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Lurasidone composition

A technology of lurasidone and its composition, which is applied in the field of drug inclusion compounds containing lurasidone, can solve problems such as intolerance of patients, affect bone development, severe burning pain, etc., and achieve the effect of improving water solubility

Inactive Publication Date: 2012-11-28
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, benzyl alcohol has a common clinical side effect: gluteal muscle contracture. This is because benzyl alcohol is not easily absorbed by the body, and if it accumulates at the injection site for a long time, it will cause necrosis of surrounding muscles, and in severe cases, even affect the development of bones.
DMF is used as an additive for injection, which can cause skin swelling and severe burning pain, which is usually difficult for patients to tolerate

Method used

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  • Lurasidone composition
  • Lurasidone composition
  • Lurasidone composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Mix and dissolve 10 g of SBECD and 30 ml of water, then add 0.5 g of lurasidone hydrochloride, stir and dissolve at room temperature, and filter through a 0.2 μm filter to sterilize. The filtrate is divided into ampoules and freeze-dried by a freeze dryer to obtain clathrates.

Embodiment 2

[0028] Mix and dissolve 10 g of HBECD and 30 ml of water, then add 0.5 g of lurasidone hydrochloride, stir and dissolve at room temperature, and filter through a 0.2 μm filter to sterilize. The filtrate is divided into ampoules and freeze-dried by a freeze dryer to obtain clathrates.

Embodiment 3

[0030] Mix and dissolve 10 g of SBECD and 40 ml of water, then add 0.5 g of lurasidone mesylate, stir and dissolve at room temperature, and filter through a 0.2 μm filter to sterilize. The filtrate is divided into ampoules and freeze-dried by a freeze dryer to obtain clathrates.

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Abstract

The invention discloses a lurasidone composition, which consists of lurasidone or pharmaceutically acceptable salt and cyclodextrin, wherein the cyclodextrin is hydroxypropyl-beta-cyclodextrin or sulfobutylether-beta-cyclodextrin. By the composition, the water solubility of the lurasidone and the pharmaceutically acceptable salt can be improved; and a feasible preparation method is provided for a lurasidone injection preparation.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing lurasidone, in particular to a drug inclusion compound containing lurasidone. Background technique [0002] Mental illness is a common and serious disease in humans, with an incidence rate of about one percent of the population. With the acceleration of the pace of life and the increase of social interactions, mental illness has become a frequent disease, especially in cities with a relatively concentrated population. Currently, the global market for antipsychotics has an annual sales of $16.2 billion, making it the fifth largest therapeutic category after cholesterol-lowering drugs. [0003] According to statistics, among mental patients, 15-35% of inpatients and 20-65% of outpatients refuse to take medicine and need to be administered by injection. However, in the current antipsychotic drugs, the types of injections are lacking. [0004] Among the existing anti-schizophrenia drugs, h...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K47/40A61P25/18
Inventor 隋强包泳初王小梅王凤娟翟雪时惠麟陈庆华
Owner SHANGHAI INST OF PHARMA IND
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