CN104000791A - Ferric citrate chewable tablet - Google Patents
Ferric citrate chewable tablet Download PDFInfo
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- CN104000791A CN104000791A CN201410253983.XA CN201410253983A CN104000791A CN 104000791 A CN104000791 A CN 104000791A CN 201410253983 A CN201410253983 A CN 201410253983A CN 104000791 A CN104000791 A CN 104000791A
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- ferric citrate
- chewable tablet
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Abstract
The invention relates to a bitter-taste-masking direct-pressure chewable tablet by taking ferric citrate hydrate as the active component, which contains effective amount of ferric citrate hydrate with the average particle size of 300-500 mu m, neosperidin dihydrochalcone as a bitter-taste-masking agent, and pharmaceutical compositions of other pharmaceutically acceptable carriers. The ferric citrate chewable tablet disclosed by the invention has the advantages of simple process, direct pressing, low cost, sweet taste, good mouth feel, high bioavailability and the like.
Description
Technical field
The present invention is field of pharmaceutical preparations, be specifically related to a kind of taste masking vertical compression chewable tablet that ferric citrate hydrate is active component of take, its mean diameter that comprises effective therapeutic dose is that 300 μ m～500 μ m ferric citrate hydrates and NHDC are the pharmaceutical composition of odor mask and pharmaceutically acceptable other carrier.
Background technology
Hyperphosphatemia is chronic kidney disease (chronic kidney disease, CKD), especially one of CKD modal complication of later stage, is the key factor of heterotopic calcification, secondary hyperparathyroidism and renal osteodystrophy.Along with going deep into that serum paraoxonase metabolism disorder is familiar with, increasing scholar thinks that hyperphosphatemia is the important risk factor that CKD increases patient's sickness rate, admission rate and mortality rate.Thereby, effectively control the level of serum paraoxonase by the key that is CKD patient's prognosis.
At present, the treatment measure of hyperphosphatemia comprises diet control, dialysis, use phosphate binder.Although CKD patient can take in to reduce serum paraoxonase level by the middle phosphorus of keeping on a diet, and still has Most patients cannot reach control criterion, thereby need to reach control object by application phosphate binder.Even when the CKD later stage starts dialysis treatment, still need to coordinate phosphate binder to assist the level that reduces serum paraoxonase.
Oral phosphate binder can reduce the phosphatic absorption of intestinal, is the critical treatment measure of CKD patient's hyperphosphatemia.The New Phosphorus bonding agent of the non-aluminum of non-calcium is calcic, aluminum not, is difficult for causing serum calcium, aluminum rising, and untoward reaction is relatively little, thereby more and more New Phosphorus bonding agent develops growth rapidly, constantly enters among clinical or research.
Citric acid iron plate (ferric citrate) is a kind of iron-based phosphate binder, by Keryx biopharmaceutical company, is developed.On January 20th, 2014 Japan take the lead in listing, Keryx biopharmaceutical company and affiliate Panacor company in August, 2013 the You Xiang U.S. submitted the application for quotation of this medicine to.Ferric citrate in conjunction with phosphorus, can increase phosphorus excretion at intestinal, reduces phosphorus and absorbs, and also can prevent the abnormal progress of heterotopic calcification, secondary hyperparathyroidism and bone.The effect that serum paraoxonase falls in ferric citrate presents dosage correlation, and toleration is better, and untoward reaction is less.
Ferric citrate, taste is extremely bitter and puckery, the citric acid iron plate of Japan's listing, adopt IR film coating, but appointing so can not taste masking, flavoring agent and general coating are not reliable method for ferric citrate hydrate, because its bitterness is extremely difficult, cover to considerable degree.
In the citric acid iron plate of Japan's listing, adjuvant is IR, cellulose, polyvinyl alcohol acrylic acid methylmethacrylate copolymer, hydroxypropyl cellulose, polyvinylpolypyrrolidone, calcium stearate, hypromellose, titanium dioxide, Talcum, Polyethylene Glycol.Ferric citrate hydrate is due to its special physical property, the easy moisture absorption, and hardening after the moisture absorption, has a strong impact on mouthfeel and drug effect.The former powder poor fluidity of ferric citrate hydrate, and do not possess cohesive and compressibility, therefore there is following difficulty in preparation: the one, use traditional wet granulation technology to lump; The 2nd, if adopt traditional dry method direct compression technique, need again to add dry binder, as PVP, dextrin etc., but the just easy moisture absorption of conventional binding agent itself, also easily moisture absorption hardening in storage process; The 3rd, it is poor compared with the easy mouthfeel of words chewable tablet of multiple auxiliary materials to use, and has grittiness.Therefore be necessary to screen that supplementary product kind is few, consumption is few, efficacy stability, ferric citrate preparation that mouthfeel is good, to improve patient's compliance.
