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Temozolomide sustained-release implant for treating solid tumor

A technology for sustained-release implants and temozolomide, applied in the field of medicine, can solve the problems of fast release and instability of sustained-release preparations

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 sustained-release preparations made by the existing methods release faster and unstable, so that they cannot bring into play their clinical effects well.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Put the weighed (85 mg) sustained-release excipient (PLGA with a molecular weight of 20,000-25,000, 75:25) into a container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add 10 mg of temozolomide and 5mg of mannitol, re-shake and vacuum dry to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a slow-release implant containing 10% temozolomide. The release time of the sustained-release implant in physiological saline in vitro is 28-36 days, and the release time in mice subcutaneously is 30-35 days, without burst release.

Embodiment 2

[0065] 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:

[0066] (1) 1%-10% temozolomide and 90%-99% glycolic acid and glycolic acid copolymer and 0.5%-15% mannitol;

[0067] (2) 10%-20% temozolomide, 80%-90% glycolic acid and glycolic acid copolymer and 0.5%-10% sorbitol;

[0068] (3) 20%-30% temozolomide and 70%-80% glycolic acid and glycolic acid copolymer and 0.5%-10% sodium chloride;

[0069] (4) 30%-40% temozolomide, 60%-70% glycolic acid and glycolic acid copolymer and 0.25%-5% mannitol;

[0070] (5) 5% temozolomide and 93% glycolic acid and glycolic acid copolymer and 2% sodium chloride;

[0071] (6) 10% temozolomide and 85% glycolic acid and glycolic acid copolymer and 5% mannitol;

[0072] (7) 20% temozolomide and 75% glycolic acid and glycolic acid copolymer and 5% mannitol;

[0073] (8) 30% temozolomide and 65% copolymer of glycolic acid and glycolic ...

Embodiment 3

[0075] Put the weighed (80mg) slow-release excipient (PLGA with a molecular weight of 15000-25000, 50:50) and 5mg of sodium chloride into the container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution) , add 15 mg temozolomide, re-shake, and then vacuum-dry to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a slow-release implant containing 15% temozolomide. The release time of the sustained-release implant in physiological saline in vitro is 24-28 days, and the release time in mice subcutaneous is 24-30 days, without burst release.

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PUM

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Abstract

A temozolomide sustained release implant for treating solid tumors is characterized in that the sustained release implant includes effective dose of anticancer temozolomide, sustained release excipients and a certain quantity of sustained release moderator. Solid tumors include pancreatic cancer, lung cancer, liver cancer, breast cancer, cerebroma, ovarian cancer, prostatic carcinoma, esophageal carcinoma, lymphadenoma, osteosarcoma and colorectal cancer. Sustained release excipients mainly are one or combination of copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, and poly(L-lactide-co-ethyl phosphate); in the process of decompression, temozolomide 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 temozolomide, 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 temozolomide 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 c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4188A61K47/34A61P35/00
Inventor 孔庆忠张伟
Owner SHANDONG LANJIN PHARMA
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