CN104523633A - Topiroxostat dispersible tablets and preparation method of topiroxostat dispersible tablets - Google Patents
Topiroxostat dispersible tablets and preparation method of topiroxostat dispersible tablets Download PDFInfo
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- CN104523633A CN104523633A CN201510062969.6A CN201510062969A CN104523633A CN 104523633 A CN104523633 A CN 104523633A CN 201510062969 A CN201510062969 A CN 201510062969A CN 104523633 A CN104523633 A CN 104523633A
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Abstract
The invention provides topiroxostat dispersible tablets and a preparation method of the topiroxostat dispersible tablets. The topiroxostat dispersible tablets are prepared from an active ingredient topiroxostat and medicinal auxiliary materials: filler, a disintegrating agent, a lubricant, a flow aid, a solubilizer and an acid-base regulator. The dissolution rate of the topiroxostat dispersible tablets prepared by the invention reaches over 90% and the topiroxostat dispersible tablets are high in bioavailability and stable and reliable in quality and have an extreme market development prospect.
Description
Technical field
The invention belongs to technical field of medicine, relate to a kind of holder his dispersible tablet of department and preparation method thereof, invention also provides his dispersible tablet of a holder department of a kind of quality safety, good stability.
Background technology
Gout be due to produce in body uric acid too much and kidney Scavenging activity decline, uric acid body accumulation, causes urate crystal in joint and each internal organs deposition.Along with improving constantly of people's living standard, the change of dietary structure and living habit (food being rich in nucleoprotein increases), the prolongation of average life, the understanding of the mankind to 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, current China Patients with Hyperuricemia number is more than 1.5 hundred million, wherein patient with gout is more than 7,500 ten thousand people, and increase with annual 0.97% annual rate of growth, gout has become China with the same second largest metabolism class disease of diabetes, and the life and health of people in serious threat.
The conventional current kind of antigout drug is few clinically at present, and clinical treatment is mainly based on colchicine, nonsteroidal antiinflammatory drug, hormone, promotion urate excretion medicine (as probenecid, sulfinpyrazone and benzbromarone) and suppression uric acid synthetic drug (allopurinol).These medicines are all defectiveness in treatment.Weak curative effect, side effect become greatly the bottleneck of its clinical practice.
Holder department he (Topirixostat)) by Fuji of Amada Co., Ltd. medicine in June, 2013 obtain Japanese MHLW ratify listing, for gout, hyperuricemia.This medicine, by suppressing xanthine oxidoreductase enzyme, suppresses uric acid to produce.
A kind of 1,2,4-triazole class compounds and preparation method thereof is disclosed in CN1561340B.A kind of 1,2,4-triazole compounds manufacture method and its intermediate is disclosed in CN1826335A.CN104230891A discloses a kind of holder his preparation method of department.CN104042577A discloses a kind of stable holder his sheet of department and preparation method thereof, described holder his sheet of department is made up of principal agent, lactose, microcrystalline Cellulose, cross-linked carboxymethyl cellulose, low-substituted hydroxypropyl cellulose and magnesium stearate, by always mixing after principal agent and adjuvant respectively micronization processes, direct powder compression is adopted to obtain.
Due to a holder department, he is an almost water-fast medicine, and the absorption of medicine depends primarily on the dissolution of medicine, and existing holder his preparation of department exists the not high defect of quality instability, dissolution.
Summary of the invention
The present invention aims to provide high, the stay-in-grade holder of a kind of dissolution his dispersible tablet of department and preparation method thereof.
Holder his dispersible tablet of department prepared by the present invention forms by by active component and filler, disintegrating agent, lubricant, fluidizer, solubilizing agent and acid-base modifier pharmaceutic adjuvant.
His dispersible tablet of above-mentioned holder department by supplementary material process, binding agent preparation, soft material processed, granulation, drying, granulate, always mix, the process such as tabletting is obtained.
