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Tadalafil solid dispersion and its tablet

A technology of solid dispersion and tadalafil, which is applied in the directions of non-active ingredients medical preparations, pill delivery, organic active ingredients, etc. problems, to achieve the effect of improving poor oral absorption, simple preparation process and reducing dosage

Inactive Publication Date: 2017-12-22
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Tadalafil currently available in the market only has ordinary tablets, because tadalafil has poor water solubility and low bioavailability, so the oral dosage of ordinary tablets sold in the market is large, and there are many adverse reactions

Method used

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  • Tadalafil solid dispersion and its tablet
  • Tadalafil solid dispersion and its tablet
  • Tadalafil solid dispersion and its tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1 The preparation of tadalafil solid dispersion

[0031] Take 100 mg of tadalafil, add it to 80 ml of absolute ethanol, and dissolve it by ultrasonication, weigh 100 mg of PVP K30 and add it to the above absolute ethanol solution, and dissolve it by ultrasonication. Put the ethanol solution on a rotary evaporator at 60°C to evaporate under reduced pressure to remove absolute ethanol, dry the product in a vacuum oven for 24 hours, pulverize, grind and sieve to obtain a solid dispersion of tadalafil.

Embodiment 2

[0032] Embodiment 2 The preparation of tadalafil solid dispersion

[0033] Take 100 mg of tadalafil, add it to 80 ml of absolute ethanol, and dissolve it by ultrasonication, weigh 500 mg of PVP K30 and add it to the above absolute ethanol solution, and dissolve it by ultrasonication. Put the ethanol solution on a rotary evaporator at 60°C to evaporate under reduced pressure to remove absolute ethanol, dry the product in a vacuum oven for 24 hours, pulverize, grind and sieve to obtain a solid dispersion of tadalafil.

Embodiment 3

[0034] Embodiment 3 The preparation of tadalafil solid dispersion

[0035] Take 100 mg of tadalafil, add it to 80 ml of absolute ethanol, and dissolve it by ultrasonication, weigh 300 mg of PVP K30 and add it to the above absolute ethanol solution, and dissolve it by ultrasonication. Put the ethanol solution on a rotary evaporator at 60°C to evaporate under reduced pressure to remove absolute ethanol, dry the product in a vacuum oven for 24 hours, pulverize, grind and sieve to obtain a solid dispersion of tadalafil.

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Abstract

The invention discloses a preparation method of tadalafil solid dispersion: dissolving tadalafil and a carrier material in absolute ethanol, and evaporating under reduced pressure at 50-90°C to obtain it; the tadalafil and The mass ratio of the carrier material is 1:0.5-1:13; the carrier material is selected from one or both of polyvinylpyrrolidone K30 and poloxamer. The present invention also provides a tadalafil solid dispersion tablet: made of tadalafil solid dispersion, filler, disintegrant, lubricant, wherein, the amount of filler accounts for 40% of the total weight of the tablet % to 70%; the amount of disintegrant accounts for 0.5% to 10% of the total weight of the tablet; the amount of lubricant accounts for 0.1% to 5% of the total weight of the tablet. The tadalafil solid dispersion and the tablet of the invention improve the in vitro dissolution rate of the tadalafil, and improve the disadvantages of poor oral absorption and low bioavailability.

Description

technical field [0001] The invention relates to a tadalafil solid dispersion, a tablet thereof, and a preparation method thereof. Background technique [0002] Erectile dysfunction (ED) is the inability to consistently obtain or maintain an erection sufficient for sexual intercourse. ED is one of the common diseases of andrology, its incidence rate accounts for about 10% of adult males, and its prevalence rate increases gradually with age. With the in-depth study of the pathogenesis of ED, the treatment of ED has also made a breakthrough. Sildenafil is the first approved selective phosphodiesterase inhibitor type 5 (PED-5) and is considered to be the first oral drug that can effectively treat ED. The currently marketed PED-5 inhibitor There are three kinds, namely sildenafil, vardenafil, and tadalafil, among which tadalafil is the only ED drug that is not affected by diet, and has a long half-life (17.5h) and good tolerance Etc. [0003] The chemical name of tadalafil is...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/20A61K31/4985A61K47/32A61K47/10A61P15/10
Inventor 黄桂华王龙梅刘聪慧李爱国
Owner SHANDONG UNIV
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