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Slow release microsphere containing hormone kind anti cancer medicine and its application

A technology of anticancer drugs and sustained-release microspheres, applied in the field of medicine, can solve the problems of treatment failure and enhanced tolerance

Inactive Publication Date: 2006-08-30
JINAN KANGQUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In addition, the DNA repair function in many tumor cells is significantly enhanced after hormonal anticancer drugs, which in turn leads to the enhancement of tumor cell resistance to hormonal anticancer drugs, resulting in treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Put 70 mg of polyglycolic acid and glycolic acid copolymer (PLGA, 65:35) with a peak molecular weight of 20,000-40,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, then add 10 mg of 5-fluorouracil and 20 mg of other Moxifen, shake again and dry in vacuo to remove organic solvents. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to prepare an anticancer implant containing 10% 5-fluorouracil and 20% tamoxifen. The drug release time of the anticancer implant in physiological saline in vitro is 15-20 days, and the drug release time of subcutaneous implantation in mice is 25-40 days.

Embodiment 2

[0100] The method steps of being processed into anticancer implants are the same as in Example 1, but the difference is that the contained anticancer active ingredients are:

[0101] 20% triptorelin, goserelin, leuprolide, anastrozole, edoxifene, milprexifene, tamoxifen, comoxifen, raloxifene, steroids , anticancer stenol, 4-hydroxytamoxifen, flutamide, aminoglutethimide, pirumide, megestrol, medroxyprogesterone, clomiphene, toremifene, Trazole or exemestane with 10% 6-mercaptopurine, 5-fluorouracil (5-FU), methotrexate, pemetrexed, raltitrexed, raltitrexate, carmofur, Fluoride, midazocitabine, galocitabine, ibacitabine, enoxitabine, ancitabine, decitabine, flucitabine, enoxitabine, midazocitabine, methoquinone, rice A combination of totane, cytarabine, hydroxyurea, 5-fluorouridine, capecitabine, gemcitabine, fazarabine, fludarabine, cladribine, or pentosine.

Embodiment 3

[0103] Put 70 mg of polylactic acid (PLGA, 50:50) with a peak molecular weight of 15,000-25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of anastrozole and 20 mg of methotrexate, and shake again Then dry in vacuo to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anticancer implant containing 10% anastrozole and 20% mg methotrexate. The drug release time of the anticancer implant in the physiological saline in vitro is 15-20 days, and the drug release time when placed subcutaneously in mice is 25-40 days.

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PUM

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Abstract

A slow-release microball of the anticancer medicine containing hormone component for preparing the slow-release implant or slow-release injection is composed of the active anticancer component chosen from hormone-type anticancer medicine and its synergist and antimetabolic anticancer medicine, and the medicinal additive chosen from polylactic acid, the copolymer of polyoxyacetic acid and hydroxyacetic acid, ethene-vinyl acetate copolymer and polifeprosan.

Description

(1) Technical field [0001] The invention relates to a slow-release microsphere of hormone anticancer drugs and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology [0002] The development of many cancers is related to hormones. Therefore, the application of hormonal anticancer drugs is more effective in treating tumors, such as lung cancer, breast cancer, pancreas, ovarian cancer, endometrial cancer, prostate cancer, and colorectal cancer. [0003] Further studies have found that blood vessels, connective tissue, matrix proteins, fibrinoproteins, and collagens in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the ability of chemotherapy drugs to spread around and around the tumor. Infiltration and diffusion in tumor tissue (see Netti et al. "The influence of the condition of the extracellular matrix on the delivery of drugs in solid tumors" "Cancer Research...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/496A61K31/7028A61K9/16A61K9/10A61P35/00
Inventor 孙娟孙中厚孔庆新田绍兰
Owner JINAN KANGQUAN PHARMA TECH
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