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Cladribine sustained-release implantation agent for treating solid tumors

A technology of slow-release implants and slow-release modulators, which is applied in the field of medicine and can solve the problems of systemic toxic and side effects limiting clinical application and unclear effects

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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Put the weighed (90 mg) sustained-release excipient (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), then add 10 mg of carat Drubine, 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 slow-release implant containing 10% cladribine. The drug release time of the slow-release implant in physiological saline in vitro is 14-20 days, and the drug release time in mouse subcutaneous is 20-30 days.

Embodiment 2

[0071]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:

[0072] (A) 1% cladribine and 99% polylactic acid;

[0073] (B) 5% cladribine and 95% polylactic acid;

[0074] (C) 10% cladribine and 90% polylactic acid;

[0075] (D) 15% cladribine and 85% polylactic acid;

[0076] (E) 20% cladribine and 80% polylactic acid.

Embodiment 3

[0078] 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), and then add 15mg of clarytrol 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 slow-release implant containing 15% cladribine. The release time of the slow-release implant in physiological saline in vitro is 14-22 days, and the release time in mouse subcutaneous is 20-26 days.

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PUM

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Abstract

The invention relates to a sustained-release implant for treating solid tumors, which is characterized in that the sustained-release implant contains Cladribine and sustained-release excipient of effective anticancer amount. The solid tumors comprise brain tumor, liver cancer, lung cancer, esophageal cancer, carcinoma ventriculi, mammary cancer, pancreatic cancer, cancerous goiter, nasopharyngeal darcinoma, oophoroma, endometrial carcinoma, carcinoma of uterine cervix, renal carcinoma, prostatic carcinoma, carcinoma of urinary bladder, carcinoma of colon, rectal cancer, cutaneum carcinoma, head and neck cancer and primary or secondary cancer, caruncle or carcinosarcoma from peripheral nervous system, mucosa, body of gland, blood vessel, bone tissue and absorbent gland. The sustained-release excipient is mainly degradable high molecular polymer with biological capacitability, and carmustine is slowly released into local tumor during the degradation and absorption process, therefore the invention not only obviously reduces the toxic reaction to the whole body, but also maintains effective drug concentration at the local tumor. The sustained-release implant is arranged in the local tumor, which not only reduces the carmustine toxic reaction to the whole body, but also increases the drug concentration at the local tumor selectively, thereby improving treatment effect of chemotherapeutics, radiotherapeutics and other non-operative treatment.

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): A61K9/00A61K31/7076A61K47/34A61P35/00
Inventor 孔庆忠孔庆新
Owner SHANDONG LANJIN PHARMA
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