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Chidamide solid dispersion and preparing method and application thereof

A technology of solid dispersion and chidamide, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., which can solve the problem of low bioavailability, affecting drug absorption, and almost insoluble And other issues

Inactive Publication Date: 2015-07-15
SHENZHEN CHIPSCREEN BIOSCIENCES CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Insoluble drugs have slow action and low bioavailability because their dissolution rate is limited by solubility, which affects drug absorption.
[0004] Chidamide has very little solubility in water, almost insoluble, and low bioavailability

Method used

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  • Chidamide solid dispersion and preparing method and application thereof
  • Chidamide solid dispersion and preparing method and application thereof
  • Chidamide solid dispersion and preparing method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: Preparation of chidamide-povidone K30 solid dispersion (weight ratio 1:1)

[0038] Get 4g of Chidamide and 4g of Povidone K30, add 800g of absolute ethanol, heat in a water bath at 60°C to completely dissolve Chidamide and Povidone K30, and evaporate the absolute alcohol with a rotary evaporator under reduced pressure, Collect the solid, dry it in a hot air circulating oven at 60°C for 8 hours, pulverize it, and pass it through a 60-mesh sieve to obtain a solid dispersion of Chidamide. The dissolution rate of 45min of this solid dispersion is 60.3%, and its X-ray powder diffraction pattern is shown in figure 2 .

Embodiment 2

[0039] Example 2: Preparation of chidamide-povidone K30 solid dispersion (weight ratio 1:5)

[0040] Get 4g of Chidamide and 20g of Povidone K30, add 1000g of absolute ethanol, and heat in a water bath at 90°C to completely dissolve Chidamide and Povidone K30, and evaporate the absolute alcohol with a rotary evaporator under reduced pressure, Collect the solid, dry it in a hot air circulating oven at 80°C for 2 hours, pulverize it, and pass it through a 100-mesh sieve to obtain a solid dispersion of Chidamide. The dissolution rate of 45min of this solid dispersion is 79.1%, and its X-ray powder diffraction pattern is shown in image 3 .

Embodiment 3

[0041] Example 3: Preparation of chidamide-povidone K30 solid dispersion (weight ratio 1:20)

[0042] Take 4g of Chidamide and 80g of Povidone K30, add 4000g of absolute ethanol, and heat in a water bath at 90°C to completely dissolve the Chidamide and Povidone K30, and evaporate the absolute alcohol with a rotary evaporator under reduced pressure, Collect the solid, dry it in a hot air circulation oven at 80°C for 4 hours, pulverize it, and pass it through a 100-mesh sieve to obtain a solid dispersion of Chidamide. The dissolution rate of 45min of this solid dispersion is 82.2%, and its X-ray powder diffraction pattern is shown in Figure 4 .

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Abstract

The invention relates to the chemical pharmaceutical field, and discloses a chidamide solid dispersion and a preparing method and an application thereof. The invention also discloses an oral preparation containing the chidamide solid dispersion. The chidamide solid dispersion is composed of chidamide and a water soluble carrier material, and the weight ratio of chidamide to the water soluble carrier material is 1:1 to 1:20. Chidamide of the chidamide solid dispersion can be highly dispersed in the water soluble carrier material in a molecular form or an amorphous state, and thus the water solubility of chidamide is greatly improved, and the dissolution rate and bioavailability of chidamide are improved.

Description

technical field [0001] The invention relates to the field of chemical pharmacy, in particular to a chidamide solid dispersion and a preparation method and application thereof. Especially relate to a kind of N-(2-amino-4-fluorophenyl)-4-[N-[(E)-3-(3-pyridine) acryloyl] aminomethyl] benzamide solid dispersion and its Preparation method and application. Background technique [0002] Chidamide (English name: Chidamide) is a new type of anticancer drug with a new chemical structure and global intellectual property rights independently designed and synthesized by Shenzhen Microchip Biotechnology Co., Ltd. Chidamide has histone deacetylase inhibitory activity and can be used to treat diseases related to differentiation and proliferation, such as cancer and psoriasis, especially for blood cancer and solid tumors. The completed phase I clinical research results show that chidamide has definite curative effect on various lymphomas including skin lymphoma, and it also has certain cur...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/4406A61K47/32A61K47/34A61P35/00
Inventor 鲁先平李志斌
Owner SHENZHEN CHIPSCREEN BIOSCIENCES CO LTD
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