Above-mentioned holder his dispersible tablet of department consists of the following composition by weight percentage: active component 15% ~ 50%, filler 40% ~ 65%, disintegrating agent 3% ~ 10%, binding agent 0.2% ~ 2.0%, lubricant 0.2% ~ 2.0%, fluidizer 0.2% ~ 2.0%, solubilizing agent 1% ~ 10%, acid-base modifier 1% ~ 5%.
Above-mentioned filler is one or more the mixture in starch, Icing Sugar, dextrin, lactose, pregelatinized Starch, mannitol, microcrystalline Cellulose, the mixture of preferred mannitol and microcrystalline Cellulose; Disintegrating agent is one or more the mixture in dried starch, carboxymethyl starch sodium, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, preferred polyvinylpolypyrrolidone; Binding agent is one or more the mixture in hypromellose, hyprolose, polyvinylpyrrolidone, sodium carboxymethyl cellulose; Lubricant is one or more the mixture in magnesium stearate, stearic acid, zinc stearate, preferred magnesium stearate; Fluidizer is one or more the mixture in micropowder silica gel, magnesium silicate, Pulvis Talci, preferred micropowder silica gel; Solubilizing agent is one or more the mixture in meglumine, sodium lauryl sulphate, tween 80, poloxamer, preferred meglumine; Acid-base modifier is one or more the mixture in sodium hydroxide, potassium hydroxide, calcium carbonate, sodium bicarbonate, sodium carbonate, preferred sodium hydroxide.
Prepare above-mentioned holder his dispersible tablet of department and comprise following steps:
1. supplementary material process: solubilizing agent and acid-base modifier are dissolved in purified water, add ethanol in proper amount, then add recipe quantity holder and take charge of him, be stirred to entirely molten; It is for subsequent use that 60-200 mesh sieve crossed by all the other adjuvants.
2. take diluent, binding agent and appropriate disintegrating agent mix homogeneously by recipe quantity, add above-mentioned medicinal liquid, make soft material;
3. the wet grain of system: get above-mentioned soft material granulation;
4. dry: by wet grain drying;
5. granulate: by dried particles granulate;
6. always mix: granulate granule is added the lubricant of recipe quantity, fluidizer and appropriate disintegrating agent, mixing, intermediate inspection is carried out in sampling;
7. intermediate carries out tabletting according to different sizes such as 20mg, 40mg and 60mg after the assay was approved;
treat that Bao Pin packs after the assay was approved and get final product.
In above-mentioned holder his a dispersible tablet preparation process of department, granulation and granulate mesh size used are 16 order ~ 40 orders, preferably 18 order ~ 30 orders; It is 40 DEG C ~ 65 DEG C that dry materials temperature controls, preferably 50 DEG C ~ 60 DEG C; Pellet moisture controls 1% ~ 4%, and preferably 2% ~ 3%; Always doing time is 15 ~ 40 minutes, preferably 30 minutes.
Tool of the present invention has the following advantages:
1, supplementary material of the present invention is through strict proportioning, and adjuvant selects kind few, cheap and easy to get, good stability, and drug safety is good;
2, this product dissolution reaches more than 90%, and absorption of human body is fast, good drug efficacy, and bioavailability is high;
3, production technology simplifies, and is applicable to enterprise scale and produces;
4, this product is dispersible tablet, and disintegration rate is fast, puts into water and dispersibles uniformly suspension, taking convenience.Overcome conventional tablet and capsule need use mixing in water for oral taking, take inconvenience, particularly always, children and have the constant defect of the clothes for patients of dysphagia.
