CN101836965A - Orally disintegrating tablet containing fexofenadine or salts of fexofenadine, and preparation method thereof - Google Patents
Orally disintegrating tablet containing fexofenadine or salts of fexofenadine, and preparation method thereof Download PDFInfo
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- CN101836965A CN101836965A CN201010184558A CN201010184558A CN101836965A CN 101836965 A CN101836965 A CN 101836965A CN 201010184558 A CN201010184558 A CN 201010184558A CN 201010184558 A CN201010184558 A CN 201010184558A CN 101836965 A CN101836965 A CN 101836965A
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- oral cavity
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- cavity disintegration
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Abstract
The invention provides an orally disintegrating tablet containing fexofenadine or salts of fexofenadine, which is prepared by the inclusion technology. When main drugs and inclusions exist at a specific ratio, the tablet can effectively solve the problems of the taste and disintegration of the main drugs, is convenient for operating, transporting and storing, has wide application range and is suitable for large-scale production.
Description
Technical field
The invention provides a kind of oral cavity disintegration tablet that contains fexofenadine or its salt.
Background technology
Histamine H 1 receptor antagonist is mainly used in allergic disease, and the diphenhydramine of the first generation, chlorphenamine, promethazine etc. to the poor selectivity of receptor, have tangible calmness and cholinolytic effect; The second filial generation has terfenadine, astemizole, loratadine, cetirizine etc., though selectivity height to receptor, the central untoward reaction is few, but some can bring out serious cardiac toxicity the patient is died suddenly, share with liver drug enzyme inhibitor such as macrolide antibiotics (except the azithromycin), imidazoles antifungal agent, the incidence rate of cardiac toxicity increases, thereby application still is restricted.
In recent years, clinical research finds that the metabolite fexofenadine (Fexofenadine) of terfenadine has antihistamine effect, and untoward reaction is few, and better tolerance is the antihistaminic of new generation that has good prospects.Fexofenadine does not only have the maincenter sedation of first generation antihistaminic, do not have yet second filial generation antihistaminic cardiac toxicity and with the untoward reaction of liver drug enzyme inhibitor such as imidazoles antifungal agent, macrolide antibiotics and usefulness, also have good tolerability simultaneously, be applicable to seasonal allergic rhinitis, chronic idiopathic urticaria.
The fexofenadine oral cavity disintegration tablet is specially at child's research and development in 6 to 11 years old, compare with ordinary preparation, taking convenience is arranged, absorb fast, bioavailability is high, to advantages such as digestion mucous membrane zest are little, and oral cavity disintegration tablet has pleasant mouthfeel and has improved the compliance of patient to medicine greatly.
Summary of the invention
The ultimate challenge of exploitation oral cavity disintegration tablet is exactly the taste and the disintegrating property of principal agent, fexofenadine especially its esters chemical compound has the unacceptable bitterness of adult, the commercially available fexofenadine especially conventional tablet of its esters chemical compound all adopts coating method to cover the bad bitterness of major ingredient, but this method is infeasible for oral cavity disintegration tablet.
The applicant was once attempting adopting general odor mask or sweeting agent to cover the bitterness of principal agent, but effect is undesirable, though can effectively cover the bitterness of principal agent behind the employing inclusion technique, but the cohesive of enclose material itself, delayed the disintegration rate of oral cavity disintegration tablet, the applicant creatively adopts specific clathrate and specific ratio that inclusion technique is applied in the oral cavity disintegration tablet, has solved the bitterness of principal agent and the problem of disintegration rate in the oral cavity disintegration tablet effectively.
The invention provides a kind of oral cavity disintegration tablet that contains fexofenadine or its salt, this oral cavity disintegration tablet adopts the technology preparation of enclose, when principal agent and clathrate exist with specific ratio, can solve the taste of principal agent and the problem of disintegrate effectively.
This oral cavity disintegration tablet is made up of following ingredients and percentage ratio: the enclose material of the fexofenadine of 5-20% or its salt, 5-30%,
The filler of 30-70%, the disintegrating agent of 8-20%, 1% lubricant.
