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Sorafenib sustained-release implant treating for solid tumor

A slow-release implant, soferanib technology, applied in the field of medicine, can solve the problems of systemic toxicity and side effects that limit clinical application

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

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

[0082] Put the weighed (90 mg) sustained-release excipient (polylactic acid (PLA) with a molecular weight of 10000-20000) into a container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), and then add 10 mg of sol Firanid, re-shake well and vacuum dry to remove organic solvents. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a sustained-release implant containing 10% soferanib. The release time of the sustained-release implant in physiological saline in vitro is 18-26 days, and the drug release time in mouse subcutaneous is 15-28 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% soferanib and 99% polylactic acid;

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

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

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

[0089] (E) 20% soferanib 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 Sophie Rani, shake again and dry in vacuo to remove organic solvents. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a slow-release implant containing 15% soferanib. The drug release time of the slow-release implant in physiological saline in vitro is 18-24 days, and the drug release time in mouse subcutaneous is 18-28 days.

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Abstract

The invention relates to a Sorafenib sustained-release implant for treating a solid tumor, which is characterized in that: the sustained-release implant contains an effective anticancer amount of Sorafenib and sustained-release excipients and a certain amount of sustained-release regulators. The solid tumors comprise the esophageal canner, the gastric canner, the breast canner, the ovarian canner, the prostate canner, the bladder canner, the liver canner, the lung canner, and the rectum canner. The sustained-release excipients are mainly a copolymer of glycollic acid and hydroxyacetic acid and one of the two materials, polifeprosan and poly-(L-lactide-co-ethyl phosphonate), or a combination of the two materials, in the process of the degradation and absorption of which the Sorafenib is continuously released to part of the tumor, thus the entire toxicity of the Sorafenib 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 Sorafenib 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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IPC IPC(8): A61K9/00A61K31/4412A61K47/34A61P35/00
Inventor 孙娟孔庆新
Owner JINAN SHUAIHUA PHARMA TECH
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