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Cabozantinib dispersible tablets and preparation method thereof

A technology of dispersible tablets and weight percent, applied in the directions of heterocyclic compound active ingredients, drug combinations, pill delivery, etc., can solve the problems of low bioavailability, irritation to the body, and no acidifying agent, etc., to improve bioavailability. , increase compliance, reduce the effect of body stimulation

Inactive Publication Date: 2014-04-30
QINGDAO TUMOR HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The present invention provides a Cabozantinib dispersible tablet, which is based on the existing Cabozantinib pharmaceutical preparations or the addition of surfactants is irritating to the body, and the bioavailability is not high, or no acidifying agent is used.

Method used

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  • Cabozantinib dispersible tablets and preparation method thereof
  • Cabozantinib dispersible tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Cabozantinib 250g

[0038] Lactose 120g

[0039] Cross-linked polyvinylpyrrolidone 25g

[0040] Carboxymethyl Starch Sodium 50g

[0041] Hypromellose 4g

[0042] Micronized silica gel 15g

[0043] Magnesium Stearate 10g

[0044] water 60g

[0045] 95% ethanol 122g

[0046] Made in 1000 pieces.

[0047] Preparation:

[0048] Step 1: Pass the crushed Cabozantinib 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%.

[0049] Step 2: Mix Cabozantinib, lactose, crospovidone, and micronized silica gel evenly according to the prescription amount, and add the hypromellose solution described in Step 1 to make a soft material.

[0050] Step 3: Pass the soft material prepared in step 2 through a 18-mesh sieve to granulate, dry at 50°C, the water content is 2.8%, and granulate through an 18-mesh sieve.

[0051] Step 4: Mix the ...

Embodiment 2

[0055] Cabozantinib 250g

[0056] Lactose 80g

[0057] Cross-linked polyvinylpyrrolidone 14g

[0058] Carboxymethyl Starch Sodium 20g

[0059] Hypromellose 4g

[0060] Citric acid 100g

[0061] Micronized silica gel 15g

[0062] Magnesium Stearate 7.5g

[0063] water 250

[0064] 95% ethanol 125g

[0065] Made in 1000 pieces.

[0066] Preparation:

[0067] Step 1: Pass the crushed Cabozantinib 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 170 g of water, add citric acid and mix well.

[0068] Step 2: The prescribed amount of Cabozantinib and the citric acid solution in step 1 are embedded in the fluidized bed acid solution, and then mixed with the prescribed amount of lactose, cross-linked polyvinylpyrrolidone, sodium carboxymeth...

Embodiment 3

[0074] Cabozantinib 250g

[0075] Cross-linked polyvinylpyrrolidone 40g

[0076] Carboxymethyl Starch Sodium 40g

[0077] Hypromellose 3.5g

[0078] Citric acid 100g

[0079] Micronized silica gel 15g

[0080] Magnesium Stearate 7.5g

[0081] water 250

[0082] 95% ethanol 125g

[0083] Made in 1000 pieces.

[0084] The preparation method is the same as in Example 2.

[0085] Implementation 3 increased the content of cross-linked polyvinylpyrrolidone and sodium starch glycolate, and the dispersibility of the dispersible tablets met the requirements of the 2010 edition of the Pharmacopoeia, and the dissolution rate was better.

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Abstract

The invention discloses cabozantinib dispersible tablets and a preparation method and application thereof. The cabozantinib dispersible tablets consist of the following components in percent by weight: 10-60 percent of cabozantinib, 10-40 percent of filler, 10-50 percent of disintegrating agent, 10-50 percent of acidifying agent, 0.1-10 percent of adhesive and 0.1-20 percent of lubricating agent and flow aids. Compared with common tablets, the dispersible tablets have the advantages that the cabozantinib dispersible tablets do not contain surfactants, are high in solubleness, dispersing property and disintegration property and can be completely disintegrated within 1 minute. The cabozantinib dispersible tablets prepared by the method are high in dissolution degree, high in bioavailability, rapid in in-vivo distribution, stable in quality, good in taste, simple and feasible in preparation method and suitable for industrial production.

Description

field of invention [0001] The invention relates to the field of chemical pharmacy, in particular to a Cabozantinib dispersible tablet and a preparation method thereof. Background of the invention [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 the use of molecular targeted drugs can specifically block the biological functions of the targets,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/47A61P35/00
Inventor 彭宗玉李然郑飞波
Owner QINGDAO TUMOR HOSPITAL
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