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Lapatinib sustained-release implantation agent for treating solid tumors

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

Inactive Publication Date: 2008-07-16
SHANDONG LANJIN PHARMA +1
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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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  • Lapatinib sustained-release implantation agent for treating solid tumors
  • Lapatinib sustained-release implantation agent for treating solid tumors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Put the weighed (80mg) 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), then add 20 mg of Latex For Patinib, 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 sustained-release implant containing 20% ​​lapatinib. The release time of the slow-release implant in physiological saline in vitro is 12-16 days, and the release time in mouse subcutaneous is 10-15 days.

Embodiment 2

[0085] 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:

[0086] (A) 1% lapatinib and 99% polylactic acid;

[0087] (B) 5% lapatinib and 95% polylactic acid;

[0088] (C) 10% lapatinib and 90% polylactic acid;

[0089] (D) 15% lapatinib and 85% polylactic acid;

[0090] (E) 20% lapatinib and 80% polylactic acid.

Embodiment 3

[0092]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 Lapa 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% lapatinib. The release time of the slow-release implant in physiological saline in vitro is 12-16 days, and the release time in mouse subcutaneous is 13-18 days.

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Abstract

The invention relates to a solid tumors-curing Lapatinib sustained-release implant, which is characterized in that the sustained-release implant contains effective anti-tumor dose of Lapatinib, sustained-release auxiliary material and a certain amount of sustained-release regulator. Solid tumors consist of lung cancer, esophageal cancer, gastric cancer, liver cancer, breast cancer, ovarian cancer, prostatic cancer, bladder cancer and colorectal cancer. The sustained-release auxiliary materials are mainly one or mixture of copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate) and poly (L-lactide-co-propyl phosphate). When the sustained-release auxiliary materials are degrading and absorbed, Lapatinib is slowly released into tumor part, thus while reducing toxic reaction of the whole body, the sustained-release auxiliary materials can sustain concentration of effective drug at the tumor part. Placing the anti-tumor sustained-release implant at the tumor part can not only reduce toxic reaction of the whole body of Lapatinib, but also improve drug concentration at the tumor part and enhance treatment effects of nonspecific treatments, such as chemotherapeutics, radiotherapy, etc.

Description

(1) Technical field [0001] The invention relates to a lapatinib 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 canc...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/506A61K47/34A61P35/00
Inventor 孔庆忠张伟
Owner SHANDONG LANJIN PHARMA
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