Preparation method of cariprazine-hydrophilic material blend solid preparation

A technology of hydrophilic materials and solid preparations, which is applied in the direction of drug combinations, pharmaceutical formulations, organic active ingredients, etc., and can solve problems that affect the therapeutic effect, are difficult to dissolve, and affect bioavailability

Inactive Publication Date: 2019-04-09
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Cariprazine is almost insoluble in water and difficult to dissolve in solid preparations, which seriously affects its bioavailability and thus affects the therapeutic effect

Method used

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  • Preparation method of cariprazine-hydrophilic material blend solid preparation
  • Preparation method of cariprazine-hydrophilic material blend solid preparation
  • Preparation method of cariprazine-hydrophilic material blend solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012]

[0013] Preparation Process

[0014] Mix cariprazine and 10 times the weight of lactose through an 80-mesh sieve for 3 times, add microcrystalline cellulose and sodium carboxymethyl starch and pass through an 80-mesh sieve for 3 times and mix well, 2% hydroxypropyl cellulose is used as a binder, Granulate with a 24-mesh sieve, air-dry at 50°C, dry to 1-3% moisture, pass the dried granules through a 24-mesh sieve for granulation, weigh, convert the yield, add sodium carboxymethyl starch, aspartame and Magnesium stearate, mix-filled capsules.

Embodiment 2

[0016]

[0017] Preparation Process

[0018] Mix cariprazine and 15 times the weight of mannitol through an 80 mesh sieve for 5 times, add microcrystalline cellulose and pass through an 80 mesh sieve for 3 times and mix evenly, 2% povidone is used as a binder, 30 mesh sieve is granulated, 50 Blow dry at ℃, dry to 1~3% moisture, pass the dried granules through a 30-mesh sieve to sieve, weigh, convert the yield, add sodium carboxymethyl starch, silicon dioxide and mint essence, mix and fill capsules.

Embodiment 3

[0020]

[0021] Preparation Process

[0022] Mix cariprazine and 30 times the weight of lactose through an 80-mesh sieve for 4 times, add the remaining lactose, microcrystalline cellulose and sodium carboxymethyl starch, pass through an 80-mesh sieve for 3 times and mix well, and use 2% povidone as a binder , 24-mesh sieve granulation, blast drying at 50 ℃, drying to 1~3% moisture, passing the dried granules through a 24-mesh sieve for granulation, weighing, conversion yield, plus aspartame, magnesium stearate, Mix filling capsules.

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PUM

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Abstract

The invention discloses a preparation method of a cariprazine-hydrophilic material blend solid preparation. The solid preparation comprises a cariprazine-hydrophilic material blend and other pharmaceutically acceptable ingredients, wherein the cariprazine-hydrophilic material blend effectively improves the dissolution speed of cariprazine in the solid preparation, is favorable for improving the bioavailability of a drug, and is used to treat a patient with schizophrenia and diphasic I type related psychlampsia or mixed episode, and the process is simple and convenient and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a cariprazine dissolution solid preparation and a preparation method thereof. Background technique [0002] The chemical name of cariprazine (CARIPRAZINE) is N'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N , N-dimethylurea, a once-daily oral atypical antipsychotic drug, can partially stimulate D3 / D2 receptors, which preferentially bind to D3 receptors. The mechanism for the treatment of schizophrenia and bipolar disorder is not yet clear, and its therapeutic effect may be through partially activating D2 receptors and 5-hydroxytryptamine 1A receptors, and antagonizing 5-HT2A receptors. [0003] Cariprazine is an atypical antipsychotic first developed by FOREST RES INST INC for the treatment of acute manic or mixed episodes associated with schizophrenia and bipolar I disorder. New data from a phase 3 clinical trial of carip...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K47/26A61K31/495A61P25/18
CPCA61K9/4858A61K31/495
Inventor 刘英甜马莉
Owner BEIJING VENTUREPHARM BIOTECH
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