CN102895209B - Febuxostat tablet - Google Patents
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- CN102895209B CN102895209B CN 201210414080 CN201210414080A CN102895209B CN 102895209 B CN102895209 B CN 102895209B CN 201210414080 CN201210414080 CN 201210414080 CN 201210414080 A CN201210414080 A CN 201210414080A CN 102895209 B CN102895209 B CN 102895209B
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Abstract
The invention discloses a Febuxostat tablet. The Febuxostat tablet comprises a tablet core and a coating, wherein the tablet core comprises the following components in weight percentage: 5-30 percent of Febuxostat, 15-60 percent of filler, 1-20 percent of disintegrating agent, 0.1-5 percent of surface active agent, 0.1-8 percent of lubricant and a right amount of adhesive. According to the Febuxostat tablet, trough adopting the powerful disintegrating agent within a reasonable proportional region, and meanwhile, through jointly using the surface active agent, the poorly water-soluble drug Febuxostat dissolves out, and further, the dissolvability of the Febuxostat is increased, and the bioavailability of the Febuxostat is improved. Moreover, the Febuxostat tablet is simple in preparation method, controllable in quality and high in stability.
Description
Technical field
The present invention relates to field of medicaments, particularly relate to a kind of Febustat tablet.
Background technology
Gout be too much to reach kidney removing ability and descend owing to producing uric acid in body, the uric acid body accumulation, cause urate crystal in joint and each internal organs deposition.Uric acid does not have any physiological function in human body, under normal circumstances, the uric acid produced in body, 2/3 is discharged by kidney, and 1/3 of remainder is discharged from intestinal.In body, uric acid constantly generates and drains, so it maintains certain concentration in blood.Contained uric acid in every liter of blood of normal person, the male is below 0.42mmol, the women is no more than 0.357mmol.In the composition and decomposition process of purine, the participation of plurality of enzymes is arranged, due to 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 and reduce, and result all can cause hyperuricemia.As hyperuricemia excessive concentration time>0.44mmol/L), uric acid is deposited in joint, soft tissue, cartilage and 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, the mankind 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 increased 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 related symptoms.The generation of uric acid is relevant with purine metabolism in body, the purine metabolism process finally, hypoxanthine generates xanthine under the effect of xanthine oxidoreductase enzyme (XOR), more further generates uric acid.The activity that suppresses this enzyme can effectively reduce the generation of uric acid.Allopurinol has inhibitory action to XOR, is unique for suppressing the medicine of uricopoiesis clinically over 30 years, is the first-line treatment medicine of current gout.
Allopurinol is used for the treatment of chronic gout, be applicable to uricopoiesis too much, to uricosuric allergy, and the patient who is not suitable for using uricosuric, especially gouty nephropathy or uric acid renal calculus person are had to 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 be used 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, inhibitory action to the XO enzyme has high selectivity, can be simultaneously the XO of oxidized form and reduced form be produced to remarkable inhibitory action.Febustat is compared with current 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 is simple and easy to get, stripping is complete, stay-in-grade Febustat tablet.
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 appropriate.Febustat tablet prepared by the present invention, performance according to the Febustat medicine, by reasonably in proportion, adopting potent disintegrating agent, combine 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 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 appropriate binding agent according to weight percentage.In this Febustat tablet, various ingredients are controlled in this scope, more are conducive to active component Febustat stripping in 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 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 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 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 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, in above-mentioned Febustat tablet, coating calculates according to coat weight, 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 chloroform.
Simultaneously, a kind of preparation method of above-mentioned Febustat tablet also is provided in the present invention, comprise the following steps: (1), by filler and the surfactant mix homogeneously of Febustat, filler gross weight 30-40%, carries out micronizing, controls its mean diameter below 50 μ m; (2) will pulverize rear mixture and mix homogeneously with the disintegrating agent of residue filler, disintegrating agent gross weight 50-70%, add binding agent soft material processed, granulation, drying; (3) after granule after above-mentioned drying is arranged, add lubricant and residue disintegrating agent, mix homogeneously, tabletting obtains label; (4) label is put in coating pan, coating, obtain the Febustat tablet after 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, combines simultaneously and uses surfactant etc. to make the stripping of insoluble drug Febustat; Adopt the micronization mode in technique, increase the dissolubility of Febustat, improve its bioavailability.By prescription and the improvement of technique, 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, consist of the first filler and the second filler, and the first filler accounts for the 30-40% of filler gross weight; Disintegrating agent consists of the first disintegrating agent and the second disintegrating agent, and the first disintegrating agent accounts for the 50-70% of weight in described disintegrating agent; Now, the preparation process of Febustat tablet comprises: (1), by Febustat, the first filler and surfactant mix homogeneously, carries out micronizing, controls its mean diameter below 30 μ m; (2) will pulverize rear mixture and mix homogeneously with the second filler, the first disintegrating agent, add binding agent soft material processed, granulation, drying; (3) after granule after above-mentioned drying is arranged, add lubricant and the second disintegrating agent, mix homogeneously, tabletting obtains label; (4) label is put in coating pan, coating, obtain the Febustat tablet after drying.
