CN101234094B - Dipyridamole orally disintegrating tablet - Google Patents
Dipyridamole orally disintegrating tablet Download PDFInfo
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- CN101234094B CN101234094B CN2008101019461A CN200810101946A CN101234094B CN 101234094 B CN101234094 B CN 101234094B CN 2008101019461 A CN2008101019461 A CN 2008101019461A CN 200810101946 A CN200810101946 A CN 200810101946A CN 101234094 B CN101234094 B CN 101234094B
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- dipyridamole
- orally disintegrating
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- oral cavity
- tablet
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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
The present invention relates to the dipyridamole medicament, be specifically related to dipyridamole orally disintegrating tablet dosage form and preparation method thereof.
Background technology
Along with the prolongation of human average life and the decline of age growth swallow, the oral tablet administering mode becomes the problem that people pay close attention to.According to estimates, there is 50% people that swallow tablet and capsule are had any problem approximately, influenced the compliance of Drug therapy.In department of pediatrics and old medicine and pharmacology field, to in water, dissolving or suspend, can chew or can in mouth, very big demand being arranged rapid dissolved solid preparation, need not the oral quick dispersible preparation that water and swallowing act just can disperse or dissolve rapidly and just can address this problem.This dosage form can be dispersed or dissolved in saliva rapidly after putting into mouth, and medicine can absorb by oral cavity or intraesophageal mucosa, and bioavailability is than ordinary preparation height, and the side effect that is caused by first pass metabolism also can alleviate.
Oral cavity disintegration tablet (orally disintegrating tablet) is emerging in recent years novel form, compare with conventional tablet, this dosage form need not water and also need not to chew, medicine places on the tongue, after meeting the rapid disintegrate of saliva, borrow swallowing act to go into the stomach onset, also can place the Sublingual, medicine absorbs onset by mucosa after the disintegrate rapidly.This dosage form is particularly suitable for some old peoples, child, swallow inconvenient patient or the hydropenia condition of going out under patient take, and have the characteristics rapid-action, that bioavailability is high.
Dipyridamole has the breeding that suppresses platelet aggregation and have anti-thrombosis function and inhibition virus, suppress the synthetic of viral RNA, (gold is eaten in the clinical treatment that is used to prevent and treat thrombosis, viral upper respiratory tract infection, mumps, infant acute diarrhea, Xie Li. persantin treatment influenza observation of curative effect [J]. Strait Pharmaceutical Journal, 2002,14 (3): 52-53; Sun Xiuting. QINGKAILING, persantin treatment mumps [J]. Inner Mongol medicine, 2001 (5): 11; Zou Huaili. dipyridamole treatment epidemic encephalitis type B [J]. new drug and clinical, 1993,12 (2): 125.)
The preparation of dipyridamole mainly contains injection, slow releasing tablet, conventional tablet etc. clinically at present, and injection exists the shortcoming of patient's medication inconvenience when curative effect can be affirmed.Problems such as Zantine exist to absorb slowly, bioavailability is little and the performance that affects the treatment, and need quick-acting medicines under a lot of situations of clinical application, the clinical rapid release oral formulations that does not also have dipyridamole at present.
Summary of the invention
The object of the present invention is to provide a kind of dipyridamole orally disintegrating tablet and preparation method thereof with rapid release effect.
Dipyridamole orally disintegrating tablet provided by the present invention is to be active component with the dipyridamole, is adjuvant with potent disintegrating agent, filler, correctives, effervescent, binding agent etc., and concrete component and mass percent thereof are as follows:
Dipyridamole 5～50%
Filler 20～70%
Disintegrating agent 10～40%
Effervescent 1～5%
Correctives 0～3%
Lubricant 0.5～1.8%
Binding agent 8～20%
Wherein, the mass percent of active component dipyridamole preferred 10～40%, especially preferred 12.5～25% in the dipyridamole orally disintegrating tablet.
Described filler is selected from microcrystalline Cellulose, dextrin, mannitol, sorbitol, lactose or the starch a kind or multiple; The purpose that adds filler is to make the oral cavity disintegration tablet easy-formation; The mass percent of the filler described in the oral cavity disintegration tablet preferred 30～60%.
Described disintegrating agent is selected from one or more in carboxymethyl starch sodium, low-substituted hydroxypropyl methylcellulose, the crospolyvinylpyrrolidone; The purpose that adds disintegrating agent is to quicken disintegrate, to reach the disintegrate requirement of oral cavity disintegration tablet; The mass percent of the disintegrating agent described in the oral cavity disintegration tablet preferred 15～25%.
