Slow released anticancer injection

A technology of slow-release injections and slow-release implants, which is applied to antineoplastic drugs, medical preparations containing active ingredients, organic active ingredients, etc., and can solve problems such as poor curative effect, difficult operation, and many complications

Inactive Publication Date: 2007-01-03
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

[0111] Put 80mg of polyphenylpropanine (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) 20:80) copolymer into the container, add 100ml of dichloromethane, dissolve and mix well, add 10mg Actinomycin D and 10 mg formustine were shaken again and spray-dried to prepare injection microspheres containing 10% actinomycin D and 10% formustine. Then the microspheres were suspended 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 release time of the sustained-release injection in physiological saline in vitro is 10-15 days, and the release time under the skin of mice is about 20-30 days.

Embodiment 2

[0113] The method steps for processing into a sustained-release injection are the same as in Example 1, but the difference is that the anti-cancer active ingredients and their weight percentages are:

[0114] (1) 2-40% of formustine or bendamustine and 2-40% of melphalan, 4H-peroxycyclophosphamide, vinorelbine, tamoxifen, methotrexate, doxorubicin , Epirubicin or Actinomycin D;

[0115] (2) 2-40% of tamustine or carmustine and 2-40% of melphalan, 4H-peroxycyclophosphamide, vinorelbine, tamoxifen, methotrexate, adriamycin, Combination of epirubicin or actinomycin D;

[0116] (3) 2-40% of Nimustine or Lomustine and 2-40% of Melphalan, 4H-Peroxycyclophosphamide, Vinorelbine, Tamoxifen, Methotrexate, Adriamycin, Combination of Epirubicin or Actinomycin D; or

[0117] (4) 2-40% of semustine or ramustine and 2-40% of melphalan, 4H-peroxycyclophosphamide, vinorelbine, tamoxifen, methotrexate, adriamycin, Combination of epirubicin or actinomycin D.

[0118] The sustained-release excipient...

Embodiment 3

[0120] Put 70mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65000 into a container, add 100ml of dichloromethane, dissolve and mix well, add 15mg of carmustine and 15mg of melphalan, shake well and vacuum Dry to remove organic solvents. The dried drug-containing solid composition was freeze-pulverized into a micropowder containing 15% carmustine and 15% melphalan, and then suspended in physiological saline containing 1.5% sodium carboxymethyl cellulose to prepare the corresponding Suspension type sustained-release injection, viscosity of 300cp-400cp (at 20℃-30℃). The release time of the sustained-release injection in physiological saline in vitro is 10-15 days, and the release time under the skin of mice is about 20-30 days.

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Abstract

The slow released anticancer injection consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is composition of fotemustine, bendamustine, tallimustine and other cell toxicant medicines. The slow releasing supplementary material is polylactic acid and its copolymer, EVAc, etc. The .suspending agent is carboxymethyl cellulose sodium, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent. The present invention has raised local concentration for 30-40 days, and may be used alone or together with chemotherapy, radiotherapy and other non-operative treatment.

Description

(1) Technical field [0001] The invention relates to a new anti-cancer sustained-release injection and a preparation method thereof, and belongs to the technical field of medicines. Specifically, the present invention provides a sustained-release anti-cancer drug containing formustine and / or a cytotoxic drug, which is mainly a sustained-release injection and a sustained-release implant. (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 its clinical application. [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 to form an effective dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K45/00A61K31/4184A61K31/7076A61K47/34A61K47/38A61P35/00
Inventor 孔庆伦
Owner JINAN SHUAIHUA PHARMA TECH
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