CN106309390A - Topiroxostat tablets and preparation method thereof - Google Patents
Topiroxostat tablets and preparation method thereof Download PDFInfo
- Publication number
- CN106309390A CN106309390A CN201610795207.1A CN201610795207A CN106309390A CN 106309390 A CN106309390 A CN 106309390A CN 201610795207 A CN201610795207 A CN 201610795207A CN 106309390 A CN106309390 A CN 106309390A
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- Prior art keywords
- topiroxostat
- weight portion
- compositions
- tablet
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Classifications
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- 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
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
Abstract
The invention provides topiroxostat tablets and a preparation method thereof. The topiroxostat tablets comprise a main drug and excipients. The topiroxostat tablets are characterized in that the main drug is, by weight, 3-5 parts of topiroxostat, and the excipients are composed of, by weight, 10-15 parts of water-soluble filling agent, 2-4 parts of disintegrant, 1-3 parts of binder and 0.5-1.2 parts of lubricant. The topiroxostat tablets are high in dissolution rate, bioavailability, stability and practicability.
Description
Technical field
The present invention relates to pharmaceutical preparations technology field, be specifically related to a kind of Topiroxostat tablet and preparation method thereof.
Background technology
Gout is purine substance metabolism disorder, serum Uric Acid Concentration persistently increase cause urate crystal deposit soft tissue institute
The one group of metabolic disease caused.Clinical signs is hyperuricemia, gouty acute arthritis, tophaceous deposition, characteristic
Chronic arthritis and arthritis deformans, often involve kidney, causes chronic interstitial nephritis and kidney urate calculus, and gouty arthritis is normal
First presentation for this syndrome.The biochemical marker of gout is hyperuricemia, with hypertension, hyperlipidemia, atherosclerosis,
Generation fat, insulin resistant is closely related, it has also become threaten the serious metabolic disease of human health.In recent years, the whole world
Gout sickness rate substantially increases, and especially in developed regions, the gout sickness rate in China's affluence city is apparently higher than rural area, and gout is
It is increasingly becoming a kind of affluenza.But, the medicine for the treatment of hyperuricemia is limited at present, and toxic and side effects is big, and patient is the most not
It is resistant to.Therefore, along with the pathogenetic research of hyperuricemia deepens continuously, the research of anti-gout drugs is also increasingly subject to close
Note.Topiroxostat (Topiroxostat), by the research and development of Japanese fuji medicine Co., Ltd., gets the Green Light in Japan in June, 2013
Listing.Topiroxostat all has significant inhibitory action to the XOR of oxidized form and reduced form, thus its effect reducing uric acid is higher
Greatly, persistently, therefore can be used for treating the chronic hyperuricemia of gout.But, Topiroxostat is the medicine being insoluble in water, and medicine
The absorption of thing depends primarily on the dissolution of medicine, and existing Topiroxostat preparation exists that quality is unstable, dissolution is the most high
Defect, bioavailability is low.
Summary of the invention
For the problem of above-mentioned existence, the present invention propose a kind of dissolution is high, stability is strong Topiroxostat tablet and
Preparation method.
In order to realize above-mentioned purpose, the present invention uses following technical scheme:
A kind of Topiroxostat tablet, including principal agent and adjuvant, described principal agent be weight portion be the Topiroxostat of 3-5, adjuvant by
The water-soluble filler of weight portion 10-15, the disintegrating agent of weight portion 2-4, weight portion be the binding agent of 1-3, weight portion be 0.5-
The lubricant composition of 1.2.
Preferably, in Topiroxostat tablet principal agent be weight portion be the Topiroxostat of 4-5, adjuvant is by the water of weight portion 12-15
Soluble filler, the disintegrating agent of weight portion 3-4, weight portion be the binding agent of 2-3, weight portion be the lubricant composition of 0.7-1.2.
Preferably, Topiroxostat tablet also includes the water soluble oligo-chitosan of 1.5-2.5 weight portion.
Preferably, water-soluble filler be pregelatinized Starch, anhydrous alpha-lactose, microcrystalline Cellulose, the one of mannitol or
Two kinds and above compositions.
Preferably, disintegrating agent be mass ratio be carboxymethyl starch sodium and the compositions of polyvinylpolypyrrolidone of 1:1.2-1.5.
Preferably, lubricant be mass ratio be the polyethylene glycol 6000 of 1:1-1.5:0.8-1.2, Stepanol MG,
The compositions of politef.
Preferably, binding agent be mass ratio be 1:0.5-0.7 hydroxypropyl methyl cellulose and polyethylene oxide azo ketone
Compositions.