Described effervescent is the mixture of citric acid or tartaric acid and sodium bicarbonate; Effervescent is the power of disintegrate; The mass percent of the effervescent described in the oral cavity disintegration tablet preferred 2～4%.
Described correctives is selected from one or more of aspartame, mannitol, stevioside; Add or do not add correctives all can, the purpose of interpolation is to improve mouthfeel, so that the more pleased acceptance of patient; The mass percent of the correctives described in the oral cavity disintegration tablet preferred 0.5～1.5%.
Described lubricant is selected from magnesium stearate, Stepanol MG or Pulvis Talci; The purpose of adding lubricant is to increase particulate lubricity, so that the oral cavity disintegration tablet surface is brighter and cleaner.
Described binding agent is selected from dehydrated alcohol and glycerol mixed solution; The purpose of adding binding agent is, is used to make soft material, makes oral cavity disintegration tablet have certain rigidity and wearability; The mass percent of the binding agent described in the oral cavity disintegration tablet preferred 10～15%.
The preparation method of dipyridamole orally disintegrating tablet provided by the present invention is to adopt wet method to prepare granule, and drying, compacting specifically may further comprise the steps in flakes:
1) press the mass percent of component in the dipyridamole orally disintegrating tablet, take by weighing each component:
Dipyridamole 5～50%
Filler 20～70%
Disintegrating agent 10～40%
Effervescent 1～5%
Correctives 0～3%
Lubricant 0.5～1.8%
Binding agent 8～20%
2) filler in the step 1), disintegrating agent, correctives and effervescent are ground 30～60min respectively, abundant then mix homogeneously obtains blending ingredients A;
3) will the dipyridamole in the step 1) grind the back and join step 2 with the equivalent method of progressively increasing) in blending ingredients A in, cross 100 mesh sieves 2～3 times repeatedly after fully mixing, obtain blending ingredients B;
4) with the binding agent in the step 1) blending ingredients B in the step 3) is made soft material, cross 16 mesh sieves and granulate, 40～50 ℃ of forced air dryings 4～6 hours, with 20 mesh sieve granulate, the mix lubricant in the adding step 1) is even, and the punching press film-making makes dipyridamole orally disintegrating tablet.
Dipyridamole orally disintegrating tablet among the present invention can pass through oral administration, every day 3 times, each 25～100mg.
Compare with existing dipyridamole formulation and preparation method thereof, the present invention has following beneficial effect:
Needn't only need contact saliva disintegrate rapidly in 30 seconds in the oral cavity for water when 1) needing, stripping quantity is more than 85% in 2 minutes, help the medicine stripping and absorb, shorten arriving blood medicine time to peak, thereby make the rapid onset in the oral back of dipyridamole and improve its bioavailability.
2) the oral cavity disintegration tablet taking convenience among the present invention, especially be fit under part dysphagia or the special environment emergency case patient such as old man, child, coma patient, gulp down patient's medication that water is promptly vomitted.
The specific embodiment
Oral cavity disintegration tablet among the present invention is to adopt conventional tablet pharmaceutical equipment production.
Embodiment 1
1) take by weighing respectively after microcrystalline Cellulose 38.7g, low-substituted hydroxypropyl cellulose 10.0g, crospolyvinylpyrrolidone 5.2g, carboxymethyl starch sodium 4.8g, tartaric acid 0.9g and sodium bicarbonate 0.9g grind 60min, fully mix homogeneously obtains blending ingredients A;
2) adopt the equivalent dipyridamole 10.7g of method after that progressively increase to join among the blending ingredients A in the step 1), fully mix, cross 100 mesh sieves 3 times repeatedly, obtain blending ingredients B porphyrize;
3) with the blending ingredients B system soft material of 11.0g binding agent (dehydrated alcohol: glycerol=12: 1) with step 2) preparation, the extruding of 16 mesh sieves is granulated, 50 ℃ of following freeze-day with constant temperature 5 hours, and 20 mesh sieve granulate add Pulvis Talci 1.5g, and mixing, tabletting promptly get dipyridamole orally disintegrating tablet.
The heavy 195mg of every sheet of oral cavity disintegration tablet, wherein the shared mass percent of each component is dipyridamole 12.80%, microcrystalline Cellulose 46.23%, low-substituted hydroxypropyl cellulose 11.94%, carboxymethyl starch sodium 5.79%, crospolyvinylpyrrolidone 6.14%, tartaric acid 1.09%, sodium bicarbonate 1.09%, binding agent 13.13%, Pulvis Talci 1.79%.
