CN105919968A - Topiroxostat preparation and application thereof - Google Patents
Topiroxostat preparation and application thereof Download PDFInfo
- Publication number
- CN105919968A CN105919968A CN201610406286.2A CN201610406286A CN105919968A CN 105919968 A CN105919968 A CN 105919968A CN 201610406286 A CN201610406286 A CN 201610406286A CN 105919968 A CN105919968 A CN 105919968A
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- Prior art keywords
- topiroxostat
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Classifications
-
- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
Abstract
The invention discloses a topiroxostat preparation and application thereof. The topiroxostat preparation is prepared from topiroxostat, lactose, microcrystalline cellulose and a medically acceptable carrier. The obtained topiroxostat preparation has higher flowability, stability and dissolubility, and is suitable for large-scale industrial production. The topiroxostat preparation is a medicine combination for treating gout and hyperuricemia, and is reasonable in proportion; the medicine can be quickly released, so that an extremely good treating effect can be achieved on diseases.
Description
Technical field
The present invention relates to Topiroxostat for preparing the purposes of medicine, in particular for preparation be suitable to the tablet that is administered orally and
Capsule.
Topiroxostat (Topiroxostat), molecular formula: C13H8N6, molecular weight: 248.24282
It is three kind new medicines for treating gout, hyperuricemia, currently carries out preclinical study.
Background technology
Gout is the disease caused by one group of purine metabolic disturbance, and its clinical characters is hyperuricemia and causes therefrom
Gouty acute arthritis recurrent exerbation, tophaceous deposition, tophaceous chronic arthritis and joint deformity, often involve kidney,
Chronic interstitial nephritis and uric acid kidney stones is caused to be formed.Primary disease can divide constitutional and the big class of Secondary cases two.Constitutional person's minority
Owing to enzyme defect causes, often accompany hyperlipemia, obesity, diabetes, hypertension, arteriosclerosis and coronary heart disease etc..Secondary cases person
Can be caused by many reasons such as nephropathy, hematopathy and medicines.
Being more common in male, the ratio of men and women is about 20: 1, and women seldom falls ill, if any occurring mostly after the menopause.Abroad
Report that many cases have Positive family history.The gout course of disease is the longest, and the person that do not involves kidney is through effectively preventing and treating prognosis bona, but as anti-
It is improper to control, and is easily caused the serious consequences such as joint deformity, renal calculus, renal damage.Renal insufficiency person's prognosis is poor.Uric acid height is people
Internal have a kind of material being called purine to get muddled because of metabolism, causes uric acid in blood to increase and a kind of metabolic disease of causing
Disease, growing amount and the excretion of internal uric acid every day are the most equal, growing amount aspect, and 1/3rd is by food, and three
/ bis-is internal to synthesize voluntarily, and excretion pathway is then 1/3rd to be discharged by intestinal, and 2/3rds from renal excretion.Above-mentioned respectively
As long as kind of an approach has any one to go wrong, will result in uric acid and raise.Uric acid rises, because it can hinder blood to secrete
The process of uric acid, makes uric acid to discharge.Uric acid is too high, also can cause other diseases.
Past more rare patient with gout to get up, and is not only late adult onset, but also occurs in that rejuvenation
Trend, become a kind of commonly encountered diseases.Clinically, man's uric acid normal value: 149～416 μm ol/L.Women uric acid normal value: 89
～357 μm o1/L.If beyond index, it is simply that uric acid is high.
Summary of the invention
The present invention relates to the pharmaceutical composition containing Topiroxostat and this based composition and treat gout, height for safely and effectively
Lithemic application.
The invention still further relates to the pharmaceutical composition containing Topiroxostat Yu the oral administration of other drug active substance.This group
Compound is to be obtained by the surface making the granule of pharmaceutically active substance adhere to carrier matrix.Pharmaceutically active substance calmness is made to exist
Method on carrier matrix is minimum in order to make the gathering of active substance/carrier substrate particles be reduced to.
The present invention relates to the pharmaceutical composition containing about 10mg--300 mg Topiroxostat, said composition is given daily 2 times
For treating gout, hyperuricemia.Preferably pharmaceutical composition contains the Topiroxostat of about 10mg--200 mg, most preferably
Pharmaceutical composition contains the Topiroxostat of about 10mg--150 mg.Further, this kind of preferred and most preferred pharmaceutical composition is every
It is administered day and is used for for 2 times treating gout, hyperuricemia.
