CN102488665B - Febuxostat tablet and preparation method thereof - Google Patents
Febuxostat tablet and preparation method thereof Download PDFInfo
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- CN102488665B CN102488665B CN 201110419209 CN201110419209A CN102488665B CN 102488665 B CN102488665 B CN 102488665B CN 201110419209 CN201110419209 CN 201110419209 CN 201110419209 A CN201110419209 A CN 201110419209A CN 102488665 B CN102488665 B CN 102488665B
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Abstract
The invention discloses a febuxostat tablet and a preparation method thereof. The febuxostat tablet comprises a tablet core and a coating, the tablet core comprises the following compositions: by weight percentage, from 5% to 30% of febuxostat, from 15% to 60% of filler, from 1% to 20% of disintegrating agent, from 0.1% to 5% of surfactant, from 0.1% to 8% of lubricating agent and a defined amount of adhesive. The febuxostat tablet adopts the high-efficient disintegrating agent within a reasonable proportion range, simultaneously, the febuxostat which is difficultly soluble medicine is dissolved by the aid of the surfactant and the high-efficient disintegrating agent, so that solubility of the febuxostat is improved, and bioavailability of the febuxostat is increased. In addition, the preparation method for the febuxostat tablet is simple, and is controllable in quality and fine in stability.
Description
Technical field
The present invention relates to field of medicaments, particularly relate to a kind of Febustat tablet and preparation method thereof.
Background technology
Gout be that the uric acid body accumulation causes urate crystal in the joint and each internal organs deposition owing to producing uric acid in the body and too much reach kidney removing ability and descend.Uric acid does not have any physiological function in human body, under normal circumstances, the uric acid that produces in the body, 2/3 is discharged by kidney, and remaining 1/3 discharges from intestinal.Uric acid constantly generates and drains in the body, so it keeps certain concentration in blood.Contained uric acid in every liter of blood of normal person, the male is below the 0.42mmol, the women then is no more than 0.357mmol.In the composition and decomposition process of purine, the participation of plurality of enzymes is arranged, because the birth defect of enzyme or the factor that some is not yet clear and definite, metabolism gets muddled, and makes the synthetic increase of uric acid or discharges minimizing, the result all can cause hyperuricemia.When the hyperuricemia excessive concentration＞0.44mmol/L), uric acid namely is deposited in joint, soft tissue, cartilage and the kidney with the form of sodium salt, causes the foreign body inflammatory reaction of tissue, has become to cause the seed of trouble of gout.
Along with the prolongation of the change of the improving constantly of people's living standard, dietary structure and living habit (food that is rich in nucleoprotein increases), average life, human to the understanding of gout and the raising of diagnostic level, no matter be in American-European countries or in countries in Asia, the prevalence of gout has the trend that increases year by year, and the prevalence of China's hyperuricemia and gout is ascendant trend linearly especially.The prevalence of American-European hyperuricemia is up to 2%～18%; The prevalence of the adult hyperuricemia of China Taiwan more than 30 years old is 17.3%.China more than 20 years old the crowd approximately 2.4%～5.7% have the too high situation of blood uric acid; There were significant differences for the prevalence of age groups hyperuricemia, and old people's prevalence of hyperuricemia can be up to more than 24%; The total prevalence of all age bracket gouts is about 0.84%.
The means of at present treatment of gout being taked usually are to promote urate excretion and suppress uricopoiesis, and adopt adequate measure to improve relevant symptoms.The generation of uric acid is relevant with purine metabolism in the body, the purine metabolism process at last, hypoxanthine generates xanthine under the effect of xanthine oxidoreductase enzyme (XOR), further generate uric acid again.The activity that suppresses this enzyme can effectively reduce the generation of uric acid.Allopurinol has inhibitory action to XOR, is unique medicine for suppressing uricopoiesis clinically over 30 years, is the first-line treatment medicine of present gout.
Allopurinol is used for the treatment of chronic gout, be applicable to uricopoiesis too much, irritated to uricosuric, and the patient who is not suitable for using uricosuric, especially gouty nephropathy or uric acid renal calculus person had good effect, being the medicine that the level that onlyly before this can effectively reduce uricopoiesis, reduce blood and urine uric acid is treated primary gout, is the gold medicine for the treatment of gout.But because allopurinol has certain infringement to liver, therefore liverish gout patients generally should not use this medicine.In addition, allopurinol can cause the bone marrow infringement and produce leukopenia a few patients.Therefore the untoward reaction of allopurinol is more.
