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Slow-released anticancer injection

A technology for sustained-release injections and sustained-release excipients, which can be used in antitumor drugs, medical preparations with inactive ingredients, organic active ingredients, etc., and can solve the problems of poor curative effect, many complications, and difficult operation

Inactive Publication Date: 2006-10-18
SHANDONG LANJIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, solid sustained-release implants (Chinese Patent No. ZL96115937.5; ZL97107076.8) and existing sustained-release microspheres for the treatment of brain tumors (ZL00809160.9) or U.S. Patent (US5,651,986) all have inadequacies. Easy operation, poor curative effect, many complications, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0110] Put 80mg of polyphenylpropane (p-CPP: 20:80 of sebacic acid (SA)) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg5 -FU and 10 mg doxorubicin, re-shake and prepare microspheres for injection containing 10% 5-FU and 10% doxorubicin by spray drying. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

Embodiment 2

[0112] 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 and their weight percentages are:

[0113] 2-40% 5-FU and 2-40% bleomycin, daunomycin, ararubicin, doxorubicin, epirubicin, edarubicin, pirarubicin, valerubicin Combinations of Bicin, Mitomycin C, Actinomycin D, Loxoxantrone, Mitoxantrone, Piroxantrone, Tiloxantrone, or Clozocin.

Embodiment 3

[0115] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of 5-FU and 15 mg of nimustine, re-shake and dry in vacuum Remove organic solvents. The dried drug-containing solid composition was frozen and pulverized to make a micropowder containing 10% 5-FU and 10% nimustine, and then suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding Suspension-type sustained-release injection. The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

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PUM

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Abstract

The slow released anticancer injection consists of slow released microballoon and solvent. The slow released microballoon includes effective anticancer component and slow releasing supplementary material, and the solvent is common solvent or special solvent containing suspending agent. The effective anticancer component is 5-FU synergist or the combination of 5-FU and 5-FU synergist selected from antitumor antibiotic, antimetabolite, taxane and plant alkaloid; the slow releasing supplementary material is PLA, PLGA, EVAc, etc or their composition; and the suspending agent is sodium carboxymethyl cellulose, mannitol, sorbitol, Tween-80 or their composition. The slow released microballoon may be also prepared into slow released implantation preparation. Implanting or injecting the slow released preparation to local tumor part can lower the systematic toxic reaction of the medicine and raise the medicine concentration of local tumor part selectively to raise the treating effect.

Description

(1) Technical field [0001] The invention relates to an anti-cancer sustained-release injection and a preparation method thereof, belonging to the technical field of medicines. Specifically, the present invention provides a sustained-release preparation of anticancer drugs containing 5-FU synergist or a combination of 5-FU and its synergist, mainly sustained-release injections and sustained-release implants. (2) Background technology [0002] As a commonly used chemotherapeutic drug, 5-fluorouracil (5-FU) has been widely used in the treatment of various malignant tumors, and the effect is more obvious. However, its unexpected neurotoxicity greatly limits the application of this drug. Blood vessels, connective tissue, matrix proteins, fibrinoproteins, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the diffusion of chemotherapy drugs around the tumor and in the tumor tissue. Infiltration and d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/337A61K31/513A61K45/00A61K47/26A61K47/32A61K47/34A61K47/38A61P35/00
Inventor 高化兰
Owner SHANDONG LANJIN PHARMA
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