The enclose material of this oral cavity disintegration tablet is water-insoluble polyacrylic acid resinoid, and the latter is selected from various models such as EudragitE, EudragitL, EudragitS, and the enclose material of this oral cavity disintegration tablet is selected from polyacrylic resin E100.
The ratio of the principal agent of this oral cavity disintegration tablet and enclose material is 2: 1～1: 4, and the ratio of the principal agent of this oral cavity disintegration tablet and enclose material is 1: 2.
The clathrate of oral cavity disintegration tablet of the present invention adopts conventional preparation technologies such as fluid bed, spray drying, hypobaric drying method.
The filler of this oral cavity disintegration tablet is selected from mannitol, lactose, starch or microcrystalline Cellulose, two or more mixture.
The disintegrating agent of this oral cavity disintegration tablet is selected from cross-linked carboxymethyl cellulose sodium, crosslinked carboxymethylstach sodium or low carboxy-propyl cellulose, two or three mixture of replacing.
The lubricant of this oral cavity disintegration tablet is selected from one or more in magnesium stearate, stearic acid, the sodium stearyl fumarate.
The present invention also provides a kind of preparation technology of fexofenadine oral cavity disintegration tablet, is specially: with the enclose dispersion of materials in disperse medium; After being uniformly dispersed, add the fexofenadine hydrochloride of recipe quantity, stir, it is dissolved fully; Rotary evaporation gets the fexofenadine hydrochloride clathrate.Take by weighing the fexofenadine clathrate of recipe quantity, with filler, system empty agent and the disintegrating agent equivalent mix homogeneously that progressively increases; Add binding agent, the system soft material is granulated; Forced air drying, granulate; Add the disintegrating agent and the lubricant of recipe quantity, mix homogeneously; Tabletting.
The specific embodiment
The present invention is further elaborated by following examples, but whether will limit the invention by any way with it.
Embodiment 1
| Supplementary material | Percentage by weight (%) |
| Fexofenadine | ??6 |
| Eudragit E 100 | ??12 |
| Mannitol | ??39.6 |
| Starch | ??18 |
| Ethyl cellulose | ??5 |
| Starch slurrying | ??2.4 |
| Cross-linked carboxymethyl cellulose sodium (interior) | ??5 |
| Crosslinked carboxymethylstach sodium (outward) | ??3 |
| Magnesium stearate | ??1 |
Preparation technology:
Eudragit E 100 is scattered in 95% ethanol of recipe quantity; After being uniformly dispersed, add the fexofenadine hydrochloride of recipe quantity, stir 30min, it is dissolved fully; The about 3h of 50 degree rotary evaporations gets the fexofenadine hydrochloride clathrate.Take by weighing the fexofenadine clathrate of recipe quantity, mannitol, starch, ethyl cellulose and cross-linked carboxymethyl cellulose sodium equivalent mix homogeneously that progressively increases; As binding agent, make soft material with starch slurry, 16 orders are granulated; 50 degree forced air dryings, 24 mesh sieve granulate; Add the crosslinked carboxymethylstach sodium and the magnesium stearate of recipe quantity, mix homogeneously; Tabletting.
Embodiment 2:
| Supplementary material | Percentage by weight (%) |
| Fexofenadine | ??15 |
| Eudragit E 100 | ??30 |
| Lactose | ??18.5 |
| Starch | ??14.8 |
| Ethyl cellulose | ??6 |
| Starch slurrying | ??2.7 |
| Hyprolose (interior) | ??8 |
| Crosslinked carboxymethylstach sodium (outward) | ??3 |
| Stearic acid | ??1 |
Preparation technology:
Eudragit E 100 is scattered in 95% ethanol of recipe quantity; After being uniformly dispersed, add the fexofenadine hydrochloride of recipe quantity, stir 30min, it is dissolved fully; The about 3h of 50 degree rotary evaporations gets the fexofenadine hydrochloride clathrate.Take by weighing the fexofenadine clathrate of recipe quantity, mannitol, starch, ethyl cellulose and the hyprolose equivalent mix homogeneously that progressively increases; As binding agent, make soft material with starch slurry, 16 orders are granulated; 50 degree forced air dryings, 24 mesh sieve granulate; Add the crosslinked carboxymethylstach sodium and the magnesium stearate of recipe quantity, mix homogeneously; Tabletting.
