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Tantudinun sustained-release implantation agent for curing entity tumour

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

Inactive Publication Date: 2008-05-21
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the effect of using it alone to treat 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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  • Tantudinun sustained-release implantation agent for curing entity tumour
  • Tantudinun sustained-release implantation agent for curing entity tumour

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Put 80 mg of sustained-release excipients (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), add 20 mg of tandotinib, and re- Shake well and dry under vacuum to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a sustained-release implant containing 20% ​​tandotinib. The drug release time of the sustained-release implant in physiological saline in vitro is 20-26 days, and the drug release time in mice subcutaneously is 20-28 days

Embodiment 2

[0087] 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:

[0088] (A) 1% tandotinib and 99% polylactic acid;

[0089] (B) 5% tandotinib and 95% polylactic acid;

[0090] (C) 10% tandotinib and 90% polylactic acid;

[0091] (D) 15% tandotinib and 85% polylactic acid;

[0092] (E) 20% tandotinib and 80% polylactic acid.

Embodiment 3

[0094]Put the weighed sustained-release excipient (PLGA with a molecular weight of 15000-25000, 50:50) (85 mg) into the container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add 15 mg of frank 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% tandotinib. The release time of the sustained-release implant in physiological saline in vitro is 22-30 days, and the release time in mouse subcutaneous is 23-28 days.

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Abstract

The invention relates to a tandutinib sustained-release implant for the treatment of solid tumors, which is characterized in that the sustained-release implant contains anti-cancer effective amount of tandutinib, sustained-release excipient and certain amount of sustained-release regulator. The solid tumors include lung cancer, esophageal cancer, stomach cancer, liver cancer, breast cancer, ovarian cancer, prostate cancer, bladder cancer and colorectal cancer. The sustained-release excipient mainly comprises one or the combination of the copolymer of lactic acid and glycolic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate) and poly (L-lactide-co-propyl phosphate). The invention can slowly release the tandutinib in the local part of the tumor during the degradation and absorption process, so the invention can maintain the effective drug concentration at the local part of the tumor at the same time of significantly reducing the systemic toxic reaction. The sustained-release implant is arranged at the local part of the tumor, which can not only reduce the systemic toxic reaction of tandutinib, but can also selectively improve the drug concentration at the local part of the tumor and strengthen the treatment effects of chemotherapy drugs, radiation therapy and other non-surgical therapies.

Description

(1) Technical field [0001] The invention relates to a sustained-release implant of tandotinib 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 trea...

Claims

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Application Information

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