Topiroxostat tablet and preparation method thereof

A technology of topinostat and sita tablets, applied in the field of pharmaceutical preparations, to achieve the effects of stable quality, stable and controllable process, and high feasibility

Inactive Publication Date: 2016-04-06
SHANGHAI STEPPHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Topicastat is almost insoluble in water, how to improve the dissolution rate of the preparation, and then improve its bioavailability and curative effect is a big challenge

Method used

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  • Topiroxostat tablet and preparation method thereof
  • Topiroxostat tablet and preparation method thereof
  • Topiroxostat tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Specification: 20mg

[0031] Element

[0032] Specific process: Airflow pulverization of topinostat, control the air pressure at 0.3-0.8 MPa, make the particle size D90 less than 50 μm, weigh the micronized topinostat according to the prescription amount, and mix with the prescription amount of lactose and microcrystalline fiber Sodium croscarmellose and 1 / 2 recipe quantity were mixed through a 30-mesh sieve in a wet granulator, stirred at 600rpm for 10 minutes, added 5% hydroxypropyl cellulose aqueous solution, stirred at 600rpm, and sheared at 2000rpm to prepare grains for 2 minutes. Pass through a 24-mesh sieve for wet trimming, dry at 60°C until the moisture content is 0.5% to 4.0%, pass through a 20-mesh sieve for granulation. Add the prescription amount of magnesium stearate and 1 / 2 the prescription amount of croscarmellose sodium, and mix in a three-dimensional mixer for 5 minutes. Tablets were compressed with a 6mm round die.

Embodiment 2

[0034] Specification: 40mg

[0035] Element

[0036] Specific process: Airflow pulverization of topinostat, control the air pressure at 0.3-0.8 MPa, make the particle size D90 less than 50 μm, weigh the micronized topinostat according to the prescription amount, and mix with the prescription amount of lactose and microcrystalline fiber Sodium croscarmellose and 1 / 2 recipe quantity were mixed through a 30-mesh sieve in a wet granulator, stirred at 600rpm for 10 minutes, added 5% hydroxypropyl cellulose aqueous solution, stirred at 600rpm, and sheared at 2000rpm to prepare grains for 2 minutes. Pass through a 24-mesh sieve for wet trimming, dry at 60°C until the moisture content is 0.5% to 4.0%, pass through a 20-mesh sieve for granulation. Add the prescription amount of magnesium stearate and 1 / 2 the prescription amount of croscarmellose sodium, and mix in a three-dimensional mixer for 5 minutes. Tablets were compressed with a 7mm round die.

Embodiment 3

[0038] Specification: 60mg

[0039] Element

[0040] lactose

[0041] Specific process: Airflow pulverization of topinostat, control the air pressure at 0.3-0.8 MPa, make the particle size D90 less than 50 μm, weigh the micronized topinostat according to the prescription amount, and mix with the prescription amount of lactose and microcrystalline fiber Sodium croscarmellose and 1 / 2 recipe quantity were mixed through a 30-mesh sieve in a wet granulator, stirred at 600rpm for 10 minutes, added 5% hydroxypropyl cellulose aqueous solution, stirred at 600rpm, and sheared at 2000rpm to prepare grains for 2 minutes. Pass through a 24-mesh sieve for wet trimming, dry at 60°C until the moisture content is 0.5% to 4.0%, pass through a 20-mesh sieve for granulation. Add the prescription amount of magnesium stearate and 1 / 2 the prescription amount of croscarmellose sodium, and mix in a three-dimensional mixer for 5 minutes. Tablets were pressed with an 8mm round die...

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Abstract

The invention relates to a topiroxostat tablet. The topiroxostat tablet is prepared from, by weight, 5%-60% of raw material topiroxostat, 10%-80% of auxiliary material filler, 1%-30% of disintegrating agent, 0.1%-5% of bonding agent and 0.2%-5% of lubricating agent. The topiroxostat tablet has the advantages that the topiroxostat tablet is prepared by adding an appropriate amount of the auxiliary material to the topiroxostat subjected to air jet pulverization, the drug content uniformity is good, dissolution is rapid and safe, the quality is stable, the topiroxostat tablet is suitable for industrial production, and the bioavailability is improved, so that the curative effect is improved, and the topiroxostat tablet is convenient to store and use.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a preparation method of a tablet containing topinostat. Background technique [0002] Gout is a crystal-associated arthropathy caused by the deposition of monosodium urate (MSU), which is directly related to hyperuricemia caused by purine metabolic disorders and / or decreased uric acid excretion, especially acute characteristic arthritis and Chronic tophi diseases mainly include acute onset arthritis, tophi formation, tophi chronic arthritis, urate nephropathy and uric acid urolithiasis. In severe cases, joint disability and renal insufficiency may occur. Gout is often accompanied by abdominal obesity, hyperlipidemia, hypertension, type 2 diabetes and cardiovascular disease. [0003] For the treatment of gout, the current main clinical drug is allopurinol. Allopurinol is a purine analogue, which affects the activity of other enzymes in the metabolism of puri...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4439A61P19/06
Inventor 安日明唐飞宇廖文胜
Owner SHANGHAI STEPPHARM CO LTD
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