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High-dissolution rate topiroxostat pharmaceutical composition and preparation method thereof

A technology of topinostat and its composition, which is applied in the field of pharmaceutical preparations, can solve the problems of special particle size requirements, low dissolution rate, and unstable quality of raw materials, and achieve high drug dissolution rate, simple and stable production process good sex effect

Inactive Publication Date: 2015-04-22
CHANGSHA BAISHUN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN104042577A discloses a kind of stable topinostat tablet and preparation method thereof, described topinostat tablet is made of principal agent, lactose, microcrystalline cellulose, cross-linked carboxymethyl cellulose, low-substituted hydroxypropyl cellulose and Composed of magnesium stearate, the main drug and auxiliary materials are micronized and mixed together, and the powder is directly compressed into tablets. The defect is that there are special requirements for the particle size of the raw material drug
[0006] Because topinastat is a drug that is insoluble in water, the absorption of the drug mainly depends on the dissolution rate of the drug. The existing topinostat preparations have defects such as unstable quality, low dissolution rate, and requirements for particle size.

Method used

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  • High-dissolution rate topiroxostat pharmaceutical composition and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Prescription of Topicastat Tablets (Specification: 40mg):

[0034] Topicastat 40.0 g (dry and pure)

[0035] Polyethylene glycol 6000 80.0 g

[0036] Crospovidone 8.0 g

[0037] Magnesium stearate 1.0 g

[0038] A total of 1000 pieces were made

[0039] Preparation:

[0040] 1. Preparation of drug-containing tablet cores

[0041] ① Processing of raw materials and auxiliary materials: Mix topicastat and polyethylene glycol 6000 evenly, and sieve cross-linked povidone with an 80-mesh sieve for later use;

[0042] ②Add 2kg of absolute ethanol to the above mixture of topinastat and polyethylene glycol 6000, heat in a water bath at 70°C, and stir until completely dissolved;

[0043] ③ After complete dissolution, raise the temperature to 90°C to recover absolute ethanol. When the absolute ethanol is recovered to 40-50ml, add 6g of crospovidone and mix well to make a soft material;

[0044] ④ Wet granulation: take the above-mentioned soft material and gra...

Embodiment 2

[0050] Topicastat tablet core prescription (specification: 20mg):

[0051] Topicastat 20.0 g (dry and pure)

[0052] Polyethylene glycol 6000 60.0 g

[0053] Croscarmellose Sodium 6.0 g

[0054] Micronized silica gel 1 .0 g

[0055] A total of 1000 pieces were made

[0056] Coating Solution Prescription:

[0057] Opadry 85F42129 7.0 g

[0058] 75% ethanol 93.0 g

[0059] Preparation:

[0060] 1. Preparation of drug-containing tablet cores

[0061] ① Processing of raw materials and auxiliary materials: Mix topicastat and polyethylene glycol 6000 evenly, and sieve croscarmellose sodium with an 80-mesh sieve for later use;

[0062] ② Add 1.5 kg of absolute ethanol to the above mixture of topinastat and polyethylene glycol 6000, heat in a water bath at 65°C, and stir until completely dissolved;

[0063] ③ After complete dissolution, raise the temperature to 88°C to recover absolute ethanol. When the absolute ethanol is recovered to 2...

Embodiment 3

[0073] Topicastat tablet core prescription (specification: 60mg):

[0074] Topicastat 60.0 g

[0075] Povidone K30 150.0 g

[0076] Low-substituted hydroxypropyl cellulose 18.0 g

[0077] Magnesium stearate 2.0 g

[0078] A total of 1000 pieces were made

[0079] Coating Solution Prescription:

[0080] Opadry 85F18422 16.0 g

[0081] 80% ethanol 184.0 g

[0082] Preparation:

[0083] 1. Preparation of drug-containing tablet cores

[0084] ① Processing of raw and auxiliary materials: Mix topinostat and povidone evenly, and sieve low-substituted hydroxypropyl cellulose with a 100-mesh sieve for later use;

[0085] ②Add 5.0kg of absolute ethanol to the above mixture of topinastat and povidone, heat at 75°C, and stir until completely dissolved;

[0086] ③ After complete dissolution, heat up to 85°C to recover absolute ethanol. When the absolute ethanol is recovered to 40-60ml, add 15g of low-substituted hydroxypropyl cellulose, mix...

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Abstract

The invention provides a high-dissolution rate topiroxostat pharmaceutical composition and a preparation method thereof. The topiroxostat pharmaceutical composition comprises an active ingredient topiroxostat, and pharmaceutical adjuvants including a water-soluble solid dispersing carrier, a disintegrating agent and a lubricant. The prepared topiroxostat pharmaceutical composition does not have special requirements for the particle size of the active ingredient and does not need superfine grinding, so that the energy consumption is low, the dissolution rate is above 95%, the bioavailability is high, the defect that the active ingredient is bad in solubility and low in bioavailability is solved, the quality is stable and reliable and the market development prospect is good.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a high-dissolution topicastat pharmaceutical composition and a preparation method thereof. The invention also provides a topirestat pharmaceutical composition with high quality, safety and good stability. Background technique [0002] The occurrence of gout is due to the excessive production of uric acid in the body and the decline in the ability of the kidneys to clear it. The accumulation of uric acid in the body leads to the deposition of urate crystals in the joints and various organs. With the continuous improvement of people's living standards, changes in dietary structure and living habits (increase in nucleoprotein-rich foods), the extension of average life expectancy, and the improvement of human understanding and diagnosis of gout, no matter in European and American countries or in Asia In all countries, the prevalence of gout is increasing year by year...

Claims

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Application Information

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IPC IPC(8): A61K31/444A61P19/06
CPCA61K31/444
Inventor 不公告发明人
Owner CHANGSHA BAISHUN BIOTECH
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