Febustat is a novel xanthine oxidase (XO) inhibitor over nearly 40 years, it is the XO inhibitor of first non-purine type, effect has high selectivity to the XO enzymeinhibition, can be simultaneously the XO of oxidized form and reduced form be produced remarkable inhibitory action.Febustat is compared with present gout gold medicine allopurinol, has stronger pharmacologically active, and higher effect selectivity shows better curative effect and good safety in clinical.Therefore, Febustat is a kind of newtype drug that more can safe and effective treatment hyperuricemia, extremely has clinical meaning.
But because the dissolubility of Febustat itself is less, there are the problems such as the poor and bioavailability of dissolution is not high in the common oral solid formulation that contains this active component, medicinal effects in Febustat in a lot of situations does not reach desirable requirement, this has just caused the medicinal content of Febustat higher, and the undesirable problem of effect.
Summary of the invention
The objective of the invention is to overcome the deficiencies in the prior art, provide that a kind of prescription composition is few, adjuvant be simple and easy to, complete, the stay-in-grade Febustat tablet of stripping.
For this reason, a kind of Febustat tablet is provided in the present invention, this Febustat tablet comprises label and coating, and label comprises following component according to weight percentage: Febustat 5%-30%, filler 15%-60%, disintegrating agent 1%-20%, surfactant 0.1%-5%, lubricant 0.1%-8%, binding agent are an amount of.The Febustat tablet of the present invention's preparation, performance according to the Febustat medicine, by reasonably adopting potent disintegrating agent in the proportion, unite simultaneously and use surfactant and other adjuvant to make the stripping of insoluble drug Febustat, and then the dissolubility of increase Febustat, improve its bioavailability.
Those skilled in the art are reading on the basis of the present invention, can access the suitable amounts of binding agent according to rational analysis, do not repeat them here.
Preferably, above-mentioned label comprises the Febustat of following component: 10%-25%, the filler of 30%-60%, the disintegrating agent of 5%-15%, the surfactant of 0.5%-3%, the lubricant of 0.5%-5% and an amount of binding agent according to weight percentage.Various ingredients are controlled in this scope in this Febustat tablet, more are conducive to active component Febustat stripping in the use procedure, and then increase the dissolubility of Febustat, improve its bioavailability.
Preferably, in the present invention operable filler includes but not limited to a kind of, two or more the compositions in lactose, microcrystalline Cellulose, calcium sulfate, pre-paying starch, mannitol or the dextrin.
Operable disintegrating agent includes but not limited to a kind of, two or more the compositions in sodium carboxymethyl cellulose, cross-linking sodium carboxymethyl cellulose, carboxymethylstach sodium, CCMS-Na, polyvinylpolypyrrolidone or the low-substituted hydroxypropyl cellulose in the present invention.
Operable surfactant includes but not limited to a kind of, two or more the compositions in sodium lauryl sulphate, tween or the span in the present invention.
Operable lubricant includes but not limited to a kind of, two or more the compositions in micropowder silica gel, Pulvis Talci, magnesium stearate or the sodium stearyl fumarate in the present invention.
Operable binding agent includes but not limited to a kind of, two or more mixture of water, ethanol, hydroxypropyl emthylcellulose, ethyl cellulose, polyvidone or starch in the present invention.
In a kind of concrete embodiment of the present invention, coating calculates according to coat weight in the above-mentioned Febustat tablet, comprises the water solublity coating material of following component: 5%-20%, the coating solvent of 80%-95%.Wherein the water solublity coating material includes but not limited to polyvinylpyrrolidone or Opadry; The coating solvent includes but not limited to a kind of, two or more the compositions in water, ethanol, acetone or the chloroform.
Simultaneously, a kind of preparation method of above-mentioned Febustat tablet also is provided in the present invention, may further comprise the steps: (1) carries out micronizing with filler and the surfactant mix homogeneously of Febustat, filler gross weight 30-40%, controls its mean diameter below 50 μ m; (2) will pulverize rear mixture and the disintegrating agent mix homogeneously that remains filler, disintegrating agent gross weight 50-70%, add binding agent soft material processed, granulation, drying; (3) with after the granule arrangement after the above-mentioned drying, add lubricant and residue disintegrating agent, mix homogeneously, tabletting namely get label; (4) label is put in the coating pan, coating namely gets the Febustat tablet after the drying.
