Slow releasing injection containing anti-mitosis medicine

A slow-release injection, anti-mitotic technology, applied in the field of medicine, can solve the problems of large trauma, treatment failure, decreased immunity, etc.

Inactive Publication Date: 2006-03-22
孔庆忠
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, further studies have found that inappropriate drug administration often leads to the development of tolerance, which eventually leads to the failure of treatment
Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor. See Kong Qingzhong "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of brain tumors in rats", "Journal of Surgical Oncology", 1998, 69, pages 76-82 (Kong Q et al., J Surg Oncol.1998 Oct; 69 (2) :76-82), simply increasing the dosage is limited by systemic reactions
Drug implantation may solve the problem of drug concentration to some extent. However, the operation of drug implantation is more complicated and traumatic. In addition to easily causing various complications such as bleeding, infection, and decreased immunity, it can also cause or accelerate tumor spread and metastasis

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Put 80 mg of pharmaceutical excipient ethylene vinyl acetate copolymer (EVAc) into a container, add 100 ml of dichloromethane to dissolve and mix well, add 20 mg of nocodazole, re-shake, and vacuum dry to remove the organic solvent. The dried solid composition is melted to prepare sustained-release pellets containing 20% ​​by weight of nocodazole, which are subpackaged and sterilized by radiation. The sustained-release pellets are suspended in water for injection containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The release time of the sustained-release injection in physiological saline in vitro is 14-24 days, and the release time in mouse breast cancer is 20-35 days.

Embodiment 2

[0038] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that the contained anticancer active ingredients are:

[0039] 30% by weight of cytochalasin, ellipticine chloride, ellipticine, ellipticine methyl, mitocloramine, mitoradone, mitorguanidine hydrazone, mitonaphthine, Mitohydrazine, Mitoquinone, Mitospex, Mitotane, Mitonamamine, Mitozolid, Mitoransone, Salicylate, Colchicine, Colchicine, Norcolchicine Alkaline, Thio-colchicine, Colcemid, Colchicamide, Colchicine, Norcolchicine, Thio-colchicine, Colchicamine, Colchicamide, Colchicine, Cytochalasin , naphthyl carbamate, naphthol, α-naphthol, β-naphthol, α-naphthol phosphate, alcodazole, procodazole, giladazole, nocodazole or malonate ( Salt)

Embodiment 3

[0041] Put 80 mg of PLGA (copolymer of glycolic acid and glycolic acid with a ratio of 75:25) with a molecular weight of 20,000 into a container, add 100 ml of dichloromethane to dissolve and mix well, add 20 mg of cytochalasin, and shake well again Dry in vacuo to remove the organic solvent. The dried solid composition is prepared by a melting method to obtain sustained-release pellets containing 20% ​​by weight of cytochalasin, which are subpackaged and sterilized by radiation. The sustained-release pellets are suspended in water for injection containing 1.5% carboxymethylcellulose and 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The release time of the sustained-release injection in physiological saline in vitro is 14-24 days, and the release time in mouse liver cancer is 20-35 days.

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PUM

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Abstract

The slow releasing injection containing antimiotic medicine belongs to the field of slow releasing anticancer medicine technology. The injection includes the components of anticancer medicine, slow releasing supplementary material, suspending agent and/or solvent. The anticancer medicine includes cytochalasin, colchicines, beta-naphthol, acodazole, giracodazole, nocodazole or other antimiotic medicine; the slow releasing supplementary material is polylactic acid, glycolic acid-hydroxyacetic acid copolymer, EVA, polifeprosan or their composition; the suspending agent is carboxymethyl cellulose, mannitol, etc.; the solvent is selected from distilled water, injection water, anhydrous alcohol, etc. The slow releasing anticancer injection may be injected in different modes and has reduced systemic toxic reaction, raised local medicine concentration and raised treating effect.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection containing antimitotic drugs, belonging to the technical field of medicines. (2) Background technology [0002] Antimitotic drugs, as commonly used chemotherapeutic drugs, have been widely used in the treatment of various malignant tumors, and have achieved relatively obvious effects. However, further studies have found that inappropriate drug administration often leads to the generation of tolerance, which eventually leads to the failure of treatment. Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor. See Kong Qingzhong "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of brain tumors in ra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/16A61K9/10A61K31/415A61K31/165A61K47/30A61P35/00
Inventor 孔庆忠孙娟贺润萍刘恩祥
Owner 孔庆忠
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