CN107648229B - A kind of Febustat composition - Google Patents
A kind of Febustat composition Download PDFInfo
- Publication number
- CN107648229B CN107648229B CN201710848020.8A CN201710848020A CN107648229B CN 107648229 B CN107648229 B CN 107648229B CN 201710848020 A CN201710848020 A CN 201710848020A CN 107648229 B CN107648229 B CN 107648229B
- Authority
- CN
- China
- Prior art keywords
- febustat
- unit dose
- glucosamine
- composition according
- lactose
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7008—Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
Abstract
The present invention relates to a kind of Febustat composition and its manufacturing methods, belong to pharmaceutical technology field.The technical scheme is that a kind of Febustat composition, in each unit dose, contain Febustat 10-40mg, Glucosamine 240-600mg.The side effect of Febustat is reduced on the basis of guaranteeing curative effect by reasonable compatibility；By reasonable preparation method, the characteristic of Febustat piece is changed, while guaranteeing its dissolution rate, obtains the stable tablet of the resistance to moisture absorption.
Description
Technical field
The present invention relates to a kind of Febustat compositions and preparation method thereof, belong to pharmaceutical technology field.
Background technique
Gout is disease caused by a kind of metabolic system dysfunction, is increased with uric acid as one of distinctive marks.It is several recently
Nian Lai, with the improvement of the quality of life, the number and disease incidence of patient with gout have the tendency that gradually increasing.Especially in
For the elderly, this has been a kind of relatively conventional metabolic disease.The joint of morbidity will appear swelling, stiff, lopsided, just
The first sample of image-stone, asymmetric, size is also inconsistent.The places such as it is more common between ear profile, toe, finger, patient suffering is abnormal,
Serious person's action is limited.Ventilation patient needs long-term administration.
Febustat is xanthine oxidase (XO) inhibitor, suitable for the long-term of the hyperuricemia with gout symptom
Treatment.It is the preferably anti-ventilation drug of clinical use effect in recent years, but long-term administration can cause certain damage, table to liver
It is the raising of total bilirubin and glutamic-pyruvic transaminase in present index.
Summary of the invention
Goal of the invention: the object of the present invention is to provide a kind of Febustat compositions, while providing treatment for patient,
Lower the side effect of Febustat.
Present inventors have surprisingly found that a certain amount of Glucosamine is added in Febustat composition, treatment ventilation
Effect increase, meanwhile, the side effect of liver is also reduced.
Technical solution
The technical scheme is that a kind of Febustat composition, in each unit dose, contain Febustat 10-
40mg, Glucosamine 240-600mg.
Glucosamine: is extracted by natural shrimp and crab shells, and cartilage cell can be activated to synthesize polysaccharide and collagenous fibres,
Cartilage matrix is generated, repairing articular cartilage expedites the emergence of knuckle synovia.After the 1970s, American-European, Japan and other countries are risen
" ammonia sugar " therapy, as the preferred specific drug for the treatment of osteoarthritis, ammonia sugar is widely used in the treatment of bone and joint diseases
With prevention, significant effect is achieved.European ammonia sugar be medical field uniquely approve to bone and joint diseases have therapeutic effect
Nutrient and healthcare products.
The present composition, dosage form can be tablet or capsule.Instructions of taking is daily Fei Busi one time a day
His amount is 30-40mg.
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
10-30mg, Glucosamine 240-400mg.
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
10mg, Glucosamine 240mg.
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
30mg, Glucosamine 400mg.
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
15mg, Glucosamine 360mg.
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
20mg, Glucosamine 360mg.
The auxiliary material of the present composition can be the auxiliary material of common dosage forms, such as: crospovidone, cross-linked carboxymethyl cellulose
Sodium, lactose, hydroxymethyl cellulose, polyethylene pyrrole network alkanone etc..
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
10-30mg, Glucosamine 240-400mg, hydroxypropyl-β-cyclodextrin 10-30mg, lactose 10-30mg, microcrystalline cellulose 10-
30mg, povidone k30 10-20mg, lauryl sodium sulfate 1-3mg, magnesium stearate 4-8mg.