The preparation method of Febustat tablet provided by the present invention has that technique is simple, quality controllable, the advantage such as have good stability, and it is by adopting potent disintegrating agent, unites simultaneously and uses surfactant etc. to make the stripping of insoluble drug Febustat; In technique, adopt the micronization mode, increase the dissolubility of Febustat, improve its bioavailability.Improvement by prescription and technique has significantly improved effective ingredient, the dissolution of insoluble drug Febustat, thus the bioavailability that has improved medicine improves curative effect.
Filler in the preparation method of above-mentioned Febustat tablet is made of the first filler and the second filler, and the first filler accounts for the 30-40% of filler gross weight; Disintegrating agent is made of the first disintegrating agent and the second disintegrating agent, and the first disintegrating agent accounts for the 50-70% of weight in the described disintegrating agent; At this moment, the preparation process of Febustat tablet comprises: (1) carries out micronizing with Febustat, the first filler and surfactant mix homogeneously, controls its mean diameter below 30 μ m; (2) will pulverize rear mixture and the second filler, the first disintegrating agent mix homogeneously, add binding agent soft material processed, granulation, drying; (3) with after the granule arrangement after the above-mentioned drying, add lubricant and the second disintegrating agent, mix homogeneously, tabletting namely get label; (4) label is put in the coating pan, coating namely gets the Febustat tablet after the drying.
The preparation method of Febustat tablet provided by the present invention has improved the disintegration rate of this Febustat tablet by adopting two kinds of different filleies and two kinds of different disintegrating agents, has improved its dissolubility and stability.
Preferably, in the above-mentioned label: the first filler and the second filler are selected from respectively a kind of in lactose, microcrystalline Cellulose, calcium sulfate, pre-paying starch, mannitol or the dextrin; More preferably, the first filler is a kind of in lactose, the pre-paying starch; The second filler is a kind of in calcium sulfate, microcrystalline Cellulose, mannitol or the dextrin.
Preferably, above-mentioned the first disintegrating agent and the second disintegrating agent are selected from respectively a kind of in sodium carboxymethyl cellulose, cross-linking sodium carboxymethyl cellulose, carboxymethylstach sodium, CCMS-Na, polyvinylpolypyrrolidone or the low-substituted hydroxypropyl cellulose; More preferably, the first disintegrating agent is a kind of in carboxymethylstach sodium, sodium carboxymethyl cellulose, cross-linking sodium carboxymethyl cellulose or the CCMS-Na; The second disintegrating agent is a kind of in polyvinylpolypyrrolidone or the low-substituted hydroxypropyl cellulose.
Surfactant is selected from a kind of, two or more the compositions in sodium lauryl sulphate, tween or the span.
The label lubricant is selected from a kind of, two or more the compositions in micropowder silica gel, Pulvis Talci, magnesium stearate or the sodium stearyl fumarate.
Binding agent is selected from a kind of, two or more mixture of water, ethanol, hydroxypropyl emthylcellulose, ethyl cellulose, polyvidone or starch.
Preferably, in the above-mentioned Febustat tablet, described the first filler is lactose; Described the second filler is microcrystalline Cellulose; Described the first disintegrating agent is carboxymethylstach sodium; Described the second disintegrating agent is low-substituted hydroxypropyl cellulose; Described surfactant is sodium lauryl sulphate; Described lubricant is the compositions of micropowder silica gel and magnesium stearate; Described binding agent is the mixture of polyvidone and water.
More preferably, in the preparation method of above-mentioned Febustat tablet, the first filler is microcrystalline Cellulose in the label; The second filler is pre-paying starch; Disintegrating agent is sodium carboxymethylstarch; Surfactant is sodium lauryl sulphate; Lubricant is the compositions of micropowder silica gel and magnesium stearate; Binding agent is polyvidone.
The specific embodiment:
The present invention is described in detail below in conjunction with specific embodiment 1-5, and embodiment provided by the present invention understands technical scheme provided by the present invention in order to help, and can not limit protection scope of the present invention; The multitude of different ways that the present invention can be defined by the claims and cover is implemented.
To make respectively 1000 according to the prescription that embodiment 1-5 provides, among each embodiment 6 of samplings respectively at 5min, 10min, 20min, 30min, 45min, tested the dissolution of this Febustat tablet in 60 minutes, and preparation dissolution spectrogram.
