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Sustained-release agent containing hormone anti-cancer medicine

A technology of anti-cancer drugs and hormones, applied in the field of drugs, can solve problems such as enhanced tolerance and treatment failure

Inactive Publication Date: 2008-08-27
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

[0100] 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 colchicine 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% colchicine 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

[0102] The method steps of being processed into anticancer implants are the same as in Example 1, but the difference is that the anticancer active ingredients contained in the anticancer implants are:

[0103] 5-30% triptorelin, goserelin, leuprolide, anastrozole, edoxifene, milprexifen, tamoxifen, comoxifen, raloxifene, steroid Antiestrogens, anticancer sterols, 4-hydroxytamoxifen, flutamide, aminoglutethimide, piglutamide, megestrol, medroxyprogesterone, clomiphene, toremifene, Letrozole or Exemestane with 5-30% Cytochalasin, Mitoclomin, Mitopradone, Mitoguanidine Hydrazone, Mitonaphthamide, Mitohydrazine, Mitoquinone, Mito Sepe, Mitotane, Mitonamamine, Mitozolomide, Mitoransone, Colchicine Salicylate, Colchicine, Colcemid, Cytochalasin, Naphthol, Alpha-Naphthol , β-naphthol, α-naphthol phosphate, alcodazole, procodazole, arsenic, giraladazole or nocodazole in combination.

Embodiment 3

[0105] 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 20 mg of anastrozole and 10 mg of Xylomustine, and re-shake 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 implant containing 20% ​​anastrozole and 10% sapromustine. The drug release time of the anticancer implant in physiological saline in vitro is 15-25 days, and the drug release time of the implant subcutaneously placed in mice is 25-45 days.

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PUM

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Abstract

A sustained-release steroid preparation with antitumor effect is provided, which is characterized in that an antitumor component is coated inside pharmaceutically-acceptable adjuvant to make a sustained-release implant or sustained-release injection. The antitumor component is an antitumor steroid drug or synergists thereof. The antitumor steroid drug is selected from chlormethine drugs and / or antimitotic drugs and / or plant alkaloids. The pharmaceutically-acceptable adjuvant is selected from polylactic acid-polyglycolic acid-hydroxyacetic acid copolymer, ethylene-vinyl acetate copolymer and / or polifeprosan. The sustained-release injection contains sustained-release microspheres and solvents, wherein the solvents include common solvents and special solvents containing a suspending agent, wherein the suspending agent is selected from sodium carboxymethylcellulose, mannitol and the like and used to suspend sustained-release granules or microspheres, thereby facilitating injection. The sustained-release preparation is administered by local delivery in the tumor site or injection, which can not only reduce systemic toxicity but also selectively increase local drug concentration in the tumor site and enhance the therapeutic effect of nonoperative treatment such as drug therapy and radiotherapy.

Description

(1) Technical field [0001] The invention relates to a sustained release agent of hormone anticancer drugs and a preparation method thereof, which belongs 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 movement of drugs in solid tumors" "Cancer Resea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K45/00A61K47/34A61P35/00A61K47/36A61K47/38A61K47/42
Inventor 孙娟孙中厚孔庆新田绍兰
Owner JINAN KANGQUAN PHARMA TECH
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