Preferably, the preparation method of Topiroxostat tablet, preparation process is as follows: weigh raw material by weight, first will torr department
He pulverized 350 mesh sieves, it is desirable to residue amount≤0.1% on screen cloth, the Topiroxostat after then processing and water soluble oligomer
Chitosan, water-soluble filler, disintegrating agent and binding agent are blended, and are placed in pelletize in high shear granulator, and pelletize is sent into after completing
Fluid bed drying, it is desirable to dried moisture is 1.5%-2.5%, after 20-30 mesh sieve granulate;It is eventually adding lubricant to mix
Close, tabletting,.
Owing to using above-mentioned technical scheme, the invention has the beneficial effects as follows: present invention process is simple, stablizes controlled, system
The Topiroxostat tablet dissolution obtained is high, and disintegration is short, and stability is strong, and bioavailability is high, tabletting disqualification rate <
2.2%, practical.
Detailed description of the invention
For making the purpose of the embodiment of the present invention, technical scheme and advantage clearer, below in conjunction with the embodiment of the present invention,
Technical scheme in the embodiment of the present invention is clearly and completely described.Based on embodiments of the invention, the common skill in this area
The every other embodiment that art personnel are obtained under not making creative work premise, broadly falls into the model of present invention protection
Enclose.
Embodiment 1:
A kind of Topiroxostat tablet, including principal agent and adjuvant, wherein principal agent be weight portion be the Topiroxostat of 3.6, adjuvant by
The anhydrous alpha-lactose of weight portion 12 and microcrystalline cellulose compositions, the carboxymethyl starch sodium that mass ratio is 1:1.4 of weight portion 2.8
Even with the hydroxypropyl methyl cellulose that mass ratio is 1:0.6 that the compositions of polyvinylpolypyrrolidone, weight portion are 1 and polyethylene oxide
The compositions of azone, weight portion be the mass ratio of 0.8 be the polyethylene glycol 6000 of 1:1.2:0.9, Stepanol MG, poly-four
The compositions composition of fluorothene;Topiroxostat tablet also includes the water soluble oligo-chitosan of 1.8 weight portions.
The preparation method of Topiroxostat tablet, preparation process is as follows: weighs raw material by weight, was first pulverized by Topiroxostat
350 mesh sieves, on screen cloth, residue amount is 0.08%, Topiroxostat and water soluble oligo-chitosan after then processing, anhydrous
Alpha-lactose and the compositions of microcrystalline cellulose compositions, carboxymethyl starch sodium and polyvinylpolypyrrolidone, hydroxypropyl methyl cellulose and
The compositions of polyethylene oxide azo ketone is blended, and is placed in pelletize in high shear granulator, and pelletize sends into fluid bed drying after completing,
Require that dried moisture is 1.8%, after 20 mesh sieve granulate;Be eventually adding polyethylene glycol 6000, Stepanol MG,
The compositions mixing of politef, tabletting,.
Embodiment 2:
A kind of Topiroxostat tablet, including principal agent and adjuvant, wherein principal agent be weight portion be the Topiroxostat of 3.2, adjuvant by
The anhydrous alpha-lactose of weight portion 14, the carboxymethyl starch sodium that mass ratio is 1:1.3 of weight portion 3.5 and the combination of polyvinylpolypyrrolidone
Thing, weight portion are the hydroxypropyl methyl cellulose that mass ratio is 1:0.5 and the compositions of polyethylene oxide azo ketone, the weight of 1.5
Amount part is the compositions that mass ratio is the polyethylene glycol 6000 of 1:1.1:0.8, Stepanol MG, politef of 0.5
Composition;Topiroxostat tablet also includes the water soluble oligo-chitosan of 2 weight portions.
The preparation method of Topiroxostat tablet, preparation process is as follows: weighs raw material by weight, was first pulverized by Topiroxostat
350 mesh sieves, on screen cloth, residue amount is 0.1%, Topiroxostat and the water soluble oligo-chitosan after then processing, anhydrous α-
The compositions of lactose, carboxymethyl starch sodium and polyvinylpolypyrrolidone, hydroxypropyl methyl cellulose and the group of polyethylene oxide azo ketone
Compound is blended, and is placed in pelletize in high shear granulator, and pelletize sends into fluid bed drying after completing, it is desirable to dried moisture is
2.4%, after 25 mesh sieve granulate;Be eventually adding polyethylene glycol 6000, Stepanol MG, politef compositions mix
Close, tabletting,.
Embodiment 3:
A kind of Topiroxostat tablet, including principal agent and adjuvant, wherein principal agent be weight portion be the Topiroxostat of 3, adjuvant is by weight
The amount microcrystalline Cellulose of part 15, the carboxymethyl starch sodium that mass ratio is 1:1.5 of weight portion 4 and the compositions of polyvinylpolypyrrolidone,
Weight portion be 3 the hydroxypropyl methyl cellulose that mass ratio is 1:0.7 and the compositions of polyethylene oxide azo ketone, weight portion be
The mass ratio of 1 is the compositions composition of the polyethylene glycol 6000 of 1:1:1.2, Stepanol MG, politef;Torr department
His sheet also includes the water soluble oligo-chitosan of 2.5 weight portions.