The preparation method of Febustat tablet provided by the present invention, by adopting two kinds of different filleies and two kinds of different disintegrating agents, has improved the disintegration rate of this Febustat tablet, has improved its dissolubility and stability.
Preferably, in 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 dextrin; More preferably, the first filler is a kind of in lactose, pre-paying starch; The second filler is a kind of in calcium sulfate, microcrystalline Cellulose, mannitol or 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 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 CCMS-Na; The second disintegrating agent is a kind of in polyvinylpolypyrrolidone or low-substituted hydroxypropyl cellulose.
Surfactant is selected from a kind of, two or more the compositions in sodium lauryl sulphate, tween or span.
The label lubricant is selected from a kind of, two or more the compositions in micropowder silica gel, Pulvis Talci, magnesium stearate or 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.
More preferably, in the preparation method of above-mentioned Febustat tablet, in label, the first filler is microcrystalline Cellulose; 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:
Below in conjunction with specific embodiment 1-5, the present invention is described in detail, and embodiment provided by the present invention is only in order to help understanding technical scheme provided by the present invention, 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.
The formula that will provide according to embodiment 1-5 is made respectively 1000, in each embodiment 6 of samplings respectively at 5min, 10min, 20min, 30min, 45min, within 60 minutes, test the dissolution of this Febustat tablet, and prepare the dissolution spectrogram.
Embodiment mono-:
Core formulation:
Binding agent
Coating fluid prescription
Preparation technology:
1, will after the Febustat of recipe quantity, lactose and sodium lauryl sulphate mix homogeneously, with super micron mill, be pulverized, controlled mean diameter below 50 μ m;
2, after the mixture after pulverizing and recipe quantity microcrystalline Cellulose, 10g carboxymethylstach sodium mix homogeneously, add binding agent 8% starch slurry soft material processed, cross 18 mesh sieves, make wet granular;
3, wet granular is placed in to drying baker, 50～60 ℃ of forced air dryings are dried;
4, dry granule is crossed to 18 mesh sieve granulate, added recipe quantity lubricant and remaining carboxymethylstach sodium, after mix homogeneously, tabletting obtains label;
5, with Opadry alcoholic solution coating, the coating weightening finish is about 3%, after coating, is drying to obtain.
6, the gained tablet is carried out to the dissolution investigation, experimental result is in 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, will after the Febustat of recipe quantity, pre-paying starch and tween mix homogeneously, with super micron mill, be pulverized, controlled mean diameter below 30 μ m;
2, after the mixture after pulverizing and recipe quantity microcrystalline Cellulose, 10g carboxymethylstach sodium/mix homogeneously, add binding agent 8% starch slurry soft material processed, cross 18 mesh sieves, make wet granular;
3, wet granular is placed in to drying baker, 50～60 ℃ of forced air dryings are dried;
4, dry granule is crossed to 18 mesh sieve granulate, added recipe quantity lubricant and remaining carboxymethylstach sodium, after mix homogeneously, tabletting obtains label;
5, with Opadry alcoholic solution coating, the coating weightening finish is about 3%, after coating, is drying to obtain.6, the gained tablet is carried out to the dissolution investigation, experimental result is in 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, will after the Febustat of recipe quantity, lactose and sodium lauryl sulphate mix homogeneously, with super micron mill, be pulverized, controlled mean diameter below 30 μ m;
2, after the mixture after pulverizing and recipe quantity microcrystalline Cellulose, 10g carboxymethylstach sodium mix homogeneously, add binding agent 8% starch slurry soft material processed, cross 18 mesh sieves, make wet granular;
3, wet granular is placed in to drying baker, 50～60 ℃ of forced air dryings are dried;
4, dry granule is crossed to 18 mesh sieve granulate, added recipe quantity lubricant and remaining carboxymethylstach sodium, after mix homogeneously, tabletting obtains label;
5, with Opadry alcoholic solution coating, the coating weightening finish is about 3%, after coating, is drying to obtain.
