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Composition containing fluoxertine hydrochloride and enteric acrylic resin and preparation method thereof

A technology for fluoxetine hydrochloride and a composition is applied in the field of a composition containing fluoxetine hydrochloride and enteric materials and the field of preparation thereof, which can solve the problems of high drug loss, influence on taste-masking effect, gritty feeling and the like, and achieve solvent-free residual effect

Inactive Publication Date: 2015-06-10
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method requires fluidized coating of the granules, which is a complex process. If the granules are too small, the coating process is prone to adhesion and is difficult to control; when the granules are large, it will cause a gritty feeling in the mouth, which is not suitable for making orally disintegrating tablets. , chewable tablets, in addition, the process of compressing tablets is also easy to break the coating film, which affects the taste-masking effect
Patent CN 102430122 discloses fluoxetine hydrochloride orally disintegrating tablets and its preparation method. Ion-exchange resin is used to mask the taste of fluoxetine hydrochloride. However, the taste-masking method has the disadvantages of more drug loss and slower drug dissolution. question

Method used

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  • Composition containing fluoxertine hydrochloride and enteric acrylic resin and preparation method thereof
  • Composition containing fluoxertine hydrochloride and enteric acrylic resin and preparation method thereof
  • Composition containing fluoxertine hydrochloride and enteric acrylic resin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Weigh 70g of enteric-coated acrylic resin Eudragit L30D-55 aqueous dispersion, add 300mL of water, and stir evenly to obtain a diluted resin aqueous dispersion solution; disperse 20g of fluoxetine hydrochloride drug powder in 100mL of water, stir evenly, and cut for 15min , to obtain a drug suspension; add the diluted resin water dispersion solution dropwise to the drug suspension, then add 15g of maltodextrin and 5g of micropowdered silica gel, and stir evenly. When the inlet air temperature is 180°C, the outlet air temperature is 105°C, and the feed rate is 420mL h -1 Under the condition of spray drying, the composition powder containing fluoxetine hydrochloride and enteric acrylic resin is obtained.

[0026] Fluoxetine hydrochloride orally disintegrating tablet prescription (percentage by weight):

[0027]

[0028] Mix the composition powder of prescription amount with microcrystalline cellulose, lactose, mannitol, low-substituted hydroxypropyl cellulose, asparta...

Embodiment 2

[0030] Weigh 360g of deionized water, add 36g of fluoxetine hydrochloride, and disperse under high shear for 15 minutes to obtain a drug suspension; weigh 96g of Eudragit L-30D-55, dissolve it with 1N sodium hydroxide solution, and obtain a resin water dispersion Add the drug suspension slowly to the resin aqueous dispersion solution, and stir continuously to obtain the drug resin solution; weigh 4 g each of aspartame and acesulfame potassium, 8 g of micropowder silica gel, add 40 mL of water, and mix evenly to prepare The suspension is added to the above drug resin solution, continuously stirred, the solid product is collected by suction filtration, dried at 45°C, crushed through a 120-mesh sieve to obtain a composition powder containing fluoxetine hydrochloride and enteric acrylic resin.

[0031] Fluoxetine hydrochloride orally disintegrating tablet prescription (percentage by weight):

[0032]

[0033]Mix the prescription amount of composition powder with microcrystallin...

Embodiment 3

[0035] Weigh 40g of hydroxypropylmethylcellulose phthalate (HP-55), dissolve it in 800mL of 80% (V / V) ethanol aqueous solution, add 20g of fluoxetine hydrochloride, stir to make it fully dissolve, then add 2g of micropowdered silica gel , Stir to make the dispersion uniform, remove the organic solvent by rotary evaporation, dry, pulverize and pass through a 100-mesh sieve to obtain a composition powder containing fluoxetine hydrochloride and enteric-coated materials.

[0036] Fluoxetine hydrochloride orally disintegrating tablet prescription (percentage by weight):

[0037]

[0038] Mix the composition powder of the prescribed amount with the above-mentioned auxiliary materials evenly, and directly compress the powder into tablets to obtain chewable tablets (each containing 20 mg of fluoxetine). According to the oral chewing test of 6 volunteers, the taste is good, without bitterness and numbness.

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Abstract

The invention provides a composition containing fluoxertine hydrochloride and enteric materials and a preparation method thereof. The mass ratio between the enteric materials and the fluoxertine hydrochloride ranges from 1:3 to 3:1, and the composition further contains additives which can be used in pharmaceutic preparation. The preparation method of the composition is a spray drying method, or a solvent evaporation method, or a sedimentation centrifugal method or a filtration method. According to the method, the preparation technology is simple, no coating is needed, obtained products are in a powder state or can be produced into powder or small particles by smashing and screening, the bitter taste masking effect is good, and it can be achieved that medicine is dissolved out rapidly in an acid gastric juice medium. By the adoption of conventional preparation technologies, the composition can be further produced into oral preparation forms such as oral cavity disintegration tablets, dispersible tablets, chewable tablets and dry suspension.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a composition containing fluoxetine hydrochloride and enteric materials and a preparation method thereof. Background technique [0002] Fluoxetine hydrochloride, (+ / -)-N-methyl-3-(p-trifluoromethylphenoxy)-3-phenylpropylamine hydrochloride, is a serotonin (5-HT) The reuptake inhibitor can selectively inhibit the uptake of pre-synaptic 5-HT release in the central nervous system, thereby increasing the concentration of 5-HT in the synaptic cleft, and is suitable for treating various depressive neurological disorders. Because of its small dose, obvious drug effect and mild side effects, it has a good application prospect in the clinical treatment of depression. [0003] However, fluoxetine hydrochloride is both bitter and numb, and has a very poor taste, which limits the development and application of its diversified oral pharmaceutical preparations, such as fast-...

Claims

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Application Information

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IPC IPC(8): A61K47/32A61K47/38A61K47/34A61K31/138A61P25/24
Inventor 赵会英孔圆圆
Owner BEIJING UNIV OF CHEM TECH