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Mitoxantrone sustained-release implantation agent for curing entity tumour

A slow-release implant, mitoxantrone technology, applied in the field of medicine, can solve the problems of limiting clinical application, systemic toxicity and side effects limiting clinical application, systemic toxicity, etc.

Inactive Publication Date: 2008-05-14
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In 5 days after administration, about 21% of it is excreted in feces and about 6.5% in urine. Its large-scale application often causes severe bone marrow suppression and systemic toxicity of heart, liver and lungs, which greatly limits its clinical application.
Although alone or in 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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  • Mitoxantrone sustained-release implantation agent for curing entity tumour
  • Mitoxantrone sustained-release implantation agent for curing entity tumour

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] 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), and then add 10 mg of rice Toxantrone, 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 slow-release implant containing 10% mitoxantrone. The release time of the sustained-release implant in physiological saline in vitro is 20-26 days, and the release time in mouse subcutaneous is 24-28 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% mitoxantrone and 99% polylactic acid;

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

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

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

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

Embodiment 3

[0092]Put the weighed (80mg) 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 25mg of Mito Anthraquinone, 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 slow-release implant containing 20% ​​mitoxantrone. The release time of the sustained-release implant in physiological saline in vitro is 18-26 days, and the release time of the drug subcutaneously in mice is 18-24 days.

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Abstract

The invention relates to a mitoxantrone sustained-release implant capability of curing solid tumors, such as lung cancer, esophageal cancer, gastric cancer, liver cancer, breast cancer, ovarian cancer, prostatic cancer, bladder cancer, colon cancer and rectum cancer. The invention is characterized in that: the sustained-release implant comprises mitoxantrone, sustained-release excipient and a certain amount of sustained-release regulator; the amount of the mitoxantrone and sustained-release excipient is sufficient to control cancer; the sustained-release excipient is mainly one or the combination of the copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate) and poly (L-lactide-co-propyl phosphate); the mitoxantrone can be released slowly into part of the tumor during the degradation and adsorption, significantly reducing the systemic toxicity and sustaining the effective medicine concentration simultaneously. The invention has the advantages that: the systemic toxicity of mitoxantrone can be significantly reduced; the effective medicine concentration can be improved selectively at part of the tumor, and the therapeutic effects of non-operative treatments such as chemotherapeutic drugs and radiotherapy can be reinforced.

Description

(1) Technical field [0001] The invention relates to a mitoxantrone 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): A61K9/00A61K31/136A61K47/34A61P35/00
Inventor 孙娟魏明星
Owner JINAN SHUAIHUA PHARMA TECH
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