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Domperidone sustained release preparation and sustained release carrier

A technology for domperidone and sustained-release preparations, applied in the field of medicine, can solve the problems of low bioavailability and the like, and achieve the effects of improving bioavailability, reducing toxicity, and good drug sustained-release performance.

Pending Publication Date: 2022-03-11
NORTHWEST NORMAL UNIVERSITY +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the release rate is too low for domperidone, which mainly acts on the gastrointestinal tract to regulate gastrointestinal motility, and cannot improve its bioavailability.

Method used

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  • Domperidone sustained release preparation and sustained release carrier
  • Domperidone sustained release preparation and sustained release carrier
  • Domperidone sustained release preparation and sustained release carrier

Examples

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preparation example Construction

[0044] The preparation process of domperidone sustained-release preparation of the present invention comprises the following steps:

[0045] (1) Mix and ball-mill domperidone and sustained-release carrier first to obtain composite powder;

[0046] (2) The composite powder is then mixed with pharmaceutically acceptable excipients.

[0047] Compared with simultaneous mixing, domperidone is ball-milled and compounded with the slow-release carrier first, and then mixed with other excipients after compounding, which is beneficial to the mechanochemical effect of domperidone and the sodium attapulgite modified by vinylpyrrolidone as the slow-release carrier, so that Domperidone is firmly combined on the surface of the sustained-release carrier, reducing the occupation of other auxiliary materials on the surface of the sustained-release carrier, and providing stable release of the domperidone drug.

[0048] Take the tablet as a class, mix the compound powder and the pharmaceutically...

Embodiment 1

[0087] Step 1: Add 100g of attapulgite and 5g of sodium carbonate into 1.9 liters of deionized water together, at a stirring rate of 400-550 r min -1 Stir for 4-6 h under certain conditions to ion exchange sodium carbonate and attapulgite, then centrifuge, wash, dry, pulverize and sieve the mixed solution to obtain sodium attapulgite, marked as Na-ATP.

[0088] Step 2: Dissolve a certain amount of vinylpyrrolidone (NVP) in water, and add sodiumized attapulgite, wherein the concentration of sodiumized attapulgite is 10wt%, and the amount of vinylpyrrolidone is the mass of sodiumized attapulgite 10%, shaken at constant temperature for 3 hours, and then the mixed solution was filtered, washed with deionized water, dried, crushed, and sieved to obtain organic attapulgite, marked as M-ATP.

[0089] Step 3: Mix the organic attapulgite and domperidone in step 2 evenly at a mass ratio of 5:10, ball mill, dry and sieve to obtain a composite powder of organic attapulgite and domperidone...

Embodiment 2

[0092] Step 1: The preparation of sodium attapulgite is the same as in Example 1.

[0093] Step 2: Dissolving a certain amount of vinylpyrrolidone in water, adding sodiumized attapulgite, wherein the concentration of sodiumized attapulgite is 10wt%, and the amount of vinylpyrrolidone is 15% of the quality of sodiumized attapulgite, Shake at constant temperature for 3 hours, and then filter the mixed solution, wash with deionized water, dry, pulverize, and sieve to obtain organic attapulgite, which is marked as M-ATP.

[0094] Step 3: Mix the organic attapulgite and domperidone in step 2 evenly at a mass ratio of 10:10, ball mill, dry and sieve to obtain a composite powder of organic attapulgite and domperidone, labeled M-ATP / DOM. The particle size of the powder used for final tableting should not be less than 75 um.

[0095] Step 4: Through the direct powder compression method, the composite powder in step 3 is uniformly mixed with other excipients and then compressed into ...

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Abstract

The invention discloses a slow release carrier of domperidone. The slow release carrier is sodium modified attapulgite modified by vinyl pyrrolidone. The invention also discloses a domperidone sustained release preparation, which comprises domperidone, the vinyl pyrrolidone modified sodium modified attapulgite as a sustained release carrier, and pharmaceutically acceptable auxiliary materials. Compared with the existing domperidone preparation, the domperidone sustained-release preparation disclosed by the invention not only has good drug sustained-release performance and remarkably improves the bioavailability of domperidone, but also can reduce the toxicity of drugs to cells.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a sustained-release preparation of domperidone. Background technique [0002] Domperidone is a gastrointestinal motility regulator, which mainly acts on the proximal gastrointestinal tract, can accelerate the digestion of food, and treat nausea and vomiting. It is widely used clinically. Due to the low bioavailability and short half-life of existing domperidone tablets, it is inevitable to develop sustained-release preparations. [0003] The use of sustained-release carriers is one of the ways to prepare sustained-release preparations, but there are large differences in the binding strength between different sustained-release carriers and different drug molecules and lack of predictability. If the binding effect is too weak, it is easy to produce burst release. If the binding effect is too strong and it is easy to make the drug difficult to release, in order to achieve the ef...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/32A61K47/02A61K9/22A61K31/454A61P1/08
CPCA61K47/32A61K47/02A61K9/2027A61K9/2009A61K31/454A61P1/08
Inventor 张哲郑海宇张娟红封润田邹童李月彭辉马国富
Owner NORTHWEST NORMAL UNIVERSITY
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