Disintegration time 18.36 ± 1.65s, external stripping experiment 2min stripping quantity 86% in water, the experiment of volunteer Orally disintegrating, disintegration time is 17.00 ± 1.32s.
Embodiment 2
1) take by weighing after microcrystalline Cellulose 63.7g, citric acid 1.0g, sodium bicarbonate 1.0g, low-substituted hydroxypropyl cellulose 5.4g, carboxymethyl starch sodium 4.6g grind 30min respectively, mix homogeneously obtains blending ingredients A;
2) with stevioside 1.3g and dipyridamole 5.0g polishing mix homogeneously;
3) with step 2) in the stevioside and the mixture of dipyridamole join among the blending ingredients A in the step 1) with the equivalent method of progressively increasing, mixing, sieve repeatedly 100 orders 3 times are with binding agent (dehydrated alcohol: 8.5g glycerol=8: 1), system soft material, the extruding of 16 mesh sieves is granulated, 50 ℃ of following freeze-day with constant temperature 6 hours, 20 mesh sieve granulate add magnesium stearate 0.5g, tabletting promptly gets dipyridamole orally disintegrating tablet.
The heavy 230mg of every sheet of oral cavity disintegration tablet, wherein the shared mass percent of each component is dipyridamole 5.49%, microcrystalline Cellulose 70.00%, low-substituted hydroxypropyl cellulose 5.93%, carboxymethyl starch sodium 5.06%, stevioside 1.43%, citric acid 1.10%, sodium bicarbonate 1.10%, binding agent 9.34%, magnesium stearate 0.55%.
Disintegration time 8.42 ± 1.12s, external stripping experiment 2min stripping quantity 90.67% in water, the experiment of volunteer Orally disintegrating, disintegration time is 8.66 ± 1.81s.
Embodiment 3
1) takes by weighing microcrystalline Cellulose 17.5g, low-substituted hydroxypropyl cellulose 7.4g, crospolyvinylpyrrolidone 5.9g, tartaric acid 1.8g, sodium bicarbonate 1.8g mixed grinding 60min, obtain blending ingredients A;
2) with behind the dipyridamole 30.0g porphyrize, join among the blending ingredients A in the step 1) and fully mix, cross 100 mesh sieves 3 times repeatedly, obtain blending ingredients B;
3) with the system of the blending ingredients B in binding agent (dehydrated alcohol: glycerol=15: 1) 8.0g is with step 2) soft material, the extruding of 16 mesh sieves is granulated, 50 ℃ of following freeze-day with constant temperature 5 hours, and 20 mesh sieve granulate add Pulvis Talci 0.5g mixing, and tabletting promptly gets dipyridamole orally disintegrating tablet.
The heavy 120mg of every sheet of oral cavity disintegration tablet, wherein the shared mass percent of each component is dipyridamole 41.15%, microcrystalline Cellulose 24.01%, low-substituted hydroxypropyl cellulose 10.15%, crospolyvinylpyrrolidone 8.09%, tartaric acid 2.47%, sodium bicarbonate 2.47%, binding agent 10.98%, Pulvis Talci 0.68%.
Disintegration time 28.16 ± 1.85s, external stripping experiment 2min stripping quantity 83.35% in water, the experiment of volunteer Orally disintegrating, disintegration time is 26.32 ± 1.62s.
Embodiment 4
1) take by weighing microcrystalline Cellulose 42g, citric acid 0.65g, sodium bicarbonate 0.65g, crospolyvinylpyrrolidone 16g, carboxymethyl starch sodium 31.9g grinds 40min respectively, mix homogeneously obtains blending ingredients A;
2) will join among the blending ingredients A in the step 1) with the equivalent method of progressively increasing behind dipyridamole 6.0g and the aspartame 3.5g mixing porphyrize, mixing, 100 orders 3 times of sieving repeatedly obtain blending ingredients B;
3) with the blending ingredients B system soft material of preparation in binding agent (dehydrated alcohol: glycerol=10: 1) 17.4g is with step 2), the extruding of 16 mesh sieves is granulated, 50 ℃ of following freeze-day with constant temperature 6 hours, and 20 mesh sieve granulate add magnesium stearate 1.9g, and tabletting promptly gets oral cavity quick disintegrating slice.