6, the gained tablet is carried out to the dissolution investigation, experimental result is in 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, will after the Febustat of recipe quantity, lactose and sodium lauryl sulphate mix homogeneously, with super micron mill, be pulverized, controlled mean diameter below 50 μ m;
2, after the mixture after pulverizing and recipe quantity microcrystalline Cellulose, 10g carboxymethylstach sodium/mix homogeneously, add binding agent 8% starch slurry soft material processed, cross 18 mesh sieves, make wet granular;
3, wet granular is placed in to drying baker, 50～60 ℃ of forced air dryings are dried; 4, dry granule is crossed to 18 mesh sieve granulate, added recipe quantity lubricant and low-substituted hydroxypropyl cellulose, after mix homogeneously, tabletting obtains label;
5, with Opadry alcoholic solution coating, the coating weightening finish is about 3%, after coating, is drying to obtain.
6, the gained tablet is carried out to the dissolution investigation, experimental result is in 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 |
| 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 after the Febustat of recipe quantity, 35% lactose and sodium lauryl sulphate mix homogeneously, with super micron mill, be pulverized, controlled mean diameter below 50 μ m;
2, after the mixture after pulverizing and remaining lactose, low-substituted hydroxypropyl cellulose mix homogeneously, add binding agent 8% starch slurry soft material processed, cross 18 mesh sieves, make wet granular;
3, wet granular is placed in to drying baker, 50～60 ℃ of forced air dryings are dried;
4, dry granule is crossed to 18 mesh sieve granulate, added recipe quantity lubricant and carboxymethylstach sodium, after mix homogeneously, tabletting obtains label;
5, with Opadry alcoholic solution coating, the coating weightening finish is about 3%, after coating, is drying to obtain.
6, the gained tablet is carried out to the dissolution investigation, experimental result is in 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 |
In above-mentioned table 1-table 5, the test data result is known, the Febustat tablet that embodiment of the present invention 1-5 provides there is extraordinary dissolution, apparently higher than the market product.
Below will further to Febustat provided by the present invention, carry out medicine stability test by the medicine stability of Febustat provided by the present invention in order further to prove.
The Febustat tablet that embodiment of the present invention 1-5 provides all there is stability preferably, 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:
Medicine stability test: (1) sample thief, respectively at placing under 60 ℃ of high temperature, 40 ℃, RH75%, RH92.5% and intensity of illumination 4500Lx ± 500Lx condition, respectively at sampling in 5 days, 10 days, detect, and compared with 0 day, result of the test is in Table 7.
Table 7 Febustat sheet influence factor result of the test
(2) sample thief, press commercially available back, under the condition of 40 ℃ ± 2 ℃ of temperature, RH75% ± 5%, places 6 months.Sample once and detected respectively 1st month, 2 months, 3 months, 6 the end of month, and compare with 0 month result, result of the test is in Table 8.
Table 8 Febustat sheet accelerated test result
(3) sample thief is placed 6 months under the condition of 25 ℃ ± 2 ℃ of temperature, RH60% ± 10%.Sampling in every 3 months 1 time, detected respectively at sampling in 0 month, 3 months, 6 months, 9 months, 12 months, and, by result and comparison in 0 month, result of the test is in Table 9.
The table 9 Febustat sheet room temperature result of the test that keeps sample
From above-mentioned test data result, tablet in the present invention in influence factor, acceleration and long-term stable experiment process dissolution, content and related substance inspection with within 0 day, compare and have no significant change.Thereby absolutely prove the superiority of the prepared Febustat sheet of Febustat sheet provided by the present invention and preparation method thereof aspect raising stability.Conclusion, Febustat tablet provided by the present invention, by reasonably in proportion, adopting potent disintegrating agent, is combined simultaneously and is used surfactant to make the stripping of insoluble drug Febustat, and then increase the dissolubility of Febustat, 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, adopt the micronization mode in technique, increase the dissolubility of Febustat, improve its bioavailability.By prescription and the improvement of technique, significantly improved effective ingredient, the dissolution of insoluble drug Febustat, thus the bioavailability that has improved medicine improves curative effect.
