Enzalutamide soft capsule and preparation method thereof

A technology of enzalutamide and soft capsule, applied in the field of medicine, can solve the problems of incompleteness, low bioavailability, low solubility and the like

Active Publication Date: 2015-08-26
NANJING HEALTHNICE MEDICAL TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] 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...

Method used

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  • Enzalutamide soft capsule and preparation method thereof
  • Enzalutamide soft capsule and preparation method thereof
  • Enzalutamide soft capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019]

[0020]

[0021] Preparation:

[0022] (1) Preparation of the contents: heat caprylic capric acid macrogol glyceride to 60-70°C, add butylated hydroxyanisole, butylated hydroxytoluene and enzalutamide, and stir until the raw and auxiliary materials are completely dissolved;

[0023] (2) Preparation of capsule shell glue: add purified water, glycerin and sorbitol into the glue tank and heat to 60-80°C, stir until the solution is clear; add titanium dioxide, stir until the gelatin is evenly dispersed; add gelatin, then add prescription amount of gelatin. Turn on the vacuum pump, degas for ≥3 hours under the condition of ≤-0.08Mpa, keep warm at 70±5°C, and set aside;

[0024] (3) Preparation of soft capsules: take the prepared contents and capsule shells, make soft capsules by pressing, shape, dry, wash pills, pick pills, and pack.

Embodiment 2

[0026]

[0027] Preparation:

[0028] (1) Preparation of the contents: heat caprylic capric acid macrogol glyceride to 60-70°C, add butylated hydroxyanisole, butylated hydroxytoluene and enzalutamide, and stir until the raw and auxiliary materials are completely dissolved;

[0029] (2) Preparation of capsule shell glue: add purified water, glycerin and sorbitol into the glue tank and heat to 60-80°C, stir until the solution is clear; add titanium dioxide, stir until the gelatin is evenly dispersed; add gelatin, then add prescription amount of gelatin. Turn on the vacuum pump, degas for ≥3 hours under the condition of ≤-0.08Mpa, keep warm at 70±5°C, and set aside;

[0030] (3) Preparation of soft capsules: take the prepared contents and capsule shells, make soft capsules by pressing, shape, dry, wash pills, pick pills, and pack.

Embodiment 3

[0032]

[0033] Preparation:

[0034] (1) Preparation of the contents: heat caprylic capric acid macrogol glyceride to 60-70°C, add butylated hydroxyanisole, butylated hydroxytoluene and enzalutamide, and stir until the raw and auxiliary materials are completely dissolved;

[0035] (2) Preparation of capsule shell glue: add purified water, glycerin and sorbitol into the glue tank and heat to 60-80°C, stir until the solution is clear; add titanium dioxide, stir until the gelatin is evenly dispersed; add gelatin, then add prescription amount of gelatin. Turn on the vacuum pump, degas for ≥3 hours under the condition of ≤-0.08Mpa, keep warm at 70±5°C, and set aside;

[0036] (3) Preparation of soft capsules: take the prepared contents and capsule shells, make soft capsules by pressing, shape, dry, wash pills, pick pills, and pack.

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Abstract

The invention discloses an enzalutamide soft capsule and a preparation method thereof. The enzalutamide soft capsule comprises capsule content and a capsule shell, wherein the capsule content comprises enzalutamide and pharmaceutical adjuvants; the capsule shell is formed by gelatin, glycerin, sorbitol, titanium dioxide, purified water and the like. The soft capsule can be prepared with the method comprising following steps: Labrasol, butylated hydroxyanisole, butylated hydroxytoluene and enzalutamide are mixed to obtain the capsule content material of the soft capsule; the gelatin, the glycerin, the sorbitol, titanium dioxide and the purified water are mixed to obtain the capsule shell material of the soft capsule; the capsule content material and the capsule shell material of the soft capsule are pelleted on a soft capsule making machine to obtain the enzalutamide soft capsule. The enzalutamide soft capsule and the preparation method have the following advantages: the soft capsule is convenient to administrate and carry, the drug stability is good, effective components are dissolved quickly, and the bioavailability is high.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an enzalutamide soft capsule 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: C 21 h 16 f 4 N 4 o 2 S, molecular weight: 464.44, structural formula as follows: [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 a...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K31/4166A61K9/48A61P35/00
Inventor 曹林王华娟
Owner NANJING HEALTHNICE MEDICAL TECH
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