Embodiment 3
| Supplementary material | Percentage by weight (%) |
| Fexofenadine hydrochloride | ??6 |
| Acrylic resin RSOP | ??12 |
| Mannitol | ??39.6 |
| Starch | ??18 |
| Ethyl cellulose | ??5 |
| Supplementary material | Percentage by weight (%) |
| Starch slurrying | ??2.4 |
| Hyprolose (interior) | ??8 |
| Hyprolose (outward) | ??8 |
| Magnesium stearate | ??1 |
Preparation technology:
Acrylic resin RSOP is scattered in 95% ethanol of recipe quantity; After being uniformly dispersed, add the fexofenadine hydrochloride of recipe quantity, stir 30min, it is dissolved fully; The about 3h of 50 degree rotary evaporations gets the fexofenadine hydrochloride clathrate.Take by weighing the fexofenadine clathrate of recipe quantity, mannitol, starch, ethyl cellulose and the hyprolose equivalent mix homogeneously that progressively increases; As binding agent, make soft material with starch slurry, 16 orders are granulated; 50 degree forced air dryings, 24 mesh sieve granulate; Add the hyprolose and the magnesium stearate of recipe quantity, mix homogeneously; Tabletting.
Embodiment 4
| Supplementary material | Percentage by weight (%) |
| Fexofenadine | ??6 |
| Eudragit E 100 | ??6 |
| Mannitol | ??43.6 |
| Microcrystalline Cellulose | ??20 |
| Ethyl cellulose | ??5 |
| Starch slurrying | ??2.4 |
| Hyprolose (interior) | ??8 |
| Hyprolose (outward) | ??8 |
| Magnesium stearate | ??1 |
Preparation technology:
Eudragit E 100 is scattered in 95% ethanol of recipe quantity; After being uniformly dispersed, add the fexofenadine hydrochloride of recipe quantity, stir 30min, it is dissolved fully; The about 3h of 50 degree rotary evaporations gets the fexofenadine hydrochloride clathrate.Take by weighing the fexofenadine clathrate of recipe quantity, mannitol, starch, ethyl cellulose and the hyprolose equivalent mix homogeneously that progressively increases; As binding agent, make soft material with starch slurry, 16 orders are granulated; 50 degree forced air dryings, 24 mesh sieve granulate; Add the hyprolose and the magnesium stearate of recipe quantity, mix homogeneously; Tabletting.
Embodiment 5
| Supplementary material | Percentage by weight (%) |
| Fexofenadine | ??15 |
| Mannitol | ??50.275 |
| Starch | ??18 |
| Starch slurrying | ??2.625 |
| Hyprolose | ??13 |
| The Fructus Citri tangerinae powdered flavor | ??0.05 |
| Sucralose | ??0.05 |
| Magnesium stearate | ??1 |
Preparation technology:
Take by weighing the fexofenadine of recipe quantity, mannitol, starch and the hyprolose equivalent mix homogeneously that progressively increases; As binding agent, make soft material with starch slurry, 16 orders are granulated; 50 degree forced air dryings, 24 mesh sieve granulate; Add the hyprolose and the magnesium stearate of recipe quantity, mix homogeneously; Tabletting.
