Gefitinib tablet preparation method

A technology of gefitinib and tablets, which is applied in the field of antineoplastic drugs, gefitinib tablets and its preparation, can solve the problems of low drug dissolution rate, gap in release effect of Iressa, and low f2 value, and achieve Good commercial prospects, good stability, high in vitro dissolution effect

Inactive Publication Date: 2015-07-29
珠海润都制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

We found through testing that although the patent improved the dissolution rate and stability of the tablet within a certain range, we found that in pH4.5 acetate buffer and pH6.8 phosphate buffer, as well as in 5% spit In Tween 80 aqueous solution, the dissolution rate of the drug is not high, and the f2 value is relatively low, and the dissolution rate in 5% Tween 80 aqueous solution for 45 minutes only reaches 79%, indicating that the release effect of the drug and Iressa there is still a gap

Method used

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  • Gefitinib tablet preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1 Gefitinib micronization treatment

[0054] 10 kg of gefitinib raw material was placed in a jet mill (Kunshan Miyou Group Co., Ltd.) for micronization until 8.73 kg of micronized gefitinib had a yield of 87.3%. After micronization, a small sample of gefitinib was taken and detected by a Mastersizer 2000 Malvern laser particle size analyzer (Malvern Instrument Co., Ltd., UK), and the D90 was 8.488 μm.

Embodiment 2

[0055] Example 2 Gefitinib micronization treatment

[0056] 10 kg of gefitinib raw material was placed in a jet mill (Kunshan Miyou Group Co., Ltd.) for micronization until 9.21 kg of micronized gefitinib was obtained, and the yield was 92.1%. Take the micronized gefitinib sample and detect it with a Mastersizer 2000 Malvern laser particle size analyzer (Malvern Instrument Co., Ltd., UK), and the D90 is 9.796 μm.

Embodiment 3

[0057] The preparation of embodiment 3 gefitinib tablets

[0058] A. Preparation of Gefitinib Tablets

[0059] Weigh 5.0kg of purified water, add 0.3kg of povidone K30 under stirring and stir evenly to prepare a clear and transparent solution, add sodium lauryl sulfate while stirring, stir evenly, and set aside; take the raw and auxiliary materials according to the prescription in Table 3, Put the processed raw and auxiliary materials into the G6 experimental multifunctional wet mixing granulator, stir at a low speed for 300 seconds, so that the raw and auxiliary materials are mixed evenly; add the binder within 120 seconds under the low-speed stirring state, and finally shear at a low speed for 20 seconds Seconds to make soft materials with uniform particle size; discharge, put the soft materials in a swing granulator to granulate at 20 mesh; dry the wet granules at 50±5°C until the moisture content is 1% to 3%, and finish at 20 mesh. Pack it in a PE bag, weigh it, add a cer...

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Abstract

The invention relates to the field of medicines, in particular to a gefitinib tablet preparation method. The gefitinib tablet mainly comprises a main medicine and auxiliary materials. The gefitinib tablet preparation method is characterized in that the gefitinib particle diameter D90 is not more than 10 [mu]m, the proportion of lactose to microcrystalline cellulose is 1: (3-7), uniform mixing is performed according to the formula dosage, and then pelletizing, drying, granulating and tabletting are carried out. The prepared gefitinib tablet is stable in property, reliable in quality and high in bioavailability.

Description

technical field [0001] The invention belongs to the field of drugs, and relates to an antitumor drug, in particular to a gefitinib tablet and a preparation method thereof. Background technique [0002] Gefitinib tablets, trade name "Iressa", produced by AstraZeneca UK Limited, is a selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, suitable for the treatment of patients who have previously received chemotherapy Or locally advanced or metastatic non-small cell lung cancer (NSCLC) not suitable for chemotherapy. It is a small molecular compound that can enter cells and specifically inhibit the activity of epidermal growth factor receptor tyrosine kinase by competitively binding to the ATP binding region. Wherein, the structural formula of the gefitinib is as follows: [0003] [0004] It is well known that in oral solid dosage forms, the rate of drug absorption depends on the dissolution or release of the drug from the preparation, the dissolution...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/36A61K31/5377A61K47/38A61K47/26A61P35/00
Inventor 陈新民谢斌杨冬黄俊鹏
Owner 珠海润都制药股份有限公司
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