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
10mg, Glucosamine 240mg, hydroxypropyl-β-cyclodextrin 10mg, lactose 10mg, microcrystalline cellulose 10mg, povidone k30
10mg, lauryl sodium sulfate 1mg, magnesium stearate 4mg.
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
40mg, Glucosamine 600mg, hydroxypropyl-β-cyclodextrin 30mg, lactose 30mg, microcrystalline cellulose 30mg, povidone k30
20mg, lauryl sodium sulfate 3mg, magnesium stearate 8mg.
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
10mg, Glucosamine 240mg.Hydroxypropyl-β-cyclodextrin 20mg, lactose 15mg, microcrystalline cellulose 15mg, povidone k30
12mg, lauryl sodium sulfate 1.5mg, magnesium stearate 4.5mg.
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
30mg, Glucosamine 400mg.Hydroxypropyl-β-cyclodextrin 15mg, lactose 20mg, microcrystalline cellulose 18mg, povidone k30
15mg, lauryl sodium sulfate 2mg, magnesium stearate 5mg.
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
15mg, Glucosamine 360mg.Hydroxypropyl-β-cyclodextrin 16mg, lactose 18mg, microcrystalline cellulose 16mg, povidone k30
13mg, lauryl sodium sulfate 1.8mg, magnesium stearate 4.7mg.
The preferential technical solution of the present invention is: a kind of Febustat composition, in each unit dose, contains Febustat
20mg, Glucosamine 360mg.Hydroxypropyl-β-cyclodextrin 16mg, lactose 19mg, microcrystalline cellulose 23mg, povidone k30
17mg, lauryl sodium sulfate 2.3mg, magnesium stearate 5.6mg.
The preparation method of the present composition, the preparation method of Febustat of the present invention, comprising the following steps:
First step Febustat crosses 200 meshes, and Glucosamine and other auxiliary materials sieve with 100 mesh sieve.
Second step weigh the Febustat after the sieving of recipe quantity, Glucosamine, hydroxypropyl-β-cyclodextrin, three/
The lauryl sodium sulfate of the lactose of one recipe quantity, recipe quantity is uniformly mixed, with the povidone k30 water of half recipe quantity
Solution makees adhesive, granulation.
Third step dries particle obtained by second step, crushes, and crosses 40 meshes.
Particle obtained by 4th step third step, with the lactose of 2/3rds recipe quantities, be uniformly mixed, with half prescription
The povidone k30 aqueous solution of amount makees adhesive, pelletizes, and dries, and crushes, and crosses 40 meshes.
Particle obtained by the 4th step of 5th step mixes, tabletting or encapsulated with the magnesium stearate of recipe quantity.
The utility model has the advantages that reducing the side effect of Febustat on the basis of guaranteeing curative effect by reasonable compatibility；It is logical
Reasonable preparation method is crossed, the characteristic of Febustat piece is changed, while guaranteeing its dissolution rate, obtains the steady of the resistance to moisture absorption
Stator agent.
Embodiment 1, Febustat 10g, Glucosamine 240g, hydroxypropyl-β-cyclodextrin 10g, lactose 10g, crystallite are fine
Tie up element 10g, povidone k30 1mg, lauryl sodium sulfate 1g, magnesium stearate 4g.It is prepared by preparation method described in technical solution
1000.
Embodiment 2, Febustat 40g, Glucosamine 600g, hydroxypropyl-β-cyclodextrin 30g, lactose 30g, crystallite are fine
Tie up element 30g, povidone k30 2mg, lauryl sodium sulfate 3g, magnesium stearate 8g.It is prepared by preparation method described in technical solution
1000.
Embodiment 3, Febustat 10g, Glucosamine 240g.Hydroxypropyl-β-cyclodextrin 20g, lactose 15g, crystallite are fine
Tie up element 15g, povidone k30 12g, lauryl sodium sulfate 1.5g, magnesium stearate 4.5g.By preparation method described in technical solution
Preparation 1000.
