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Enzalutamide pharmaceutical composition and preparation method thereof

A technology of enzalutamide and composition, applied in the field of enzalutamide pharmaceutical composition and preparation thereof, can solve the problems of incompleteness, low bioavailability, low solubility and the like

Inactive Publication Date: 2018-03-09
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Enzalutamide is a poorly soluble drug with low solubility in aqueous solution and buffers with different pHs. If it is prepared into an ordinary oral solid preparation, such as tablet or capsule, the drug will dissolve slowly and incompletely, and the bioavailability low, which limits the efficacy of its oral preparations

Method used

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  • Enzalutamide pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Enzalutamide 20g

[0034] Hydroxypropyl-β-cyclodextrin 60g

[0035] Mannitol 20g

[0036] Microcrystalline Cellulose 20g

[0037] Croscarmellose Sodium 5g

[0038] 2% polyvinylpyrrolidone aqueous solution 100g

[0039] Magnesium Stearate 1g

[0040] Preparation Process:

[0041] Take the prescribed amount of hydroxypropyl-β-cyclodextrin and dissolve it in an appropriate amount of water to make a saturated aqueous solution. Pass enzalutamide through a 120 mesh sieve and dissolve it in an appropriate amount of ethanol. Under magnetic stirring, the ethanol solution of enzalutamide Slowly add the saturated aqueous solution of hydroxypropyl-β-cyclodextrin, continue stirring at room temperature for 3 hours after all the addition is complete, and remove most of the ethanol by rotary evaporation at 45°C. Put it into a shallow tray and put it in the freezer of the refrigerator. The pre-freezing time is 12 hours and the temperature is -50°C. When the temperature of the cold...

Embodiment 2

[0045] Enzalutamide 20g

[0046] Hydroxypropyl-β-cyclodextrin 20g

[0047] Mannitol 15g

[0048] Microcrystalline Cellulose 15g

[0049] Croscarmellose Sodium 2g

[0050] 2% polyvinylpyrrolidone aqueous solution 100g

[0051] Magnesium Stearate 2g

[0052] Its preparation process is with embodiment 1.

Embodiment 3

[0054] Enzalutamide 20g

[0055] Hydroxypropyl-β-cyclodextrin 40g

[0056] Mannitol 25g

[0057] Microcrystalline Cellulose 25g

[0058] Croscarmellose Sodium 5g

[0059] 2% polyvinylpyrrolidone aqueous solution 100g

[0060] Magnesium Stearate 2g

[0061]Its preparation process is with embodiment 1.

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Abstract

The invention belongs to the field of a pharmaceutical preparation, and specifically relates to enzalutamide tablets and a preparation method thereof. The enzalutamide tablets comprise enzalutamide, hydroxypropyl-beta-cyclodextrin, a filler, a disintegrating agent, an adhesive, and a lubricant. Enzalutamide coated with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) is extremely easy to be dissolvedin water. The stability of the tablets is improved, release of the medicine in the body is promoted, absorption is improved, and the bioavailability is increased.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to an enzalutamide pharmaceutical composition and a preparation method thereof. Background technique [0002] Enzalutamide, chemical name: 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-sulfur Oxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide, molecular formula: C21H16F4N4O2S, molecular weight: 464.44. [0003] Physical and chemical properties: This product is a white crystalline powder, easily soluble in N-methylpyrrolidone and acetonitrile, slightly soluble in methanol and absolute ethanol, almost insoluble in water. Enzalutamide is a new type of anticancer drug, which has been approved by the US FDA for the treatment of metastatic castration-resistant prostate cancer after docetaxel treatment. Patients treated with docetaxel were also effective. Enzalutamide is an androgen receptor inhibitor that acts on different steps in the androgen receptor sign...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4166A61K47/69A61K47/38A61P35/00
CPCA61K31/4166A61K9/2054
Inventor 严洁王志凤
Owner TIANJIN HANKANG PHARMA BIOTECH
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