Tablet containing escitalopram oxalate and preparation method thereof

Abstract

The invention discloses a tablet containing escitalopram oxalate and a preparation method thereof. According to the invention, the tablet containing escitalopram oxalate uses hydroxy propyl cellulose as an adhesive and uses escitalopram oxalate with median particle size less than or equal to 20mum, and the prepared tablet containing escitalopram oxalate has the advantages of beautiful appearance and stable quality. The invention also provides the preparation method of oral tablet, and has the advantages of simple process and adaptability of commercialized production.

Description

technical field

[0001] The invention belongs to the technical field of medicine, and in particular relates to a tablet containing escitalopram oxalate and a preparation method thereof. Background technique

[0002] Escitalopram oxalate is an oral selective serotonin reuptake inhibitor (SSRI). Escitalopram oxalate is the S-isomer (single isomer) of racemic citalopram. Jointly developed by Forest Laboratories and Denmark Lundbeck, escitalopram oxalate tablets (trade name: ) was launched in the United States in 2002 and was launched in China in 2005. Citalopram oxalate has the following structural formula:

[0003]

[0004] The patent EP1414435 of Yuanyan Lingbei Company discloses a method for preparing escitalopram oxalate with an average particle size of 40 μm to 200 μm. The particle size disclosed in the patent is to make the product suitable for direct compression or powder direct compression. Capsule filling, and discloses a method for preparing escitalopram oxalat...

Examples

Embodiment 1

[0042]

[0043] Escitalopram oxalate API particle size median particle size D (V, 0.5) = 11 μm

[0044] Premix escitalopram oxalate, lactose monohydrate, microcrystalline cellulose, hydroxypropyl cellulose, and croscarmellose sodium in a high-shear granulator, add purified water to granulate, and use a rotary The granulator is wet sized, and the wet granules are dried in a fluidized bed. After drying, the granules are dried with a rotary granulator to obtain dry granules. The dry granules are mixed evenly with magnesium stearate in a single-arm hopper mixer, and the rotary tabletting is used. Machine-pressed tablet, tablet weight 120mg.

[0045] According to the determination method of content uniformity (Appendix XE content uniformity inspection method of Chinese Pharmacopoeia 2010 edition), according to the pharmacopoeia standard, it is qualified when A+1.8s≤15. The results are shown in Table 1.

[0046] : Table 1: Test results of content uniformity

[0047] s...

Embodiment 2

[0055]

[0056] Escitalopram oxalate API particle size median particle size D (V, 0.5) = 11 μm

[0057] Premix escitalopram oxalate, lactose monohydrate, microcrystalline cellulose, hydroxypropyl cellulose, and partially croscarmellose sodium in a high-shear granulator, add purified water to granulate, and use Rotary granulator wet sizing, wet granules are dried in a fluidized bed, after drying, the granules are dried by a rotary granulator to obtain dry granules, and the dry granules are sequentially added with part of croscarmellose sodium and magnesium stearate. The mixture was uniformly mixed sequentially in the arm hopper mixer, and tableted with a rotary tablet press, with a tablet weight of 98.5 mg.

Embodiment 3

[0059]

[0060] Escitalopram oxalate API particle size median particle size D (V, 0.5) = 11 μm

[0061]Premix escitalopram oxalate, lactose monohydrate, microcrystalline cellulose, hydroxypropyl cellulose, and croscarmellose sodium in a high-shear granulator, add 75% ethanol to granulate, and use Rotary granulator wet sizing, the wet granules are dried in a fluidized bed, and the dried granules are dried by a rotary granulator to obtain dry granules. The dry granules are mixed with a part of magnesium stearate in a single-arm hopper mixer. Rotary tablet press tablet, tablet weight 160mg.

technical field

[0001] The invention belongs to the technical field of medicine, and in particular relates to a tablet containing escitalopram oxalate and a preparation method thereof. Background technique

[0002] Escitalopram oxalate is an oral selective serotonin reuptake inhibitor (SSRI). Escitalopram oxalate is the S-isomer (single isomer) of racemic citalopram. Jointly developed by Forest Laboratories and Denmark Lundbeck, escitalopram oxalate tablets (trade name: ) was launched in the United States in 2002 and was launched in China in 2005. Citalopram oxalate has the following structural formula:

[0003]

[0004] The patent EP1414435 of Yuanyan Lingbei Company discloses a method for preparing escitalopram oxalate with an average particle size of 40 μm to 200 μm. The particle size disclosed in the patent is to make the product suitable for direct compression or powder direct compression. Capsule filling, and discloses a method for preparing escitalopram oxalat...

Examples

Embodiment 1

[0042]

[0043] Escitalopram oxalate API particle size median particle size D (V, 0.5) = 11 μm

[0044] Premix escitalopram oxalate, lactose monohydrate, microcrystalline cellulose, hydroxypropyl cellulose, and croscarmellose sodium in a high-shear granulator, add purified water to granulate, and use a rotary The granulator is wet sized, and the wet granules are dried in a fluidized bed. After drying, the granules are dried with a rotary granulator to obtain dry granules. The dry granules are mixed evenly with magnesium stearate in a single-arm hopper mixer, and the rotary tabletting is used. Machine-pressed tablet, tablet weight 120mg.

[0045] According to the determination method of content uniformity (Appendix XE content uniformity inspection method of Chinese Pharmacopoeia 2010 edition), according to the pharmacopoeia standard, it is qualified when A+1.8s≤15. The results are shown in Table 1.

[0046] : Table 1: Test results of content uniformity

[0047] s...

Embodiment 2

[0055]

[0056] Escitalopram oxalate API particle size median particle size D (V, 0.5) = 11 μm

[0057] Premix escitalopram oxalate, lactose monohydrate, microcrystalline cellulose, hydroxypropyl cellulose, and partially croscarmellose sodium in a high-shear granulator, add purified water to granulate, and use Rotary granulator wet sizing, wet granules are dried in a fluidized bed, after drying, the granules are dried by a rotary granulator to obtain dry granules, and the dry granules are sequentially added with part of croscarmellose sodium and magnesium stearate. The mixture was uniformly mixed sequentially in the arm hopper mixer, and tableted with a rotary tablet press, with a tablet weight of 98.5 mg.

Embodiment 3

[0059]

[0060] Escitalopram oxalate API particle size median particle size D (V, 0.5) = 11 μm

[0061]Premix escitalopram oxalate, lactose monohydrate, microcrystalline cellulose, hydroxypropyl cellulose, and croscarmellose sodium in a high-shear granulator, add 75% ethanol to granulate, and use Rotary granulator wet sizing, the wet granules are dried in a fluidized bed, and the dried granules are dried by a rotary granulator to obtain dry granules. The dry granules are mixed with a part of magnesium stearate in a single-arm hopper mixer. Rotary tablet press tablet, tablet weight 160mg.

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