Embodiment 6
| Supplementary material | Percentage by weight (%) |
| Fexofenadine hydrochloride | ??15 |
| Mannitol | ??50.275 |
| Starch | ??18 |
| Starch slurrying | ??2.625 |
| Hyprolose | ??13 |
| Chocolate essence | ??0.05 |
| Mentholum | ??0.05 |
| Magnesium stearate | ??1 |
Preparation technology:
Take by weighing the fexofenadine hydrochloride of recipe quantity, mannitol, starch and the hyprolose equivalent mix homogeneously that progressively increases; As binding agent, make soft material with starch slurry, 16 orders are granulated; 50 degree forced air dryings, 24 mesh sieve granulate; Add chocolate essence, Mentholum and the magnesium stearate of recipe quantity, mix homogeneously; Tabletting.
Embodiment 7
| Supplementary material | Percentage by weight (%) |
| Fexofenadine hydrochloride | ??15 |
| Beta-schardinger dextrin- | ??15 |
| Mannitol | ??35.275 |
| Starch | ??18 |
| Starch slurrying | ??2.625 |
| Hyprolose | ??13 |
| Chocolate essence | ??0.05 |
| Mentholum | ??0.05 |
| Magnesium stearate | ??1 |
Preparation technology:
Take by weighing the beta-schardinger dextrin-of recipe quantity, add water and in 80 ℃ of waters bath with thermostatic control, make saturated solution.Under electronic stirring,
Principal agent is slowly added in the beta-schardinger dextrin-liquid, and constant temperature stirring 1 hour stops heating, continues to be stirred to room temperature, gets white suspension, and put refrigerator and cooled and hid 12 hours, sucking filtration, 60 ℃ of dryings of precipitate are crossed 80 mesh sieves, get the fexofenadine clathrate after the drying.
Take by weighing the fexofenadine clathrate of recipe quantity, mannitol, starch and the hyprolose equivalent mix homogeneously that progressively increases; As binding agent, make soft material with starch slurry, 16 orders are granulated; 50 degree forced air dryings, 24 mesh sieve granulate; Add chocolate essence, Mentholum and the magnesium stearate of recipe quantity, mix homogeneously; Tabletting.
Embodiment 8
The sample of the foregoing description is carried out the detection of bitterness, disintegration (2005 editions pharmacopeia appendix XI A inspection techniques disintegration) and dissolution (2005 editions pharmacopeia appendix XI C dissolution method first methods), and the result is as follows:
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Embodiment 6 | Embodiment 7 | |
| Bitterness | It is lighter that 7 people all feel | It is lighter that 7 people all feel | It is lighter that 7 people all feel | It is lighter that 7 people all feel | 6 people can not accept, and 1 people sensation is bitter. | 7 people all can not accept | 6 people all can not accept, and 1 people sensation is bitter. |
| Disintegration | 30s | 40s | 35s | 90s | 30s | 35s | 40s |
| The 30min stripping | 98.35% | 96.52% | 97.47% | 95.46% | 96.47% | 97.61% | 98.31% |
Can prove by above embodiment, the applicant creatively adopts specific clathrate and specific ratio that inclusion technique is applied in the oral cavity disintegration tablet, solve the bitterness of principal agent and the problem of disintegration rate in the oral cavity disintegration tablet effectively, also guaranteed the dissolution of sample simultaneously.
Claims (10)
1. an oral cavity disintegration tablet that contains fexofenadine or its salt is characterized in that principal agent exists with the form of clathrate, and wherein the enclose material is water-insoluble polyacrylic acid resinoid.
2. oral cavity disintegration tablet according to claim 1 is characterized in that being made up of following ingredients and percentage ratio: the enclose material of the fexofenadine of 5-20% or its salt, 5-30%, the filler of 30-70%, the disintegrating agent of 8-20%, the lubricant of 0.5-2%.
3. oral cavity disintegration tablet according to claim 1 is characterized in that the enclose material is selected from the various models of EudragitE, EudragitL, EudragitS.
4. oral cavity disintegration tablet according to claim 1 is characterized in that the enclose material is selected from polyacrylic resin E100.
5. oral cavity disintegration tablet according to claim 1, the ratio that it is characterized in that principal agent and enclose material is 2: 1-1: 4.