Embodiment one:
Core formulation:
Binding agent
Coating fluid prescription
Preparation technology:
1, pulverize with super micron mill behind Febustat, lactose and the sodium lauryl sulphate mix homogeneously with recipe quantity, the control mean diameter is below 50 μ m;
2, behind the mixture after will pulverizing and recipe quantity microcrystalline Cellulose, the 10g carboxymethylstach sodium mix homogeneously, add binding agent 8% starch slurry soft material processed, mistake 18 mesh sieves are made wet granular;
3, wet granular is placed drying baker, 50～60 ℃ of forced air drying oven dry;
4, dried granule is crossed 18 mesh sieve granulate, added recipe quantity lubricant and remaining carboxymethylstach sodium, behind the mix homogeneously, tabletting namely gets label;
5, with Opadry alcoholic solution coating, the coating weightening finish is about 3%, is drying to obtain behind the coating.
6, the gained tablet is carried out dissolution and investigate, experimental result sees Table 1.
The dissolution test result of table 1 example one
| Indicate cumulative release amount % | 5min | 10min | 20min | 30min | 45min | 60min |
| 1# | 82.80 | 95.79 | 98.05 | 98.66 | 98.82 | 99.87 |
| 2# | 82.20 | 96.69 | 98.81 | 100.33 | 99.30 | 98.85 |
| 3# | 83.96 | 94.74 | 99.41 | 99.74 | 101.56 | 100.38 |
| 4# | 83.25 | 96.70 | 100.18 | 99.16 | 99.62 | 100.83 |
| 5# | 83.25 | 95.64 | 101.37 | 100.21 | 99.33 | 99.63 |
| 6# | 82.65 | 96.09 | 99.71 | 99.29 | 99.90 | 99.91 |
| Mean | 83.00 | 95.94 | 99.59 | 99.56 | 99.76 | 99.91 |
Example two:
Core formulation
Binding agent
Coating fluid prescription:
Preparation technology
1, pulverize with super micron mill behind Febustat, pre-paying starch and the tween mix homogeneously with recipe quantity, the control mean diameter is below 30 μ m;
2, behind the mixture after will pulverizing and recipe quantity microcrystalline Cellulose, the 10g carboxymethylstach sodium/mix homogeneously, add binding agent 8% starch slurry soft material processed, mistake 18 mesh sieves are made wet granular;
3, wet granular is placed drying baker, 50～60 ℃ of forced air drying oven dry;
4, dried granule is crossed 18 mesh sieve granulate, added recipe quantity lubricant and remaining carboxymethylstach sodium, behind the mix homogeneously, tabletting namely gets label;
5, with Opadry alcoholic solution coating, the coating weightening finish is about 3%, is drying to obtain behind the coating.
6, the gained tablet is carried out dissolution and investigate, experimental result sees Table 2.
The dissolution test result of table 2 example two
| Indicate cumulative release amount % | 5min | 10min | 20min | 30min | 45min | 60min |
| 1# | 81.45 | 91.55 | 94.82 | 95.55 | 97.33 | 98.22 |
| 2# | 82.20 | 88.54 | 92.68 | 97.01 | 97.15 | 98.64 |
| 3# | 80.84 | 90.19 | 93.29 | 96.27 | 98.66 | 98.36 |
| 4# | 81.75 | 90.65 | 94.06 | 94.63 | 97.91 | 99.11 |
| 5# | 83.25 | 89.61 | 95.12 | 96.16 | 99.15 | 99.46 |
| 6# | 82.80 | 91.11 | 96.04 | 94.67 | 98.25 | 98.39 |
| Mean | 82.05 | 90.27 | 94.33 | 95.71 | 98.08 | 98.70 |
Example three:
Core formulation:
Binding agent
Coating fluid prescription
Technique
1, pulverize with super micron mill behind Febustat, lactose and the sodium lauryl sulphate mix homogeneously with recipe quantity, the control mean diameter is below 30 μ m;
2, behind the mixture after will pulverizing and recipe quantity microcrystalline Cellulose, the 10g carboxymethylstach sodium mix homogeneously, add binding agent 8% starch slurry soft material processed, mistake 18 mesh sieves are made wet granular;
3, wet granular is placed drying baker, 50～60 ℃ of forced air drying oven dry;
4, dried granule is crossed 18 mesh sieve granulate, added recipe quantity lubricant and remaining carboxymethylstach sodium, behind the mix homogeneously, tabletting namely gets label;
5, with Opadry alcoholic solution coating, the coating weightening finish is about 3%, is drying to obtain behind the coating.