Chewable tablet is that a class can be chewed the tablet under posterior phraynx in oral cavity, and size is general identical with conventional tablet, can make as required difform Special-shaped sheet.Tablet is convenient to swallow after chewing, and tablet surface area increases, and can promote medicine dissolving, absorption in vivo.For the not good medicine of absorbability, make chewable tablet and can accelerate its disintegrate, promote drug absorption availability.Chewable tablet taking convenience, even if also medication on time under the condition of hydropenia is specially adapted to the poor patient of children's, old man, dysphagia or gastrointestinal function, can reduces medicine gastrointestinal is born.Therefore, chewable tablet application is extensively got up gradually.
NHDC is the flavone derivative that the neohesperidin that extracts from citrus natural plants forms through over hydrogenation, is a kind of functional sweetener with good debitter and flavor improvement.These product have that sugariness is high, heat is little, sweet taste is slow, the time is long and stable well, avirulence.It is without mutagenicity, non-carcinogenesis, and without cariogenic row, without obvious poisonous effect, on health, without bad impact, accretion rate is fast.By U.S. FDA, classified as generally acknowledged non-toxic compound.
Summary of the invention
The object of the present invention is to provide a kind of ferric citrate chewable tablet compositions of taste masking vertical compression.
The present inventor shockingly finds: by mean diameter being defined as to 300 μ m～500 μ m, ferric citrate hydrate is easy to direct compression, and the bitterness of ferric citrate hydrate can effectively be covered.Therefore based on this discovery, made the present invention.
The invention provides a kind of vertical compression ferric citrate chewable tablet of taste masking.Particularly, the invention provides a kind of vertical compression ibuprofen chewable tablet of taste masking, it comprises the mean diameter for the treatment of effective dose is the ferric citrate hydrate of 300 μ m～500 μ m, and pharmaceutically acceptable carrier.
In a preferred embodiment of the invention, the mean diameter of ferric citrate hydrate is 300 μ m～400 μ m.
In a kind of ferric citrate chewable tablet of the present invention, the amount that ferric citrate hydrate exists is preferably 250mg～500mg.
In a kind of ferric citrate chewable tablet of the present invention, the measurer body that ferric citrate hydrate exists can be 250mg.
In a kind of ferric citrate chewable tablet of the present invention, the measurer body that ferric citrate hydrate exists can be 500mg.
In a kind of ferric citrate chewable tablet of the present invention, pharmaceutically acceptable carrier can be one or more in diluent, binding agent, disintegrating agent, stabilizing agent, sweeting agent, flavoring agent, flavour enhancer, coloring agent, fluidizer and lubricant.
Sweeting agent of the present invention, flavoring agent, flavour enhancer are NHDC.
The hardness of a kind of ferric citrate chewable tablet of the present invention can be 30N～90N, preferably 50N～70N.
A kind of ferric citrate chewable tablet of the present invention can be accepted in the sense of taste, can discharge fast ferric citrate active component, and can more economical preparation effectively.
By the ferric citrate chewable tablet of formula preparation disclosed by the invention, through pharmacy check, each index conformance with standard, and its hygroscopicity has larger improvement compared with conventional tablet.
The specific embodiment
The following examples can conduct further description the present invention, yet these embodiment should be as limitation of the scope of the invention.
embodiment 1
Prescription:
Ferric citrate hydrate 250g
NHDC 250g
Magnesium stearate 2.5g
Silica sol 9.0g
Make 1000
Preparation technology: take respectively NHDC, magnesium stearate and silica sol according to recipe quantity, cross respectively 100 mesh sieves, taking in addition mean diameter is that 300 μ m～400 μ m(laser particle size detectors detect) ferric citrate hydrate, put in Hoppertypeofblender and be mixed, target hardness is 50N～70N tabletting and get final product.
embodiment 2
Prescription:
Ferric citrate hydrate 250g
NHDC 150g
Hydroxypropyl methylcellulose 300g
Magnesium stearate 2.5g
Silica sol 7.0g
Make 1000
Preparation technology: take respectively NHDC, hydroxypropyl methylcellulose, magnesium stearate and silica sol according to recipe quantity, cross respectively 100 mesh sieves, taking in addition mean diameter is that 300 μ m～400 μ m(laser particle size detectors detect) ferric citrate hydrate, put in Hoppertypeofblender and be mixed, target hardness is 50N～70N tabletting and get final product.