Embodiment 4, Febustat 30g, Glucosamine 400g.Hydroxypropyl-β-cyclodextrin 15g, lactose 20g, crystallite are fine
Tie up element 18g, povidone k30 15g, lauryl sodium sulfate 2g, magnesium stearate 5g.It is prepared by preparation method described in technical solution
1000.
Embodiment 5, Febustat 15g, Glucosamine 360g.Hydroxypropyl-β-cyclodextrin 16g, lactose 18g, crystallite are fine
Tie up element 16g, povidone k30 13g, lauryl sodium sulfate 1.8g, magnesium stearate 4.7g.By preparation method described in technical solution
Preparation 1000.
Embodiment 6, Febustat 20g, Glucosamine 360g.Hydroxypropyl-β-cyclodextrin 16g, lactose 19g, crystallite are fine
Tie up element 23g, povidone k30 17g, lauryl sodium sulfate 2.3g, magnesium stearate 5.6g.By preparation method described in technical solution
Prepare capsule 1000.
Reference examples 1,
The prescription of embodiment 5, Febustat cross 200 meshes, and Glucosamine is sieved with 100 mesh sieve with other auxiliary materials.By following
Method preparation:
Febustat, Glucosamine, hydroxypropyl-β-cyclodextrin, the lactose of recipe quantity, microcrystalline cellulose, cornstarch,
Lauryl sodium sulfate is uniformly mixed, and makees adhesive with povidone k30 aqueous solution, is pelletized, and drying is made of magnesium stearate and lubricated
Agent prepares 1000.
The prescription of reference examples 2, embodiment 5 replaces hydroxypropyl-β-cyclodextrin with 16g lactose, and such words lactose dosage is total
For 34g, other supplementary product consumptions and preparation method are same as Example 5.
Test example 1, dissolution measurement
Measure the dissolution situation of reference examples and embodiment.Dissolution experiment specific implementation method: paddle method 50r/min,
900mLpH5.5Mcllvaine buffer is as dissolution medium, respectively in 15min and 60min sample detection.Detection method: it adopts
It is measured with high performance liquid chromatography.
Dissolution measurement result such as the following table 1 of reference examples and embodiment:
Table 1
| Sample time | Reference examples 1 | Reference examples 2 | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Embodiment 6 |
| 15min | 41.3% | 71.6% | 84.6% | 82.9% | 80.7% | 83.4% | 84.2% | 83.7 |
| 60min | 58.2% | 74.2% | 100% | 98.6% | 97.9% | 98.4% | 98.6% | 99.1 |
Table 1 dissolves out as the result is shown: the dissolution result of embodiment 1-6 is apparently higher than reference examples 1 and 2, illustrates that the present invention is mentioning
High Febustat dissolution aspect produces beneficial effect
2 high humidity test of test example
Embodiment 1-6 sample and reference examples sample are respectively taken 20, opening is placed in constant humidity closed container, at 25 DEG C
Under the conditions of relative humidity 75% ± 5%, places 20 days, respectively at 0 day and the 20th day precise example weight, as a result remember
It records in table 2.
Table 2
| Reference examples 1 | Reference examples 2 | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Embodiment 6 | |
| 0 day weight, mg | 8890.1 | 8890.1 | 5720.2 | 14860.4 | 6360.3 | 10100.3 | 8890.1 | 9258.3 |
| 20 days weight, mg | 9423.5 | 9807.6 | 5926.1 | 15395.5 | 6544.7 | 10372.9 | 9059.0 | 9443.4 |
| Weight gain, mg | 533.4 | 917.5 | 205.9 | 535.1 | 184.4 | 272.6 | 168.9 | 185.1 |
| Water absorption rate % | 6.0 | 10.3 | 3.6 | 3.6 | 2.9 | 2.7 | 1.9 | 2.0 |
2 data of table illustrate sample water absorption rate of the embodiment of the present invention significantly lower than reference examples.
