Novel anticancer sustained-release injection

A technology of sustained-release injections and sustained-release excipients, applied in the field of medicine, can solve the problems of many complications, poor curative effect, and difficult operation.

Inactive Publication Date: 2009-05-13
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 treatme

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0115] Put 80mg polyphenylene propane (p-CPP: sebacic acid (SA) 20:80) copolymer into a container, add 100ml methylene chloride, dissolve and mix well, then add 10mg Actinomycin D and 10 mg of formustine were re-shaken and spray-dried to prepare microspheres for injection containing 10% actinomycin D 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

[0117] 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:

[0118] (1) 2-40% formustine or bendamustine and 2-40% melphalan, 4H-peroxycyclophosphamide, vinorelbine, tamoxifen, methotrexate, doxorubicin , the combination of epirubicin or actinomycin D;

[0119] (2) 2-40% tamustine or carmustine and 2-40% melphalan, 4H-peroxycyclophosphamide, vinorelbine, tamoxifen, methotrexate, doxorubicin, A combination of epirubicin or actinomycin D;

[0120] (3) 2-40% nimustine or lomustine and 2-40% melphalan, 4H-cyclophosphamide peroxide, vinorelbine, tamoxifen, methotrexate, doxorubicin, a combination of epirubicin or actinomycin D; or

[0121] (4) 2-40% semustine or ramustine and 2-40% melphalan, 4H-peroxycyclophosphamide, vinorelbine, tamoxifen, methotrexate, doxorubicin, A combination of epirubicin or actinomycin D.

[0122] The su...

Embodiment 3

[0124] 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 carmustine and 15 mg of melphalan, re-shake and vacuum Dry to remove organic solvent. The dried drug-containing solid composition was frozen and pulverized to make micropowder containing 15% carmustine and 15% melphalan, and then suspended in physiological saline containing 1.5% carboxymethylcellulose sodium 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 novel sustained-release injection for cancer therapy. The sustained-release injection comprises sustained-release microspheres and dissolvent, wherein the sustained-release microspheres comprise active ingredients for cancer therapy and sustained-release auxiliary materials, and the dissolvent is special dissolvent containing suspending agent. The active ingredients for cancer therapy are combination of fotemustine, bendamustine, tallimustine, carmustine, nimustine, lomustine, semustine or ranimustine with cytotoxic drug of adriacin, epidoxorubicin, melphalan, 4H- cyclophosphamide peroxide, actinomycin D, vinorelbine or tamoxifen; the sustained-release auxiliary materials comprise polylactic acid and the copolymer or mixture thereof, monomethyl polyethylene glycol, polyethylene glycol/polylactic copolymer, EVAc, fatty acid and decanedioic copolymer; the viscocity of the suspending agent is 100cp to 3000cp (at 25 to 30 DEG C), and the suspending agent is selected from sodium carboxymethyl cellulose; the sustained-release microspheres can also be produced into sustained-release implant, and by injecting or positioning the sustained-release agent in tumor or tumor margin, drug release in local part of tumor can be performed for approximately 30 to 40 days; therefore, the sustained-release injection can be applied in combination with non-operative treatment such as chemical treatment and/or radiation treatment.

Description

(1) Technical field [0001] The invention relates to a novel anti-cancer sustained-release injection 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 / or 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 its clinical application. [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 con...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/08A61K9/10A61K31/662A61K38/12A61K47/34A61P35/00A61K47/10A61K47/26A61K47/36
Inventor 孔庆伦
Owner JINAN SHUAIHUA PHARMA TECH
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