Oral dispersion domperidone coutrolled-release gel and its preparing method

A technology of dipperidone gel and domperidone, applied in medical preparations containing active ingredients, organic active ingredients, pharmaceutical formulas, etc., can solve problems such as multiple side effects, low bioavailability, and inability to resist gastric acid, and achieve Accurate dosage, stable blood drug concentration, and excellent stability

Inactive Publication Date: 2009-05-27
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, domperidone cannot resist gastric acid, and it must interact with receptors to take effect, so it is difficult to quickly protect the upper digestive tract after oral administration
[0003] At present, domperidone mainly comes in tablets and suspensions, which need to be administered several times a day, which is not only inconvenient to use, but also the drug concentration in the blood fluctuates greatly, resulting in the "peak-valley" phenomenon
When the drug concentration is at the peak, it exceeds the optimum therapeutic concentration, causing more side effects and even poisoning; on the contrary, when the drug concentration drops to the trough, it is far below the required concentration, making it difficult to play a role
At the same time, due to the short retention time of tablets and suspensions in the gastrointestinal tract, and will be destroyed by gastric acid in the stomach, it is not conducive to the complete absorption of the drug, and the bioavailability is low
[0004] The existing commercially available oral dosage forms of domperidone have technical problems and deficiencies such as being unable to quickly protect the lower end of the esophagus, short residence time in the digestive tract, large fluctuations in blood drug concentration, and poor oral absorption. , easy to aggregate into blocks in the gel, not easy to disperse evenly, due to its extreme instability, it is impossible to prepare a gel that meets the requirements of pharmacy by using the existing technology
Therefore, although several drug gels have been marketed, no domperidone gel has been developed or marketed so far.

Method used

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  • Oral dispersion domperidone coutrolled-release gel and its preparing method
  • Oral dispersion domperidone coutrolled-release gel and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Weigh 0.1g of Carbomer-P934, sprinkle it into 25ml of distilled water, and let it swell for 24 hours. Weigh 500mg of domperidone and 5g of PVPk30, mix the two, add 100ml of absolute ethanol, and place in a 50°C water bath to dissolve completely. Distill under reduced pressure in a 50°C water bath to prepare a solid dispersion. Weigh 550 mg of the prepared solid dispersion, add it into the above-mentioned swollen liquid, and stir evenly. Add 2ml of 50% triethanolamine solution to adjust the pH value to 9. Then add distilled water to 50g.

Embodiment 2

[0040]Weigh 0.1g of Carbomer-P971, sprinkle it into 25ml of distilled water, and let it swell for 24 hours. Accurately weigh 500mg of domperidone and 5g of PVPk30, mix the two, add 100ml of absolute ethanol, and place in a 50°C water bath to dissolve completely. Distill under reduced pressure in a 50°C water bath to prepare a solid dispersion. Weigh 550 mg of the prepared solid dispersion, add it into the above-mentioned swollen liquid, and stir evenly. Add 2ml of 50% triethanolamine solution to adjust the pH value to 7. Then add distilled water to 50g.

Embodiment 3

[0042] Weigh 0.1g of Carbomer-P974, sprinkle it into 25ml of distilled water, and let it swell for 24 hours. Weigh 500mg of domperidone and 5g of PVPk25, mix the two, add 100ml of absolute ethanol, place in a 50°C water bath to dissolve completely. Distill under reduced pressure in a 50°C water bath to prepare a solid dispersion. Accurately weigh 550 mg of the prepared solid dispersion, add it into the above-mentioned swollen liquid, and stir evenly. Add 2ml of 50% triethanolamine solution to adjust the pH value to 9. Then add distilled water to 50g.

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PUM

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Abstract

The present invention relates to a domperidone gel preparation for curing reflux esophagitis. Said preparation includes active component and matrix, in which the active component includes the solution made up by using domperidone, polyvinylpyrrolidone and water. Its taste is good, and its stability is better.

Description

technical field [0001] The invention relates to an oral gel, more specifically, a dispersion-type domperidone gel. Background technique [0002] Domperidone is a specific peripheral dopamine receptor antagonist, which mainly acts on dopamine receptors in the gastrointestinal tract. It has strong gastric motility and antiemetic effects, can strengthen the tension of the lower esophageal sphincter, and prevent gastroesophageal reflux, etc. It is a commonly used drug for the treatment of reflux esophagitis. However, domperidone cannot resist gastric acid and can only take effect after interacting with receptors, so it is difficult to quickly protect the upper digestive tract after oral administration. [0003] At present, domperidone mainly comes in tablets and suspensions, which need to be administered several times a day. Not only is it inconvenient to use, but also the drug concentration in the blood fluctuates greatly, resulting in a "peak-valley" phenomenon. When the dru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/454A61K9/00A61P1/04
Inventor 张烜杨照罡张春晖张强
Owner PEKING UNIV
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