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Artificial bezoar inclusion compound, its preparation method and application
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A technology of artificial bezoar and clathrate, which is applied to the active ingredients of heterocyclic compounds, drug combinations, and pharmaceutical formulas, etc., can solve the problems of unacceptable, nausea, and vomiting in children and infants, and achieve the effect of covering bad smell
Active Publication Date: 2013-06-19
吉林省吴太感康药业有限公司 +1
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Gankang (Compound Amantadine Tablets) and Xiaogankang (Pediatric Amantadine Granules) are composed of acetaminophen, amantadine hydrochloride, caffeine, chlorpheniramine maleate, and artificial bezoar. composition; in the testing of its finished products, there are no specific requirements for the phenomenon of bad smell caused by artificial bezoar, but in the actual market sales process, some consumers have questioned the bad smell in the finished product, and taking it often can cause Adverse reactions such as nausea and vomiting are more difficult for children and infants to accept. Therefore, it is of great significance to provide a compound acetaminophen tablet or infantile acetaminophen granules that eliminates bad smell
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Embodiment 1
[0041] Embodiment 1 Preparation of artificial bezoar clathrate
[0042] Accurately weigh 200 g of artificial bezoar, add 1000 mL of ethanol to dissolve, and obtain artificial bezoar ethanol solution;
[0043] Accurately weigh 700g of β-cyclodextrin, add 4000mL of water to dissolve, obtain β-cyclodextrin aqueous solution, cool to 31°C for later use;
[0044] The obtained artificial bezoar ethanol solution was slowly dropped into the β-cyclodextrin aqueous solution, stirred at 31°C for 2 hours, refrigerated at 4°C for 24 hours to obtain a wet β-cyclodextrin inclusion compound, dried at 50°C for 6 hours, That is, the inclusion rate was 85.0%.
Embodiment 2
[0045] Embodiment 2 Preparation of artificial bezoar clathrate
[0046] Accurately take artificial bezoar 400g, add 2000mL ethanol to dissolve, and make artificial bezoar ethanol solution;
[0047] Accurately weigh 1800g of β-cyclodextrin, add 8000mL of water to dissolve, obtain β-cyclodextrin aqueous solution, cool to 29℃ for later use;
[0048] Take the obtained artificial bezoar ethanol solution and slowly drop it into the β-cyclodextrin aqueous solution, stir at 29°C for 3h, refrigerate at 0°C for 22h to obtain a wet β-cyclodextrin inclusion compound, dry at 40°C for 8h, That is, the inclusion rate was 89.4%.
Embodiment 3
[0049] Example 3 Preparation of artificial bezoar clathrate
[0050] Accurately take artificial bezoar 300g, add 1500mL ethanol to dissolve, and make artificial bezoar ethanol solution;
[0051] Accurately weigh 1200g of β-cyclodextrin, add 5000mL of water to dissolve, obtain β-cyclodextrin aqueous solution, cool to 30℃ for later use;
[0052] Take the prepared artificial bezoar ethanol solution and slowly drop it into the β-cyclodextrin aqueous solution, stir at 30°C for 2.5h, refrigerate at 2°C for 20h to obtain a wet β-cyclodextrin inclusion compound, and dry at 45°C for 7h , That is, the inclusion rate is 92.36%.
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Abstract
The invention relates to the medicine field, in particular to an artificial bezoarinclusion compound, its preparation method and application. The method adopts a beta-cyclodextrin inclusion technology, which is mainly directed at the special odor possessed by artificial bezoars in Gankang (compound paracetamol and amantadinehydrochloride tablets) and pediatric Gankang (pediatric compound paracetamol and amantadinehydrochloride granules). Production of Gankang (compound paracetamol and amantadinehydrochloride tablets) and pediatric Gankang (pediatric compound paracetamol and amantadine hydrochloride granules) with beta-cyclodextrin included artificial bezoars can obviously cover up the unpleasant odor of artificial bezoars, with an inclusion rate maintained at 85-92.36%.
Description
technical field [0001] The invention relates to the field of medicines, in particular to an artificial bezoar clathrate, its preparation method and its application. Background technique [0002] Calculus bezoar is the dried gallstone of bovid cattle (Bos taurus domesticus Gmelin). Traditional Chinese medicine believes that bezoar gas is fragrant, slightly bitter and then sweet, and cool in nature. It can be used for antipyretic, detoxification and calming convulsions. Oral administration to treat high fever, coma, mania, infantile convulsions, convulsions and other diseases. External use is used to control sore throat, aphthous carbuncle, and toxin. Because natural bezoar is very precious, the international price is higher than that of gold, and now most of the so-called artificial bezoar is used. Artificial bezoar is composed of bovine gallpowder, cholic acid, hyodeoxycholic acid, taurine, bilirubin, cholesterol and trace elements. Beef gallpowder has mutton, fishy s...
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