6, the gained tablet is carried out dissolution and investigate, experimental result sees Table 3.
The dissolution test result of table 3 example three
| Indicate cumulative release amount % | 5min | 10min | 20min | 30min | 45min | 60min |
| 1# | 82.80 | 98.19 | 99.89 | 99.44 | 98.98 | 101.88 |
| 2# | 84.17 | 98.60 | 101.22 | 102.32 | 100.82 | 101.74 |
| 3# | 80.84 | 99.01 | 100.41 | 98.89 | 100.11 | 100.10 |
| 4# | 81.26 | 97.19 | 99.64 | 100.26 | 99.04 | 97.95 |
| 5# | 86.78 | 94.34 | 100.13 | 98.77 | 99.83 | 98.90 |
| 6# | 90.31 | 93.92 | 98.78 | 100.47 | 101.40 | 99.57 |
| Mean | 84.36 | 96.87 | 100.01 | 100.03 | 100.03 | 100.02 |
Example four:
Core formulation:
Binding agent:
Coating fluid prescription
Preparation technology
1, pulverize with super micron mill behind Febustat, lactose and the sodium lauryl sulphate mix homogeneously with recipe quantity, the control mean diameter is below 50 μ m;
2, behind the mixture after will pulverizing and recipe quantity microcrystalline Cellulose, the 10g carboxymethylstach sodium/mix homogeneously, add binding agent 8% starch slurry soft material processed, mistake 18 mesh sieves are made wet granular;
3, wet granular is placed drying baker, 50～60 ℃ of forced air drying oven dry;
4, dried granule is crossed 18 mesh sieve granulate, added recipe quantity lubricant and low-substituted hydroxypropyl cellulose, behind the mix homogeneously, tabletting namely gets label;
5, with Opadry alcoholic solution coating, the coating weightening finish is about 3%, is drying to obtain behind the coating.
6, the gained tablet is carried out dissolution and investigate, experimental result sees Table 4.
The dissolution test result of table 4 example four
| Indicate cumulative release amount % | 5min | 10min | 20min | 30min | 45min | 60min |
| 1# | 85.30 | 97.32 | 99.30 | 99.62 | 102.67 | 100.12 |
| 2# | 83.63 | 96.54 | 99.53 | 100.51 | 100.23 | 101.45 |
| 3# | 84.84 | 97.92 | 100.82 | 101.01 | 101.34 | 100.29 |
[0096]
| 4# | 83.63 | 96.24 | 100.49 | 100.67 | 101.00 | 101.47 |
| 5# | 83.47 | 96.24 | 100.33 | 101.88 | 100.55 | 101.02 |
| 6# | 83.32 | 95.93 | 99.87 | 101.72 | 100.24 | 102.21 |
| Mean | 84.03 | 96.70 | 100.09 | 100.90 | 101.00 | 101.09 |
Example five:
Core formulation:
Binding agent
Coating fluid prescription:
Preparation technology
1, will pulverize with super micron mill behind the Febustat of recipe quantity, 35% lactose and the sodium lauryl sulphate mix homogeneously, the control mean diameter is below 50 μ m;
2, behind the mixture after will pulverizing and remaining lactose, the low-substituted hydroxypropyl cellulose mix homogeneously, add binding agent 8% starch slurry soft material processed, mistake 18 mesh sieves are made wet granular;
3, wet granular is placed drying baker, 50～60 ℃ of forced air drying oven dry;
4, dried granule is crossed 18 mesh sieve granulate, added recipe quantity lubricant and carboxymethylstach sodium, behind the mix homogeneously, tabletting namely gets label;
5, with Opadry alcoholic solution coating, the coating weightening finish is about 3%, is drying to obtain behind the coating.
6, the gained tablet is carried out dissolution and investigate, experimental result sees Table 5.
