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A kind of rhubarb anthraquinone oral colon targeted drug delivery composition and use thereof

A technology of colon-targeted drug delivery and rhubarb anthraquinone, which is applied in drug combinations, pharmaceutical formulations, plant raw materials, etc.

Inactive Publication Date: 2015-12-16
承德医学院中药研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] According to other literature records, at present, drug users in some countries have "black stools" due to long-term use of laxatives made from plants containing anthraquinones (such as aloe, rhubarb, senna, etc.). Some of them developed cancer lesions, which may be related to long-term use of laxatives according to epidemiological investigations

Method used

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  • A kind of rhubarb anthraquinone oral colon targeted drug delivery composition and use thereof
  • A kind of rhubarb anthraquinone oral colon targeted drug delivery composition and use thereof
  • A kind of rhubarb anthraquinone oral colon targeted drug delivery composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086] Embodiment 1: Preparation of powder type colon targeting drug delivery composition

[0087] Add the rhubarb anthraquinone currently on the market to 70% ethanol aqueous solution by weight, the volume ratio of the rhubarb anthraquinone and the ethanol aqueous solution is 1:1; after stirring and mixing at room temperature, let the rhubarb anthraquinone Settled naturally, then separated by filtration, the precipitate was washed with water to remove ethanol, then pre-frozen at a temperature of -25°C, and then dehydrated under a vacuum of 1.3 Pa, thus obtaining a freeze-dried rhubarb anthraquinone.

[0088] Accurately weigh 90g polyethylene glycol-6000 for heating and melting. Then weigh 5g of freeze-dried rhubarb anthraquinone, grind it finely and add it to molten polyethylene glycol-6000, stir evenly, cool it rapidly, and grind it into a fine powder. The powder is coated with 10 grams of Eudragit S100 by fluidized bed coating method Coating film, wherein the coating film ...

Embodiment 2

[0089] Embodiment 2: Preparation of powder type colon targeting drug delivery composition

[0090] The rhubarb anthraquinone sold in the market is added to the 80% ethanol aqueous solution by weight, and the volume ratio of the rhubarb anthraquinone and the ethanol aqueous solution is 1:6; after stirring and mixing at room temperature, let the rhubarb anthraquinone Settled naturally, then separated by filtration, the precipitate was washed with water to remove ethanol, then pre-frozen at a temperature of -40°C, and then dehydrated under a vacuum of 80 Pa, thus obtaining a freeze-dried rhubarb anthraquinone.

[0091] Accurately weigh 25g of freeze-dried rhubarb anthraquinone and 100g of EudragitS100, dissolve them in a mixture of ethanol and dimethyl sulfoxide (volume ratio 1:1), add 100ml of water, stir rapidly, and precipitate out, filter, and filter at a temperature of 40 It is dried under the condition of ℃, and ground into fine powder to obtain the solid powder colon targe...

Embodiment 3

[0092] Example 3: Preparation of microtablet-type colon-targeted drug delivery composition

[0093] Add the rhubarb anthraquinone currently on the market to 95% ethanol aqueous solution by weight, the volume ratio of the rhubarb anthraquinone and the ethanol aqueous solution is 1:3; after stirring and mixing at room temperature, let the rhubarb anthraquinone Settled naturally, then separated by filtration, the precipitate was washed with water to remove ethanol, then pre-frozen at a temperature of -5°C, and then dehydrated under a vacuum of 40 Pa, thus obtaining a freeze-dried rhubarb anthraquinone.

[0094] Accurately weigh 5 g of freeze-dried rhubarb anthraquinone, 50 g of microcrystalline cellulose and 50 g of starch, and mix them uniformly. 5g Eudragit S100 is dispersed in 70% ethanol as binder, granulated, the granules are placed in a tablet machine, and microtablets with a diameter of 2mm are compressed, and the microtablets are coated with 16 grams of EudragitS100, wher...

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Abstract

The invention relates to an oral colon targeted drug delivery composition capable of reducing toxic and side effects of rheum officinale anthraquinone and application of the oral colon targeted drug delivery composition. The oral colon targeted drug delivery composition is composed of rheum officinale anthraquinone subjected to freeze drying and auxiliary materials, wherein the auxiliary materials are selected from a colon specificity enzymatic degradable material, a material soluble in medium with pH more than or equal to 6.8, a filler and a bonding agent. The oral colon targeted drug delivery composition can not weaken purgation effect of rheum officinale and also can be used for effectively preventing toxicity of rheum officinale from being played after colon-targeted drug delivery and is basically non-toxic after being taken for a long time, so that the problem of pharmaceutical toxicity of rheum officinale is solved.

Description

【Technical field】 [0001] The invention belongs to the technical field of traditional Chinese medicine preparations. More specifically, the present invention relates to an oral colon-targeted drug delivery composition that reduces the toxic and side effects of rheum anthraquinone, and also relates to the use of the composition. 【Background technique】 [0002] As a commonly used traditional Chinese medicine, rhubarb has the effects of purging heat and dredging intestines, cooling blood and detoxifying, and removing blood stasis and stimulating menstruation. A large number of traditional Chinese medicine preparations contain rhubarb, which mainly uses rhubarb for its purging fire and laxative effect. Those skilled in the art know that the basic components of rhubarb for purging fire and laxative effect are anthraquinones, however, Wang Qingxiu, "Toxicology Research of Rhubarb and Its Main Components", "Doctoral Dissertation of Academy of Military Medical Sciences", 05:26-48 (...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K36/708A61K47/36A61K47/30A61P1/10
Inventor 刘翠哲刘喜纲李忠思刘沛苗光新魏宏伟常金花
Owner 承德医学院中药研究所
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