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Axitinib sustained-release implplant treating for solid tumor

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

Inactive Publication Date: 2008-06-25
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the inhibitory effect on other tumors, especially other solid tumors is not clear
Although alone or in 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

[0081] Put the weighed (90 mg) sustained-release excipient (polylactic acid (PLA) with a molecular weight of 10,000-20,000) into a container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add 10 mg of A Citinib, re-shake well and vacuum-dry to remove organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a sustained-release implant containing 10% axitinib. The release time of the slow-release implant in physiological saline in vitro is 14-20 days, and the release time in mouse subcutaneous is 15-22 days.

Embodiment 2

[0083] 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:

[0084] (A) 1% axitinib and 99% polylactic acid;

[0085] (B) 5% axitinib and 95% polylactic acid;

[0086] (C) 10% axitinib and 90% polylactic acid;

[0087] (D) 15% axitinib and 85% polylactic acid;

[0088] (E) 20% axitinib and 80% polylactic acid.

Embodiment 3

[0090] Put the weighed (85 mg) 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 15 mg of Assi 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% axitinib. The release time of the slow-release implant in physiological saline in vitro is 14-22 days, and the drug release time in mouse subcutaneous is 18-26 days.

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Abstract

The invention relates to an Axitinib sustained-release implant for treating a solid tumor, which is characterized in that: the sustained-release implant contains an effective anticancer amount of Axitinib and sustained-release excipients and a certain amount of sustained-release regulator. The solid tumors include the liver cancer, the lung cancer, the esophageal canner, the gastric canner, the breast canner, the ovarian canner, the prostate canner, the bladder canner and the rectum canner. The sustained-release excipients are mainly a copolymer of polylactic acid, glycollic acid and hydroxyacetic acid and one of the three materials, polifeprosan, poly-(L-lactide-co-ethyl phosphonate) and Poly(L-lactide-co-propyl phosphonate) or a combination of the three materials, in the degradation and absorption process of which the Axitinib is sustainedly released to part of the tumor, thus the entire toxicity of the Axitinib is significantly reduced while an effective medicine consistency is maintained on part of the tumor. That the sustained-release implant is implanted inside part of the tumor can not only reduce the entire toxicity of the Axitinib, but also enhance the medicine consistency on part of the tumor, thereby increasing the curing effect of non-operative therapeutics such as chemotherapeutic drugs and radiotherapy.

Description

(1) Technical field [0001] The invention relates to a slow-release implant for treating solid tumors, belonging to the technical field of medicines. (2) Background technology [0002] Although the research on cancer has made great progress, its mortality rate is still in 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 in 2020. Therefore, exploring an effective method or drug for treating cancer has bec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4439A61K47/34A61P35/00
Inventor 孙娟陈颖
Owner JINAN SHUAIHUA PHARMA TECH
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