The dissolution test result of table 5 example five
| Indicate cumulative release amount % | 5min | 10min | 20min | 30min | 45min | 60min |
| 1# | 83.22 | 96.27 | 98.54 | 99.92 | 99.48 | 99.02 |
| 2# | 83.52 | 95.67 | 99.15 | 100.07 | 99.64 | 99.33 |
| 3# | 84.28 | 95.22 | 99.91 | 100.24 | 101.77 | 100.88 |
| 4# | 81.55 | 97.77 | 100.97 | 99.64 | 100.11 | 100.87 |
| 5# | 83.67 | 96.12 | 101.27 | 100.10 | 99.82 | 100.12 |
| 6# | 81.85 | 96.56 | 100.20 | 100.68 | 99.34 | 100.40 |
| Mean | 83.02 | 96.27 | 100.01 | 100.11 | 100.03 | 100.11 |
By test data result in the above-mentioned table 1-table 5 as can be known, the Febustat tablet that embodiment of the invention 1-5 provides have an extraordinary dissolution, apparently higher than the market product.
In order further to prove the medicine stability of Febustat provided by the present invention, below will further carry out medicine stability test to Febustat provided by the present invention.
All having of the Febustat tablet that embodiment of the invention 1-5 provides is stable preferably, and wherein, the effect data of embodiment 2-5 is better than embodiment 1.In order to save space, below only list the stability data of the prepared Febustat tablet of embodiment 1, concrete test method is as follows:
The medicine stability test:
(1) sample thief respectively at placing under 60 ℃ of high temperature, 40 ℃, RH75%, RH92.5% and the intensity of illumination 4500Lx ± 500Lx condition, respectively at sampling in 5 days, 10 days, detects, and compared with 0 day, and result of the test sees Table 7.
Table 7 Febustat sheet influence factor result of the test
(2) sample thief is pressed commercially available back, places 6 months under the condition of 40 ℃ ± 2 ℃ of temperature, RH75% ± 5%.Take a sample respectively 1st month, 2 months, 3 months, 6 the end of month and once to detect, and compare with 0 month result, result of the test sees Table 8.
Table 8 Febustat sheet accelerated test result
(3) sample thief was placed 6 months under the condition of 25 ℃ ± 2 ℃ of temperature, RH60% ± 10%.Sampling in per 3 months 1 time detects respectively at sampling in 0 month, 3 months, 6 months, 9 months, 12 months, and with result and comparison in 0 month, result of the test sees Table 9.
The table 9 Febustat sheet room temperature result of the test that keeps sample
By above-mentioned test data result as can be known, tablet in the present invention in influence factor, acceleration and long-term stable experiment process dissolution, content and related substance inspection with compared and had no significant change in 0 day.Thereby prove absolutely that the prepared Febustat sheet of Febustat sheet provided by the present invention and preparation method thereof is at the superiority that improves aspect stable.
Conclusion, Febustat tablet provided by the present invention is united simultaneously and is used surfactant to make the stripping of insoluble drug Febustat, and then increase the dissolubility of Febustat by reasonably adopting potent disintegrating agent in the proportion, improves its bioavailability.Simultaneously, the preparation method of Febustat tablet provided by the present invention have technique simple, quality controllable, have good stability, be applicable to suitability for industrialized production.Etc. advantage, in technique, adopt the micronization mode, increase the dissolubility of Febustat, improve its bioavailability.Improvement by prescription and technique has significantly improved effective ingredient, the dissolution of insoluble drug Febustat, thus the bioavailability that has improved medicine improves curative effect.
The above is the preferred embodiments of the present invention only, is not limited to the present invention, and for a person skilled in the art, the present invention can have various modifications and variations.Within the spirit and principles in the present invention all, any modification of doing, be equal to replacement, improvement etc., all should be included within protection scope of the present invention.
Claims (2)
1. a Febustat tablet comprises label and coating, it is characterized in that, described label comprises following component according to weight percentage:
Febustat 10%-25%
Filler 30%-60%
Disintegrating agent 5%-15%
Surfactant 0.5%-3%
Lubricant 0.5%-5%
Binding agent is an amount of,
Wherein said filler is made of the first filler and the second filler, and described the first filler accounts for the 30-40% of described filler gross weight;
Described the first filler is a kind of in lactose, the pre-paying starch; The second filler is a kind of in calcium sulfate, microcrystalline Cellulose, mannitol or the dextrin;
Described disintegrating agent is made of the first disintegrating agent and the second disintegrating agent; Described the first disintegrating agent accounts for the 50-70% of weight in the described disintegrating agent;
Described the first disintegrating agent is a kind of in carboxymethylstach sodium, sodium carboxymethyl cellulose, cross-linking sodium carboxymethyl cellulose or the CCMS-Na; The second disintegrating agent is a kind of in polyvinylpolypyrrolidone or the low-substituted hydroxypropyl cellulose;
Described surfactant is a kind of, two or more the compositions in sodium lauryl sulphate, tween or the span.
