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Lurasidone pharmaceutical composition and preparation method thereof

A technology of lurasidone and lurasidone hydrochloride is applied in the field of preparation compositions and preparations of antipsychotic drugs, and can solve patient injury, organic solvent types, dosage or content restrictions, hidden dangers in production safety, etc. problems, to avoid waste of raw materials, eliminate grinding and sieving, and improve production efficiency

Active Publication Date: 2014-12-31
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the solubility of lurasidone or its free form in water is less than a few micrograms per milliliter, it has been difficult to prepare aqueous preparations containing high concentrations of lurasidone or its free form, and no research has been done on the solubility of lurasidone or its free form in water. Methods of lurasidone and its free form
The above two inventions mainly use the addition of organic solvents for solubilization. The potential problem is that organic solvents may cause harm to patients, such as local irritation, hemolysis, neurotoxicity, etc. Therefore, the type, dosage or content of organic solvents in the solution restricted
In addition, there are major hidden dangers in production safety, which will also cause harm to the health of operators in the production process, so try to avoid using them in the production process
[0016] In summary, there is a lack of a solution in the prior art that can provide a lurasidone drug that increases the solubility of the insoluble drug lurasidone and improves the dissolution rate of lurasidone on the basis of not limiting the particle size of the raw material combination

Method used

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  • Lurasidone pharmaceutical composition and preparation method thereof
  • Lurasidone pharmaceutical composition and preparation method thereof
  • Lurasidone pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] composition:

[0048] Lurasidone Hydrochloride 40 g

[0049] Hydroxypropyl-beta-cyclodextrin 86 g

[0050] Lactose 27.5 g

[0051] Croscarmellose Sodium 3.5 g

[0052] Hypromellose 2 g

[0053] Magnesium stearate 1 g

[0054] Preparation method: Add hydroxypropyl-β-cyclodextrin to water and stir to dissolve, add lurasidone hydrochloride to ethanol to dissolve, add the ethanol solution to the aqueous solution, continue to stir until the solution is clear, and spray dry to obtain lurasidone Ketocyclodextrin inclusion complex. Add lurasidone inclusion compound, lactose, and croscarmellose sodium into the fluidized bed, mix well, and then add hypromellose to granulate. Add magnesium stearate, mix well, and press into 1000 tablets.

[0055]

Embodiment 2

[0057] composition:

[0058] Lurasidone Hydrochloride 40 g

[0059] Hydroxypropyl-beta-cyclodextrin 114 g

[0060] Lactose 28.5 g

[0061] Sodium carboxymethyl starch 8 g

[0062] Hypromellose 8 g

[0063] Magnesium stearate 1 g

[0064] Preparation method: Add hydroxypropyl-β-cyclodextrin to water and stir to dissolve, add lurasidone hydrochloride to ethanol to dissolve, add the ethanol solution to the aqueous solution, continue to stir until the solution is clear, and spray dry to obtain lurasidone Ketocyclodextrin inclusion complex. Add lurasidone inclusion complex, lactose, and sodium carboxymethyl starch into the fluidized bed, mix well, and then add hypromellose to granulate. Add magnesium stearate, mix well, and press into 1000 tablets.

[0065]

Embodiment 3

[0067] composition:

[0068] Lurasidone Hydrochloride 40 g

[0069] β-cyclodextrin 128 g

[0070] Mannitol 22.5 g

[0071] Sodium carboxymethyl starch 4 g

[0072] povidone 4 g

[0073] Magnesium stearate 1.5 g

[0074] Preparation method: add β-cyclodextrin to water and stir to dissolve, add lurasidone hydrochloride to ethanol to dissolve, add the ethanol solution to the aqueous solution, continue to stir until the solution is clear, and spray dry to obtain lurasidone cyclodextrin clathrate. Add lurasidone clathrate, mannitol and sodium carboxymethyl starch into the fluidized bed, mix well, then add povidone to granulate. Add magnesium stearate, mix well, and press into 1000 tablets.

[0075]

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Abstract

The invention provides a lurasidone pharmaceutical composition, which contains lurasidone or its acid addition salt and cyclodextrin, wherein the lurasidone or its acid addition salt and cyclodextrin are in a mole ratio of 1:1-2. The lurasidone pharmaceutical composition provided by the invention can be prepared into an oral solid preparation, no harsh restriction is needed for the particle size of the raw materials, and waste of raw materials can be avoided. The lurasidone pharmaceutical composition can be prepared into sterile powder for injection, lurasidone can well dissolve, and adding of an organic solvent is avoided.

Description

technical field [0001] The invention relates to a preparation composition of antipsychotic drugs and a preparation method thereof, in particular to a preparation composition of lurasidone and a preparation method thereof. Background technique [0002] Lurasidone hydrochloride, chemical name: (3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-Benzisothiazol-3-yl)piperazine- 1-ylmethyl]cyclohexylmethyl}hexahydro-4,7-methylene-2H-isoindole-1,3-dione hydrochloride. [0003] This product is an atypical antipsychotic drug. In October 2010, the U.S. FDA approved the listing of Lurasidone Hydrochloride Tablets of Sumitomo Pharmaceutical Co., Ltd., Japan. The trade name is Latuda. It is suitable for the treatment of schizophrenia patients. The mechanism of action has not been clarified. It has been suggested that the effectiveness of lurasidone in schizophrenia is mediated by combined antagonism of central type 2 dopamine (D2) and type 2 serotonin (5HT2A) receptors, positive and Negative sympto...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/496A61P25/18
Inventor 刘峰樊俊红耿佳杨汉煜郑利刚郭文敏王旭亮王丙林容彦华安印华白晓雪张琪
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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