Anticancer slow release comprising tetrazole violet and cytotoxic drug

A violet and cytotoxic technology, applied in the field of medicine, can solve problems such as poor curative effect, many complications, and difficult operation

Inactive Publication Date: 2007-03-14
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

[0105] Put 80mg of polystyrene (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) 20:80) copolymer into the container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg Hydroxycamptothecin and 10mg tetrazolium violet were shaken again and spray-dried to prepare injection microspheres containing 10% hydroxycamptothecin and 10% tetrazolium violet. Then the microspheres were suspended in normal 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 release time of the sustained-release injection in vitro in physiological saline is 10-15 days, and the release time under the skin of mice is about 20-30 days.

Embodiment 2

[0107] The method of processing into a sustained-release injection is the same as in Example 1, but the difference is that the anti-cancer active ingredients and their weight percentages are: 2-40% hydroxycamptothecin, mitozolamide, 4-carboxytemozolomide , Docetaxel, Ifosfamide, Lomustine, Estramustine, Formustine, Samustine, Etoposide, Teniposide, Vinblastine, Anastrozole, Tamole Combination of sifen, fluorouracil or mitomycin C with 2-40% tetrazolium violet.

[0108] The auxiliary materials used are: racemic polylactic acid, racemic polylactic acid / glycolic acid copolymer, monomethyl polyethylene glycol / polylactic acid, monomethyl polyethylene glycol / polylactic acid copolymer, polyethylene glycol / Polylactic acid, polyethylene glycol / polylactic acid copolymer, carboxyl-terminated polylactic acid or carboxyl-terminated polylactic acid / glycolic acid copolymer; the viscosity of sustained-release injection is 10cp-650cp (at 20℃-30℃).

Embodiment 3

[0110] Put 70mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65000 into the container, add 100ml of dichloromethane, dissolve and mix well, add 10mg of tetrazolium violet and 20mg of mitozolamide, shake again and vacuum Dry to remove organic solvents. The dried drug-containing solid composition was freeze-pulverized into a micropowder containing 10% tetrazolium violet and 20% mitozolamide, and then suspended in physiological saline containing 1.5% sodium carboxymethyl cellulose to prepare the corresponding Suspension type sustained-release injection, viscosity is 300cp-400cp (at 20℃-30℃). The release time of the sustained-release injection in vitro in physiological saline is 10-15 days, and the release time under the skin of mice is about 20-30 days.

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Abstract

Disclosed is an anticancer slow release injection containing tetrazole Ionone and cytotoxic drugs, which comprises slow release micro-balloons and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active constituents include tetrazole lonone and cytotoxic drugs selected from docetaxel, Fotemustine, alkylating agent, Topo enzyme inhibitor and / or plant alkaloid, the slow release auxiliary materials include polylactic acid and glycollic acid copolymer, polyethylene glycol and polylactic acid copolymer, PLA-COOH copolymer, EVAc, aliphatic acid and sebacylic acid copolymer, the viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C), and is selected from sodium carboxymethylcellulose. The slow release microspheres can also be prepared into slow release implanting agent for injection or placement in or around tumor with the effects of lowering general reaction of drugs, selectively increasing and maintaining local concentration to around 30-50 days, as a result, the injection can be used for the treatment of tumor independently, and has the functions of improving the treatment effect of the non-operative methods such as chemotherapy and / or radiotheraphy.

Description

(1) Technical field [0001] The invention relates to an anti-cancer slow-release injection containing tetrazolium violet and cytotoxic drugs and a preparation method thereof, and belongs to the technical field of medicines. Specifically, the present invention provides a slow-release anti-cancer drug containing tetrazolium violet and cytotoxic drugs, mainly slow-release injections and slow-release implants. (2) Background technology [0002] As one of the conventional treatment methods for cancer, chemotherapeutics have been widely used in the treatment of various malignant tumors, and their effects are relatively obvious. However, its obvious systemic toxicity greatly limits the application of the drug. [0003] Due to the excessive swelling and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure, and interstitial viscosity are higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/41A61K45/06A61K47/34A61P35/00
Inventor 孔庆忠孙娟孙忠厚
Owner JINAN SHUAIHUA PHARMA TECH
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