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Solid dispersion system containing lurasidone hydrochloride and preparation thereof

A technology of lurasidone hydrochloride and solid dispersion, applied in the field of pharmaceutical preparations, can solve the problems of affecting bioavailability, incomplete dissolution, slow dissolution rate and the like

Inactive Publication Date: 2019-06-28
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The low solubility of lurasidone hydrochloride leads to problems such as incomplete dissolution and slow dissolution rate, which directly affect its bioavailability

Method used

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  • Solid dispersion system containing lurasidone hydrochloride and preparation thereof
  • Solid dispersion system containing lurasidone hydrochloride and preparation thereof
  • Solid dispersion system containing lurasidone hydrochloride and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1: Lurasidone Hydrochloride-Polyethylene Glycol 6000 Solid Dispersion and Preparation

[0019] 1. Preparation of lurasidone hydrochloride-polyethylene glycol 6000 solid dispersion

[0020] Lurasidone Hydrochloride 25g Macrogol 6000 50g Methanol 100g

[0021] Add lurasidone hydrochloride to the molten polyethylene glycol 6000, control the temperature at 40-50°C, add methanol dropwise while stirring until the solid is completely dissolved, keep stirring for 15 minutes, distill methanol under reduced pressure at 50-60°C, and the solid in Solidify below -15°C for 2 hours, pulverize, and pass through a 100-mesh sieve to obtain lurasidone hydrochloride solid dispersion.

[0022] 2. Preparation of preparations

[0023] The lurasidone hydrochloride solid dispersion prepared above is mixed in proportion with the following pharmaceutical excipients to prepare tablets:

[0024]

[0025] Preparation Process:

[0026] 1) Lurasidone hydrochloride-polyethylene glycol 60...

Embodiment 2

[0030] Example 2: Lurasidone Hydrochloride-Polyethylene Glycol 4000 Solid Dispersion and Preparation

[0031] 1. Preparation of lurasidone hydrochloride-polyethylene glycol 4000 solid dispersion

[0032] Lurasidone Hydrochloride 25g Macrogol 4000 50g Methanol 50g

[0033] Add lurasidone hydrochloride to the molten polyethylene glycol 4000, control the temperature at 40-50°C, add methanol dropwise while stirring until the solid is completely dissolved, keep stirring for 15 minutes, distill methanol under reduced pressure at 50-60°C, and the solid in Solidify below -15°C for 2 hours, pulverize, and pass through a 100-mesh sieve to obtain lurasidone hydrochloride solid dispersion.

[0034] 2. Preparation of preparations

[0035] The lurasidone hydrochloride solid dispersion prepared above is mixed in proportion with the following pharmaceutical excipients to prepare tablets:

[0036]

[0037] Preparation Process:

[0038] 1) Lurasidone hydrochloride-polyethylene glycol 400...

Embodiment 3

[0042] Example 3: Lurasidone Hydrochloride-Poloxamer 188 Solid Dispersion and Preparation

[0043] 1. Preparation of lurasidone hydrochloride-poloxamer 188 solid dispersion

[0044] Lurasidone Hydrochloride 50g Poloxamer 188 100g Methanol 150g

[0045]Add lurasidone hydrochloride to the molten poloxamer 188, control the temperature at 40-50°C, add methanol dropwise while stirring until the solid is completely dissolved, keep stirring for 15 minutes, distill the methanol under reduced pressure at 50-60°C, and the solid in Solidify below -15°C for 2 hours, pulverize, and pass through a 100-mesh sieve to obtain lurasidone hydrochloride solid dispersion.

[0046] 2. Preparation of preparations

[0047] The lurasidone hydrochloride solid dispersion prepared above is mixed in proportion with the following pharmaceutical excipients to prepare tablets:

[0048]

[0049] Preparation Process:

[0050] 1) Lurasidone hydrochloride-poloxamer 188 solid dispersion, mannitol, partially...

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Abstract

The invention discloses a solid preparation of a solid dispersion system containing lurasidone hydrochloride. Lurasidone hydrochloride and a carrier material are prepared into the solid dispersion system, the prepared solid dispersion system and suitable medicinal auxiliary materials are prepared into an oral solid preparation. The solid preparation of the solid dispersion system containing lurasidone hydrochloride has the advantages of being rapid in dissolution and high in biological utilization rate. The problem that dissolution is not complete and the dissolution speed is low due to the low solubility of lurasidone hydrochloride is solved; according to the preparation method, lurasidone hydrochloride does not need to be subjected to micronization, and the problems that in the prior art, due to the micronization operation, the surface of lurasidone hydrochloride carries static electricity, and the compression formability is poor are solved.

Description

technical field [0001] The invention relates to a lurasidone hydrochloride solid dispersion and an oral solid preparation containing the lurasidone hydrochloride solid dispersion, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Schizophrenia is a common mental illness whose etiology has not been fully elucidated. It usually occurs in young adults, often accompanied by obstacles in perception, thinking, emotion, and behavior, and generally unconsciousness and mental retardation. The course of the disease is often protracted and recurrent, and some patients suffer from mental activity decline and varying degrees of social function impairment, which brings serious burdens to the society, patients and their families. With the development of society and the increasing pressure of life, people's demand for antipsychotic drugs is increasing day by day. [0003] Atypical antipsychotic drugs have become the first-line antipsychotic drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/496A61K47/10A61P25/18
Inventor 王少辰王宇杰
Owner BEIJING VENTUREPHARM BIOTECH
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