Patient with gout (illness history is in 2 years) 840 people for suffering from hyperuricemia are accepted in test example 3, outpatient service for medical treatment, are randomly divided into
7 groups, every group of 120 people, respectively original grind group and embodiment 1-6 group, take original respectively and grind 40mg Febustat piece and this hair
Bright embodiment 1-6 sample, once a day medication continuous medication 3 months, during which control the diet of purine-containing food.Test process
Table 3 is recorded in result.With the 3rd the end of month, continuous one week detection blood uric acid and liver function maintain serum uric acid level to be lower than 415 μ
Mol/L be it is effective, exceeded liver function index is abnormal.
Table 3
3 data of table explanation: product of the embodiment of the present invention alleviates Febustat while effectively treatment hyperuricemia
Damage to liver.
Claims (9)
1. a kind of Febustat composition, which is characterized in that in each unit dose, contain Febustat 10-40mg, amino Portugal
Grape sugar 240-600mg.
2. composition according to claim 1, which is characterized in that in each unit dose, containing Febustat 10-30mg,
Glucosamine 240-400mg.
3. composition according to claim 1, which is characterized in that in each unit dose, contain Febustat 10mg, amino
Glucose 240mg.
4. composition according to claim 1, which is characterized in that in each unit dose, contain Febustat 30mg, amino
Glucose 400mg.
5. composition according to claim 1, which is characterized in that in each unit dose, contain Febustat 15mg, amino
Glucose 360mg.
6. composition according to claim 1, which is characterized in that in each unit dose, contain Febustat 20mg, amino
Glucose 360mg.
7. composition according to claim 1, which is characterized in that in each unit dose, containing Febustat 10-20mg,
Glucosamine 240-400mg, hydroxypropyl-β-cyclodextrin 10-30mg, lactose 10-30mg, microcrystalline cellulose 10-30mg, poly- dimension
Ketone k30 10-20mg, lauryl sodium sulfate 1-3mg, magnesium stearate 4-8mg.
8. composition according to claim 1, which is characterized in that in each unit dose, contain Febustat 30mg, amino
Glucose 400mg, hydroxypropyl-β-cyclodextrin 15mg, lactose 20mg, microcrystalline cellulose 18mg, povidone k30 15mg, dodecane
Base sodium sulphate 2mg, magnesium stearate 5mg.
9. the preparation method of composition described in claim 1, which comprises the following steps:
First step Febustat crosses 200 meshes, and Glucosamine and other auxiliary materials sieve with 100 mesh sieve；
Second step weigh the Febustat after the sieving of recipe quantity, Glucosamine, hydroxypropyl-β-cyclodextrin, at one third
The lauryl sodium sulfate of the lactose, recipe quantity just measured is uniformly mixed, with the povidone k30 aqueous solution of half recipe quantity
Adhesive is made, is pelletized；
Third step dries particle obtained by second step, crushes, and crosses 40 meshes；
Particle obtained by 4th step third step, with the lactose of 2/3rds recipe quantities, be uniformly mixed, with half recipe quantity
Povidone k30 aqueous solution makees adhesive, pelletizes, and dries, and crushes, and crosses 40 meshes；
Particle obtained by the 4th step of 5th step mixes, tabletting or encapsulated with the magnesium stearate of recipe quantity.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710848020.8A CN107648229B (en) | 2017-09-19 | 2017-09-19 | A kind of Febustat composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710848020.8A CN107648229B (en) | 2017-09-19 | 2017-09-19 | A kind of Febustat composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107648229A CN107648229A (en) | 2018-02-02 |
| CN107648229B true CN107648229B (en) | 2019-06-07 |
Family
ID=61130814
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710848020.8A Active CN107648229B (en) | 2017-09-19 | 2017-09-19 | A kind of Febustat composition |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107648229B (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108186634A (en) * | 2018-01-02 | 2018-06-22 | 迪沙药业集团（天津）药物研究有限公司 | A kind of Febustat composition |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105640890A (en) * | 2014-11-27 | 2016-06-08 | 华东理工大学 | Sparingly soluble active component particle, particle preparation and preparation method thereof |
