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Sunitinib sustained-release implantation agent for curing entity tumour

A technology of sustained-release implants and sunitinib, which is applied in the direction of antineoplastic drugs, pharmaceutical formulations, drug combinations, etc., and can solve the problems of systemic toxic and side effects limiting clinical application and unclear effects

Inactive Publication Date: 2008-05-14
JINAN SHUAIHUA PHARMA TECH
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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 (95 mg) sustained-release excipient (polylactic acid (PLA) with a molecular weight of 15000-30000) into a container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), add 5 mg of diazepam For nitinib, 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 5% sunitinib. The release time of the slow-release implant in physiological saline in vitro is 24-28 days, and the release time in mouse subcutaneous is 25-30 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% sunitinib and 99% polylactic acid;

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

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

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

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

Embodiment 3

[0091] Put the weighed (90mg) 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 10mg of Sunny 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 10% sunitinib. The release time of the sustained-release implant in physiological saline in vitro is 25-32 days, and the release time in mouse subcutaneous is 25-34 days.

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PUM

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Abstract

The invention relates to a sunitinib sustained-release implant capability for curing solid tumors, such as lung cancer, esophageal cancer, gastric cancer, liver cancer, breast cancer, ovarian cancer, prostatic cancer, bladder cancer, colon cancer and rectum cancer. The invention is characterized in that: the sustained-release implant comprises sunitinib, sustained-release excipient and a certain amount of sustained-release regulator; the sustained-release excipient is mainly one or the combination of the copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate) and poly (L-lactide-co-propyl phosphate); the sunitinib can be released slowly into part of the tumor during the degradation and adsorption, significantly reducing the systemic toxicity and sustaining the effective medicine concentration simultaneously. The invention has the advantages that: the systemic toxicity of sunitinib can be significantly reduced; the effective medicine concentration can be improved selectively at part of the tumor; the invention can be applied to the prevention of tumor recurrence after operation and chemotherapy and combined therapy of various solid tumors and metastatic tumors that are not suitable for operation.

Description

(1) Technical field [0001] The invention relates to a sunitinib slow-release implant for treating solid tumors, belonging to the technical field of medicines. (2) Background technology [0002] In the past few decades, 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. Due to the impact of environmental pollution and bad eating habits, the incidence of cancer is increasing year by year and showing a younger trend. Statistics show that in less than 20 years, the incidence of cancer in my country has increased by 69%, and the death 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 ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/404A61K47/34A61P35/00
Inventor 孙娟田绍兰
Owner JINAN SHUAIHUA PHARMA TECH
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