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Oral preparation of enzalutamide solid dispersion

A technology of solid dispersion and enzalutamide, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problem of complex soft capsule preparation process and low dissolution rate of preparations , Low bioavailability and other problems, to achieve the effect of improving bioavailability, improving dissolution rate, and simple preparation process

Active Publication Date: 2015-11-11
FERGUSON WUHAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the dissolution rate of the preparation produced by this method is not high, and its bioavailability is also low, and it is easy to precipitate crystals after entering the human body.
Moreover, the stability of enzalutamide and caprylic capric macrogol glyceride is relatively poor. The original preparation adopts the compound antioxidant of BHT and BHA to improve its stability, but these two antioxidants are not effective in clinical practice. The safety is poor, and the soft capsule preparation process is complicated and the cost is high

Method used

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  • Oral preparation of enzalutamide solid dispersion
  • Oral preparation of enzalutamide solid dispersion
  • Oral preparation of enzalutamide solid dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] 1) Get ethyl cellulose, hydroxypropyl methyl cellulose, povidone K30, polyethylene glycol 6000, poloxamer each 60g respectively, dissolve in the ethanol aqueous solution that mass concentration is 60%, obtain the concentration of 20% water-soluble polymer carrier solution;

[0026] 2) Disperse 40g of enzalutamide in the above-mentioned five kinds of water-soluble polymer carrier solutions, stir and homogenize, then spray dry, control the inlet air temperature to 150°C, the outlet air temperature to 60°C, and the feed rate to be 10mL / min, spray pressure is 0.3MPa, obtain enzalutamide solid dispersion;

[0027] 3) Add 80g of lactose (filler), 10g of croscarmellose sodium (disintegrant), and 2g of magnesium stearate (lubricant) to each of the five enzalutamide solid dispersions, and mix well Tablet.

[0028] 1. Dissolution Determination

[0029] Take the tablet prepared in the above example 1 and 6 capsules of the original enzalutamide soft capsule, according to the dis...

Embodiment 2

[0044] Enzalutamide tablets, made from the following raw materials:

[0045]

[0046] The preparation method is:

[0047] 1) dissolving povidone K30 in 50% ethanol aqueous solution to obtain a water-soluble polymer carrier solution with a mass concentration of 15%;

[0048] 2) Disperse enzalutamide in the water-soluble polymer carrier solution, stir and homogenize, then spray dry. The air pressure is 0.1MPa to obtain a solid dispersion of enzalutamide;

[0049] 3) Add microcrystalline cellulose, croscarmellose sodium, and magnesium stearate to the solid dispersion of enzalutamide, mix well and then compress into tablets.

[0050] Each tablet of this product contains 40mg of enzalutamide, and the dosage is 1 tablet each time, once a day.

Embodiment 3

[0052] Enzalutamide capsules, made from the following ingredients:

[0053]

[0054] The preparation method is:

[0055] 1) dissolving povidone in 70% ethanol aqueous solution to obtain a water-soluble polymer carrier solution with a mass concentration of 30%;

[0056]2) Disperse enzalutamide in the water-soluble polymer carrier solution, stir and homogenize, then spray dry, control the inlet air temperature to 160°C, the outlet air temperature to 70°C, the feed rate to 20mL / min, Air pressure is 0.5MPa, obtains enzalutamide solid dispersion;

[0057] 3) Add starch and magnesium stearate to the enzalutamide solid dispersion, mix well and fill with capsules to make capsules.

[0058] Each capsule of this product contains 40mg of enzalutamide, and the dosage is 1 tablet each time, once a day.

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Abstract

The invention discloses an oral preparation of enzalutamide solid dispersion. The oral preparation contains enzalutamide with effective dose, and also contains a water-soluble polymer carrier for dispersing enzalutamide, wherein the weight ratio of enzalutamide to the water-soluble polymer carrier is 1 to 0.5-3. With the oral preparation, the solubility and the dissolution rate of enzalutamide in the preparation is effectively improved, so that the bioavailability of enzalutamide is improved, and the quality stability and safety of enzalutamide are improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a solid dispersion oral preparation of enzalutamide, a drug for treating prostate cancer. Background technique [0002] Enzalutamide is an androgen receptor inhibitor, its target is different from cabazitaxel and abiraterone, it can competitively inhibit the binding of androgen to the receptor, and can inhibit the nuclear translocation of androgen receptor and the The interaction between receptors and DNA, in vitro studies have shown that enzalutamide can inhibit the proliferation of prostate cancer cells and induce their death, and enzalutamide can reduce the tumor volume in mouse prostate cancer xenograft model experiments The main metabolite of lutamide is N-desmethyl enzalutamide, which exhibits similar inhibitory activity to enzalutamide in vitro. The recommended adult dose of the drug is 160 mg per day, and it is rapidly absorbed after taking the drug. It reaches...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/4166A61K47/38A61K47/32A61K47/34A61P35/00
Inventor 黄飞赵小伟欧阳康乐
Owner FERGUSON WUHAN BIOTECH
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