embodiment 3
Prescription:
Ferric citrate hydrate 500g
NHDC 450g
Magnesium stearate 4.5g
Silica sol 12.0g
Make 1000
Preparation technology: take respectively NHDC, magnesium stearate and silica sol according to recipe quantity, cross respectively 100 mesh sieves, taking in addition mean diameter is that 300 μ m～400 μ m(laser particle size detectors detect) ferric citrate hydrate, put in Hoppertypeofblender and be mixed, target hardness is 50N～70N tabletting and get final product.
embodiment 4the contrast test of chewable tablet of the present invention and commercially available ordinary tablet
The ferric citrate chewable tablet of preparing according to above-described embodiment and ordinary tablet (リ オ Na Ingot，Birds Ju medicine Co., Ltd. manufactures, lot number AA01141) are pressed preparation conventional sense method, contrast, and the results are shown in following table:
Experimental data shows, ferric citrate chewable tablet has greatly improved in moisture absorption weightening finish and mouthfeel than ferric citrate ordinary tablet, makes it more can meet patient's needs.
Claims (9)
1. a ferric citrate chewable tablet, it comprises the mean diameter for the treatment of effective dose is that 300 μ m～500 μ m ferric citrate hydrates and NHDC are the pharmaceutical composition of odor mask and pharmaceutically acceptable other carrier.
2. ferric citrate chewable tablet according to claim 1, wherein said ferric citrate hydrate mean diameter is 300 μ m～400 μ m.
3. ferric citrate chewable tablet according to claim 1 and 2, the amount of wherein said ferric citrate hydrate is 250mg～500mg.
4. ferric citrate chewable tablet according to claim 3, the amount of wherein said ferric citrate hydrate is 250mg.
5. ferric citrate chewable tablet according to claim 3, the amount of wherein said ferric citrate hydrate is 500mg.
6. according to a kind of ferric citrate chewable tablet of claim 1, wherein said pharmaceutically acceptable carrier is one or more in diluent, binding agent, disintegrating agent, stabilizing agent, sweeting agent, flavoring agent, flavour enhancer, coloring agent, fluidizer and lubricant.
7. according to a kind of ferric citrate chewable tablet of claim 1 or 6, wherein sweeting agent, flavoring agent, flavour enhancer are NHDC.
8. according to a kind of ferric citrate chewable tablet of any one in aforementioned claim, its hardness is 30N～90N.
9. a kind of ferric citrate chewable tablet according to Claim 8, its hardness is 50N～70N.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410253983.XA CN104000791A (en) | 2014-06-10 | 2014-06-10 | Ferric citrate chewable tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410253983.XA CN104000791A (en) | 2014-06-10 | 2014-06-10 | Ferric citrate chewable tablet |
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| Publication Number | Publication Date |
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| CN104000791A true CN104000791A (en) | 2014-08-27 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201410253983.XA Pending CN104000791A (en) | 2014-06-10 | 2014-06-10 | Ferric citrate chewable tablet |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2223405A (en) * | 1988-10-04 | 1990-04-11 | Otsuka Pharma Co Ltd | Effervescent iron composition |
| CN102258490A (en) * | 2011-07-01 | 2011-11-30 | 中美天津史克制药有限公司 | Ibuprofen chewable tablet |
| CN102526752A (en) * | 2011-06-15 | 2012-07-04 | 上海现代制药股份有限公司 | Bitterness-eliminated medicinal preparation |
| CN103124553A (en) * | 2010-10-13 | 2013-05-29 | 弗雷森纽斯医疗护理德国有限责任公司 | Phosphate binder formulation for simple ingestion |
-
2014
- 2014-06-10 CN CN201410253983.XA patent/CN104000791A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2223405A (en) * | 1988-10-04 | 1990-04-11 | Otsuka Pharma Co Ltd | Effervescent iron composition |
| CN103124553A (en) * | 2010-10-13 | 2013-05-29 | 弗雷森纽斯医疗护理德国有限责任公司 | Phosphate binder formulation for simple ingestion |
| CN102526752A (en) * | 2011-06-15 | 2012-07-04 | 上海现代制药股份有限公司 | Bitterness-eliminated medicinal preparation |
| CN102258490A (en) * | 2011-07-01 | 2011-11-30 | 中美天津史克制药有限公司 | Ibuprofen chewable tablet |
Non-Patent Citations (1)
| Title |
|---|
| 罗明生，高天惠: "《药剂辅料大全（第2版）》", 31 January 2006, 四川科学技术出版社 * |
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Application publication date: 20140827 |