2. Febustat tablet according to claim 1 is characterized in that, in the described label:
Described lubricant is a kind of, two or more the compositions in micropowder silica gel, Pulvis Talci, magnesium stearate or the sodium stearyl fumarate;
Described binding agent is a kind of, two or more mixture of water, ethanol, hydroxypropyl emthylcellulose, ethyl cellulose, polyvidone or starch.
3. Febustat tablet according to claim 2 is characterized in that,
Described the first filler is lactose;
Described the second filler is microcrystalline Cellulose;
Described the first disintegrating agent is carboxymethylstach sodium;
Described the second disintegrating agent is low-substituted hydroxypropyl cellulose;
Described surfactant is sodium lauryl sulphate;
Described lubricant is the compositions of micropowder silica gel and magnesium stearate;
Described binding agent is the mixture of polyvidone and water.
4. Febustat tablet according to claim 3 is characterized in that, described coating comprises following component according to weight percentage:
Water solublity coating material 5%-20%
Coating solvent 80%-95%.
5. Febustat tablet according to claim 4 is characterized in that, in the described coating:
Described water solublity coating material is polyvinylpyrrolidone or Opadry;
Described coating solvent is a kind of, two or more the compositions in water, ethanol, acetone or the chloroform.
6. the preparation method of each described Febustat tablet is characterized in that according to claim 1-5,
(1) with Febustat, the first filler and surfactant mix homogeneously, carries out micronizing, control its mean diameter below 30 μ m;
(2) will pulverize rear mixture and the second filler, the first disintegrating agent mix homogeneously, add binding agent soft material processed, granulation, drying;
(3) with after the granule arrangement after the above-mentioned drying, add lubricant and the second disintegrating agent, mix homogeneously, tabletting namely get label;
(4) label is put in the coating pan, coating namely gets the Febustat tablet after the drying.
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| CN 201110419209 CN102488665B (en) | 2011-12-15 | 2011-12-15 | Febuxostat tablet and preparation method thereof |
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| CN 201110419209 CN102488665B (en) | 2011-12-15 | 2011-12-15 | Febuxostat tablet and preparation method thereof |
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| CN 201210414080 Division CN102895209B (en) | 2011-12-15 | 2011-12-15 | Febuxostat tablet |
| CN201210414112.2A Division CN102895210B (en) | 2011-12-15 | 2011-12-15 | Febuxostat tablet with improved dissolution rate |
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| CN102488665B true CN102488665B (en) | 2013-03-06 |
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| CN102988326B (en) * | 2012-12-14 | 2016-01-20 | 贵州信邦制药股份有限公司 | A kind of febuxostat tablet and preparation method thereof and detection method |
| CN103393617B (en) * | 2013-08-16 | 2015-11-04 | 四川峨嵋山药业股份有限公司 | Febustat tablet and preparation method thereof |
| CN104042577B (en) * | 2014-06-13 | 2016-08-24 | 安徽省逸欣铭医药科技有限公司 | A kind of stable Topiroxostat tablet and preparation method thereof |
| CN107019679A (en) * | 2017-03-27 | 2017-08-08 | 北京万全德众医药生物技术有限公司 | A kind of eplerenone tablet and preparation method thereof |
| CN107982259A (en) * | 2017-12-11 | 2018-05-04 | 佛山市腾瑞医药科技有限公司 | A kind of Febustat preparation and its application |
| CN109044983A (en) * | 2018-09-26 | 2018-12-21 | 南京海纳医药科技股份有限公司 | A kind of tablet and preparation method thereof containing Febustat |
| CN111419814B (en) * | 2020-04-22 | 2020-12-08 | 一力制药(罗定)有限公司 | Febuxostat tablet and preparation process thereof |
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| CN101862326B (en) * | 2009-04-20 | 2013-12-04 | 北京德众万全药物技术开发有限公司 | Medicine compound containing febuxostat |
| CN101953814A (en) * | 2009-07-17 | 2011-01-26 | 北京本草天源药物研究院 | Febuxostat solid preparation |
| CN101966163A (en) * | 2010-10-27 | 2011-02-09 | 江苏万邦生化医药股份有限公司 | Febuxostat dispersible tablet and preparation method thereof |
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