CN105641705A - Fesoterodine pharmaceutical composition and preparation method thereof - Google Patents
Fesoterodine pharmaceutical composition and preparation method thereof Download PDFInfo
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- CN105641705A CN105641705A CN201410628148.XA CN201410628148A CN105641705A CN 105641705 A CN105641705 A CN 105641705A CN 201410628148 A CN201410628148 A CN 201410628148A CN 105641705 A CN105641705 A CN 105641705A
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- fesoterodine
- pharmaceutical composition
- microcrystalline cellulose
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Abstract
The invention discloses a fesoterodine pharmaceutical composition. The prescription of the composition takes mannitol and microcrystalline cellulose as filling agents by dosages according to percentage by weight as follows: 40-55% of the mannitol and 20-30% of the microcrystalline cellulose. The fesoterodine pharmaceutical composition is good in stability, and the pharmaceutical composition is capable of improving product yield, reducing cost and achieving industrial production; and the pharmaceutical composition can be better applied to clinical field, and can guarantee more significant advantages, effectively improve dissolution rate thereof and obviously improve bioavailability.
Description
Technical field
The invention belongs to medical art, it is specifically related to fesoterodine pharmaceutical composition and its preparation method.
Background technology
Fesoterodine, chemically can be called as isopropylformic acid 2-[(1R)-3-(diisopropylaminoethyl)-1-phenyl propyl]-4-(hydroxymethyl) phenyl ester, molecular formula: C26H37NO3, molecular weight: 411.28. This medicine is disclosed in EP1077912B1, and it is relevant with the novel derivative of 3,3-diphenylpropylamine. The stable salt of the described novel derivative of the open 3,3-diphenylpropylamine of EP1230209B1, comprises fesoterodine difumarate.
Fumaric acid fesoterodine is slow releasing tablet, 1 time on the one oral medication, and getting permission indication is be used for the treatment of bladder excessive activities to levy symptom such as high frequent micturition, urine sense of urgency or acute urine incontinence. Fumaric acid fesoterodine has 4mg and 8mg two kinds of specifications, and patient accepts to start with 4mg/d when this medicine is treated, then visual treatment responsiveness increasing dose 8mg extremely the highest every day, and general therapeutic 2-8 Zhou Houneng obtains greatest treatment efficacy. But in use to severe hepatic or kidney function damage patient and preferably to lower dosage during fumaric acid fesoterodine to 4mg maximum every day.
With reference to oral preparations not only complex process prepared by existing method, production cost height, it is difficult to realize the big production of industrialization, and the dissolution rate of fesoterodine is also on the low side. The key in fact preparing fesoterodine sheet is to find the ratio of suitable auxiliary material and various auxiliary material, and good fluidity when ensureing compressing tablet, result of extraction is good, still needs new method at present to prepare fesoterodine tablet.
The present inventor is through the research to prior art, and unexpected discovery, applies special auxiliary material, fesoterodine pharmaceutical composition prepared by special process, reliable in quality, and dissolution rate is fast, is easy to industrialization, reduces production cost, is easy to implement, remarkable in economical benefits.
Summary of the invention
For overcoming in prior art the shortcoming existing for fesoterodine preparation, one aspect of the present invention provides a kind of pharmaceutical composition containing fesoterodine, said composition formula is simple, mature preparation process, when improving insoluble drug dissolution rate in vitro, without sand type, good mouthfeel, it is convenient to patient and takes.
2nd object of the present invention is to provide the preparation method of fesoterodine pharmaceutical composition of the present invention, and the method is simple, and prepared fesoterodine pharmaceutical composition, steady quality is reliable.
For realizing first object of the present invention, the present inventor surprisingly finds the pharmaceutical composition of a kind of fesoterodine, said composition prescription adopt N.F,USP MANNITOL and Microcrystalline Cellulose as weighting agent, its consumption N.F,USP MANNITOL 40%-55% by weight percentage, Microcrystalline Cellulose 20%-30%.
The pharmaceutical composition of the present invention also comprises auxiliary material or the additive that one or more are pharmaceutically commonly used, such as disintegrating agent, lubricant, glidant etc., wherein disintegrating agent be selected from croscarmellose sodium, polyvinylpolypyrrolidone, cross-linked polyvinylpyrrolidone or low-substituted hydroxypropyl cellulose one or more; Lubricant is selected from Magnesium Stearate or talcum powder, and glidant is selected from micropowder silica gel.
