CN103054822A - Imidafenacin tablet and preparation method thereof - Google Patents
Imidafenacin tablet and preparation method thereof Download PDFInfo
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- CN103054822A CN103054822A CN2012105858895A CN201210585889A CN103054822A CN 103054822 A CN103054822 A CN 103054822A CN 2012105858895 A CN2012105858895 A CN 2012105858895A CN 201210585889 A CN201210585889 A CN 201210585889A CN 103054822 A CN103054822 A CN 103054822A
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Abstract
The invention discloses an imidafenacin tablet which is prepared from the components including imidafenacin, water-soluble polymer, a filling agent, a disintegrating agent and lubricant; the water-soluble polymer is selected from one or more of poloxamer, polyethyleneglycol, hydroxypropyl methylcellulose, polyvinyl alcohol and copovidone and accounts for 0.1 percent to 3 percent (w/w) of the total weight of the whole tablet; and the disintegrating agent is pregelatinized starch or a mixture of common starch and pregelatinized starch and accounts for 15 percent to 50 percent (w/w) of the total weight of the whole tablet. The tablet provided by the invention can be dissolved in a water-based medium at an unexpected high level in relative time and has a very good dissolution characteristic and remarkable physical stability.
Description
Technical field
The invention belongs to the pharmaceutical preparations technology field, in particular to a kind of imidafenacin tablet and preparation method thereof, relate in particular to a kind of imidafenacin tablet and technique thereof that adopts the solid dispersions technique preparation.
Background technology
Imidafenacin (Imidafenacin) has the diphenyl butanamide structure, is a kind of new and effective anticholinergic agent, and its selectively acting is in M3 and M1 receptor, and the blocking-up choline makes detrusor lax to the contraction of detrusor, reduces side effects of pharmaceutical drugs.Imidafenacin has the contraction of the smooth muscle of bladder of inhibition and suppresses the free dual function of acetylcholine simultaneously, and the selectivity of bladder is better than salivary gland, for in the cerebral tissue but the alkali receptor affinity is lower, therefore maincenter and periphery untoward reaction are less, have height bladder selectivity, be applicable to the treatment of overactive bladder.
Imidafenacin chemistry 4-(2-methyl-1 H-imidazole-1-group)-2 by name, the 2-diphenyl butanamide, structural formula is shown in formula I, for white to the off-white color crystalline powder, be soluble in acetic acid (100), be dissolved in N, the N-dimethyl adds amide and methanol, slightly be dissolved in ethanol (99.5), be slightly soluble in acetonitrile, be insoluble in water.
Because active component imidafenacin poorly water-soluble causes the bioavailability of preparation or absorption in vivo very low, thereby causes the inadequate problem of drug effect.In order to increase its water solublity, and then increase its oral administration biaavailability, those skilled in the art can consider to adopt solid dispersions technique to prepare the imidafenacin tablet, and the active component imidafenacin is scattered in the polymer supported liquid solution with unbodied state.Yet, owing to adopt the imidafenacin tablet of conventional solid dispersion powder preparation significantly to reduce the specific surface area of slice, thin piece itself, and therefore the strong combination in mold process between the plastic deformation of amorphous drug molecule and the carrier polymer adopts the imidafenacin tablet porosity of solid dispersion powder preparation generally very low.This low-porosity so that in drug administration process hydrone slowly infiltrate tablet, so solid dispersion is difficult to performance, and it improves the internal action of stripping.In addition, in hydration or process in leaching, increase as the viscosity of the water-soluble or enteric polymer of carrier, thereby the surface of tablet forms a kind of hydrogel layer in process in leaching, so that the infiltration of water is further stoped.