Above-mentioned Topiroxostat pharmaceutical composition for being given daily also can be the most regular some patient is administered.Example
As, make their gout, hyperuricemia be controlled to being treated by daily Topiroxostat pharmaceutical composition
Patient can implement maintaining treatment scheme to protect it from further infecting.This maintaining treatment scheme includes that every day is less than one
Secondary takes Topiroxostat pharmaceutical composition.Such as, just within every three or four days, being administered once, it is enough.
The Topiroxostat pharmaceutical composition of the present invention can be configured to the form through any suitable administration, the most preferably
Oral administration combination can be tablet, capsule, granule or powder type.According to method well known in the art, Topiroxostat medicine
Compositions can be to be configured to the form that parenteral, rectum or via intranasal application are administered.This kind of preparation can include pharmaceutically acceptable excipient, institute
State excipient and include in this based composition conventional filler, fluidizer, lubricant, disintegrating agent, binding agent etc..The present invention also wraps
Include slow releasing preparation.
Tablet and capsule preparations containing about 10mg 100mg Topiroxostat can be prepared, by the following method with really
Protect the efficient of product and good uniformity.First Topiroxostat calmness is prepared combination on the surface of carrier matrix
Thing.This step is completed by following operation: forms Topiroxostat and the solution of adhesive material, then protects at carrier substrate particles
In the way of spraying, this solution is applied while holding motion.Control condition is so that the gathering of granule is preferably minimized.
Any other composition that will comprise in granule and compositions after drying, such as disintegrating agent/fluidizer/lubricant mix
Close.Then the powder obtained it is pressed into sheet or is filled into capsule.
Preferred solvent in said method is the ethanol of water or variable concentrations.
Adhesive material preferably has the polymer of high-consistency.The material being suitable for includes polyvidone, methylcellulose, hydroxyl
Methylcellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, polyvidone, hydroxymethyl cellulose are preferred
's.In whole compositions, the content of adhesive material is preferably the about 1%--about 10%(weight of compositions gross weight).
The disintegrant content that whole compositions includes is preferably the about 1%--7% of compositions gross weight.The disintegrating agent being suitable for includes
Polyvinylpolypyrrolidone, cross-linked carboxymethyl cellulose, low-substituted hydroxypropyl methylcellulose, Explotab, pregelatinized Starch and Semen Maydis
Starch, polyvinylpolypyrrolidone is preferred.
The lubricant content that whole compositions includes is preferably the about 1%--5% of compositions gross weight.The lubricant being suitable for includes
Micropowder silica gel, magnesium stearate, stearic acid, stearyl fumarate and sodium lauryl sulfate, micropowder silica gel, magnesium stearate are preferred
's.
Detailed description of the invention
The Topiroxostat compositions of the following example explanation present invention
Embodiment 1
Said method is used to prepare 10 milligrams of Topiroxostat capsules
| Composition | Amount %(w/w) | Amount/grain |
| Topiroxostat | 5 | 10mg |
| Microcrystalline Cellulose | 47.00 | 94 mg |
| Lactose | 30.00 | 60 mg |
| Polyvidone | 5.00 | 10 mg |
| Low-substituted hydroxypropyl methylcellulose | 10.00 | 20.0mg |
| Magnesium stearate | 0.90 | 1.8mg |
| Silicon dioxide | 2.1 | 4.0 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 200.00 mg |
Embodiment 2
Said method is used to prepare 40 milligrams of Topiroxostat capsules
| Composition | Amount %(w/w) | Amount/grain |
| Topiroxostat | 13.25 | 40 mg |
| Microcrystalline Cellulose | 33.11 | 100 mg |
| Lactose | 33.11 | 100 mg |
| Polyvidone | 9.90 | 30mg |
| Polyvinylpolypyrrolidone | 9.90 | 30.0mg |
| Silicon dioxide | 0.67 | 2.00mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 302.00 mg |
Embodiment 3
Said method is used to prepare 60 milligrams of Topiroxostat capsules
| Composition | Amount %(w/w) | Amount/piece |
| Topiroxostat | 17.07.50 | 60 mg |
| Microcrystalline Cellulose | 28.45 | 100 mg |
| Lactose | 42.67 | 150 mg |
| Polyvidone | 2.84 | 10 mg |
| Polyvinylpolypyrrolidone | 5.69 | 20 mg |
| Low-substituted hydroxypropyl methylcellulose | 2.84 | 10 mg |