Fesoterodine pharmaceutical composition, by weight percentage, concrete composition is as follows:
Fumaric acid fesoterodine 1-3.3%
N.F,USP MANNITOL 40-55%
Microcrystalline Cellulose 20-30%
Disintegrating agent 15-25%
Lubricant 1-2%
Glidant 0.5-2%
Preferably, the weight percent content 40-50% of N.F,USP MANNITOL in above-mentioned composition, the particle diameter of N.F,USP MANNITOL is preferably 50% particle diameter lower than 150 ��m, after adopting such particle diameter can better with other auxiliary materials particularly Microcrystalline Cellulose mix, thus play filling effect better.
Preferably, in above-mentioned composition, the content of the weight percent of Microcrystalline Cellulose is 25-30%, owing to the addition of Microcrystalline Cellulose in the present invention as auxiliary weighting agent, the consumption of N.F,USP MANNITOL is reduced, thus reduce the cost of whole prescription, overcome the tablet friability of gained that is excessive due to N.F,USP MANNITOL consumption and that cause higher, it is not suitable for the shortcoming of shipping storage and use.
N.F,USP MANNITOL and Microcrystalline Cellulose are mixed as weighting agent, the existing correlation technique about fesoterodine orally disintegrating tablet also has no relevant report.
Fesoterodine pharmaceutical composition of the present invention is adopted and is prepared with the following method, and the method comprises the steps: that getting fumaric acid fesoterodine pulverizes, and sieves, for subsequent use; Getting N.F,USP MANNITOL, Microcrystalline Cellulose sieves, for subsequent use; Take the disintegrating agent of recipe quantity, lubricant, glidant mix to obtain auxiliary material mixture; Take the fesoterodine of recipe quantity, mix with auxiliary material mixture with equivalent method of progressively increasing, measure mixture content of dispersion, calculate sheet weight, direct compression and get final product.
On the basis of existing pharmaceutical adjunct and preparation technology, the present inventor finds through a large amount of experimental studies, and fesoterodine pharmaceutical composition is above-mentioned formula and during preparation technology, and described pharmaceutical composition quality is effectively ensured.
Compared with prior art, tool of the present invention has the following advantages:
1) fesoterodine pharmaceutical composition provided by the present invention is for improving the receipts rate of this product, reduce products production cost, and being better applied to clinical treatment has very big help.
2) new fesoterodine composition provided by the present invention, through industrialized production and study on the stability, proves constant product quality.
3) preparation method of new fesoterodine composition provided by the present invention, the method is simple, prepared fesoterodine pharmaceutical composition reliable in quality.
Embodiment
Following examples are only for explaining the present invention, and are not used in restriction the present invention. Unless otherwise indicated, the experiment condition in the embodiment of the present invention is the experiment condition of this area routine.
Embodiment 1
Fesoterodine pharmaceutical composition described in every 1000, its formula consists of:
Fumaric acid fesoterodine 4g
N.F,USP MANNITOL 60g
Microcrystalline Cellulose 30g
Croscarmellose sodium 21.6g
Magnesium Stearate 2g
Micropowder silica gel 2.4
Preparation technology: get fumaric acid fesoterodine, that N.F,USP MANNITOL, Microcrystalline Cellulose cross 80 orders sieves is for subsequent use, take the N.F,USP MANNITOL of formula ratio, Microcrystalline Cellulose, croscarmellose sodium, Magnesium Stearate and micropowder silica gel and obtain auxiliary material mixture, take the fesoterodine of formula ratio, with equivalent progressively increase method and auxiliary material mixture mixture even, measure mixture content of dispersion, calculating sheet weight, direct compression, to obtain final product.
Embodiment 2
Fesoterodine pharmaceutical composition described in every 1000, its formula consists of:
Fumaric acid fesoterodine 4g
N.F,USP MANNITOL 48g
Microcrystalline Cellulose 36g
Polyvinylpolypyrrolidone 30g
Magnesium Stearate 1.2g
Differential silica gel 0.8g
Preparation technology: get fumaric acid fesoterodine, that N.F,USP MANNITOL, Microcrystalline Cellulose cross 80 orders sieves is for subsequent use, take the N.F,USP MANNITOL of formula ratio, Microcrystalline Cellulose, polyvinylpolypyrrolidone, Magnesium Stearate and micropowder silica gel and obtain auxiliary material mixture, take the fesoterodine of formula ratio, with equivalent progressively increase method and auxiliary material mixture mixture even, measure mixture content of dispersion, calculating sheet weight, direct compression, to obtain final product.
