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Erlotinib sustained-release implants for treating entity knub

A technology of slow-release implants and slow-release regulators, which is applied in the field of medicine and can solve the problems of systemic toxicity and side effects that limit clinical application.

Inactive Publication Date: 2008-04-16
DASEN BIOLOGICAL PHARMA CO LTD
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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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  • Erlotinib sustained-release implants for treating entity knub
  • Erlotinib sustained-release implants for treating entity knub

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Put the weighed (90mg) sustained-release excipient (polylactic acid (PLA) with a molecular weight of 10000-20000) into the container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add 10 mg Rotinib, 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% erlotinib. 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

[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% erlotinib and 99% polylactic acid;

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

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

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

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

Embodiment 3

[0094] 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 Erlo 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% erlotinib. 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

An erlotinib slow release implant for treating solid tumor is characterized in that the slow release implant contains anti-cancer effective amount erlotinib, slow release supplementary materials and some slow release regulator. The solid tumors comprise esophagus cancer, stomach cancer, breast cancer, ovarian cancer, prostatic cancer, bladder cancer, liver cancer, lung cancer and colorectal cancer. The slow release supplementary materials mainly are one or their combination of co-polymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate), and poly (L-lactide-co-propyl phosphate), during its degradation and absorption, slow releasing erlotinib to tumor local, so it greatly decreases its whole body toxicity reaction, at the same time it also maintains effective medicine concentration of tumor local. The tumor local is arranged with the slow release implant, which can not only decrease whole body toxicity reaction of erlotinib, but also selectively promote medicine concentration of the tumor local, reinforce therapeutic effect of non-operation therapy such as chemotherapeutic drugs, radiotherapy and etc.

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): A61K9/00A61K31/517A61K47/34A61P35/00
Inventor 孙娟王明华
Owner DASEN BIOLOGICAL PHARMA CO LTD
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