Method for preparing lapatinib ditosylate solid dispersion by freeze-drying method

A technology of solid dispersion and toluenesulfonic acid, which is applied in freeze-drying transportation, pharmaceutical formulations, organic active ingredients, etc., can solve the problem of lack of bioavailability of lapatinib toluenesulfonate solid dispersion and improve bioavailability The effect of high density, large surface area and loose packing

Pending Publication Date: 2020-02-18
JINHUA VOCATIONAL TECH COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, there is a lack of a method for preparing lapatinib tosylate solid dispersion by lyophilization with high bioavailability

Method used

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  • Method for preparing lapatinib ditosylate solid dispersion by freeze-drying method
  • Method for preparing lapatinib ditosylate solid dispersion by freeze-drying method
  • Method for preparing lapatinib ditosylate solid dispersion by freeze-drying method

Examples

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Embodiment 1

[0030] A kind of freeze-drying method of the present invention prepares the method for lapatinib tosylate solid dispersion, comprises the following steps: (1) the carrier PVPS630 is macromolecular material, carries out drug loading ratio preparation physical mixture; Described drug loading The ratio is 1:1. (2) Take the physical mixture (including Lapatinib ditosylate), add it to 30mL acetonitrile solution, and ultrasonically dissolve it completely. The solution is quickly frozen in liquid nitrogen, dried in a freeze dryer for 30 hours, taken out and placed in P 2 o 5 Put in a desiccator for 30 hours, pass through a 60-mesh sieve for subsequent use, and obtain a solid dispersion of lapatinib tosylate. The weight-to-volume ratio of the physical mixture to the acetonitrile solution is 500 mg:30 mL. The volume ratio of acetonitrile and water in the acetonitrile solution is 2:1. The temperature in the freeze dryer is -40°C, and the temperature in the cold well is -60°C.

Embodiment 2

[0032] The difference between embodiment 2 and embodiment 1 is: a kind of freeze-drying method of the present invention prepares the method for lapatinib tosylate solid dispersion, comprises the following steps: (1) the carrier PVPS630 is polymer material, carries out drug The loading ratio is used to prepare the physical mixture; the drug loading ratio is 1:3. (2) Take the physical mixture (including Lapatinib ditosylate), add it to 30mL acetonitrile solution, and ultrasonically dissolve it completely. The solution is quickly frozen in liquid nitrogen, dried in a freeze dryer for 24 hours, taken out and placed in P 2 o 5 Put in a desiccator for 24 hours, pass through a 100-mesh sieve for subsequent use, and prepare a solid dispersion of lapatinib tosylate. The weight-to-volume ratio of the physical mixture to the acetonitrile solution is 500 mg:100 mL. The volume ratio of acetonitrile and water in the acetonitrile solution is 2:1. The temperature in the freeze dryer is -40...

Embodiment 3

[0034] The difference between embodiment 3 and embodiment 1 is: a kind of freeze-drying method of the present invention prepares the method for lapatinib tosylate solid dispersion, comprises the following steps: (1) the carrier PVPS630 is polymer material, carries out drug The loading ratio is used to prepare a physical mixture; the drug loading ratio is 1:2. (2) Take the physical mixture (including Lapatinib ditosylate), add it to 30mL acetonitrile solution, and ultrasonically dissolve it completely. The solution is quickly frozen in liquid nitrogen, dried in a lyophilizer for 36 hours, taken out and placed in P 2 o 5Put in a desiccator for 48 hours, pass through an 80-mesh sieve for subsequent use, and obtain a solid dispersion of lapatinib tosylate. The weight-to-volume ratio of the physical mixture to the acetonitrile solution is 500mg: 60mL. The volume ratio of acetonitrile and water in the acetonitrile solution is 2:1. The temperature in the freeze dryer is -40°C, and...

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Abstract

The invention discloses a method for preparing a lapatinib ditosylate solid dispersion by a freeze-drying method. The method comprises the following steps of (1) using a high molecular material PVPS630 as a carrier, and preparing a medicine loading ratio physical mixture; and (2) taking the physical mixture (containing Lapatinib ditosylate), adding the taken physical mixture to an acetonitrile solution, performing ultrasonic treatment so that the physical mixture totally dissolves, placing the solution in liquid nitrogen, performing quick freezing, performing placing in a freeze-drying machine, performing drying for 24-36h, performing taking out, performing placing in a P2O5 drying machine for 24-48h, and performing screening through a 60-100-mesh sieve for standby application to prepare the lapatinib ditosylate solid dispersion. The solubility and the dissolution speed of the lapatinib ditosylate solid dispersion prepared by the method in water are improved, and the biological availability of the lapatinib ditosylate solid dispersion is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a method for preparing lapatinib tosylate solid dispersion by a freeze-drying method. Background technique [0002] Lapatinib tosylate belongs to the TKI (tyrosine kinase inhibitor) class of drugs, reversibly binds to human epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (Her2) tyrosine through hydrogen bonding At the kinase ATP binding site, it prevents ArIP from binding to the tyrosine kinase domain, inhibiting the autophosphorylation and activation of tyrosine kinase. Lapatinib tosylate also inhibits the activation of the downstream effector MAPK of EGFR and Her2, thereby inhibiting tumor cell proliferation. In addition, lapatinib tosylate inhibits the activation of Akt, leading to tumor cell apoptosis, and is used for the treatment of advanced or metastatic breast cancer. [0003] Lapatinib tosylate was de...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/517A61K47/32A61P35/00A61P35/04
CPCA61K31/517A61K9/19A61K47/32A61P35/00A61P35/04
Inventor 胡献跃黄东纬
Owner JINHUA VOCATIONAL TECH COLLEGE
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