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Lurasidone nanosuspension and preparation method thereof

A nano-suspension, lurasidone technology, applied in the directions of emulsion delivery, nervous system disease, liquid delivery, etc., can solve the problems of drop, poor water solubility, etc., and achieve simple process, increase solubility, and reduce particle size. Effect

Inactive Publication Date: 2015-08-05
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Lurasidone has poor water solubility and can be dissolved in organic solvents such as ethanol and methanol
[0004] Lurasidone preparations currently on the market only have ordinary tablets, which should be taken with food (> 350 calories, and does not contain fat), otherwise the average blood concentration of this product (C max ) and the area under the drug-time curve (AUC) decreased by 3 times and 2 times respectively, and dysphagia is one of the common adverse symptoms in patients with schizophrenia. compliance is very valuable

Method used

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  • Lurasidone nanosuspension and preparation method thereof
  • Lurasidone nanosuspension and preparation method thereof
  • Lurasidone nanosuspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Put 40mg of lurasidone in a beaker, add 3mL of methanol, and ultrasonically dissolve it as the organic phase; then take 40mg of sodium lauryl sulfate, 20mg of poloxamer F68, and 20mg of polyvinylpyrrolidone K30 in another beaker, 20 mL of deionized water was added therein, stirred and dissolved by a magnetic stirrer as the water phase. Under the condition of ice-water bath, slowly inject the organic phase into the water phase, and at the same time, use a high-speed disperser to disperse at a speed of 400r / min for 5 minutes to obtain the initial suspension, and circulate the initial suspension with a pressure of 1500bar and high-pressure homogeneity for 10 The second time, the organic solvent was removed by vacuum drying at 25°C for 24 hours. The particle size was measured by a Brookhaven Instruments-ZetaPlus nanometer particle size analyzer to be 159nm, the polydispersity coefficient was 0.082, and the zeta potential was -24.8mv.

[0039] Add 2.5 g of mannitol to the pr...

Embodiment 2

[0041] Put 40mg of lurasidone in a beaker, add 3mL of methanol, and ultrasonically dissolve it as the organic phase; then take 40mg of sodium lauryl sulfate, 20mg of poloxamer F68, and 20mg of polyvinylpyrrolidone K30 in another beaker, 20 mL of deionized water was added therein, stirred and dissolved by a magnetic stirrer as the water phase. Under the condition of ice-water bath, slowly inject the organic phase into the water phase, and at the same time, use a high-speed disperser to disperse at a speed of 400r / min for 5 minutes to obtain the initial suspension, and circulate the initial suspension with a pressure of 1500bar and high-pressure homogeneity for 10 The second time, the organic solvent was removed by vacuum drying at 25°C for 24 hours. The particle size was measured by a Brookhaven Instruments-ZetaPlus nanometer particle size analyzer to be 136nm, the polydispersity coefficient was 0.142, and the zeta potential was -22.8mv.

Embodiment 3

[0043] Take 40 mg of lurasidone and place it in a beaker, add 3 mL of methanol, and ultrasonically dissolve it as the organic phase; then take 40 mg of sodium lauryl sulfate, 10 mg of poloxamer F68, and 5 mg of polyvinylpyrrolidone K30 in another beaker, 20 mL of deionized water was added therein, stirred and dissolved by a magnetic stirrer as the water phase. Under the condition of ice-water bath, slowly inject the organic phase into the water phase, and at the same time, use a high-speed disperser to disperse at a speed of 400r / min for 5 minutes to obtain the initial suspension, and circulate the initial suspension with a pressure of 1500bar and high-pressure homogeneity for 10 The second time, the organic solvent was removed by vacuum drying at 25°C for 24 hours. The particle size was measured by Brookhaven Instruments-ZetaPlus nanometer particle size analyzer to be 281nm, the polydispersity coefficient was 0.054, and the zeta potential was -26.4mv.

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Abstract

A lurasidone nanosuspension and its preparation method are disclosed. The invention relates to the field of medicinal preparation, specifically to a lurasidone nanosuspension and a preparation method of a freeze-dried powder thereof. The suspension provided by the invention comprises, by weight, 2-20% of lurasidone, 1-36% of a stabilizer and 0-95% of a freeze-drying protective additive. The ratio of lurasidone to the stabilizer is 1:0.5-1:2. Particle size of the suspension is 130-460 nm. The invention also relates to a preparation method of the lurasidone nanosuspension. The lurasidone nanosuspension is prepared by combination of a precipitation method and a high-pressure homogenization method. The preparation method is suitable for industrial production. Quality of the prepared lurasidone nanosuspension is stable, and dissolution speed of lurasidone is raised.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a lurasidone nanosuspension and a preparation method thereof. Background technique [0002] Schizophrenia is a relatively common mental illness. According to the World Health Organization, the global lifetime prevalence of schizophrenia is about 3.8‰-8.4‰. At present, the pathogenesis of schizophrenia has not been fully elucidated. The onset of schizophrenia is often young adults with various symptoms, which are manifested as mental disorders in thinking, perception, volitional behavior, emotion, etc. Mental activity and inner experience. Schizophrenia generally has no disturbance of consciousness and obvious mental retardation, but it can damage some cognitive functions and deficits of social functions to varying degrees, and some patients will also experience a decline in mental activity. [0003] Lurasidone is a novel atypical antipsychotic indicated for the treatm...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/496A61P25/18
Inventor 张建军吴小每
Owner CHINA PHARM UNIV
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