CN101983054A discloses in a kind of oral cavity of containing imidafenacin rapidly disintegrative tablet, it contains (1) with polyvidone or gastric solubility macromolecule granules coating, that contain imidafenacin or imidafenacin granule, contain the compositions of excipient and disintegrating agent and the compressed shaping of described compositions with (2).Yet, what this imidafenacin tablet adopted is fluidized-bed spray granulation, the filleies such as imidafenacin and starch are prepared into granule, then water-soluble polymer is sprayed the outside of parcel and granule, then at tabletting, say the tablet that has obtained having certain light-shading effect, but this kind way obtains granule behind tabletting, the water-solubility membrane clothing of parcel can break under the effect of pressure in deformation, and the preparation tablet weight of this patent is bigger than normal, complex manufacturing is infeasible, has increased a lot of production costs, and efficient is lower.
CN102579393A discloses a kind of solid composite medicament that contains imidafenacin, with hydrophilicity condiment and imidafenacin micronization, the material particular diameter that requirement obtains is less than 5 microns, and lower and micronizing materials particle diameter reproducibility remains to be investigated yet the operational approach of this patent is in commercial production efficient.
Summary of the invention
In view of the deficiencies in the prior art, the present invention studies the solid dispersion technology of preparing of imidafenacin by lot of experiments, find when the water-soluble polymer that adds particular types and consumption and disintegrating agent, the disintegrative of the tablet that obtains by the mold pressing solid dispersion does not reduce, and has excellent dissolution.Therefore, the object of the present invention is to provide a kind of under various conditions equal stable and imidafenacin tablet that can Fast Stripping, and the method for preparing said preparation.
The object of the present invention is achieved like this:
A kind of imidafenacin tablet, be prepared from by the component that comprises imidafenacin, water-soluble polymer, filler, disintegrating agent and lubricant, described water-soluble polymer be selected from polyethylene adjoin pyrrolidone, hypromellose, Polyethylene Glycol, polyvinyl alcohol and poloxamer one or more, consumption accounts for the 0.1-3%(w/w of whole weight), described disintegrating agent is the mixture of pre-paying starch or common starch and pregelatinized Starch, and consumption accounts for the 15-50%(w/w that is of whole weight).
Preferably, above-mentioned imidafenacin tablet, wherein said water-soluble polymer is poloxamer, preferably consumption accounts for the 0.5-2%(w/w of whole weight).
Preferably, above-mentioned imidafenacin tablet, wherein said disintegrating agent are pre-paying starch, and consumption accounts for the 23.5-33.5%(w/w that is of whole weight).
Preferably, the imidafenacin tablet of the above, wherein said filler is selected from one or more of microcrystalline Cellulose, starch, lactose, sucrose, mannitol and anhydrous calcium phosphate.
Further preferably, above-mentioned imidafenacin tablet, wherein said filler are microcrystalline Cellulose.
Preferably, above-mentioned imidafenacin tablet, wherein said lubricant is selected from one or more of magnesium stearate, Pulvis Talci, castor oil hydrogenated, stearic acid and Polyethylene Glycol.
A kind of preparation method of above-mentioned imidafenacin tablet comprises the steps: water-soluble polymer dissolves in solvent, adds imidafenacin and makes Uniform Dispersion or dissolving, mix with filler and disintegrating agent, wet granulation, 40 ℃ of-60 ℃ of dryings, direct compression after dried granule and the mix lubricant.
The preparation method of above-mentioned imidafenacin tablet, wherein said solvent is preferably the aqueous solution of methanol, ethanol, dichloromethane or acetone.
Compared with prior art, imidafenacin tablet that the present invention relates to and preparation method thereof has following advantage and significant progressive: the whole disintegrates of medicine in the tablet of the imidafenacin that the present invention obtains 10 minutes, the concentration of imidafenacin in the stripping system is more than 85% of dosage, therefore shows high disintegrative and high stripping property.
Description of drawings
Fig. 1 is the stripping curve figure of the imidafenacin sheet of embodiment 1 and comparative example 1 preparation.
Fig. 2 is the stripping curve figure of the imidafenacin sheet of embodiment 2 and comparative example 2 preparations.
