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Anti-schizophrenia composition and application thereof

A technology for schizophrenia and a composition, applied in the field of medicine, can solve the problems of diabetes, increased cardiometabolic risk, weight gain, etc., and achieve the effect of reducing weight gain and reducing side effects

Pending Publication Date: 2022-04-08
JIANGSU OCEAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Second-generation (atypical antipsychotics) associated with increased weight gain, diabetes, and cardiometabolic risk

Method used

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  • Anti-schizophrenia composition and application thereof
  • Anti-schizophrenia composition and application thereof
  • Anti-schizophrenia composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Evaluation of the efficacy of olanzapine combined with SEP-363856 on the climbing model of mice induced by APO in the animal model of schizophrenia

[0026] Experimental animals: 72 adult male ICR mice, weighing (22±4g), purchased from Pizhou Dongfang Breeding Farm, certificate number: NO.202149615.

[0027] Experimental materials: Olanzapine was purchased from Aladdin Reagent Network; the purity of SEP-363856 was >95%. Apomorphine (APO) was purchased from Sigma-Aldrich Chemical Co.

[0028] Dispensing method:

[0029] Olanzapine:

[0030]Accurately weigh 2mg, 3mg, 5mg of olanzapine, dissolve in the minimum volume of glacial acetic acid, adjust the pH value to 6.0 with 0.1M NaOH, and then add purified water. Prepare solutions with concentrations of 0.1mg / mL, 0.3 mg / mL, and 0.6mg / mL, respectively.

[0031] SEP-363856:

[0032] Accurately weigh SEP-363856, 2mg, 3mg, 6mg, and dissolve in pure water. Prepare solutions with concentrations of 0.1mg / mL, 0.3mg / ...

Embodiment 2

[0042] Example 2: Evaluation of the efficacy of olanzapine combined with SEP-363856 on the hyperactive mouse model induced by the animal model of schizophrenia MK-801

[0043] Experimental animals: 72 adult male ICR mice, weighing (22±4g), purchased from Pizhou Dongfang Breeding Farm, certificate number: NO.202149615.

[0044] Experimental materials: Olanzapine was purchased from Aladdin Reagent Network; the purity of SEP-363856 was >95%. Dizozepine maleate (MK-801) was purchased from Shanghai Macklin Biochemical Co., Ltd.

[0045] Dispensing method:

[0046] Olanzapine:

[0047] Accurately weigh 2mg of olanzapine, dissolve it in the minimum volume of glacial acetic acid, and adjust the pH value to 6.0 with 0.1M NaOH, then add purified water to prepare a 3mg / kg solution. Diluted into solutions with concentrations of 0.01mg / mL, 0.03mg / mL, and 1mg / mL, respectively.

[0048] SEP-363856:

[0049] Accurately weigh SEP-3638563mg, dissolve it in purified water to prepare a 3mg / k...

Embodiment 3

[0060] Example 3: Evaluation of the efficacy of olanzapine combined with SEP-363856 in the water maze model induced by the animal model of schizophrenia MK-801

[0061] Experimental animals: 72 adult male ICR mice, weighing (22±4g), purchased from Pizhou Dongfang Breeding Farm, certificate number: NO.202149615.

[0062] Experimental materials: Olanzapine was purchased from Aladdin Reagent Network; the purity of SEP-363856 was >95%. Dizozepine maleate (MK-801) was purchased from Shanghai Macklin Biochemical Co., Ltd.

[0063] Dispensing method:

[0064] Olanzapine:

[0065] Accurately weigh 2mg of olanzapine, dissolve it in the minimum volume of glacial acetic acid, and adjust the pH value to 6.0 with 0.1M NaOH, then add purified water to prepare a 3mg / kg solution. Diluted into solutions with concentrations of 0.005mg / mL, 0.01mg / mL, and 0.02mg / mL, respectively.

[0066] SEP-363856:

[0067] Accurately weigh 3mg of SEP-363856, dissolve it in purified water to make a 3mg / kg ...

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Abstract

The invention discloses an anti-schizophrenia composition and application thereof, SEP-363856 and olanzapine are combined to have a synergistic anti-schizophrenia effect, so that the use dosage of olanzapine can be remarkably reduced, side effects caused by olanzapine can be relieved, and the composition can be used for treating the positive symptoms of schizophrenia, such as the positive symptoms of olanzapine, the positive symptoms of olanzapine and the negative symptoms of olanzapine. Compared with the prior art, the pharmaceutical composition has the advantages that the pharmaceutical composition has better effects on the side effects caused by cognitive impairment and olanzapine compared with single use of the two substances, and olanzapine and SEP-363856 are combined to prepare the anti-schizophrenia medicine, so that the pharmaceutical composition has a good application value and a wide development prospect.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an anti-schizophrenia composition and its application. Background technique [0002] Schizophrenia is a psychiatric disorder characterized by continuous or recurrent episodes of psychosis and affects approximately 1% of the population worldwide. The main symptoms include positive symptoms (eg, hallucinations and delusions, disorganized thinking), mostly caused by excess dopamine (DA) in the mesolimbic system; negative symptoms (eg, willpower and psychomotor impoverishment) and cognitive deficits (eg, memory loss and Attention deficit disorder) is thought to result from a lack of DA in the prefrontal cortex (PFC); although schizophrenia has been extensively studied, its etiology and pathology have not been largely elucidated. So far, the exploration of the pathogenesis of schizophrenia has not been successful. This makes it extremely difficult to develop a method that can treat all three...

Claims

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Application Information

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IPC IPC(8): A61K31/5513A61K31/381A61P25/18A61P25/28
Inventor 张桂森梁灵芝庄涛
Owner JIANGSU OCEAN UNIV
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