepare colon coating solution; and coating in the conventional way till the weight of the coating is increased by over 35 percent. The intestine-protecting and detoxifying micro pellets has functions of protecting intestine barrier, removing toxin in intestines and reducing damage of cell factors and other inflammatory mediator to the liver.

Description

technical field [0001] The invention relates to a kind of micropill for removing intestinal-derived endotoxin through colon-targeted drug delivery—Huchangqingdu micropill. Background technique [0002] my country is a highly prevalent area of ​​hepatitis B virus (Hepatitis B Virus, HBV) infection, the positive rate of hepatitis B surface antigen (HBsAg) is 9.09%, about 120 million people, of which about 30 million people are chronic hepatitis B patients. A large number of data confirm that most chronic liver diseases are accompanied by intestinal endotoxemia (Intestinal Endotoxemia, IETM). The incidences of IETM in patients with severe hepatitis, hepatitis cirrhosis, chronic hepatitis and acute hepatitis were 93.3%, 84.3%, 79.0% and 75.0%, respectively. The pathogenesis and progression of chronic hepatitis B liver disease, the role of intestinal endotoxemia has been paid more and more attention. Endotoxin and endotoxin activate the cascade chain release of Kupffer cell infl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K36/8994A61K9/16A61P1/00A61P1/16A61P31/04
Inventor 李勇孙欢娜胡冬青孙萍
Owner THE AFFILIATED HOSPITAL OF SHANDONG UNIV OF TCM
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