The preparation method of Topiroxostat tablet, preparation process is as follows: weighs raw material by weight, was first pulverized by Topiroxostat
350 mesh sieves, on screen cloth, residue amount is 0.07%, the Topiroxostat after then processing and water soluble oligo-chitosan, crystallite
The compositions of cellulose, carboxymethyl starch sodium and polyvinylpolypyrrolidone, hydroxypropyl methyl cellulose and polyethylene oxide azo ketone
Compositions is blended, and is placed in pelletize in high shear granulator, and pelletize sends into fluid bed drying after completing, it is desirable to dried moisture
It is 2.3%, after 30 mesh sieve granulate;It is eventually adding the compositions of polyethylene glycol 6000, Stepanol MG, politef
Mixing, tabletting,.
Embodiment 4:
A kind of Topiroxostat tablet, including principal agent and adjuvant, wherein principal agent be weight portion be the Topiroxostat of 4.5, adjuvant by
The anhydrous alpha-lactose of weight portion 13 and microcrystalline cellulose compositions, the carboxymethyl starch sodium that mass ratio is 1:1.2 of weight portion 2 and
The compositions of polyvinylpolypyrrolidone, weight portion are the hydroxypropyl methyl cellulose that mass ratio is 1:0.6 and the polyethylene oxide idol of 2.4
The compositions of azone, weight portion be the mass ratio of 1.2 be the polyethylene glycol 6000 of 1:1.5:0.9, Stepanol MG, poly-four
The compositions composition of fluorothene;Topiroxostat tablet also includes the water soluble oligo-chitosan of 1.5 weight portions.
The preparation method of Topiroxostat tablet, preparation process is as follows: weighs raw material by weight, was first pulverized by Topiroxostat
350 mesh sieves, on screen cloth, residue amount is 0.08%, Topiroxostat and water soluble oligo-chitosan after then processing, anhydrous
Alpha-lactose and the compositions of microcrystalline cellulose compositions, carboxymethyl starch sodium and polyvinylpolypyrrolidone, hydroxypropyl methyl cellulose and
The compositions of polyethylene oxide azo ketone is blended, and is placed in pelletize in high shear granulator, and pelletize sends into fluid bed drying after completing,
Require that dried moisture is 2%, after 25 mesh sieve granulate;It is eventually adding polyethylene glycol 6000, Stepanol MG, gathers
The compositions mixing of tetrafluoroethene, tabletting,.
Embodiment 5:
A kind of Topiroxostat tablet, including principal agent and adjuvant, wherein principal agent be weight portion be the Topiroxostat of 4, adjuvant is by weight
The anhydrous alpha-lactose of amount part 13 and the compositions of pregelatinized Starch, the carboxymethyl starch sodium that mass ratio is 1:1.4 of weight portion 2.2
Even with the hydroxypropyl methyl cellulose that mass ratio is 1:0.5 that the compositions of polyvinylpolypyrrolidone, weight portion are 2 and polyethylene oxide
The compositions of azone, weight portion be the mass ratio of 0.9 be the polyethylene glycol 6000 of 1:1.3:1, Stepanol MG, polytetrafluoro
The compositions composition of ethylene;Topiroxostat tablet also includes the water soluble oligo-chitosan of 1.9 weight portions.
The preparation method of Topiroxostat tablet, preparation process is as follows: weighs raw material by weight, was first pulverized by Topiroxostat
350 mesh sieves, on screen cloth, residue amount is 0.09%, Topiroxostat and water soluble oligo-chitosan after then processing, anhydrous
Alpha-lactose and the compositions of the compositions of pregelatinized Starch, carboxymethyl starch sodium and polyvinylpolypyrrolidone, hydroxypropyl methyl cellulose
Being blended with the compositions of polyethylene oxide azo ketone, be placed in pelletize in high shear granulator, pelletize is sent into fluid bed after completing and is done
Dry, it is desirable to dried moisture is 2.5%, after 30 mesh sieve granulate;It is eventually adding polyethylene glycol 6000, lauryl sulphate acid
Magnesium, the compositions mixing of politef, tabletting,.
Embodiment 6:
A kind of Topiroxostat tablet, including principal agent and adjuvant, wherein principal agent be weight portion be the Topiroxostat of 5, adjuvant is by weight
The amount mannitol of part 10, the carboxymethyl starch sodium that mass ratio is 1:1.2 of weight portion 3 and the compositions of polyvinylpolypyrrolidone, weight
Part be 2.8 the hydroxypropyl methyl cellulose that mass ratio is 1:0.6 and the compositions of polyethylene oxide azo ketone, weight portion be
The mass ratio of 0.7 is the compositions composition of the polyethylene glycol 6000 of 1:1.4:1.1, Stepanol MG, politef;Torr
Taking charge of his sheet also includes the water soluble oligo-chitosan of 2.3 weight portions.
