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Pimavanserin nanocrystalline capsule and preparation method thereof

A technology of pimavanserin and nanocrystals, which is applied in the field of pimavanserin nanocrystal capsules and its preparation, and can solve the problems of poor dissolution rate and low bioavailability of pimavanserin

Inactive Publication Date: 2020-10-27
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved in the present invention is to overcome the problems of poor dissolution of pimavanserin and low bioavailability, and the invention provides a nanocrystalline capsule of pimavanserin and a preparation method thereof

Method used

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  • Pimavanserin nanocrystalline capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Take 2g of pimavanserin and 6g of poloxamer 188, add them to 60mL of water, and stir evenly with magnetic force; put the above mixed solution into a high-pressure homogenizer, control the temperature of the preparation process at 35°C, and circulate and homogenize under the pressure of 750Bar 3 times to obtain pimavanserin nanocrystal suspension; take the pimavanserin nanocrystal suspension and place it in a spray dryer for spray drying, and the spray drying inlet temperature is 120°C to obtain pimavanserin Nanocrystalline spray-dried product; pass the pimavanserin nanocrystalline spray-dried product through an 80-mesh sieve, mix it with the prescribed amount of spray-dried lactose, microcrystalline cellulose and magnesium stearate, and fill it into capsules to obtain pimavanserin Vanserin nanocrystalline capsules.

Embodiment 2

[0021] Take 2g of pimavanserin and 12g of poloxamer 188, add it to 200mL of water, and stir evenly with a magnetic force; put the above mixed solution into a high-pressure homogenizer, control the temperature of the preparation process at 35°C, and circulate and homogenize under the pressure of 750Bar 3 times to obtain pimavanserin nanocrystal suspension; take the pimavanserin nanocrystal suspension and place it in a spray dryer for spray drying, and the spray drying inlet temperature is 150°C to obtain pimavanserin Nanocrystalline spray-dried product; pass the pimavanserin nanocrystalline spray-dried product through an 80-mesh sieve, mix it with the prescribed amount of spray-dried lactose, microcrystalline cellulose and magnesium stearate, and fill it into capsules to obtain pimavanserin Vanserin nanocrystalline capsules.

Embodiment 3

[0023] Take 2g of pimavanserin and 8g of poloxamer 188, add it to 100mL of water, and stir evenly with a magnetic force; put the above mixed solution into a high-pressure homogenizer, control the temperature of the preparation process at 35°C, and circulate and homogenize under the pressure of 750Bar 3 times to obtain pimavanserin nanocrystal suspension; take the pimavanserin nanocrystal suspension and place it in a spray dryer for spray drying, and the spray drying inlet temperature is 150°C to obtain pimavanserin Nanocrystalline spray-dried product; pass the pimavanserin nanocrystalline spray-dried product through an 80-mesh sieve, mix it with the prescribed amount of spray-dried lactose, microcrystalline cellulose and magnesium stearate, and fill it into capsules to obtain pimavanserin Vanserin nanocrystalline capsules.

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Abstract

The invention belongs to the field of pharmaceutical preparations and particularly relates to a pimavanserin nanocrystalline capsule and a preparation method thereof. The preparation method comprisesthe following steps: 1) adding pimavanserin and poloxamer 188 to water, and carrying out mixing to obtain a mixed solution; 2) homogenizing the mixed solution for 3 times to obtain a suspension; 3) performing spray drying on the suspension in a spray dryer; and 4) after mixing with other auxiliary materials, performing capsule filling. The prepared pimavanserin capsule can significantly increase the dissolution rate so as to improve the bioavailability of the medicine in vivo.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a pimavanserin nanocrystal capsule and a preparation method thereof. Background technique [0002] Pimavanserin (Pimavanserin), chemical name, 1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)urea , the original research is Arcadia Pharmaceuticals. The reversal and antagonism of pimavanserin on 5-HT2A receptors has high targeting and specificity, and its selectivity is 40 times that of 5-HT2C receptors and dopamine receptors. The curative effect is good, the specificity is good, the deterioration of muscle movement is avoided, and the side effects are few. On February 9, 2014, it was granted the title of Breakthrough Therapy by the FDA. On April 29, 2016, it was approved by the FDA for the treatment of Parkinson's hallucinations and delusions. It is currently the first and only drug approved for the treatment of Parkinson's mental illness. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K47/10A61K31/4468A61P25/16
CPCA61K9/4866A61K31/4468A61P25/16
Inventor 李春王宇杰
Owner BEIJING VENTUREPHARM BIOTECH
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