Fig. 3 is the stripping curve figure of the imidafenacin sheet of embodiment 3 and comparative example 3 preparations.
The specific embodiment
Form is described in further detail foregoing of the present invention again by the following examples, but this should be interpreted as that the scope of the above-mentioned theme of the present invention only limits to following embodiment, all technology that realizes based on foregoing of the present invention all belong to scope of the present invention.
Embodiment 1 and comparative example 1:
| Prescription | Embodiment 1 | Comparative example 1 | |
| Imidafenacin | 0.1g | 0.1g | |
| Microcrystalline Cellulose (PH101) | 100g | 100g | |
| Pregelatinized Starch | 32g | 32g | |
| Magnesium | 1g | 1g | |
| 70% alcohol solvent | In right amount | ||
| 5% poloxamer ethanol (70%) solution | 1.5g(in poloxamer) |
Embodiment 1 preparation technology: poloxamer is dissolved in 70% ethanol water, add imidafenacin and make Uniform Dispersion or dissolving, the microcrystalline Cellulose (PH101) and the pregelatinized Starch that then add the recipe quantity of mix homogeneously, wet granulation, after mixing with magnesium stearate, 40 ℃ of-60 ℃ of dryings, dried granule directly press 1000.
Comparative example 1 preparation technology: with imidafenacin and microcrystalline Cellulose (PH101) and pregelatinized Starch mix homogeneously, with 70% ethanol water as binding agent, wet granulation, 40 ℃ of-60 ℃ of dryings are directly pressed 1000 after dried granule mixes with magnesium stearate.
Stripping curve figure (accompanying drawing 1) by the imidafenacin sheet of embodiment 1 and Comparative Examples 1 preparation can find out that the stripping of the imidafenacin tablet of water-soluble polymer preparation has obvious quickening.
Embodiment 2 and comparative example 2:
| Prescription | Embodiment 2 | Comparative example 2 |
| Imidafenacin | 0.1g | 0.1g |
| Microcrystalline Cellulose (PH101) | 100g | 100g |
| Pregelatinized Starch | 32g | 32g |
| Magnesium stearate | 1g | 1g |
| 5%PVP.K30 ethanol (70%) solution | 1.5g(in PVP.K30) | |
| 5% poloxamer ethanol (70%) solution | 1.5g(in poloxamer) |
Embodiment 2 preparation technologies: poloxamer is dissolved in 70% ethanol water, add imidafenacin and make Uniform Dispersion or dissolving, then add the microcrystalline Cellulose of the recipe quantity of mix homogeneously (PH101) and pregelatinized Starch, wet granulation, after mixing with magnesium stearate, 40 ℃ of-60 ℃ of dryings, dried granule directly press 1000.
Comparative example 2 preparation technologies: imidafenacin is mixed with microcrystalline Cellulose (PH101) and pregelatinized Starch, with 5%PVP.K30 ethanol (70%) solution as binding agent, wet granulation, 40 ℃ of-60 ℃ of dryings are directly pressed 1000 after dried granule mixes with magnesium stearate.
Stripping curve figure (accompanying drawing 3) by the imidafenacin sheet of embodiment 2 and Comparative Examples 2 preparations can find out, adopts the stripping of the imidafenacin tablet that preparation technology of the present invention obtains that obvious quickening is arranged.
Embodiment 3 and comparative example 3:
Preparation process: poloxamer is dissolved in 70% ethanol water, add imidafenacin and make Uniform Dispersion or dissolving, then add the microcrystalline Cellulose of the recipe quantity of mix homogeneously (PH101) and pregelatinized Starch, wet granulation, after mixing with magnesium stearate, 40 ℃ of-60 ℃ of dryings, dried granule directly press 1000.
Stripping curve figure (accompanying drawing 3) by the imidafenacin sheet of embodiment 3 and Comparative Examples 3 preparations can find out, adopts the dissolution of imidafenacin tablet of the poloxamer preparation of large recipe quantity can reduce on the contrary, also increases simultaneously production cost.