Detailed description of the invention
Enforcement below can illustrate in greater detail the present invention, but does not limit the present invention in any form.
embodiment 1
Prescription (specification: 20mg):
His 20.0 g are taken charge of in holder
Microcrystalline Cellulose 60.0 g
Lactose 20.0 g
Polyvinylpolypyrrolidone 40.0 g
Sodium hydroxide 2.0 g
Meglumine 6.0 g
PVP K30 2.0 g
Magnesium stearate 2.0 g
micropowder silica gel 2.0 g
Make 1000 altogether
Preparation method:
1. supplementary material process: sodium hydroxide and meglumine are dissolved in 9g purified water, adds 25g ethanol, then adds recipe quantity holder and take charge of him, is stirred to entirely molten; It is for subsequent use that the above standard screen of 60 order crossed by all the other adjuvants.
2. take diluent, binding agent and 30g polyvinylpolypyrrolidone mix homogeneously by recipe quantity, add above-mentioned medicinal liquid, make soft material
3. the wet grain of system: get above-mentioned soft material and granulated by 24 eye mesh screens;
4. dry: by wet grain drying, control temperature of charge 50 DEG C ~ 55 DEG C, make pellet moisture reach about 2%;
5. granulate: by dried particles 24 eye mesh screen granulate;
6. always mix: granulate granule is added the magnesium stearate of recipe quantity, micropowder silica gel and 10g polyvinylpolypyrrolidone, mixing, incorporation time is 30 minutes, and intermediate inspection is carried out in sampling;
7. intermediate tabletting after the assay was approved, to obtain final product.
embodiment 2
Prescription (specification: 40mg):
His 40.0 g are taken charge of in holder
Microcrystalline Cellulose 100.0 g
Lactose 40.0 g
Carboxymethylstach sodium 80.0 g
Sodium hydroxide 4.0 g
Meglumine 15.0 g
Hypromellose 5.0 g
Magnesium stearate 4.0 g
micropowder silica gel 4.0 g
Make 1000 altogether
Preparation method:
1. supplementary material process: sodium hydroxide and meglumine are dissolved in 20g purified water, adds 50g ethanol, then adds recipe quantity holder and take charge of him, is stirred to entirely molten; It is for subsequent use that the above standard screen of 60 order crossed by all the other adjuvants.
2. take diluent, binding agent and 70g carboxymethylstach sodium mix homogeneously by recipe quantity, add above-mentioned medicinal liquid, make soft material
3. the wet grain of system: get above-mentioned soft material and granulated by 24 eye mesh screens;
4. dry: by wet grain drying, control temperature of charge 55 DEG C ~ 60 DEG C, make pellet moisture reach 2% ~ 3%;
5. granulate: by dried particles 24 eye mesh screen granulate;
6. always mix: granulate granule is added the magnesium stearate of recipe quantity, micropowder silica gel and 10g carboxymethylstach sodium, mixing, incorporation time is 30 minutes, and intermediate inspection is carried out in sampling;
7. intermediate tabletting after the assay was approved, to obtain final product.
embodiment 3
Prescription (specification: 60mg):
His 60.0 g are taken charge of in holder
Microcrystalline Cellulose 120.0 g
Mannitol 120.0 g
Polyvinylpolypyrrolidone 120.0 g
Sodium hydroxide 6.0 g
Meglumine 20.0 g
Hyprolose 6.0 g
Magnesium stearate 4.0 g
micropowder silica gel 6.0 g
Make 1000 altogether
Preparation method:
1. supplementary material process: sodium hydroxide and meglumine are dissolved in 30g purified water, adds 80g ethanol, then adds recipe quantity holder and take charge of him, is stirred to entirely molten; It is for subsequent use that the above standard screen of 60 order crossed by all the other adjuvants.
2. take diluent, binding agent and 100g polyvinylpolypyrrolidone mix homogeneously by recipe quantity, add above-mentioned medicinal liquid, make soft material
3. the wet grain of system: get above-mentioned soft material and granulated by 24 eye mesh screens;
4. dry: by wet grain drying, control temperature of charge 50 DEG C ~ 55 DEG C, make pellet moisture reach about 2%;
5. granulate: by dried particles 24 eye mesh screen granulate;
6. always mix: granulate granule is added the magnesium stearate of recipe quantity, micropowder silica gel and 20g polyvinylpolypyrrolidone, mixing, incorporation time is 30 minutes, and intermediate inspection is carried out in sampling;
7. intermediate tabletting after the assay was approved, to obtain final product.