| Magnesium stearate | 0.11 | 1.5 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 351.50 mg |
Embodiment 4
Said method is used to prepare 40 milligrams of Topiroxostat tablets
| Composition | Amount %(w/w) | Amount/piece |
| Topiroxostat | 11.71 | 40 mg |
| Microcrystalline Cellulose | 29.28 | 100 mg |
| Lactose | 43.92 | 150 mg |
| Polyvidone | 2.93 | 10 mg |
| Low-substituted hydroxypropyl methylcellulose | 5.86 | 20 mg |
| Magnesium stearate | 2.93 | 10 mg |
| Silicon dioxide | 2.93 | 10 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 341.50 mg |
Embodiment 5
Said method is used to prepare 20 milligrams of Topiroxostat tablets
| Composition | Amount %(w/w) | Amount/piece |
| Topiroxostat | 9.09 | 20 mg |
| Microcrystalline Cellulose | 36.36 | 80 mg |
| Lactose | 45.45 | 100 mg |
| Polyvidone | 2.73 | 6mg |
| Low-substituted hydroxypropyl methylcellulose | 1.36 | 3 mg |
| Magnesium stearate | 0.45 | 1 mg |
| Silicon dioxide | 0.23 | 1 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 220.00 mg |
Embodiment 6
Said method is used to prepare 60 milligrams of Topiroxostat tablets
| Composition | Amount %(w/w) | Amount/piece |
| Topiroxostat | 23.08 | 60 mg |
| Microcrystalline Cellulose | 30.77 | 80 mg |
| Lactose | 38.46 | 100 mg |
| Polyvidone | 2.3 | 6mg |
| Low-substituted hydroxypropyl methylcellulose | 1.15 | 3 mg |
| Magnesium stearate | 0.38 | 1 mg |
| Silicon dioxide | 0.38 | 1 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 260.00 mg |
Claims (10)
1. Topiroxostat is used for preparing oral administration every day 2 times for treating gout, hyperuricemia in the form of tablets or capsules
The purposes of pharmaceutical composition, wherein said pharmaceutical composition contains the Topiroxostat of 5mg 500mg.
2. the purposes of claim 1, the content of wherein said Topiroxostat is 5mg 300mg.
3. the purposes of claim 1, the content of wherein said Topiroxostat is 5mg 100mg.
4. the purposes of claim 3, the content of wherein said Topiroxostat is 10mg.
5. the purposes of claim 3, the content of wherein said Topiroxostat is 20mg.
6. the purposes of claim 3, the content of wherein said Topiroxostat is 40mg.
7. the purposes of claim 3, the content of wherein said Topiroxostat is 60mg.
8. the purposes of claim 3, the content of wherein said Topiroxostat is 80mg.
9. the purposes of claim 1, described compositions therein contains one or more other drug active substances.
10. the purposes of claims 1, wherein said filler is selected from lactose, xylitol, microcrystalline Cellulose, dextrin, manna
Alcohol, sorbitol, sucrose, starch, pregelatinized Starch, glucose, calcium phosphate, calcium hydrogen phosphate, calcium carbonate, and mixture, and
Described Topiroxostat be by have enough stickiness polymerization emplastic stick together on described filler.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610406286.2A CN105919968A (en) | 2016-06-12 | 2016-06-12 | Topiroxostat preparation and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610406286.2A CN105919968A (en) | 2016-06-12 | 2016-06-12 | Topiroxostat preparation and application thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105919968A true CN105919968A (en) | 2016-09-07 |
Family
ID=56832655
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610406286.2A Pending CN105919968A (en) | 2016-06-12 | 2016-06-12 | Topiroxostat preparation and application thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105919968A (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104042577A (en) * | 2014-06-13 | 2014-09-17 | 安徽省逸欣铭医药科技有限公司 | Stable topiroxostat tablet and preparation method thereof |
| CN104523690A (en) * | 2015-02-08 | 2015-04-22 | 长沙佰顺生物科技有限公司 | Topiroxostat oral preparation and preparation method thereof |
| CN105456209A (en) * | 2015-02-13 | 2016-04-06 | 上海麦步医药科技有限公司 | Topiroxostat tablet and preparation method thereof |
-
2016
- 2016-06-12 CN CN201610406286.2A patent/CN105919968A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104042577A (en) * | 2014-06-13 | 2014-09-17 | 安徽省逸欣铭医药科技有限公司 | Stable topiroxostat tablet and preparation method thereof |
| CN104523690A (en) * | 2015-02-08 | 2015-04-22 | 长沙佰顺生物科技有限公司 | Topiroxostat oral preparation and preparation method thereof |
| CN105456209A (en) * | 2015-02-13 | 2016-04-06 | 上海麦步医药科技有限公司 | Topiroxostat tablet and preparation method thereof |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160907 |
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| WD01 | Invention patent application deemed withdrawn after publication |