Claims (8)
1. imidafenacin tablet, it is characterized in that: be prepared from by the component that comprises imidafenacin, water-soluble polymer, filler, disintegrating agent and lubricant, described water-soluble polymer be selected from poloxamer, hypromellose, Polyethylene Glycol, polyvinyl alcohol and polyethylene adjoin pyrrolidone one or more, consumption accounts for the 0.1-3%(w/w of whole weight), described disintegrating agent is the mixture of pre-paying starch or common starch and pregelatinized Starch, and consumption accounts for the 15-50%(w/w that is of whole weight).
2. imidafenacin tablet according to claim 1, it is characterized in that: described water-soluble polymer is poloxamer, consumption accounts for the 0.5-2%(w/w of whole weight).
3. imidafenacin tablet according to claim 1 and 2, it is characterized in that: described disintegrating agent is pre-paying starch, consumption accounts for the 23.5-33.5%(w/w that is of whole weight).
4. imidafenacin tablet according to claim 1 and 2, it is characterized in that: described filler is selected from one or more of microcrystalline Cellulose, starch, lactose, sucrose, mannitol and anhydrous calcium phosphate.
5. imidafenacin tablet according to claim 1 and 2, it is characterized in that: described filler is microcrystalline Cellulose.
6. imidafenacin tablet according to claim 1 and 2, it is characterized in that: described lubricant is selected from one or more of magnesium stearate, Pulvis Talci, castor oil hydrogenated, stearic acid and Polyethylene Glycol.
7. preparation method of described imidafenacin tablet according to claim 1 and 2, it is characterized in that: comprise the steps: water-soluble polymer dissolves in solvent, add imidafenacin and make Uniform Dispersion or dissolving, mix with filler and disintegrating agent, wet granulation, 40 ℃ of-60 ℃ of dryings, direct compression after dried granule and the mix lubricant.
8. the preparation method of described imidafenacin tablet according to claim 7, it is characterized in that: described solvent is the aqueous solution of methanol, ethanol, dichloromethane or acetone.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201210585889.5A CN103054822B (en) | 2012-12-28 | 2012-12-28 | Imidafenacin tablet and preparation method thereof |
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| CN201210585889.5A CN103054822B (en) | 2012-12-28 | 2012-12-28 | Imidafenacin tablet and preparation method thereof |
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| CN103054822A true CN103054822A (en) | 2013-04-24 |
| CN103054822B CN103054822B (en) | 2014-03-26 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103479594A (en) * | 2013-09-29 | 2014-01-01 | 扬子江药业集团四川海蓉药业有限公司 | Imidafenacin film-coated tablet and preparation method thereof |
| CN104415034A (en) * | 2013-08-29 | 2015-03-18 | 天津药物研究院 | Imidafenacin pharmaceutical composition and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579393A (en) * | 2012-03-19 | 2012-07-18 | 北京德众万全药物技术开发有限公司 | Solid composition for improving content uniformity and dissolution rate of imidafenacin |
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- 2012-12-28 CN CN201210585889.5A patent/CN103054822B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579393A (en) * | 2012-03-19 | 2012-07-18 | 北京德众万全药物技术开发有限公司 | Solid composition for improving content uniformity and dissolution rate of imidafenacin |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104415034A (en) * | 2013-08-29 | 2015-03-18 | 天津药物研究院 | Imidafenacin pharmaceutical composition and preparation method thereof |
| CN104415034B (en) * | 2013-08-29 | 2018-03-02 | 天津药物研究院有限公司 | A kind of imidafenacin pharmaceutical composition and preparation method thereof |
| CN103479594A (en) * | 2013-09-29 | 2014-01-01 | 扬子江药业集团四川海蓉药业有限公司 | Imidafenacin film-coated tablet and preparation method thereof |
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| CN103054822B (en) | 2014-03-26 |
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