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Technology for improving solubility of brexpiprazole and method for preparing brexpiprazole tablet

A technology of ebiprazole tablets and ebiprazole, which is applied to medical preparations containing no active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., and can solve problems such as limiting bioavailability

Inactive Publication Date: 2021-03-23
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Ebiprazole is a white or white crystalline powder that is nearly insoluble in water, limiting bioavailability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Prescription composition:

[0012] name 200 tablets (g) Ebiprazole 0.8 Mannitol (bulking agent) 18 Microcrystalline Cellulose (Filler) 12 Croscarmellose sodium (disintegrant) 2 Hydroxypropyl Cellulose (Binder) 1.2 Acesulfame K (flavoring agent) 0.2 Calcium hydrogen phosphate anhydrous (diluent, stabilizer) 1.2 Sodium stearyl fumarate (lubricant) 0.3 Colloidal anhydrous silica (lubricant) 0.3

[0013] Preparation Process:

[0014] (1) Take ebiprazole and carry out jet milling, mix the jet-milled ebiprazole and mannitol in a wet mixing granulator, add a wetting agent, dry, and granulate to prepare ebiprazole Azole solid dispersion;

[0015] (2) Mix the ebiprazole solid dispersion with the prescribed amount of disintegrating agent, filler, flavoring agent and lubricant, and then press into tablets to obtain ebiprazole tablets.

[0016] test results:

[0017] 1. Compressibility: good

[0018] 2. Appear...

Embodiment 2

[0022] Prescription composition:

[0023] name 200 tablets (g) Ebiprazole 0.8 Mannitol (bulking agent) 15 Microcrystalline Cellulose (Filler) 14.2 Croscarmellose sodium (disintegrant) 3 Hydroxypropyl Cellulose (Binder) 1.2 Acesulfame K (flavoring agent) 0.2 Calcium hydrogen phosphate anhydrous (diluent, stabilizer) 1.0 Sodium stearyl fumarate (lubricant) 0.3 Colloidal anhydrous silica (lubricant) 0.3

[0024] Preparation Process:

[0025] (1) Take ebiprazole and carry out jet milling, mix the jet-milled ebiprazole and mannitol in a wet mixing granulator, add a wetting agent, dry, and granulate to prepare ebiprazole Azole solid dispersion;

[0026] (2) Mix the ebiprazole solid dispersion with the prescribed amount of disintegrating agent, filler, flavoring agent and lubricant, and then press into tablets to obtain ebiprazole tablets.

[0027] test results:

[0028] 1. Compressibility: good

[0029] 2. Appe...

Embodiment 3

[0033] Prescription composition:

[0034] name 200 tablets (g) Ebiprazole 0.8 Lactose monohydrate (bulking agent) 13.2 Microcrystalline Cellulose (Filler) 14 Croscarmellose sodium (disintegrant) 3 Hydroxypropyl Cellulose (Binder) 1.6 Calcium hydrogen phosphate anhydrous (diluent, stabilizer) 2.5 Aspartame (flavoring agent) 0.3 Sodium stearyl fumarate (lubricant) 0.3 Colloidal anhydrous silica (lubricant) 0.3

[0035] Preparation Process:

[0036] (1) Take ebiprazole for jet milling, mix jet milled ebiprazole and lactose monohydrate evenly in a wet mixing granulator, add a wetting agent, dry and granulate to prepare ebiprazole Prazole solid dispersion;

[0037] (2) Mix the ebiprazole solid dispersion with the prescribed amount of disintegrating agent, filler, flavoring agent and lubricant, and then press into tablets to obtain ebiprazole tablets.

[0038] test results:

[0039] 1. Compressibility: good

[...

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PUM

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Abstract

The invention relates to a technology for improving the solubility of insoluble medicine of brexpiprazole and preparation of a brexpiprazole tablet, and belongs to the technical field of pharmaceutical preparations. Brexpiprazole is used as a medicinal active component for jet milling, and then a hydrophilic auxiliary material is used for preparing a solid dispersion, so that the highly dispersedstate of the medicine can be ensured; the solubility and the dissolution rate of insoluble medicine are effectively improved; and the bioavailability of the medicine is improved. Then, the solid dispersion is further prepared into tablets; the medicine absorption in the body is promoted; the bioavailability of the medicine is further improved; in addition, the preparation process is simple; dust pollution is avoided; industrial production is easy; and meanwhile, the medicine taking compliance of a patient is enhanced.

Description

[0001] The invention relates to a technology for improving the solubility of ebiprazole, an insoluble drug, and the preparation of ebiprazole tablets, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Ebiprazole is a new drug with anti-schizophrenia and anti-depressant effects developed by Lundbeck Pharmaceuticals of Denmark and Otsuka Pharmaceuticals of Japan for multiple targets of monoamine neurotransmitters. It is a serotonin-dopamine activity regulator. Dopamine D 2 In addition to partial receptor agonism, it also has D 3 Partial receptor agonism, 5-HT 1 Part A receptor agonism and 5-HT 2 Part A receptor antagonism, clinically used for adjuvant treatment of schizophrenia, adult ADHD and major depression. [0003] Ebiprazole is a white or white crystalline powder that is practically insoluble in water, thereby limiting bioavailability. Therefore, it is necessary to develop ebiprazole preparations with good solubility propert...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/26A61K31/496A61P25/18A61P25/24A61P25/14
CPCA61K9/2018A61K9/2095A61K31/496A61P25/14A61P25/18A61P25/24
Inventor 杨柳王宇杰
Owner BEIJING VENTUREPHARM BIOTECH
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