Solid pharmaceutical composition of EGFR inhibitor

A composition and drug technology, applied in the field of pharmacy, can solve the problems of low bioavailability, affecting the therapeutic effect of such compounds, unfavorable dissolution and absorption process, etc.

Active Publication Date: 2018-05-22
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] WO2016070816A1 discloses a class of EGFR inhibitors. Such compounds have low water solubility, which is not conducive to the dissolution and absorption process of the drug in the gastrointestinal tract after oral administration, resulting in low bioavailability and affecting the therapeutic effect of such compounds.

Method used

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  • Solid pharmaceutical composition of EGFR inhibitor
  • Solid pharmaceutical composition of EGFR inhibitor
  • Solid pharmaceutical composition of EGFR inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] The trimesylate salt of the compound of formula 2 is crushed by airflow, and sieved; the microcrystalline cellulose is crushed by airflow, and sieved; Sodium starch and magnesium stearate were added in the mixer hopper, mixed for 30 minutes, and the tablet machine carried out dry compression to form tablets. The feeding amount of the material is 1000 tablets, each tablet is equivalent to containing 20mg of the compound of formula 2, and the composition of the prescription is as follows:

[0045] The prescription composition of the trimesylate tablet A of the compound of formula 2 in table 1

[0046]

Embodiment 2～ Embodiment 9

[0048] With reference to the preparation method of Example 1, the following tablets of Examples 2 to 9 were prepared:

Embodiment 2

[0050] The prescription composition of the trimesylate tablet B of the compound of table 2 formula 2

[0051]

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PUM

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Abstract

The invention belongs to the pharmaceutical technical field, relates to a solid pharmaceutical composition of an EGFR inhibitor, and in particular, relates to a solid pharmaceutical composition prepared with a compound represented by the formula (I) or a pharmaceutically acceptable salt as raw material and a preparation method thereof. On one hand, the solid pharmaceutical composition includes a diluent, a disintegrating agent and a lubricant; on the other hand, a carrier material is selected from a solid dispersion body of a cellulose compound. The solid pharmaceutical composition obviously improves the water solubility and stability of the compound, has faster release rate, and helps to improve the bioavailability.

Description

technical field [0001] The invention relates to a solid pharmaceutical composition of an EGFR inhibitor, in particular to a solid pharmaceutical composition prepared from a compound of formula (I) or a pharmaceutically acceptable salt thereof and a preparation method thereof, belonging to the technical field of pharmacy. Background technique [0002] The epidermal growth factor receptor (EGFR) signal transduction pathway plays an important role in regulating tumor cell growth, damage repair and survival, angiogenesis, invasion and metastasis, and is expressed in a considerable part of human tumors. Epidermal growth factor receptor (EGFR) widely exists in a variety of epidermal malignant tumor cells: non-small cell lung cancer, breast cancer, colorectal cancer, gastric cancer, prostate cancer, ovarian cancer, head and neck tumors. [0003] Oral administration is the most common way of drug delivery. Following oral administration, drugs can be absorbed at many different sites...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K9/20A61K47/38A61K47/36A61P35/00
CPCA61K9/2054A61K9/2059A61K31/506
Inventor 鲁锡峰张伟何雄雄董平沈永铭刘崇皓
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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