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Dipyridamole orally disintegrating tablet and preparation

A technology of dipyridamole and orally disintegrating tablets, which is applied in the field of dipyridamole pharmaceuticals, can solve the problems of inconvenient medication for patients, slow absorption of dipyridamole tablets, and low bioavailability, so as to shorten the peak time of blood drug, Conducive to dissolution and absorption, improve the effect of bioavailability

Inactive Publication Date: 2008-08-06
BIOCHEM ENG COLLEGE OF BEIJING UNION UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the preparations of dipyridamole mainly include injections, sustained-release tablets, ordinary tablets, etc., while the curative effect of injections can be confirmed, there are disadvantages of inconvenient medication for patients.
Dipyridamole tablets have problems such as slow absorption and low bioavailability, which affect the curative effect. In many cases, quick-acting drugs are needed in clinical use. At present, there is no immediate-release oral preparation of dipyridamole.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] 1) Weigh 38.7g of microcrystalline cellulose, 10.0g of low-substituted hydroxypropyl cellulose, 5.2g of cross-linked polyvinylpyrrolidone, 4.8g of sodium carboxymethyl starch, 0.9g of tartaric acid and 0.9g of sodium bicarbonate and grind for 60min , fully mixed uniformly to obtain mixed component A;

[0041] 2) Add 10.7 g of the ground dipyridamole to the mixed component A in step 1) by using the equal amount incremental method, mix well, and repeatedly pass through a 100-mesh sieve for 3 times to obtain the mixed component B;

[0042] 3) Use 11.0 g of binder (absolute ethanol: glycerol = 12: 1) to extrude and granulate the mixed component B soft material prepared in step 2) with a 16-mesh sieve, and dry it at a constant temperature at 50°C for 5 hours. Mesh sieve for granulation, add 1.5 g of talcum powder, mix well, and press into tablets to obtain dipyridamole orally disintegrating tablets.

[0043] Each orally disintegrating tablet weighs 195 mg, and the weight pe...

Embodiment 2

[0046] 1) Weigh and grind 25.5g of microcrystalline cellulose, 12.7g of low-substituted hydroxypropyl cellulose, 1.2g of aspartame, 2.4g of sodium carboxymethyl starch, 1.8g of tartaric acid, and 1.8g of sodium bicarbonate for 40 minutes. , fully mixed uniformly to obtain mixed component A;

[0047] 2) After pulverizing 21.3 g of dipyridamole, add it to the mixing component A in step 1) and mix thoroughly, and repeatedly pass through a 100-mesh sieve for 3 times to obtain the mixing component B;

[0048] 3) Use 13.5g of binder (absolute ethanol) to extrude and granulate the mixed component B soft material prepared in step 2) with a 16-mesh sieve, dry at a constant temperature at 40°C for 6 hours, granulate with a 20-mesh sieve, add 1.0 g of talcum powder, compressed into tablets to obtain dipyridamole orally disintegrating tablets.

[0049] Each orally disintegrating tablet weighs 200mg, and the mass percentage of each component is dipyridamole 25.00%, microcrystalline cellul...

Embodiment 3

[0052] 1) Weigh 63.7g of microcrystalline cellulose, 1.0g of citric acid, 1.0g of sodium bicarbonate, 5.4g of low-substituted hydroxypropyl cellulose, and 4.6g of sodium carboxymethyl starch, grind them for 30 minutes, and mix them evenly to obtain a mixed composition Point A;

[0053]2) Mix 1.3 g of stevioside and 5.0 g of dipyridamole evenly by grinding;

[0054] 3) Add the mixture of stevioside and dipyridamole in step 2) to the mixed component A in step 1) in equal increments, mix well, and repeatedly sieve through 100 mesh 3 times, use the adhesive (absolute ethanol:glycerin=8:1) 8.5g, make soft material, extrusion granulation with 16 mesh sieve, constant temperature drying at 50°C for 6 hours, granulate with 20 mesh sieve, add 0.5g magnesium stearate, tablet , that is, dipyridamole orally disintegrating tablets.

[0055] Each orally disintegrating tablet weighs 230 mg, and the mass percentage of each component is 5.49% of dipyridamole, 70.00% of microcrystalline cellul...

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PUM

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Abstract

The invention relates to dipyradimole orally disintegrating tablet and a preparation method thereof, which pertains to a pharmaceutic preparation field. Components and mass percentages thereof of the orally disintegrating tablet are: 5-50 percent of dipyradimole, 20-70 percent of stuffing agent, 10-40 percent of disintegrating agent, 1-5 percent of effervescent, 0-3 percent of correctant, 0.5-1.8 percent of lubricant and 8-20 percent of adhesive. The method of the invention comprises the following steps: 1) the stuffing agent, the disintegrating agent, the correctant and the effervescent are respectively ground for 30-60min and then fully blended into a mixture; 2) the dipyradimole is ground and added in the mixture cumulatively; after fully blended, the mixture passes through a 100 mesh sieve for 2-3 times; 3) the mixture is made into soft material by the adhesive; then the soft material is pelletized through a 16 mesh sieve and forced-air dried for 4-6 hours at the temperature ranging from 40-50 DEG C; the pelletized granules are sifted by a 20 mesh sieve; the lubricant is added in the pelletized granules and fully blended to prepare the dipyradimole orally disintegrating tablet after stamping and slice production. The orally disintegrating tablet of the invention has the advantages of short disintegrating time, rapid effect and convenient using, etc.

Description

technical field [0001] The invention relates to a dipyridamole medicament, in particular to a dipyridamole orally disintegrating tablet dosage form and a preparation method thereof. Background technique [0002] Oral tablet delivery is a matter of concern as the average human lifespan increases and swallowing ability declines with age. It is estimated that about 50% of the population has difficulty swallowing tablets and capsules, affecting compliance with drug therapy. In the field of pediatrics and geriatrics, there is a great demand for solid dosage forms that can be dissolved or suspended in water, chewable or rapidly dissolved in the mouth. can solve this problem. This dosage form can quickly disperse or dissolve in saliva after being put into the mouth, and the drug can be absorbed through the mucous membrane in the oral cavity or esophagus. The bioavailability is higher than that of ordinary preparations, and the side effects caused by first-pass metabolism can also...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/519A61K47/38A61P7/02A61P31/12
Inventor 冯淑华宋杨李可意陈超任超
Owner BIOCHEM ENG COLLEGE OF BEIJING UNION UNIV
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