The preparation method of Topiroxostat tablet, preparation process is as follows: weighs raw material by weight, was first pulverized by Topiroxostat
350 mesh sieves, on screen cloth, residue amount is 0.09%, the Topiroxostat after then processing and water soluble oligo-chitosan, manna
The compositions of alcohol, carboxymethyl starch sodium and polyvinylpolypyrrolidone, hydroxypropyl methyl cellulose and the combination of polyethylene oxide azo ketone
Thing is blended, and is placed in pelletize in high shear granulator, and pelletize sends into fluid bed drying after completing, it is desirable to dried moisture is
1.5%, after 20 mesh sieve granulate;Be eventually adding polyethylene glycol 6000, Stepanol MG, politef compositions mix
Close, tabletting,.
Embodiment of the present invention product and 5 groups of commercially available Topiroxostat tablets are made dissolution detection, and data are as follows:
Taking embodiment of the present invention group 6 groups and do tablet hardness test, often group 100 with commercially available group 5 groups, embodiment product is average
Hardness is 50.6N, commercially available product average hardness 38.7N.
Above example only in order to technical scheme to be described, is not intended to limit;Although with reference to previous embodiment
The present invention is described in detail, it will be understood by those within the art that: it still can be to aforementioned each enforcement
Technical scheme described in example is modified, or wherein portion of techniques feature is carried out equivalent;And these amendment or
Replace, do not make the essence of appropriate technical solution depart from the spirit and scope of various embodiments of the present invention technical scheme.
Claims (8)
1. a Topiroxostat tablet, including principal agent and adjuvant, it is characterised in that: described principal agent be weight portion be 3-5 torr department
He, adjuvant is the binding agent of 1-3, weight by the water-soluble filler of weight portion 10-15, the disintegrating agent of weight portion 2-4, weight portion
Part is the lubricant composition of 0.5-1.2.
Topiroxostat tablet the most according to claim 1 and 2, it is characterised in that: described principal agent be weight portion be the torr of 4-5
Taking charge of him, adjuvant is the binding agent of 2-3, weight by the water-soluble filler of weight portion 12-15, the disintegrating agent of weight portion 3-4, weight portion
Amount part is the lubricant composition of 0.7-1.2.
Topiroxostat tablet the most according to claim 1 and 2, it is characterised in that: described Topiroxostat tablet also includes 1.5-2.5
The water soluble oligo-chitosan of weight portion.
Topiroxostat tablet the most according to claim 1 and 2, it is characterised in that: described water-soluble filler is that pregelatinated forms sediment
Powder, anhydrous alpha-lactose, microcrystalline Cellulose, one or both and above compositions thereof of mannitol.
Topiroxostat tablet the most according to claim 1 and 2, it is characterised in that: described disintegrating agent be mass ratio be 1:1.2-
The carboxymethyl starch sodium of 1.5 and the compositions of polyvinylpolypyrrolidone.
Topiroxostat tablet the most according to claim 1 and 2, it is characterised in that: described lubricant be mass ratio be 1:1-
The polyethylene glycol 6000 of 1.5:0.8-1.2, Stepanol MG, the compositions of politef.
Topiroxostat tablet the most according to claim 1 and 2, it is characterised in that: described binding agent be mass ratio be 1:0.5-
The hydroxypropyl methyl cellulose of 0.7 and the compositions of polyethylene oxide azo ketone.
The preparation method of Topiroxostat tablet the most according to claim 1 and 2, it is characterised in that preparation process is as follows: by weight
Amount part weighs raw material, Topiroxostat is first pulverized 350 mesh sieves, it is desirable to residue amount≤0.1% on screen cloth, after then processing
Topiroxostat and water soluble oligo-chitosan, water-soluble filler, disintegrating agent and binding agent be blended, be placed in high shear granulator
Middle pelletize, pelletize sends into fluid bed drying after completing, it is desirable to dried moisture is 1.5%-2.5%, after 20-30 mesh sieve
Granulate;It is eventually adding mix lubricant, tabletting,.
Priority Applications (1)
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CN201610795207.1A CN106309390A (en) | 2016-08-31 | 2016-08-31 | Topiroxostat tablets and preparation method thereof |
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CN201610795207.1A CN106309390A (en) | 2016-08-31 | 2016-08-31 | Topiroxostat tablets and preparation method thereof |
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Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
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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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Publication number | Priority date | Publication date | Assignee | Title |
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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 |
Non-Patent Citations (1)
Title |
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万荣欣等: "水溶性壳聚糖的研究进展", 《透析与人工器官》 * |
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Application publication date: 20170111 |