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Lapatinib ditosylate tablet and preparation method thereof

A technology for lapatinib xylene sulfonate and patinib tablets, which is applied in the directions of pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve unfavorable product dissolution and sample flocculation. , poor solubility and other problems, to achieve the effect of improving the accumulation of agglomeration, ensuring stability, and the preparation process being mature and stable

Active Publication Date: 2017-02-15
SICHUAN KELUN PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although the above-mentioned patents use fluidized bed technology to solve the problem of material fluidity, the particles are loose, and the final dissolution rate is high, but there are still big problems
During the experiment it was found that N-{3-chloro-4-[(3-chlorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino} Methyl)-2-furyl]-4-quinazolinamine xylenesulfonate monohydrate has strong viscosity and poor solubility, and strict particle size control is required to achieve high bioavailability
Generally, for this type of drug, micronization treatment is required, but the fine particle size of this compound will lead to sample flocculation during dissolution analysis, which is not conducive to the final dissolution of the product, so it is only necessary to control the active ingredient within a certain particle size range
At the same time, it is not easy to directly micronize or sieve through vibrating sieves for materials with too high viscosity. Therefore, developing a suitable method for controlling the particle size of active ingredients is a key issue for the smooth industrial production of this product. However, the original patent did not give a clear definition Solution

Method used

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  • Lapatinib ditosylate tablet and preparation method thereof
  • Lapatinib ditosylate tablet and preparation method thereof
  • Lapatinib ditosylate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The preparation of embodiment 1 lapatinib ditosylate tablet of the present invention

[0039] The lapatinib ditosylate tablet of the present invention comprises the following compositions by weight:

[0040]

[0041]Preparation: The dosage form can be produced using conventional tablet pharmaceutical equipment, and the specific preparation method is as follows: initially mix the raw material lapatinib ditosylate and colloidal silicon dioxide, pass through a 100-mesh sieve, and mix evenly. Microcrystalline cellulose and mannitol were respectively passed through 100 mesh sieves, then weighed respectively with croscarmellose sodium and hypromellose according to the amount, and added to the above mixture in sequence, Mix under the wet granulator, the mixing speed is 300rpm, the cutter speed is 500rpm; then add purified water to prepare soft material, during the soft material production, the stirring speed is 300rpm, the cutter speed is 1200rpm, after granulation with 24 ...

Embodiment 2

[0048] Embodiment 2 The preparation of lapatinib ditosylate tablet of the present invention

[0049] The lapatinib ditosylate tablet of the present invention comprises the following compositions by weight:

[0050]

[0051] Preparation: The dosage form can be produced using conventional tablet pharmaceutical equipment, and the specific preparation method is as follows: pass the raw drug lapatinib ditosylate and colloidal silicon dioxide through a 150-mesh sieve, and mix well. Microcrystalline cellulose and mannitol were respectively passed through a 100-mesh sieve, and then added to the above-mentioned mixture in sequence with croscarmellose sodium and hydroxypropyl cellulose and mixed evenly, and mixed in a high-shear wet granulator. Mix at the bottom, the mixing speed is 200rpm, the cutter speed is 600rpm; then add purified water to prepare the soft material, during the soft material production, the stirring speed is 400rpm, the cutter speed is 1000rpm, and the 20-mesh si...

Embodiment 3

[0052] Embodiment 3 The preparation of lapatinib ditosylate tablet of the present invention

[0053] The lapatinib ditosylate tablet of the present invention comprises the following compositions by weight:

[0054]

[0055] Preparation: The dosage form can be produced using conventional tablet pharmaceutical equipment, and the specific preparation method is as follows: pass the raw drug lapatinib ditosylate and colloidal silicon dioxide through a 200-mesh sieve, and mix well. Microcrystalline cellulose KG802 and mannitol were passed through a 80-mesh sieve, and then added to the above-mentioned mixture in sequence with croscarmellose sodium and hypromellose, and mixed evenly under a high-shear wet granulator. The mixing speed is 400rpm, the cutter speed is 600rpm; then add purified water to prepare soft materials, the stirring speed is 400rpm, the cutter speed is 800rpm, granulate with a 16-mesh sieve and dry at 50°C until the water content is about 2%, after 24 After mesh...

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Abstract

The present invention provides a lapatinib ditosylate tablet, which is prepared from a bulk drug lapatinib ditosylate and an auxiliary material colloidal silicon dioxide according to a certain weight ratio, wherein the active ingredient is 45-60 parts, and the colloidal silicon dioxide is 0.25-2 parts. The present invention further provides a preparation method of the tablet. According to the present invention, the operability of the process is strong, the fluidity of the intermediate particles is good, the tablet weight difference is stable, the compressibility is strong, and the in vitro dissolution characteristics under different medias and the stability test results of the lapatinib ditosylate tablet of the present invention are consistent with the originally-researched preparation; and the primary pharmacological test results show that the efficacy is consistent with the original research.

Description

technical field [0001] The invention relates to a lapatinib ditosylate tablet, which belongs to the field of pharmaceutical preparations. Background technique [0002] N-{3-chloro-4-[(3-chlorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2- Furyl]-4-quinazolinamine xylenesulfonate monohydrate, also known as lapatinib monohydrate xylenesulfonate, acts as a protein tyrosine kinase EGFR (epidermal growth factor receptor-abbreviated erbB -1) and the 4-quinazolinamine compound of erbB-2 dual inhibitors were published in the patent (WO02 / 02552) on January 10, 2002. The compound has also been shown to be useful in the treatment of various cancers, including breast, lung, bladder, head and neck, and stomach cancers. The solubility of this compound in the physiologically relevant pH range is extremely poor. For such a drug with poor solubility and large specifications and poor fluidity, the required high dissolution properties and good flow characteristics cannot...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K31/517A61K47/04A61K47/38A61K47/26A61P35/00
Inventor 何江孟景沛肖凤为王利春王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD
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