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A kind of gefitinib dispersible tablet and its preparation method and application

A technology of gefitinib and dispersible tablets, applied in the field of medicine, can solve the problems of low bioavailability, high price, body irritation, etc., and achieve the effects of high bioavailability, rapid dissolution and stable properties

Active Publication Date: 2011-12-07
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Gefitinib is a poorly soluble substance, which may lead to low bioavailability
The current market only sells gefitinib ordinary tablets, the average absolute bioavailability is only 59%, the price is expensive, and it is added with surfactants, which are irritating to the body

Method used

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  • A kind of gefitinib dispersible tablet and its preparation method and application
  • A kind of gefitinib dispersible tablet and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Gefitinib 250g

[0034] Lactose 130g

[0035] Cross-linked polyvinylpyrrolidone 25g

[0036] Carboxymethyl Starch Sodium 50g

[0037] Hypromellose 3.5g

[0038] Micronized silica gel 15g

[0039] Magnesium Stearate 7g

[0040] water 53g

[0041] 95% ethanol 122g

[0042] Made in 1000 pieces.

[0043] Preparation:

[0044] Step 1: Pass the pulverized gefitinib and pharmaceutical excipients through a 120-mesh sieve, swell the hydroxypropyl methylcellulose with hot water, stir until dissolved, and then add ethanol to make the ethanol concentration reach 70%.

[0045] Step 2: Mix gefitinib, lactose, crospovidone, and micropowdered silica gel evenly according to the prescription amount, and add the hypromellose solution described in step 1 to make a soft material.

[0046] Step 3: Pass the soft material prepared in step 2 through an 18-mesh sieve to granulate, dry at 50°C, and have a moisture content of 2.7%, and granulate through an 18-mesh sieve.

[00...

Embodiment 2

[0051] Gefitinib 250g

[0052] Lactose 80g

[0053] Cross-linked polyvinylpyrrolidone 14.3g

[0054] Carboxymethyl Starch Sodium 20g

[0055] Hypromellose 3.5g

[0056] Citric acid 100g

[0057] Micronized silica gel 15g

[0058] Magnesium Stearate 7.2g

[0059] water 253g

[0060] 95% ethanol 122g

[0061] Made in 1000 pieces.

[0062] Preparation:

[0063] Step 1: Pass the pulverized gefitinib and pharmaceutical excipients through a 120-mesh sieve, swell the hydroxypropyl methylcellulose with hot water, stir until dissolved, and then add ethanol to make the ethanol concentration reach 70%. Separately take 50 g of the above-mentioned hydroxypropyl methylcellulose solution, add 180 g of water, add citric acid and mix well.

[0064] Step 2: The prescribed amount of gefitinib and the citric acid solution in step 1 are embedded in fluidized bed acid, and then mixed with the prescribed amount of lactose, cross-linked polyvinylpyrrolidone, sodium carboxymethyl st...

Embodiment 3

[0070] Gefitinib 250g

[0071] Cross-linked polyvinylpyrrolidone 20.9g

[0072] Carboxymethyl Starch Sodium 50g

[0073] Hypromellose 3.5g

[0074] Citric acid 100g

[0075] Micronized silica gel 15g

[0076] Magnesium stearate 7.8g

[0077] water 253g

[0078] 95% ethanol 122g

[0079] Made in 1000 pieces.

[0080] The preparation method is the same as in Example 2.

[0081] Implementation 3 increased the content of cross-linked polyvinylpyrrolidone and carboxymethyl starch sodium, and the dispersibility of the dispersible tablet met the requirements of the 2010 edition of the Pharmacopoeia for dispersible tablets, and the dissolution rate was better.

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Abstract

The invention discloses a gefitinib dispersible tablet, a preparation method and an application thereof. The gefitinib dispersible tablet of the invention comprises the following components by weight: 10-65% of gefitinib, 1-30% of fillers, 10-50% of disintegrants, 1-60% of acidifiers, 0.1-20% of adhesives, and 0.1-30% of lubricants and glidants. According to the invention, gefitinib is wrapped bythe acidifier or gefitinib and the acidifier are wrapped with each other so as to reach the embedding effect. Compared with commercially available common tablets, the gefitinib dispersible tablet of the invention does not contain surfactants, has good dissolvability, dispersibility and disintegrability, and can be disintegrated completely within one minute. The gefitinib dispersible tablet prepared by the method of the invention has a high dissolution rate, good bioavailability, rapid distribution in vivo, and stable quality, and the preparation method is simple and practical, and is applicable to industrial production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a gefitinib dispersible tablet and a preparation method and application thereof. Background technique [0002] According to the third national cause of death survey in my country released by the Ministry of Health in April 2008, malignant tumors accounted for the first cause of death in cities, and lung cancer was the first cause of cancer death, accounting for 22.7% of the total number of deaths from malignant tumors. An upward trend, up 46.5% over the past 30 years. R.Peto, a famous British oncologist, predicted that if it is not controlled in time, the annual number of lung cancer patients in my country will exceed 1 million by 2025, becoming the world's largest lung cancer country. [0003] Molecular targeted therapy of tumors uses specific molecules in tumor cells as targets, and molecular targeted drugs can specifically block the biological functions of the targets, thereb...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/5377A61P35/00A61P35/04
Inventor 余楚钦林华庆刘妍侯悦翰雷伟
Owner GUANGDONG PHARMA UNIV
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