Test example 1
The sample of embodiment 1,2,3 is placed in relative humidity (RH) is 75%, temperature is that 40 DEG C of incubators are placed 6 months continuously, respectively at the 0th, 1,2,3, June time pick test.Result all samples all conforms with the regulations, and shows that products obtained therefrom of the present invention has good stability, reliable in quality, and wherein content, related substance (always mixing), dissolution results are in table 1.
Table 1 accelerated test investigates result
Claims (6)
1. holder his dispersible tablet of department and preparation method thereof, it is characterized in that, his dispersible tablet of a holder department prepared by the method is made up of active component holder department he and filler, disintegrating agent, lubricant, fluidizer, solubilizing agent and an acid-base modifier pharmaceutic adjuvant.
2. holder his dispersible tablet of department and preparation method thereof, is characterized in that, prepares his dispersible tablet of a described holder department and is obtained by supplementary material process, binding agent preparation, soft material processed, granulation, drying, granulate, always mixed, tabletting.
3. one holder according to claim 1 his dispersible tablet of department and preparation method thereof, it is characterized in that, his dispersible tablet of described holder department consists of the following composition by weight percentage: an active component holder department he 15% ~ 50%, filler 40% ~ 65%, disintegrating agent 3% ~ 10%, binding agent 0.2% ~ 2.0%, lubricant 0.2% ~ 2.0%, fluidizer 0.2% ~ 2.0%, solubilizing agent 1% ~ 10%, acid-base modifier 1% ~ 5%.
4. one holder according to claim 1 his dispersible tablet of department and preparation method thereof, it is characterized in that, described filler is one or more the mixture in starch, Icing Sugar, dextrin, lactose, pregelatinized Starch, mannitol, microcrystalline Cellulose, the mixture of preferred mannitol and microcrystalline Cellulose; Disintegrating agent is one or more the mixture in dried starch, carboxymethyl starch sodium, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, preferred polyvinylpolypyrrolidone; Binding agent is one or more the mixture in hypromellose, hyprolose, polyvinylpyrrolidone, sodium carboxymethyl cellulose; Lubricant is one or more the mixture in magnesium stearate, stearic acid, zinc stearate, preferred magnesium stearate; Fluidizer is one or more the mixture in micropowder silica gel, magnesium silicate, Pulvis Talci, preferred micropowder silica gel; Solubilizing agent is one or more the mixture in meglumine, sodium lauryl sulphate, tween 80, poloxamer, preferred meglumine; Acid-base modifier is one or more the mixture in sodium hydroxide, potassium hydroxide, sodium bicarbonate, calcium carbonate, sodium carbonate, preferred sodium hydroxide.
5. one holder according to claim 1 his dispersible tablet of department and preparation method thereof, it is characterized in that, described supplementary material processing procedure, for be dissolved in purified water by solubilizing agent and acid-base modifier, adds ethanol in proper amount, add recipe quantity holder again and take charge of him, be stirred to entirely molten; It is for subsequent use that 60-200 mesh sieve crossed by all the other adjuvants.
