Quinazoline molecular targeted medicinal composition

A molecular targeted drug, quinazoline technology, applied in drug combinations, anti-tumor drugs, pharmaceutical formulations, etc., can solve the problems of unsatisfactory anti-tumor effect, short half-life, etc., to help target distribution, half-life The effect of prolonging and improving the tumor suppressing effect

Inactive Publication Date: 2013-10-30
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] However, in the current clinical application, these drugs still have many disadvantages. When these drugs are administered alone, the half-life is short, so frequent dosing is required.

Method used

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  • Quinazoline molecular targeted medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0036] Example 1

[0037] Dissolve 55mg of soybean phospholipid, 15mg of cholesterol and 50mg of long-cycle material PEG1000-DSPE in 150ml of absolute ethanol, and remove the absolute ethanol by rotary evaporation; take 10mg of gefitinib and 50mg of dibasic calcium phosphate in 150ml of water; add the aqueous solution In the evaporated carrier material, keep it at 40°C-60°C for 1 hour, and then homogenize it with a high-pressure homogenizer (25000psi) to obtain it. The measured particle size is 80 nm.

Example Embodiment

[0038] Example 2

[0039] Dissolve 400mg of soybean phospholipid, 180mg of cholesterol and 300mg of long-cycle material PEG2000-DSPE in 650ml of acetone, and remove acetone by rotary evaporation; take 10mg of lapatinib and 100mg of dibasic calcium phosphate in 100ml of water; add the aqueous solution to the evaporated carrier In the material, keep it at 40℃~60℃ for 3 hours, and then homogenize it with a high-pressure homogenizer (25000psi). The measured particle size is 75nm.

Example Embodiment

[0040] Example 3

[0041] Dissolve 300 mg of lecithin, 50 mg of cholesterol, and 100 mg of long-cycle material PEG1000-DSPE in 200 ml of absolute ethanol, and remove the ethanol by rotary evaporation; take 10 mg of gefitinib and 400 mg of copper citrate and dissolve in 200 ml of water; add the aqueous solution to steam In the dry carrier material, keep it at 40°C-60°C for 1.5 hours, and then homogenize it with a high-pressure homogenizer (25000psi) to obtain it. The measured particle size is 60 nm.

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Abstract

The invention provides a quinazoline molecular targeted medicinal composition and a method for preparing the quinazoline molecular targeted medicinal composition. The quinazoline molecular targeted medicinal composition comprises a quinazoline medicine, phospholipid, cholesterol, a long-circulating material and additives. The quinazoline molecular targeted medicinal composition provided by the invention has high encapsulation efficiency. By using the quinazoline molecular targeted medicinal composition, the medicine can stay for a long time during blood circulation and has long half life, the inconvenient frequent administration of the medicine can be avoided, the function of the molecular targeted medicine (a tyrosine kinase inhibitor) can be strengthened, the apoptosis of tumor cells can be accelerated, and particularly the glioblastoma in the human brain can be inhibited better.

Description

technical field [0001] The present invention relates to the field of pharmaceutical preparations, in particular to a quinazoline molecular targeted drug composition, more specifically to a molecular targeted drug combination comprising quinazoline drugs, phospholipids, cholesterol, long-circulation materials and additives and the preparation method of the pharmaceutical composition. Background technique [0002] The incidence of malignant tumors is increasing year by year in our country. Although surgical resection is still the main method of treatment, however, for advanced patients, chemotherapy or prevention of distant metastasis is often required. Traditional chemotherapeutic drugs are cytotoxic drugs, which also have a strong killing effect on normal tissues, such as digestive tract mucosa, bone marrow and other cells with active proliferation, so it will cause vomiting, diarrhea, leukopenia, bone marrow suppression, etc. Severe side effects may affect the progress of...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/5377A61K31/517A61K47/28A61K47/34A61K9/127A61P35/00
Inventor 李亚平陈伶俐樊继涛顾王文张志文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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