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A kind of gefitinib pharmaceutical composition without surfactant and preparation method thereof

A technology of surfactant and gefitinib, which is applied in the field of gefitinib composition and its preparation to achieve the effect of ensuring safety and reducing the types of excipients

Active Publication Date: 2017-12-26
CHENGDU SINO STRONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] It can be seen from the analysis of the prior art that the ultimate goal is to improve the dissolution rate of gefitinib in vitro, but each has its own limitations.

Method used

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  • A kind of gefitinib pharmaceutical composition without surfactant and preparation method thereof
  • A kind of gefitinib pharmaceutical composition without surfactant and preparation method thereof
  • A kind of gefitinib pharmaceutical composition without surfactant and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Weigh each component according to prescription 1, mix mannitol, lactose monohydrate and gefitinib evenly through an 80-mesh sieve, and perform micronization. The particle size distribution of the mixed material is required to be D50=0.1-5um, D90=1-10um. Take the mixture that meets the particle size distribution requirements to monitor the content of gefitinib, and convert the ratio in the material. Take the mixture with known solid content, put it in a mixer, add microcrystalline cellulose and croscarmellose sodium and mix for 10 minutes. Collect materials. Take the mixed material and put it on the dry granulator, adjust the rotation speed of the extrusion wheel (3.6-5.3rpm), the rotation speed of the feeding screw (12-24rpm), the pressure of the oil cylinder (the pressure of the oil cylinder is 1.0MPa-3.0MPa) to make it three Those who cooperate effectively, until the hardness of the pressed medicine block is 2-4kg, and the material is collected. The material is size...

Embodiment 2-5

[0046] Weigh each component according to prescription 2-5, and the preparation method is the same as that in Example 1.

Embodiment 6

[0048] The dissolution rate measurement of embodiment 1-5 preparation

[0049] Dissolution method: paddle method, 75 rpm, solvent: 1000 ml of 0.1 mol / L hydrochloric acid solution (1% V / V-SDS).

[0050]At 5min, 10min, 15min, 30min, 45min, and 60min, take 10ml and filter it, dilute it with dissolution medium and measure it; the concentration of the reference solution is 10μg / ml. The drug concentration detection method is UV method; the detection wavelength is 352nm.

[0051] Table 1 Dissolution curve cumulative data table

[0052]

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PUM

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Abstract

The invention discloses a surfactant-free gefitinib pharmaceutical composition, comprising 150-300 parts by weight of gefitinib, 90-270 parts by weight of a diluent, 40-110 parts by weight of a disintegrant, and a lubricant 5‑10 parts by weight. The invention also discloses a preparation method of the pharmaceutical composition. The pharmaceutical composition of the present invention does not contain surfactants, does not affect the in vitro dissolution of the formula, meets the principle of minimizing the types of auxiliary materials required by drug development, and ensures the safety of clinical use.

Description

technical field [0001] The invention relates to a surfactant-free gefitinib composition and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Gefitinib (English name: Gefitinib), chemical name N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholine-4-propoxy)quinazole Lin-4-amine, whose structure is shown in formula I, is a selective epidermal growth factor receptor (EGFR) protein tyrosine kinase inhibitor developed by AstraZeneca. The trade name of gefitinib is Iressa, which was first listed in Japan in July 2002 for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) who have previously received chemotherapy. In May 2003, it was approved by the FDA to go on the market in the United States, and in February 2005 it was approved by the SFDA to go on the market in China. The structure of the gefitinib compound: [0003] [0004] The solubility of gefitinib has a certain dependen...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/28A61K31/5377A61K47/38A61K47/26A61K47/10A61P35/00
Inventor 蒲洪李长生陈小宁许娟
Owner CHENGDU SINO STRONG PHARMA