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Gefinitib medicinal composite and method for preparing same

A gefitinib and composition technology, which is applied in the field of gefitinib-containing pharmaceutical compositions and the preparation thereof, can solve the problems of low bioavailability, complicated preparation process, low gefitinib bioavailability and the like , to achieve the effect of excellent quality, simple and easy preparation process, and good dissolution effect

Active Publication Date: 2012-08-15
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] In order to solve the problems of complicated preparation process and low bioavailability of the product in the prior art, the present invention provides a gefitinib oral solid drug with simple composition, convenient preparation, and effective dissolution of gefitinib drug combination
[0012] The inventors of the present invention unexpectedly found through a large number of experiments that limiting the ratio of raw and auxiliary materials in the gefitinib pharmaceutical composition to a certain range can greatly improve the dissolution efficiency and solve the problem of low bioavailability of gefitinib

Method used

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  • Gefinitib medicinal composite and method for preparing same
  • Gefinitib medicinal composite and method for preparing same
  • Gefinitib medicinal composite and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] components Weight (g) content(%) Gefitinib 50.0 50.0 lactose monohydrate 32.7 32.7 microcrystalline cellulose 10.0 10.0 Croscarmellose Sodium 4.0 4.0 Povidone 2.0 2.0 Sodium dodecyl sulfate 0.3 0.3 Magnesium stearate 1.0 1.0 Total 100.0 100.0

[0046] Preparation Process:

[0047] i) povidone and sodium lauryl sulfate are dissolved in water to form a granulation solution;

[0048] ii) Weigh uncrushed gefitinib, lactose, microcrystalline cellulose, and croscarmellose sodium powder according to the prescription amount and mix them evenly;

[0049] iii) adding granulation solution to granulate;

[0050] iv) drying the resulting granules using a fluidized bed;

[0051] v) Whole grains, add magnesium stearate, and mix well;

[0052] vi) Compressed into tablets.

Embodiment 2

[0054] Prescription is identical with embodiment 1.

[0055] Preparation Process:

[0056] i) Gefitinib, povidone and sodium lauryl sulfate are dissolved in aqueous hydrochloric acid solution at pH=1 to form a granulation solution;

[0057] ii) Weigh lactose, microcrystalline cellulose, and croscarmellose sodium powder according to the prescription amount and mix them evenly;

[0058] iii) adding granulation solution to granulate;

[0059] iv) drying the resulting granules using a fluidized bed;

[0060] v) Whole grains, add magnesium stearate, and mix well;

[0061] vi) Compressed into tablets.

Embodiment 3

[0063] components Weight (g) content(%) Gefitinib 61.5 61.5 microcrystalline cellulose 25.0 25.0 Croscarmellose Sodium 7.5 7.5 Povidone 3.5 3.5 Sodium dodecyl sulfate 0.5 0.5 Magnesium stearate 2 2 Total 100.0 100.0

[0064] Preparation Process:

[0065] i) povidone and sodium lauryl sulfate are dissolved in water to form a granulation solution;

[0066] ii) Weigh uncrushed gefitinib, microcrystalline cellulose and croscarmellose sodium powder according to the prescription amount and add them to the fluidized bed, and top-spray granulation with granulation solution;

[0067] iii) Whole grains, add magnesium stearate, and mix well;

[0068] iv) Compressed into tablets.

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Abstract

The invention relates to a gefinitib medicinal composite, which consists of the following components in proportion by weight: 20%-65% gefinitib, 20%-75% diluent, 0.1%-3% solubilizer, 1%-5% adhesive, 2%-10% disintegrant and 0.4%-2% lubricant. The gefinitib in the composite provided in the invention also can exist in an amorphous state, and accordingly, the dissolution efficiency is further improved. The gefinitib medicinal composite provided in the invention adopts conventional adjuvant, has a simple and easy preparing technology, and dissolution experiments prove that a better dissolution effect can be achieved, and the quality of the gefinitib medicinal composite is obviously better than products on the market.

Description

technical field [0001] The invention relates to a pharmaceutical composition for treating non-small cell lung cancer (NSCLC), in particular to a pharmaceutical composition containing gefitinib and a preparation method thereof. Background technique [0002] Gefitinib was first disclosed in the international patent WO96 / 33980 and is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. The structure is as follows: [0003] . [0004] After intravenous administration, the mean elimination half-life of gefitinib was 48 hours. After oral administration in cancer patients, absorption is slow, with an average terminal half-life of 41 hours. Gefitinib accumulated 2-8 times after daily dosing and reached steady state after 7-10 doses. After reaching a steady state, the drug is administered at intervals of 24 hours, and the ratio of the highest and lowest plasma drug concentrations is generally maintained in the range of 2-3 times. [0005] After oral administ...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61P35/00
Inventor 张志宏王悦金丽丽张素娟刘亚英池晓雷耿佳
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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