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Pirarubicin sustained-release implant treating for solid tumor

A technology for sustained-release implants and pirarubicin, which is used in antitumor drugs, medical preparations containing active ingredients, organic active ingredients, etc. Short half-life and other issues

Inactive Publication Date: 2008-06-25
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, short half-life is not conducive to drug efficacy, wide tissue distribution and poor selectivity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Put the weighed (90mg) slow-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), add 10 mg of pyridine Rubicin, shake well and vacuum dry to remove organic solvent. The dried solid composition is immediately shaped, and then sterilized by radiation after being subpackaged to obtain a sustained-release implant containing 10% pirarubicin. The drug release time of the sustained-release implant in physiological saline in vitro is 20-26 days, and the drug release time in mice subcutaneously is 24-28 days.

Embodiment 2

[0085] The sustained-release implant is made by the method described in Example 1, but the anti-cancer active ingredient contained in it is one of the following:

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

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

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

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

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

Embodiment 3

[0092] Put the weighed (85mg) slow-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), add 15mg of pyrrolidone Thanxing, re-shake and vacuum dry to remove organic solvent. The dried solid composition is formed immediately, and then sterilized by radiation after being divided into packages to obtain a sustained-release implant containing 15% pirarubicin. The drug release time of the sustained-release implant in physiological saline in vitro is 20-26 days, and the drug release time in mice subcutaneously is 20-28 days.

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Abstract

The invention relates to a Pirarubicin sustained-release implant for treating a solid tumor, which is characterized in that: the sustained-release implant contains an effective anticancer amount of Pirarubicin and sustained-release excipients and a certain amount of sustained-release regulator. The solid tumors include the esophageal canner, the gastric canner, the breast canner, the ovarian canner, the prostate canner, the bladder canner, the liver canner, the lung canner, and the rectum canner. The sustained-release excipients are mainly a copolymer of glycollic acid and hydroxyacetic acid and one of the two materials, polifeprosan and poly-(L-lactide-co-ethyl phosphonate), or a combination of the two materials, in the process of degradation and absorption of which the Pirarubicin is sustainedly released to part of the tumor, thus the entire toxicity of the Pirarubicin is significantly reduced while an effective medicine consistency is maintained on part of the tumor. That the sustained-release implant is implanted inside part of the tumor can not only reduce the entire toxicity of the Pirarubicin but also enhance the medicine consistency on part of the tumor, thereby increasing the curing effect of non-operative therapeutics such as chemotherapeutic drugs and radiotherapy.

Description

(1) Technical field [0001] The invention relates to a pirarubicin sustained-release implant for treating solid tumors, belonging to the technical field of medicine. (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 showing a trend of younger people. According to data, 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 will increase by 50% by 2020, and the number of cases 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 can...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/704A61K47/34A61P35/00
Inventor 孙娟孙中厚
Owner JINAN SHUAIHUA PHARMA TECH
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