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Novel sorafenib eutectic and preparation method thereof

A technology of sorafenib and co-crystal, applied in the field of drug crystal forms, can solve the problems of low bioavailability, side effects, large oral dose, etc., achieve loose storage and transportation conditions, reduce production costs, and simple and stable preparation processes. Effect

Pending Publication Date: 2019-08-23
HANGZHOU ZHONGMEI HUADONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although sorafenib is a relatively successful oral small-molecule multi-target anti-tumor drug, because of its extremely small solubility in water (about 1.7 μg / mL) and high gastrointestinal permeability, drug dissolution is the rate-limiting process of absorption. Be classified as BCS II class drug, so the oral relative bioavailability of Sorafenib preparation is low (about 38-49%), oral dose is bigger (400mg / time, 2 times / day), long-term use has certain effect. side effects

Method used

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  • Novel sorafenib eutectic and preparation method thereof
  • Novel sorafenib eutectic and preparation method thereof
  • Novel sorafenib eutectic and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Take 200 mg of sorafenib free base and 41 mg of 2-aminopyrimidine, mix them, add 8 mL of tetrahydrofuran to dissolve at room temperature, and concentrate under reduced pressure at 35°C to obtain sorafenib 2-aminopyrimidine cocrystal A.

Embodiment 2

[0036] Take 20 mg of sorafenib free base and 4.09 mg of 2-aminopyrimidine, add 0.8 mL of tetrahydrofuran to dissolve it, and volatilize it in the open at 40 ° C to obtain sorafenib 2-aminopyrimidine cocrystal A.

Embodiment 3

[0038] Add 20 mg of sorafenib free base and 4.09 mg of 2-aminopyrimidine into a mortar, add 0.8 mL of tetrahydrofuran, and grind to obtain sorafenib 2-aminopyrimidine cocrystal A.

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Abstract

The invention relates to a sorafenib 2-aminopyrimidine eutectic A and a preparation method thereof. The crystal form preparation process is simple, improvement of the batch reproducibility is facilitated, and the stability of the crystal form in a raw material or preparation preparing process is ensured. Moreover, the sorafenib 2-aminopyrimidine eutectic A provided by the invention is excellent inroom temperature stability and convenient for long-term storage and transport, and the medicine quality and medication safety are ensured.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical crystal forms, and in particular relates to a sorafenib 2-aminopyrimidine co-crystal and a preparation method thereof. As well as further systematic analysis of crystallinity, water solubility, thermal properties, hygroscopicity, etc. Background technique [0002] Sorafenib is a new type of signal transduction inhibitor and multi-target anti-tumor drug jointly developed by Bayer and Onxy in Germany, and it is also the first oral multi-kinase inhibitor. In December 2005, Sorafenib in the form of its tosylate salt was approved by the US FDA for use in patients with advanced renal cell carcinoma (RCC) who had previously failed to respond to α-interferon or IL-2 or were not suitable for these therapies , and was successfully launched in China in 2006, and in 2008, China approved it for the treatment of advanced liver cancer. The chemical name of sorafenib p-toluenesulfonate is: N-[4-chloro-3-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/81C07D239/42A61K31/44A61K31/505A61P35/00
CPCC07D213/81C07D239/42A61K31/44A61K31/505A61P35/00C07B2200/13A61K2300/00
Inventor 章杜前关体红夏颖邵青凌
Owner HANGZHOU ZHONGMEI HUADONG PHARMA
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