6. one holder according to claim 2 his dispersible tablet of department and preparation method thereof, is characterized in that, in described holder his a dispersible tablet preparation process of department, granulation and granulate mesh size used are 16 order ~ 40 orders, preferably 18 order ~ 30 orders; It is 40 DEG C ~ 65 DEG C that dry materials temperature controls, preferably 50 DEG C ~ 60 DEG C; Pellet moisture controls 1% ~ 4%, and preferably 2% ~ 3%; Always doing time is 15 ~ 40 minutes, preferably 30 minutes.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510062969.6A CN104523633A (en) | 2015-02-08 | 2015-02-08 | Topiroxostat dispersible tablets and preparation method of topiroxostat dispersible tablets |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510062969.6A CN104523633A (en) | 2015-02-08 | 2015-02-08 | Topiroxostat dispersible tablets and preparation method of topiroxostat dispersible tablets |
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| CN104523633A true CN104523633A (en) | 2015-04-22 |
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104814937A (en) * | 2015-04-22 | 2015-08-05 | 青岛正大海尔制药有限公司 | Topiroxostat tablet |
| CN105343020A (en) * | 2015-10-30 | 2016-02-24 | 济南康和医药科技有限公司 | Topiroxostat tablet and preparation method thereof |
| CN106074405A (en) * | 2016-06-12 | 2016-11-09 | 佛山市腾瑞医药科技有限公司 | A kind of Topiroxostat dispersible tablet and preparation method thereof |
| CN106880619A (en) * | 2015-12-15 | 2017-06-23 | 北大方正集团有限公司 | A kind of Topiroxostat capsule and preparation method thereof |
| CN106880603A (en) * | 2015-12-15 | 2017-06-23 | 北大方正集团有限公司 | A kind of oral disnitegration tablet containing Topiroxostat and preparation method thereof |
| CN106880600A (en) * | 2015-12-15 | 2017-06-23 | 北大方正集团有限公司 | A kind of Topiroxostat dispersible tablet and preparation method thereof |
| CN108379232A (en) * | 2018-03-21 | 2018-08-10 | 宁波蒙曼生物科技有限公司 | A kind of dispersible tablet and its preparation process containing LCZ-696 |
Citations (3)
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|---|---|---|---|---|
| CN101780073A (en) * | 2009-01-21 | 2010-07-21 | 重庆圣华曦药业有限公司 | Febuxostat dispersible tablet drug and preparing method thereof |
| WO2014125504A2 (en) * | 2013-02-18 | 2014-08-21 | Hetero Research Foundation | Pharmaceutical compositions of febuxostat |
| 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 |
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2015
- 2015-02-08 CN CN201510062969.6A patent/CN104523633A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101780073A (en) * | 2009-01-21 | 2010-07-21 | 重庆圣华曦药业有限公司 | Febuxostat dispersible tablet drug and preparing method thereof |
| WO2014125504A2 (en) * | 2013-02-18 | 2014-08-21 | Hetero Research Foundation | Pharmaceutical compositions of febuxostat |
| 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 |
Non-Patent Citations (1)
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| 彭礼明: "分散片处方、工艺特点及其进展", 《DRUG EVALUATION》 * |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104814937A (en) * | 2015-04-22 | 2015-08-05 | 青岛正大海尔制药有限公司 | Topiroxostat tablet |
| CN104814937B (en) * | 2015-04-22 | 2018-03-09 | 青岛正大海尔制药有限公司 | A kind of Topiroxostat tablet |
| CN105343020A (en) * | 2015-10-30 | 2016-02-24 | 济南康和医药科技有限公司 | Topiroxostat tablet and preparation method thereof |
| CN106880619A (en) * | 2015-12-15 | 2017-06-23 | 北大方正集团有限公司 | A kind of Topiroxostat capsule and preparation method thereof |
| CN106880603A (en) * | 2015-12-15 | 2017-06-23 | 北大方正集团有限公司 | A kind of oral disnitegration tablet containing Topiroxostat and preparation method thereof |
| CN106880600A (en) * | 2015-12-15 | 2017-06-23 | 北大方正集团有限公司 | A kind of Topiroxostat dispersible tablet and preparation method thereof |
| CN106074405A (en) * | 2016-06-12 | 2016-11-09 | 佛山市腾瑞医药科技有限公司 | A kind of Topiroxostat dispersible tablet and preparation method thereof |
| CN108379232A (en) * | 2018-03-21 | 2018-08-10 | 宁波蒙曼生物科技有限公司 | A kind of dispersible tablet and its preparation process containing LCZ-696 |
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Application publication date: 20150422 |