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Dacomitinib quick-release preparation and preparation method thereof

A kind of preparation, Nisu’s technology, which is applied in the field of dacomitinib immediate-release preparations and its preparation, can solve the problems of poor dissolution of dacomitinib, and achieve the effects of improved in vivo and in vitro performance, high degree of automation, and high stability

Pending Publication Date: 2021-01-22
REYOUNG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of the deficiencies in the prior art, the object of the present invention is to provide a dacomitinib immediate-release preparation, which solves the problem of poor dissolution of dacomitinib in vitro, improves its bioavailability in vivo, and improves the therapeutic effect; At the same time, the invention also provides a preparation method thereof, which is simple, does not use organic solvents, has a high degree of automation, is easy to realize continuous production and is suitable for industrial production

Method used

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  • Dacomitinib quick-release preparation and preparation method thereof
  • Dacomitinib quick-release preparation and preparation method thereof
  • Dacomitinib quick-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] A dacomitinib immediate-release preparation is made of the following components by mass percentage:

[0034]

[0035] Preparation:

[0036] (1) Pass dacomitinib, mannitol and hypromellose phthalate through an 80-mesh sieve and mix with a three-dimensional mixer to obtain a physical mixture;

[0037] (2) Set the hot-melt extrusion temperature to 120°C, and the screw speed to 50r / min. After the temperature reaches the set temperature, add the physical mixture evenly into the filler hopper of the hot-melt extruder, and pass through the hot-melt extruder The screw melts, mixes, and extrudes to obtain a strip-shaped extrudate;

[0038] (3) After the strip-shaped extrudate is cooled to room temperature, it is pulverized into particles with a pulverizer, and the particles pass through a 60-mesh sieve to obtain a solid dispersion of Dacomitinib;

[0039] (4) After mixing the solid dispersion of Dacomitinib with lactose, microcrystalline cellulose, sodium starch glycolate a...

Embodiment 2

[0044] A dacomitinib immediate-release preparation is made of the following components by mass percentage:

[0045]

[0046] Preparation:

[0047] (1) Pass dacomitinib, mannitol and hypromellose phthalate through an 80-mesh sieve and mix with a three-dimensional mixer to obtain a physical mixture;

[0048] (2) Set the hot-melt extrusion temperature to 120°C, and the screw speed to 50r / min. After the temperature reaches the set temperature, add the physical mixture evenly into the filler hopper of the hot-melt extruder, and pass through the hot-melt extruder The screw melts, mixes, and extrudes to obtain a strip-shaped extrudate;

[0049] (3) After the strip-shaped extrudate is cooled to room temperature, it is pulverized into particles with a pulverizer, and the particles pass through a 60-mesh sieve to obtain a solid dispersion of Dacomitinib;

[0050] (4) After mixing the solid dispersion of Dacomitinib with lactose, microcrystalline cellulose, sodium starch glycolate a...

Embodiment 3

[0053] A dacomitinib immediate-release preparation is made of the following components by mass percentage:

[0054]

[0055] Preparation:

[0056] (1) Pass dacomitinib, mannitol and hypromellose acetate phthalate through an 80-mesh sieve and mix with a three-dimensional mixer to obtain a physical mixture;

[0057] (2) Set the hot-melt extrusion temperature to 120°C, and the screw speed to 50r / min. After the temperature reaches the set temperature, add the physical mixture evenly into the filler hopper of the hot-melt extruder, and pass through the hot-melt extruder The screw melts, mixes, and extrudes to obtain a strip-shaped extrudate;

[0058] (3) After the strip-shaped extrudate is cooled to room temperature, it is pulverized into particles with a pulverizer, and the particles pass through a 60-mesh sieve to obtain a solid dispersion of Dacomitinib;

[0059] (4) After mixing the solid dispersion of Dacomitinib with lactose, microcrystalline cellulose, sodium starch glyco...

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Abstract

The invention relates to the technical field of pharmacy, in particular to a dacomitinib quick-release preparation and a preparation method thereof. The dacomitinib quick-release preparation is prepared by the following steps: taking hydroxypropyl methylcellulose phthalate acetate or hydroxypropyl methylcellulose phthalate as a dispersion carrier material, adding a sugar alcohol functional auxiliary material as a plasticizer, performing high-temperature extrusion on the plasticizer and a dacomitinib bulk drug by virtue of a hot melt extruder, performing cooling and crushing, fully mixing a crushed mixture with a filler, a disintegrating agent and a lubricating agent, and performing tabletting directly to prepare the preparation. According to the dacomitinib quick-release preparation, the problems of poor solubility and poor in-vitro dissolution of dacomitinib are solved, the in-vivo bioavailability of dacomitinib is improved, and finally, the treatment effect is improved. The preparation method is simple in process, free of organic solvent, high in automation degree, easy for continuous production and suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a dacomitinib quick-release preparation and a preparation method thereof. Background technique [0002] Dacomitinib is a second-generation epidermal growth factor receptor small molecule tyrosine kinase inhibitor (EGFR-TKIs) and irreversible kinase activity of certain EGFR activating mutations (exon 19 deletion or exon 21L858R substitution mutation) Inhibitor for the first-line treatment of patients with advanced non-small cell lung cancer (NSCLC) carrying EGFR activating mutations. However, dacomitinib belongs to the class II drug of the biopharmaceutical classification system (BCS), which has poor water solubility and low bioavailability. [0003] At present, the commonly used methods to improve the solubility of drugs generally include the following: micronization, complexation (surfactant, cyclodextrin, etc.), changing the crystal form, making soluble prodrugs, double salts...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/517A61K47/38A61K47/36A61K47/26A61K47/32A61P11/00A61P35/00
CPCA61K31/517A61K9/2054A61K9/2059A61K9/2018A61K9/2027A61P35/00A61P11/00
Inventor 苗得足胡清文刘金华王向华杨书华
Owner REYOUNG PHARMA
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