6. oral cavity disintegration tablet according to claim 1, the ratio that it is characterized in that principal agent and enclose material is 1: 2.
7. oral cavity disintegration tablet according to claim 1 is characterized in that clathrate adopts preparation technologies such as fluid bed, spray drying, hypobaric drying method.
8. oral cavity disintegration tablet according to claim 1 is characterized in that filler is selected from mannitol, lactose, starch or microcrystalline Cellulose, two or more mixture.
9. oral cavity disintegration tablet according to claim 1 is characterized in that disintegrating agent is selected from cross-linked carboxymethyl cellulose sodium, crosslinked carboxymethylstach sodium or low carboxy-propyl cellulose, two or three mixture of replacing.
10. oral cavity disintegration tablet according to claim 1 is characterized in that lubricant is selected from one or more in magnesium stearate, stearic acid, the sodium stearyl fumarate.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201010184558A CN101836965A (en) | 2010-05-27 | 2010-05-27 | Orally disintegrating tablet containing fexofenadine or salts of fexofenadine, and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201010184558A CN101836965A (en) | 2010-05-27 | 2010-05-27 | Orally disintegrating tablet containing fexofenadine or salts of fexofenadine, and preparation method thereof |
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| CN101836965A true CN101836965A (en) | 2010-09-22 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201010184558A Pending CN101836965A (en) | 2010-05-27 | 2010-05-27 | Orally disintegrating tablet containing fexofenadine or salts of fexofenadine, and preparation method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102512389A (en) * | 2011-12-27 | 2012-06-27 | 天津市嵩锐医药科技有限公司 | Fexofenadine hydrochloride oral disintegrating drug composition |
| CN105997910A (en) * | 2016-06-09 | 2016-10-12 | 北京化工大学 | Taste masking preparation and preparing method thereof |
| CN118217258A (en) * | 2024-05-27 | 2024-06-21 | 中仁康博(天津)生物医药技术中心(有限合伙) | Orally disintegrating tablet and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1592622A (en) * | 2001-11-16 | 2005-03-09 | 爱的发 | Orodispersible tablets containing fexofenadine |
| CN1744882A (en) * | 2003-01-30 | 2006-03-08 | 埃迪制药公司 | Taste-masking coated particles, process for the preparation thereof and orodispersible tablets containing said coated particles |
| CN101103980A (en) * | 2006-07-14 | 2008-01-16 | 海南盛科生命科学研究院 | Fexofenadine medicinal composition |
-
2010
- 2010-05-27 CN CN201010184558A patent/CN101836965A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1592622A (en) * | 2001-11-16 | 2005-03-09 | 爱的发 | Orodispersible tablets containing fexofenadine |
| CN1744882A (en) * | 2003-01-30 | 2006-03-08 | 埃迪制药公司 | Taste-masking coated particles, process for the preparation thereof and orodispersible tablets containing said coated particles |
| CN101103980A (en) * | 2006-07-14 | 2008-01-16 | 海南盛科生命科学研究院 | Fexofenadine medicinal composition |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102512389A (en) * | 2011-12-27 | 2012-06-27 | 天津市嵩锐医药科技有限公司 | Fexofenadine hydrochloride oral disintegrating drug composition |
| CN102512389B (en) * | 2011-12-27 | 2013-08-21 | 天津市嵩锐医药科技有限公司 | Fexofenadine hydrochloride oral disintegrating drug composition |
| CN105997910A (en) * | 2016-06-09 | 2016-10-12 | 北京化工大学 | Taste masking preparation and preparing method thereof |
| CN118217258A (en) * | 2024-05-27 | 2024-06-21 | 中仁康博(天津)生物医药技术中心(有限合伙) | Orally disintegrating tablet and preparation method thereof |
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Addressee: Wanquan Sunlight Medicine Science and Technology Co., Ltd., Beijing Document name: Notification of Patent Invention Entering into Substantive Examination Stage |
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Application publication date: 20100922 |