Embodiment 3
Fesoterodine pharmaceutical composition described in every 1000, its formula consists of:
Fumaric acid fesoterodine 4g
N.F,USP MANNITOL 66g
Microcrystalline Cellulose 24g
Low-substituted hydroxypropyl cellulose 21.6g
Magnesium Stearate 2g
Differential silica gel 2.4g
Preparation technology: get fumaric acid fesoterodine, that N.F,USP MANNITOL, Microcrystalline Cellulose cross 80 orders sieves is for subsequent use, take the N.F,USP MANNITOL of formula ratio, Microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, Magnesium Stearate and micropowder silica gel and obtain auxiliary material mixture, take the fesoterodine of formula ratio, with equivalent progressively increase method and auxiliary material mixture mixture even, measure mixture content of dispersion, calculating sheet weight, direct compression, to obtain final product.
Test example 1
Sample thief, places respectively at high temperature 60 DEG C, RH92.5% and intensity of illumination 4500Lx �� 500Lx when, respectively at sampling in 5 days, 10 days, detection, and compares with 0 day, and experimental result sees the following form.
This fesoterodine pharmaceutical composition has good stability and dissolution rate under the environment of high temperature, high wet and illumination.
Claims (7)
1. a fesoterodine pharmaceutical composition, it is characterised in that: prescription adopt N.F,USP MANNITOL and Microcrystalline Cellulose as weighting agent, its consumption N.F,USP MANNITOL 40%-55% by weight percentage, Microcrystalline Cellulose 20%-30%.
2. fesoterodine pharmaceutical composition according to claim 1, it is characterised in that: by weight percentage, concrete composition is as follows:
Fumaric acid fesoterodine 1-3.3%
N.F,USP MANNITOL 40-55%
Microcrystalline Cellulose 20-30%
Disintegrating agent 15-25%
Lubricant 1-2%
Glidant 0.5-2%.
3. fesoterodine pharmaceutical composition according to claim 1 and 2, it is characterised in that the particle diameter of N.F,USP MANNITOL is that 50% particle diameter is lower than 150 ��m.
4. fesoterodine pharmaceutical composition according to claim 1 and 2, it is characterised in that the consumption of N.F,USP MANNITOL is 40-50% by weight percentage, and Microcrystalline Cellulose is 25-30%.
5. fesoterodine pharmaceutical composition according to claim 2, it is characterised in that described disintegrating agent be selected from croscarmellose sodium, polyvinylpolypyrrolidone, cross-linked polyvinylpyrrolidone or low-substituted hydroxypropyl cellulose one or more.
6. fesoterodine pharmaceutical composition according to claim 2, it is characterised in that described lubricant is selected from Magnesium Stearate or talcum powder, and glidant is selected from micropowder silica gel.
7. the preparation method of fesoterodine pharmaceutical composition described in the arbitrary item of claim 1-6, the method comprises the steps: to take fumaric acid fesoterodine, the N.F,USP MANNITOL of recipe quantity, and Microcrystalline Cellulose sieves, for subsequent use; Take the disintegrating agent of recipe quantity, lubricant, glidant mix to obtain auxiliary material mixture; Take the fesoterodine of recipe quantity, mix with auxiliary material mixture with equivalent method of progressively increasing, measure mixture content of dispersion, calculate sheet weight, direct compression and get final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410628148.XA CN105641705A (en) | 2014-11-11 | 2014-11-11 | Fesoterodine pharmaceutical composition and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410628148.XA CN105641705A (en) | 2014-11-11 | 2014-11-11 | Fesoterodine pharmaceutical composition and preparation method thereof |
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| CN105641705A true CN105641705A (en) | 2016-06-08 |
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| CN201410628148.XA Pending CN105641705A (en) | 2014-11-11 | 2014-11-11 | Fesoterodine pharmaceutical composition and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110151720A (en) * | 2019-05-09 | 2019-08-23 | 合肥信风科技开发有限公司 | Pharmaceutical composition and preparation method thereof containing fesoterodine |
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- 2014-11-11 CN CN201410628148.XA patent/CN105641705A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110151720A (en) * | 2019-05-09 | 2019-08-23 | 合肥信风科技开发有限公司 | Pharmaceutical composition and preparation method thereof containing fesoterodine |
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Application publication date: 20160608 |