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Rheum officinale free anthraquinone self-microemulsion tablet and preparation method thereof

A free anthraquinone, self-micro-emulsifying technology, used in the digestive system, pharmaceutical formulations, emulsion delivery, etc., can solve the problems of free anthraquinone prone to polymerization, difficult to dissolve gastrointestinal fluid, and emulsion droplet aggregation, etc. The effect of drug onset time, production cost reduction and stability improvement

Inactive Publication Date: 2019-11-15
LANZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the free anthraquinone of rhubarb is insoluble in water, it is difficult to dissolve in gastrointestinal fluid after oral administration, and the absorption is poor
The inventor's previous research shows that rhubarb free anthraquinone nanoemulsion can solve the problem that rhubarb free anthraquinone is insoluble in water, and can also increase the oral bioavailability of rhubarb free anthraquinone, but it is prone to emulsion droplet aggregation after long-term storage , the particle size increases, and the free anthraquinone nanoemulsion of rhubarb is sensitive to light, and the free anthraquinone is prone to polymerization

Method used

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  • Rheum officinale free anthraquinone self-microemulsion tablet and preparation method thereof
  • Rheum officinale free anthraquinone self-microemulsion tablet and preparation method thereof
  • Rheum officinale free anthraquinone self-microemulsion tablet and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0025] The preparation of embodiment 1 rhubarb free anthraquinone self-microemulsion tablet

[0026] (1) Preparation of concentrated rhubarb free anthraquinone nanoemulsion: take the prescribed amount of polyoxyethylene hydrogenated castor oil (emulsifier), heat and melt in a water bath at 35°C, and add co-emulsifier according to 1:1 (w / w) Diethylene glycol monoethyl ether (co-emulsifier), stirred evenly at room temperature to obtain a mixed emulsifier; uniformly mixed propylene glycol monocaprylate and ethyl oleate at a ratio of 3:1 (w / w), and added Rhubarb free anthraquinone so that its concentration is 5.1 mg / mL to obtain a mixed oil phase. Mix the mixed oil phase and the mixed emulsifier at a ratio of 31.45:68.55 (w / w), pay attention not to add water to the system, and gently stir for 15 minutes to obtain a clear and uniform concentrated rhubarb free anthraquinone nanoemulsion.

[0027] figure 1 It is the HPLC chromatogram of rhubarb free anthraquinone used in the presen...

Embodiment 2

[0039] Embodiment 2 self-emulsification of rhubarb free anthraquinone self-microemulsification tablet in water

[0040] Rhubarb free anthraquinone self-microemulsifying tablet disintegrates and dissolves in water, artificial gastric juice or intestinal juice, and the emulsion droplets after self-emulsification are spherical, with a particle size between 20-100nm (see Figure 5 ).

[0041] The morphology of emulsion droplet after emulsification of rhubarb free anthraquinone from microemulsion sheet was observed by transmission electron microscope. Put rhubarb free anthraquinone self-microemulsified tablet in distilled water at 37±0.5°C, stir at 100rpm for 30min to completely disperse the tablet in purified water, and filter the resulting suspension with a 0.45μm organic microporous membrane. Drop the filtrate on the copper grid (common carbon coating), and then dye it with 2.0% phosphotungstic acid, and dry the coated grid at room temperature. The electron microscope shows tha...

Embodiment 3

[0043] Example 3 The in vitro release of rhubarb free anthraquinone from microemulsified tablets

[0044] Rhubarb free anthraquinone powder is directly mixed with aluminum magnesium silicate, cross-linked polyvinylpyrrolidone and magnesium stearate, and dry-pressed to obtain rhubarb free anthraquinone ordinary tablets (control sample); Anthraquinone self-microemulsifying tablet (test sample). In vitro release tests were carried out in accordance with the relevant regulations of the 2015 edition of the Chinese Pharmacopoeia.

[0045] The release rate of rhubarb free anthraquinone from rhubarb free anthraquinone self-microemulsified tablets and rhubarb free anthraquinone ordinary tablets was determined by small cup method using RC-8D dissolution tester. The speed of the stirring paddle of the dissolution apparatus is 100rpm, the temperature of the water bath is 37±0.5°C, and the release media are respectively pH 1.2 hydrochloric acid solution (artificial gastric juice) and pH 6...

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Abstract

The invention provides a rheum officinale free anthraquinone self-microemulsion tablet. The rheum officinale free anthraquinone self-microemulsion tablet comprises, by weight, 40-50% concentrated rheum officinale free anthraquinone nanoemulsion, 40-50% of a solid adsorbent, 5-10% of a disintegrating agent and 0.5-1% of a lubricant. The invention also provides a corresponding preparation method. The problem that the rheum officinale free anthraquinone nano-emulsion is unstable can be solved, rapid release of an insoluble rheum officinale free anthraquinone preparation in gastrointestinal fluidcan be realized, the onset time of the rheum officinale free anthraquinone can be shortened, the blood drug concentration can be increased, and the oral bioavailability can be improved. The rheum officinale free anthraquinone self-microemulsion tablet is simple in preparation process, capable of realizing industrial production, good in stability, capable of being stored for a long time, convenientto carry and good in patient compliance.

Description

technical field [0001] The invention relates to rhubarb free anthraquinone self-microemulsified tablet and a preparation method thereof. Background technique [0002] Rhubarb free anthraquinone is the main active ingredient in the dry rhizome and root of Rheum officinale, a plant of the Liao family. It mainly includes five monomers of aloe-emodin, rhein, emodin, chrysophanol and emodin methyl ether. Rhubarb free anthraquinone has a wide range of pharmacological activities, such as antibacterial, anti-inflammatory, anti-viral, anti-tumor, diarrhea, nerve protection, cardiovascular protection, hypoglycemic, anti-pulmonary fibrosis, anti-leukemia and weight loss effects. However, the free anthraquinone of rhubarb is insoluble in water, it is difficult to dissolve in gastrointestinal fluid after oral administration, and the absorption is poor. The inventor's previous research shows that rhubarb free anthraquinone nanoemulsion can solve the problem of rhubarb free anthraquinone ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/32A61K36/708A61K9/107A61K47/44A61K47/10A61P31/04A61P31/12A61P35/00A61P1/12A61P25/00A61P9/00A61P3/10A61P11/00A61P3/04A61P35/02
CPCA61K9/1075A61K9/2027A61K36/708A61K47/10A61K47/44A61P1/12A61P3/04A61P3/10A61P9/00A61P11/00A61P25/00A61P31/04A61P31/12A61P35/00A61P35/02
Inventor 史彦斌徐晓霞牛婧娥杨志刚
Owner LANZHOU UNIVERSITY
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