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Novel anticancer sustained-release agent

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

Inactive Publication Date: 2008-09-24
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

[0115] 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 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

A new anticarcinogenic sustained-release injection consists of sustained-release microballoon sphere and menstruum; wherein, the sustained-release microballoon sphere comprises anticarcinogenic active ingredient and sustained-release accessory material; the menstruum is special menstruum containing suspending agent. The anticarcinogenic active ingredient is the combination of cytotoxic drugs of fotemustine, bendamustine, tallimustine, carmustinum, nimustine, lomustine, semustine or ranimustine and adriamycin, epirubicin, melphalan, 4H peroxide cyclophosphamide, actinomycin D, vinorelbine or nolvadex, etc.; the sustained-release accessory material is selected from polylactic acid and the multipolymer or mixture thereof, mono-methyl polyethyleneglycol, polyethyleneglycol or polylactic acid multipolymer, EVAc, the multipolymer of fatty acid and decanedioic acid, etc.; the viscosity of the suspending agent is 100cp-3000cp (at the temperature of 25 DEG C-30 DEG C), the suspending agent is selected from sodium carboxymethyl cellulose, etc. The sustained-release microballoon sphere also can be made into sustained-release implant which can be injected and placed in tumor or around tumor and can release medicine at the local parts of the tumor for 30 to 40 days; therefore, the anticarcinogenic sustained-release injection can be separately united together with non-operativetreatment such as chemo-treatment and / or radiation treatment, etc. for application.

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): A61K9/00A61K9/08A61K9/10A61K31/17A61K31/704A61K47/34A61P35/00
Inventor 孔庆伦
Owner JINAN SHUAIHUA PHARMA TECH
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