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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

AI Technical Summary

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.
Although as molecularly targeted drugs, these drugs have certain anti-tumor effects, their anti-tumor effects are still unsatisfactory, and there is still a distance from people's expectations.

Method used

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  • Quinazoline molecular targeted medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Dissolve 55mg of soybean lecithin, 15mg of cholesterol and 50mg of long-circulation material PEG1000-DSPE in 150ml of absolute ethanol, remove the absolute ethanol by rotary evaporation; take 10mg of gefitinib and 50mg of calcium hydrogen phosphate and dissolve in 150ml of water; In the carrier material evaporated to dryness, heat it at 40°C-60°C for 1 hour, and then pass through a high-pressure homogenizer (25000psi) to homogenize it to obtain the product. The measured particle size was 80 nm.

Embodiment 2

[0039]Dissolve 400mg of soybean lecithin, 180mg of cholesterol and 300mg of long-cycle material PEG2000-DSPE in 650ml of acetone, remove the acetone by rotary evaporation; take 10mg of lapatinib and 100mg of calcium hydrogen phosphate and dissolve in 100ml of water; add the aqueous solution to the evaporated carrier The material is kept at 40°C to 60°C for 3 hours, and then homogenized by a high-pressure homogenizer (25000psi). The measured particle size was 75 nm.

Embodiment 3

[0041] Take 300mg of lecithin, 50mg of cholesterol and 100mg of long-circulation material PEG1000-DSPE dissolved in 200ml of absolute ethanol, remove ethanol by rotary evaporation; take 10mg of gefitinib and 400mg of copper citrate and dissolve in 200ml of water; In the dry carrier material, heat it under the condition of 40°C-60°C for 1.5 hours, and then pass through a high-pressure homogenizer (25000psi) to homogenize it to obtain the product. The measured particle size was 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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