Dronedarone hydrochloride tablet and preparation method thereof

Abstract

The invention belongs to the field of pharmaceutical preparations, and specifically relates to a surfactant-free dronedarone hydrochloride tablet. The dronedarone hydrochloride tablet comprises the following components in parts by weight: 400 parts of dronedarone hydrochloride, 100-1200 parts of hydroxypropyl methyl cellulose, 20-640 parts of disintegrating agent, 7-10 parts of lubricant, and zero surfactant. The technical scheme of the dronedarone hydrochloride tablet is characterized in that no surfactant is added, so that the safety is improved, and the problems of low melting point and easy sticking of the surfactant in the production process of the preparation are also avoided; and simultaneously, the dissolution rate of dronedarone hydrochloride is obviously improved. In the preparation process, the dronedarone hydrochloride and hydroxypropyl methyl cellulose are together ground until the particle size thereof is not greater than 1 micron, and then the obtained powder is formed into tablets with other suitable accessories; the process is quite simple, convenient to operate and suitable for industrial large-scale production.

Description

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, in particular to a dronedarone hydrochloride tablet, more specifically, to a dronedarone hydrochloride tablet without a surfactant. Background technique

[0002] Dronedarone hydrochloride (dronedarone hydrochloride), the chemical name is 2-n-butyl-3-[4-(3-di-n-butyl-aminopropoxy)benzoyl]-5-methylsulfabenzoyl Furan hydrochloride, CAS: 141625-93-6, is a newly developed drug for the treatment of arrhythmia by Sanofi-Aventis. In 2009, it was approved by the US FDA and Europe for the treatment of paroxysmal or persistent atrial fibrillation.

[0003] Dronedarone hydrochloride has very low solubility in aqueous media, especially its solubility is pH-dependent at room temperature, and has a maximum solubility in the range of pH 3 to 5, which is about 1-2mg / ml, and at pH about 6 The solubility becomes very low at pH=7, and the solubility is only 10 μg / ml at pH=7.

[0004] Because of its diss...

Examples

Embodiment 1

[0026]

[0027] Preparation Process:

[0028] Add dronedarone hydrochloride and hydroxypropyl methylcellulose into a ball mill to pulverize until the particle size is less than 1 μm, then mix them with microcrystalline cellulose and crospovidone evenly, add half the amount of calcium stearate, and dry process Granules, the remaining amount of calcium stearate is added to the granules, mixed and compressed into tablets.

Embodiment 2

[0030]

[0031] Preparation Process:

[0032] Add dronedarone hydrochloride and hydroxypropyl methylcellulose into a ball mill to pulverize until the particle size is less than 1 μm, then mix with lactose and crospovidone evenly, add half the amount of magnesium stearate, dry granulate, granulate Add the remaining amount of magnesium stearate to the mixture, mix and compress into tablets.

Embodiment 3

[0034]

[0035]

[0036] Preparation Process:

[0037] Add dronedarone hydrochloride and hydroxypropyl methylcellulose into a ball mill to pulverize until the particle size is less than 1 μm, then mix them with microcrystalline cellulose and sodium carboxymethyl starch, add pure water to granulate, dry, and granulate Add magnesium stearate, mix and compress into tablets.

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, in particular to a dronedarone hydrochloride tablet, more specifically, to a dronedarone hydrochloride tablet without a surfactant. Background technique

[0002] Dronedarone hydrochloride (dronedarone hydrochloride), the chemical name is 2-n-butyl-3-[4-(3-di-n-butyl-aminopropoxy)benzoyl]-5-methylsulfabenzoyl Furan hydrochloride, CAS: 141625-93-6, is a newly developed drug for the treatment of arrhythmia by Sanofi-Aventis. In 2009, it was approved by the US FDA and Europe for the treatment of paroxysmal or persistent atrial fibrillation.

[0003] Dronedarone hydrochloride has very low solubility in aqueous media, especially its solubility is pH-dependent at room temperature, and has a maximum solubility in the range of pH 3 to 5, which is about 1-2mg / ml, and at pH about 6 The solubility becomes very low at pH=7, and the solubility is only 10 μg / ml at pH=7.

[0004] Because of its diss...

Examples

Embodiment 1

[0026]

[0027] Preparation Process:

[0028] Add dronedarone hydrochloride and hydroxypropyl methylcellulose into a ball mill to pulverize until the particle size is less than 1 μm, then mix them with microcrystalline cellulose and crospovidone evenly, add half the amount of calcium stearate, and dry process Granules, the remaining amount of calcium stearate is added to the granules, mixed and compressed into tablets.

Embodiment 2

[0030]

[0031] Preparation Process:

[0032] Add dronedarone hydrochloride and hydroxypropyl methylcellulose into a ball mill to pulverize until the particle size is less than 1 μm, then mix with lactose and crospovidone evenly, add half the amount of magnesium stearate, dry granulate, granulate Add the remaining amount of magnesium stearate to the mixture, mix and compress into tablets.

Embodiment 3

[0034]

[0035]

[0036] Preparation Process:

[0037] Add dronedarone hydrochloride and hydroxypropyl methylcellulose into a ball mill to pulverize until the particle size is less than 1 μm, then mix them with microcrystalline cellulose and sodium carboxymethyl starch, add pure water to granulate, dry, and granulate Add magnesium stearate, mix and compress into tablets.

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