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Fluorouracil containing anti-cancer sustained-release injection

A sustained-release injection and fluorouracil technology, applied in the field of medicine, can solve problems such as poor curative effect, difficult operation, and many complications

Inactive Publication Date: 2008-08-06
JINAN SHUAIHUA PHARMA TECH
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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

[0116] 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 10mg Hydroxycamptothecin and 10 mg of formustine were re-shaken and spray-dried to prepare injection microspheres containing 10% hydroxycamptothecin and 10% formustine. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 220cp-460cp (at 20°C-30°C). 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

[0118] 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:

[0119] (1) 2-40% of formustine, nimustine or carmustine and 2-40% of cytotoxic drugs including hydroxycamptothecin, mitozolomide, 4-carboxy temozolomide, A combination of cetaxel, ifosfamide, etoposide, teniposide, vinblastine, anastrozole, tamoxifen, fluorouracil (5-FU), or mitomycin C;

[0120] (2) 2-40% of bendamustine and 2-40% of cytotoxic drugs including hydroxycamptothecin, mitozolomide, 4-carboxy temozolomide, docetaxel, ifosfamide, A combination of etoposide, teniposide, vinblastine, anastrozole, tamoxifen, fluorouracil (5-FU), or mitomycin C;

[0121] (3) 2-40% of lomustine and 2-40% of cytotoxic drugs including hydroxycamptothecin, mitozolomide, 4-carboxy temozolomide, docetaxel, ifosfamide, and combinations of poside, teniposide, vinblastine, anastrozole, ...

Embodiment 3

[0126]Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of nimustine and 15 mg of mitozolomide, and re-shake Dry in vacuo to remove the organic solvent. The dried drug-containing solid composition was frozen and pulverized to make micropowder containing 15% nimustine and 15% mitozolomide, and then suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding Suspension-type sustained-release injection with a viscosity of 300cp-400cp (at 20°C-30°C). 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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Abstract

The invention relates to anticancer sustained release injection which comprises sustained release microspheres and menstruum, wherein, the sustained release microspheres comprise anticancer active components and sustained release auxiliary material; the menstruum is special menstruum that contains suspending agent. The anticancer active components are fotemustine, nimustine, carmustine or combination of bendamustine and mitozolomide, docetaxel, etoposide, teniposide, vinblastine, anastrozole, tamoxifen, fluorouracil or mitomycin C; the sustained release auxiliary material is polylactic acid and polylactic acid copolymer, polyethylene glycol and polylactic acid copolymer of polyethylene glycol, terminal carboxyl group polylactic acid copolymer, EVAc, fatty acid and decanedioic acid copolymer, etc.; viscosity of the suspending agent is 100cp-3,000cp (at 25 DEG C-30 DEG C), and the suspending agent is selected from sodium carboxymethylcellulose, etc. The sustained release microspheres can also be made into sustained release implant; the injection or implant is injected or placed in or around tumor so as to reduce general reaction of the drug and selectively improve and keep local concentration for about 30-50 days. The anticancer sustained release injection can be used solely and can also promote anti-tumor effects of non-operative treatments, such as chemotherapy and / or radiotherapy, etc.

Description

(1) Technical field [0001] The invention relates to an anticancer sustained-release agent and a preparation method thereof, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release preparation of anticancer drugs containing formustine and cytotoxic drugs, mainly slow-release injections and slow-release implants. (2) Background technology [0002] As one of the conventional treatment methods for cancer, chemotherapy drugs have been widely used in the treatment of various malignant tumors, and the effect is relatively obvious. However, its obvious systemic toxicity greatly limits the application of this drug. [0003] 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 concentratio...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/08A61K31/513A61K45/06A61K47/34A61P35/00
Inventor 孙娟
Owner JINAN SHUAIHUA PHARMA TECH
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