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Bosutinib sustained release implant for treating solid tumors

A slow-release implant, bosutinib technology, applied in the field of medicine, can solve the problems of systemic toxicity and side effects, limited clinical application, unclear effect, etc.

Inactive Publication Date: 2008-07-23
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the efficacy of this alone in the treatment of other tumors is unclear
Although the combination with other anticancer drugs may have a certain effect on some tumors, the systemic side effects caused by conventional administration limit its clinical application

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Put the weighed (80 mg) sustained-release excipient (polylactic acid (PLA) with a molecular weight of 15000-25000) into a container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add 20 mg of primary For sutinib, re-shake well and dry in vacuo to remove organic solvents. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a sustained-release implant containing 20% ​​bosutinib. The drug release time of the slow-release implant in physiological saline in vitro is 18-26 days, and the drug release time in mouse subcutaneous is 20-25 days.

Embodiment 2

[0084] Sustained-release implants were made according to the method described in Example 1, but the anti-cancer active ingredients contained were one of the following:

[0085] (A) 1% bosutinib and 99% polylactic acid;

[0086] (B) 5% bosutinib and 95% polylactic acid;

[0087] (C) 10% bosutinib and 90% polylactic acid;

[0088] (D) 15% bosutinib and 85% polylactic acid;

[0089] (E) 20% bosutinib and 80% polylactic acid.

Embodiment 3

[0091] Put the weighed (85mg) sustained-release excipient (PLGA with a molecular weight of 15000-25000, 50:50) into the container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add 15mg of Boshu Tini, re-shake well and dry in vacuo to remove organic solvents. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a sustained-release implant containing 15% bosutinib. The release time of the sustained-release implant in physiological saline in vitro is 22-28 days, and the release time in mouse subcutaneous is 23-28 days.

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PUM

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Abstract

The invention relates to a bertschtinib sustained-release implant for treating solid tumors, which is characterized in the sustained-release implant contains anti-cancer effective dose of bertschtinib, sustained-released auxiliary materials and a certain amount of sustained-release regulator. Solid tumors comprise lung cancer, esophageal cancer, gastric cancer, liver cancer, mammary cancer, oophoroma, prostatic cancer, carcinoma of urinary bladder and colorectal cancer. The sustained-released auxiliary materials are mainly one or composition of the copolymer of glycolic acid and glycollic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate) and poly (L-lactide-co- propyl phosphate), which can slowly release bertschtinib to the tumor local during degeneration and absorption, thus keeping concentration of effective medicine in the part of the tumor while distinctively reducing overall toxic reaction. Putting the sustained-release implant in the tumor can not only reduce overall toxic reaction of bertschtinib, but also selectively improve drug concentration in the part of the tumor, thereby promoting treatment effect of non-operative treatment, such as chemotherapeutics, radiotherapy, etc.

Description

(1) Technical field [0001] The invention relates to a bosutinib slow-release implant for treating solid tumors, belonging to the technical field of medicines. (2) Background technology [0002] Although cancer research has made great progress, its mortality rate still ranks among the forefront of various common causes of death. The latest data show that in 2006, 3 million people died of cancer in my country. The incidence of cancer is increasing year by year and tends to be younger. Statistics show that in less than 20 years, the incidence of cancer in my country has increased by 69%, and the mortality rate has increased by 29.4%. According to the latest statistics from the World Health Organization, the global cancer incidence rate will increase by 50% by 2020, and the number of patients will increase to 15 million. It is estimated that 4 million people will die of cancer every year in my country by 2020. [0003] Chemotherapy is one of the commonly used treatments for c...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/496A61K47/34A61P35/00
Inventor 孔庆忠刘恩祥
Owner SHANDONG LANJIN PHARMA
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