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Lonafarnib sustained-release implant for treating solid tumor

A slow-release implant and tumor technology, applied in the field of medicine, can solve the problems of systemic toxic and side effects limiting clinical application and unclear effect

Inactive Publication Date: 2008-05-28
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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Put the weighed (80mg) 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 20 mg of Ro Nafarni, shake again and dry in vacuo to remove organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a sustained-release implant containing 20% ​​ronafarib. 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

[0079] 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:

[0080] (A) 1% ronafarib and 99% polylactic acid;

[0081] (B) 5% ronafarib and 95% polylactic acid;

[0082] (C) 10% ronafarib and 90% polylactic acid;

[0083] (D) 15% ronafarib and 85% polylactic acid;

[0084] (E) 20% ronafarib and 80% polylactic acid.

Embodiment 3

[0086] Put the weighed (85mg) sustained-release excipient (PLGA with a molecular weight of 15000-30000, 50:50) into the container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add 15mg of Rhona Farney, 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 15% ronafarib. The release time of the slow-release implant in physiological saline in vitro is 16-26 days, and the release time in mouse subcutaneous is 18-24 days.

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PUM

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Abstract

A ranophanib sustained release implant for treating solid tumors is characterized in that the sustained release implant includes effective dose of anticancer ranophanib, sustained release excipients and a certain quantity of sustained release moderator. Solid tumors include lung cancer, esophageal carcinoma, gastric cancer, liver cancer, breast cancer, ovarian cancer, prostatic carcinoma, bladder carcinoma and colorectal cancer. Sustained release excipients are mainly one or combination of the copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly(L-lactide-co-ethyl phosphate) and poly (L-lactide-co- phosphoric acid propyl); in the process of decompression, ranophanib can be slowly released to local tumor, thus maintaining effective drug concentration of local tumor as well as significantly reducing overall toxic reaction. Being placed in local tumor, the sustained release implant not only reduces overall toxic reaction of ranophanib, but also selectively improves drug concentration in local tumor, enhancing the therapeutic effects of non-operative therapy such as chemotherapy drugs and radiotherapy.

Description

(1) Technical field [0001] The invention relates to a ronafarib sustained-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...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/4545A61K47/34A61P35/00
Inventor 孔庆忠刘恩祥
Owner SHANDONG LANJIN PHARMA
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