The heavy 250mg of every sheet of oral cavity disintegration tablet, wherein the shared mass percent of each component is dipyridamole 5.00%, microcrystalline Cellulose 35.00%, aspartame 2.91%, carboxymethyl starch sodium 26.66%, crospolyvinylpyrrolidone 13.33%, citric acid 0.54%, sodium bicarbonate 0.54%, binding agent 14.5%, magnesium stearate 1.61%.
Disintegration time 15.50 ± 1.60s, external stripping experiment 2min stripping quantity 85.53% in water, the experiment of volunteer Orally disintegrating, disintegration time is 16.23 ± 1.81s.
Claims (8)
1. dipyridamole orally disintegrating tablet, it is characterized in that each component and mass percent thereof are in the described oral cavity disintegration tablet: dipyridamole 5～50%, filler 20～70%, disintegrating agent 10～40%, effervescent 1～5%, correctives 0～3%, lubricant 0.5～1.8%, binding agent 8～20%; Wherein, filler is selected from microcrystalline Cellulose, dextrin or lactose; Disintegrating agent is selected from one or more in carboxymethyl starch sodium, low-substituted hydroxypropyl methylcellulose, the crospolyvinylpyrrolidone; Effervescent is the mixture of citric acid or tartaric acid and sodium bicarbonate; Correctives is selected from aspartame, mannitol, stevioside; Lubricant is selected from magnesium stearate, Stepanol MG or Pulvis Talci; Binding agent is dehydrated alcohol and glycerol mixed solution;
Its preparation method may further comprise the steps:
1) press the mass percent of component in the dipyridamole orally disintegrating tablet, take by weighing each component:
2) filler in the step 1), disintegrating agent, correctives and effervescent are ground 30～60min respectively, abundant then mix homogeneously obtains blending ingredients A;
3) will the dipyridamole in the step 1) grind the back and join step 2 with the equivalent method of progressively increasing) in blending ingredients A in, cross 100 mesh sieves 2～3 times repeatedly after fully mixing, obtain blending ingredients B;
4) with the binding agent in the step 1) blending ingredients B in the step 3) is made soft material, cross 16 mesh sieves and granulate, 40～50 ℃ of forced air dryings 4～6 hours, with 20 mesh sieve granulate, the mix lubricant in the adding step 1) is even, and the punching press film-making makes dipyridamole orally disintegrating tablet.
2. dipyridamole orally disintegrating tablet according to claim 1 is characterized in that, the mass percent of the dipyridamole described in the oral cavity disintegration tablet is 10～40%.
3. dipyridamole orally disintegrating tablet according to claim 2 is characterized in that, the mass percent of the dipyridamole described in the oral cavity disintegration tablet is 12.5～25%.
4. dipyridamole orally disintegrating tablet according to claim 1 is characterized in that, the mass percent of the filler described in the oral cavity disintegration tablet is 30～60%.
5. dipyridamole orally disintegrating tablet according to claim 1 is characterized in that, the mass percent of the disintegrating agent described in the oral cavity disintegration tablet is 15～25%.
6. dipyridamole orally disintegrating tablet according to claim 1 is characterized in that, the mass percent of the effervescent described in the oral cavity disintegration tablet is 2～4%.
7. dipyridamole orally disintegrating tablet according to claim 1 is characterized in that, the mass percent of the correctives described in the oral cavity disintegration tablet is 0.5～1.5%.
8. dipyridamole orally disintegrating tablet according to claim 1 is characterized in that, the mass percent of the binding agent described in the oral cavity disintegration tablet is 10～15%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008101019461A CN101234094B (en) | 2008-03-14 | 2008-03-14 | Dipyridamole orally disintegrating tablet |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008101019461A CN101234094B (en) | 2008-03-14 | 2008-03-14 | Dipyridamole orally disintegrating tablet |
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| Publication Number | Publication Date |
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| CN101234094A CN101234094A (en) | 2008-08-06 |
| CN101234094B true CN101234094B (en) | 2010-09-22 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101780037B (en) * | 2010-02-03 | 2011-11-16 | 南昌大学 | Dipyridamole self-emulsifying medicament administration system and preparation method thereof |
| CN101919822B (en) * | 2010-07-16 | 2013-10-23 | 钟术光 | Tablet with improved combination properties and preparation method thereof |
| CN104644577A (en) * | 2013-11-23 | 2015-05-27 | 天津市汉康医药生物技术有限公司 | Rivaroxaban orally-disintegrating tablet and preparation method thereof |
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Granted publication date: 20100922 Termination date: 20110314 |