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A kind of preparation method of gefitinib composite particle

A technology of gefitinib and composite particles, applied in the field of medicine, can solve the problems of high cost, achieve high dissolution rate, improve solubility, and improve bioavailability

Active Publication Date: 2021-09-07
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, Chinese patent CN108309934A ("a kind of gefitinib nanosuspension and its preparation method and application") prepared a kind of gefitinib nanosuspension, but need to use high-pressure homogenizer, Freeze dryer and other equipment, the cost is relatively high

Method used

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  • A kind of preparation method of gefitinib composite particle
  • A kind of preparation method of gefitinib composite particle
  • A kind of preparation method of gefitinib composite particle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] At room temperature, 100 mg of gefitinib bulk drug was dissolved in 1 mL of dimethyl sulfoxide to obtain a good solvent phase. 300 mg of zein was dissolved in 100 mL of deionized water, and the pH was adjusted to 9 with 0.5 M NaOH solution until the zein was completely dissolved to obtain an aqueous phase. When the temperature is 25°C, inject the good solvent phase into the water phase, stir for 30 minutes, then filter with suction, collect the filter cake, wash with deionized water 90 times the mass of gefitinib, and place the filter cake in vacuum drying after suction filtration Dry in an oven at 60°C for 8 hours to obtain gefitinib composite particles. The particle size is shown in Table 1, and Table 1 is the particle size distribution parameters of the gefitinib composite particles.

[0039] Before collecting the gefitinib composite microparticles, inject the good solvent phase into the aqueous phase and stir the suspension for 30 minutes, and use a Malvern 2000 pa...

Embodiment 2

[0057] Dissolve 99.7mg of gefitinib raw material in 1mL of N,N-dimethylformamide, heat to 45°C and ultrasonically dissolve to obtain a good solvent phase. 501.3 mg of zein was dissolved in 100 mL of deionized water, and the pH was adjusted to 9 with 0.5 M NaOH solution until the zein was completely dissolved to obtain an aqueous phase. When the temperature is 25°C, inject the good solvent phase into the water phase, stir for 30 minutes, then filter with suction, collect the filter cake, wash with deionized water 90 times the mass of gefitinib, and place the filter cake in vacuum drying after suction filtration Dry in an oven at 60°C for 7 hours to obtain gefitinib composite particles.

[0058] Before collecting the gefitinib composite particles, inject the good solvent phase into the water phase and stir the suspension for 30 minutes, and measure the particle size with a Malvern 2000 particle size analyzer. The D90 is 8.287 μm, and X-ray is carried out on the dried particle po...

Embodiment 3

[0060] Under the condition of temperature of 40°C, 102.2mg of gefitinib bulk drug was dissolved in 1mL of dimethyl sulfoxide to obtain a good solvent phase. 300.2 mg of zein was dissolved in 100 mL of deionized water, and the pH was adjusted to 9 with 0.5 M NaOH solution until the zein was completely dissolved to obtain an aqueous phase. When the temperature is 20°C, inject the good solvent phase into the water phase, stir for 30 minutes, then filter with suction, collect the filter cake, wash with deionized water 90 times the mass of gefitinib, and place the filter cake in vacuum drying after suction filtration Dry in an oven at 70°C for 8 hours to obtain gefitinib composite particles.

[0061] Before collecting the gefitinib composite microparticles, inject the good solvent phase into the aqueous phase and stir the suspension for 30 minutes, measure the particle size with a Malvern 2000 particle size analyzer, D90 is 9.846 μm, and carry out X-ray analysis on the dried microp...

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Abstract

The invention discloses a preparation method of gefitinib composite particles, which comprises the following steps: the first step, dissolving gefitinib in an organic solvent to obtain a good solvent phase; the second step, dissolving zein in deionized In water, adjust the pH to completely dissolve to obtain an aqueous phase; in the third step, mix the good solvent phase prepared in the first step with the aqueous phase prepared in the second step, separate out the gefitinib composite particles after precipitation. The gefitinib composite microparticles provided by the present invention have stable crystal form, small particle size and high dissolution rate, which improves the solubility of gefitinib, thereby improving its bioavailability, and provides a new development for the development of gefitinib oral solid preparations. s Choice.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of gefitinib composite particles. Background technique [0002] Gefitinib (GTN), its chemical name is N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholine-4-propoxy)quinazole Phenyl-4-amine, an epidermal growth factor (EGFR) tyrosine kinase inhibitor, can hinder tumor growth, metastasis and angiogenesis, and increase tumor cell apoptosis, developed by AstraZeneca, a commercial product Iressa It was approved by the FDA in 2015 for the first-line treatment of patients with non-small cell lung cancer. In clinical treatment, the required dose of GTN is relatively large, reaching 250mg. Higher doses are likely to cause adverse reactions, such as nausea, diarrhea and vomiting, which is not conducive to the treatment of patients. [0003] Gefitinib belongs to Class II drugs in the Biopharmaceutics Classification System (BCS), and is almost insolubl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/42A61K31/5377A61P35/00A61P35/04
CPCA61K9/1658A61K31/5377A61P35/00A61P35/04
Inventor 任福正许佳晨景秋芳宁尚琦曹文峰金玲
Owner EAST CHINA UNIV OF SCI & TECH
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