-
2017
- 2017-09-19 CN CN201710848020.8A patent/CN107648229B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105640890A (en) * | 2014-11-27 | 2016-06-08 | 华东理工大学 | Sparingly soluble active component particle, particle preparation and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 氨基葡萄糖对CCl4所致小鼠肝损伤的改善作用;金黎明等;《郑州大学学报(医学版)》;20090131;第44卷(第1期);全文 |
| 非布司他临床应用及不良反应;杨雪 等;《药物不良反应杂志》;20140630;全文 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN107648229A (en) | 2018-02-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN102657629B (en) | Ticagrelor sustained-release tablet system and preparation method thereof | |
| CN104523633A (en) | Topiroxostat dispersible tablets and preparation method of topiroxostat dispersible tablets | |
| CN107432869A (en) | Include net double-layer tablets of Metformin hydrochloride and En Gelie and preparation method thereof | |
| CN107648229B (en) | A kind of Febustat composition | |
| CN101181264A (en) | Pharmaceutical composition taking metformin hydrochloride and vigelegting as active component as well as preparing method and uses thereof | |
| CN101990427A (en) | Combination of mitiglinide and metformin and process for preparing same | |
| CN106822097B (en) | Orlistat-containing pharmaceutical composition for losing weight | |
| CN101912613B (en) | Taste masking preparation | |
| CN101461832A (en) | Bioadhesive paster for treating mouth ulcer | |
| JP2014024817A (en) | Preventive or therapeutic agent for chronic renal failure | |
| CN108186634A (en) | A kind of Febustat composition | |
| CN104771400A (en) | Oral pharmaceutical composition of diacerein and berberine, and applications thereof | |
| CN107693555A (en) | A kind of medicine and purposes for treating diabetes | |
| CN100364522C (en) | Sustained releasing preparation of ferrosi succinas and its preparation method | |
| CN102716128A (en) | Pharmaceutical composition for treating asthma | |
| CN110151714A (en) | A kind of pet Cimitidine Tablets and preparation method thereof | |
| CN110604726B (en) | Sofosbuvir composition and application thereof | |
| CN107802607A (en) | A kind of Ao Gelieting tablet compositions | |
| CN103463014B (en) | A kind of α keto acid compound and preparation technology thereof | |
| CN102727624B (en) | New application of enteritis peaching composition on treatment of chronic prostatitis | |
| CN103520156B (en) | One is not containing talcous α keto acid compound and preparation technology thereof | |
| KR100788454B1 (en) | Rapid-acting fomulation containing nateglinide as an active ingredient | |
| CA2339190C (en) | Compressed compositions comprising clarified xanthan gum | |
| CN106728666A (en) | Lysinepuzinc piece | |
| CN107510696A (en) | For treating the pharmaceutical composition of NASH |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20200327 Address after: 300450 building 26, Green Valley Health Industrial Park, No. 59, Taikang Avenue, Binhai hi tech park, Binhai New Area, Tianjin Co-patentee after: DISHA PHARMACEUTICAL GROUP Co.,Ltd. Patentee after: Tianjin Disha Pharmaceutical Technology Development Co., Ltd. Address before: 300457 chamber No. 220, Dongting Road, Tianjin economic and Technological Development Zone, Tianjin peace zone, Tianjin International Institute of biology and medicine, 17 layer N1701-1 room Co-patentee before: DISHA PHARMACEUTICAL GROUP Co.,Ltd. Patentee before: DISHA PHARMACEUTICAL GROUP (TIANJIN) MEDICINE RESEARCH Co.,Ltd. |
|
| TR01 | Transfer of patent right | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20210622 Address after: No.1 Qingdao South Road, Weihai Economic and Technological Development Zone, Shandong Province Patentee after: DISHA PHARMACEUTICAL GROUP Co.,Ltd. Address before: 300450 building 26, Green Valley Health Industrial Park, 59 Taikang Avenue, Binhai science and Technology Park, Binhai New Area, Tianjin Patentee before: Tianjin Disha Pharmaceutical Technology Development Co.,Ltd. Patentee before: DISHA PHARMACEUTICAL GROUP Co.,Ltd. |
|
| TR01 | Transfer of patent right |