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Topiroxostat dispersible tablets and preparing method thereof

A technology of topinostat and dispersible tablets, which is applied in the field of topinostat dispersible tablets and its preparation, can solve the problems of difficult treatment for patients, influence on drug absorption, slow disintegration speed, etc., and achieve good drug safety and human body absorption Good, fast disintegration effect

Inactive Publication Date: 2017-06-23
PEKING UNIV FOUNDER GRP CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The main problem that topinostat exists is because it is almost insoluble in water, after making tablets, the dissolution rate is low
Ordinary tablets have the disadvantage of slow disintegration speed, which affects the absorption of drugs; in addition, ordinary tablets have a large volume, or often need to use multiple tablets (grains) at a time, and need to be washed with water, which is inconvenient to take, especially for the elderly. , young and patients with swallowing dysfunction have certain difficulties in treatment

Method used

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  • Topiroxostat dispersible tablets and preparing method thereof
  • Topiroxostat dispersible tablets and preparing method thereof
  • Topiroxostat dispersible tablets and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Prescription (Specification: 20mg)

[0033]

[0034] Preparation:

[0035] (1) Treatment of raw and auxiliary materials: the Dv90 of the co-micronized active ingredient topicastat and mannitol is 22.3 μm, and the remaining auxiliary materials are sieved through an 80-mesh sieve for later use;

[0036] (2) making soft material: after taking the co-micronized product of recipe quantity, microcrystalline cellulose, 2% carboxymethyl starch sodium and mixing evenly, make soft material with water;

[0037] (3) Granulation: get above-mentioned soft material and granulate with 18 mesh screens;

[0038] (4) Drying: dry the wet granules, control the temperature of the material at 50±5°C, and make the moisture of the granules reach about 2%;

[0039] (5) Grain sizing: the dried granules are sieved with a 24-mesh sieve;

[0040] (6) Total blending: the granulated granules are added to the converted magnesium stearate and 1% sodium carboxymethyl starch and mixed evenly. The mi...

Embodiment 2

[0043] Prescription (Specification: 40mg)

[0044]

[0045] Preparation:

[0046] (1) Treatment of raw and auxiliary materials: the Dv90 of the co-micronized active ingredient topicastat and mannitol is 19.5 μm, and the remaining auxiliary materials are passed through an 80-mesh sieve for later use;

[0047] (2) making soft material: after taking the co-micronized product of recipe quantity, microcrystalline cellulose, 2% carboxymethyl starch sodium and mixing evenly, make soft material with water;

[0048] (3) Granulation: get above-mentioned soft material and granulate with 18 mesh screens;

[0049] (4) Drying: dry the wet granules, control the temperature of the material at 50±5°C, and make the moisture of the granules reach about 2%;

[0050] (5) Grain sizing: the dried granules are sieved with a 24-mesh sieve;

[0051] (6) Total blending: the granulated granules are added to the converted magnesium stearate and 1% sodium carboxymethyl starch and mixed evenly. The mi...

Embodiment 3

[0054] Prescription (Specification: 60mg)

[0055]

[0056]

[0057] Preparation:

[0058] (1) Treatment of raw and auxiliary materials: the Dv90 of the co-micronized active ingredient topicastat and mannitol is 10.3 μm, and the rest of the auxiliary materials are passed through an 80-mesh sieve for later use;

[0059] (2) making soft material: after taking the co-micronized product of recipe quantity, microcrystalline cellulose, 2.13% sodium carboxymethyl starch and mixing evenly, make soft material with water;

[0060] (3) Granulation: get above-mentioned soft material and granulate with 18 mesh screens;

[0061] (4) Drying: dry the wet granules, control the temperature of the material at 50±5°C, and make the moisture of the granules reach about 2%;

[0062] (5) Grain sizing: the dried granules are sieved with a 24-mesh sieve;

[0063](6) Total blending: the granulated granules are added to the converted magnesium stearate and 1.07% sodium carboxymethyl starch and m...

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Abstract

The invention provides topiroxostat dispersible tablets and a preparing method thereof. The topiroxostat dispersible tablets are composed of the active constituent topiroxostat, a filler, a disintegrant, a lubricant and pharmaceutic adjuvants. The topiroxostat dispersible tablets can be completely and quickly disintegrated, time to peak is shortened, the dissolution rate is 90% or above, the topiroxostat dispersible tablets are convenient to take, the pharmacodynamic function release speed is high, and bioavailability is high; the preparing process is simple, control is easy, operation is convenient, and the preparing process is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a topicastat dispersible tablet and a preparation method thereof. Background technique [0002] With the development of society and the change of diet structure, the incidence of gout presents an increasing trend. The research on gout in China originated in the 1950s. In 1948, Chen Yueshu reported two cases of gout for the first time. Only 25 cases were reported in the literature before 1958. In 2004, the prevalence rate in Shandong coastal areas was 1.14% (increased by 3 times in the past 10 years). Taiwan Province is a province with a high incidence of gout, and the prevalence rate of gout in indigenous residents over the age of 18 is 11.70%. Gout is also a concern in other developing countries. A survey of rheumatic diseases in Africa shows that the prevalence of gout is increasing across Africa. Compared with developing countries, the prevalence of gout in developed ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/444A61P19/06
CPCA61K9/2059A61K9/0095A61K9/2018A61K31/444
Inventor 王海超易崇勤冀蕾
Owner PEKING UNIV FOUNDER GRP CO LTD
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