The foregoing is only the preferred embodiments of the present invention, be not limited to the present invention, 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., within all should being included in protection scope of the present invention.
Claims (5)
1. a Febustat tablet, comprise label and coating, it is characterized in that, described label comprises following component according to weight percentage:
Febustat 5%-30%
Filler 15%-80%
Disintegrating agent 1%-20%
Surfactant 0.1%-5%
Lubricant 0.1%-8%
Binding agent is appropriate,
Described filler is two kinds, comprises the first filler and the second filler; Described the first filler accounts for the 30-40% of described filler gross weight;
Described the first filler is a kind of in lactose or pregelatinized Starch;
Described the second filler is a kind of in microcrystalline Cellulose, calcium sulfate, mannitol or dextrin;
Described disintegrating agent is two kinds, comprises the first disintegrating agent and the second disintegrating agent; Described the first disintegrating agent accounts for the 50-70% of weight in described disintegrating agent;
Described the first disintegrating agent is a kind of in carboxymethylstach sodium, sodium carboxymethyl cellulose, cross-linking sodium carboxymethyl cellulose, CCMS-Na;
Described the second disintegrating agent is a kind of in polyvinylpolypyrrolidone or low-substituted hydroxypropyl cellulose;
Described surfactant is one or two or more kinds the compositions in sodium lauryl sulphate, tween or span;
Described label lubricant is one or two or more kinds the compositions in micropowder silica gel, Pulvis Talci, magnesium stearate or sodium stearyl fumarate;
One or two or more kinds mixture that described binding agent is water, ethanol, hydroxypropyl emthylcellulose, ethyl cellulose, polyvidone or starch,
The preparation process of described Febustat tablet is as follows:
(1) by Febustat, the first filler and surfactant mix homogeneously, carry out micronizing, control its mean diameter below 30 μ m;
(2) will pulverize rear mixture and mix homogeneously with the second filler, the first disintegrating agent, add binding agent soft material processed, granulation, drying;
(3) after granule after above-mentioned drying is arranged, add lubricant and the second disintegrating agent, mix homogeneously, tabletting obtains label;
(4) label is put in coating pan, coating, obtain the Febustat tablet after drying.
2. Febustat tablet according to claim 1, is characterized in that, described label comprises following component according to weight percentage:
Febustat 10%-25%
Filler 30%-65%
Disintegrating agent 5%-15%
Surfactant 0.5%-3%
Lubricant 0.5%-5%
Binding agent is appropriate.
3. Febustat tablet according to claim 2, is characterized in that, described coating comprises following component according to weight percentage:
Water solublity coating material 5%-20%
Coating solvent 80%-95%.
4. Febustat tablet according to claim 3, is characterized in that, in described coating:
Described water solublity coating material is polyvinylpyrrolidone or Opadry;
Described coating solvent is one or two or more kinds the compositions in water, ethanol, acetone or chloroform.
5. Febustat tablet according to claim 4, 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;
The mixture that described binding agent is polyvidone and water.
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| CN 201110419209 Division CN102488665B (en) | 2011-12-15 | 2011-12-15 | Febuxostat tablet and preparation method thereof |
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| CN103271900B (en) * | 2013-05-31 | 2014-12-17 | 河南创新药业有限公司 | Zinc citrate tablet and preparation method thereof |
| CN103893131B (en) * | 2014-04-17 | 2016-01-13 | 李宝齐 | A kind of solid composite medicament containing Febustat |
| 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 |
| 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 |
| 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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|---|---|---|---|---|
| CN101862326A (en) * | 2009-04-20 | 2010-10-20 | 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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2011
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101862326A (en) * | 2009-04-20 | 2010-10-20 | 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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| CN102895209A (en) | 2013-01-30 |
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Address after: 750002 the Ningxia Hui Autonomous Region street, Jinfeng District, Yinchuan City Fu Ning Lane No. 57 Patentee after: Ningxia Kang Ya pharmaceutical Limited by Share Ltd Address before: 750002 No. 6 road, hi tech Industrial Development Zone, the Ningxia Hui Autonomous Region, Yinchuan Patentee before: Kangya Pharmaceutical Industry Co., Ltd., Ningxia |