Anticancer slow release preparation of nimustine and its progression agent

A technology of sustained release agent and synergist, applied in the field of anticancer sustained release agent, can solve problems such as unclear effect, and achieve the effects of facilitating drug injection, reducing complications and reducing drug concentration

Inactive Publication Date: 2007-02-28
JINAN KANGQUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the effect ...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0127] Put 70 mg of polylactic acid (PLA) with a molecular weight of 20,000-40,000 as a pharmaceutical excipient into a container, add 100 ml of organic solvent dichloromethane to dissolve and mix well, add 10 mg of nimustine and 20 mg of goserelin, and shake again Then dry in vacuo to remove the organic solvent. Shake again and dry in vacuo to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 10% nimustine and 20% goserelin, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain The corresponding suspension-type sustained-release injection has a viscosity of 380cp-460cp (at 25°C-30°C). The subcutaneous release time is 25-30 days.

Embodiment 2

[0129] Put 75 mg of polylactic acid (PLA) with a molecular weight of 30,000-50,000 as a pharmaceutical excipient into a container, add 100 ml of organic solvent dichloromethane to dissolve and mix well, add 10 mg of nimustine and 15 mg of goserelin, and shake again Then dry in vacuo to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain an anticancer in vivo implant for treating solid tumors with 10 mg of nimustine and 15 mg of goserelin. The subcutaneous release time is 30-40 days.

Embodiment 3

[0131] Put 80 mg of polylactic acid (PLA) with a molecular weight of 25,000-40,000 as a pharmaceutical excipient into a container, add 100 ml of organic solvent dichloromethane to dissolve and mix well, add 5 mg of nimustine and 15 mg of goserelin, and shake again Then dry in vacuo to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain an anticancer in vivo implant containing 5% nimustine and 15% goserelin for treating solid tumors. The subcutaneous release time is 30-40 days.

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PUM

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Abstract

Disclosed is slow release anticancer agent carrying both Nimustine and its synergistic agents, which comprises slow release auxiliary materials and active anticancer constituents, wherein the active anticancer constituents include Nimustine and its synergistic agents (such as Vinblastine, Goserelin or Carmofur). The viscosity of the slow release injection is 10-650cp (at 20-30 deg C), and the active anticancer constituents can also be made into slow release implanting agent. The slow release subsidiary materials mainly comprise bio-compactable and degradable macromolecular polymers, when locally dispensed on the tumor, the composition not only can lower down the whole body toxicity reaction of the anti-cancer medicament, but also can selectively increase the tumor local medicinal concentration, the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved. The solid tumors include glioma, osteosarcoma, lymphoma, lung carcinoma, intestinal cancer, and breast cancer.

Description

(1) Technical field [0001] The invention relates to an anticancer slow-release agent loaded with nimustine and its synergist, belonging to the technical field of medicines. Mainly sustained-release injections and sustained-release implants. (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. In my country, about 1.6 million people suffer from cancer every year, and nearly 1.3 million people die of cancer, accounting for one-fifth of the total death toll. 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 ...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/505A61K31/475A61K31/513A61K38/08A61K47/34A61P35/00A61K47/26A61K47/32A61K47/36A61K47/42
Inventor 孔庆忠刘恩祥邹会凤贺润平
Owner JINAN KANGQUAN PHARMA TECH
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