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Sustained-release preparation containing chemotherapy synergist for treating solid tumors

A sustained-release agent and synergist technology, applied in the field of anti-solid tumor sustained-release agents, can solve problems such as increased tolerance, treatment failure, and limited effective drug diffusion

Inactive Publication Date: 2011-06-15
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above factors greatly limit the effective diffusion of drugs into solid tumors and tumors, thus constituting the main obstacle to tumor chemotherapy.
[0007] Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, which often lead to the enhancement of tumor cell resistance to anticancer drugs, especially single-drug chemotherapy, resulting in treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0149] Put 90 mg of polylactic acid (PLGA, 50:50) with a peak molecular weight of 25,000-40,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 2 mg of rapamycin and 8 mg of methotrexate, and re-shake After homogenization, the organic solvent was removed by vacuum drying. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain the anti-cancer sustained release containing 2% rapamycin and 8% methotrexate. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition in physiological saline in vitro is 15-25 days, and the drug release time in mouse subcutaneous is 25-50 days.

Embodiment 2

[0151] As described in Example 1, the difference is that the peak molecular weight of polylactic acid is 35000-60000 (PLGA, 75:25), and the anticancer active ingredient and weight percentage are one of the following:

[0152] (1) 0.01-5% rapamycin and 5-20% epothilone, epothilone B, doxorubicin, epirubicin, mitomycin C, actinomycin D or a combination of dactinomycin; or

[0153] (2) 0.01-5% of rapamycin and 5-20% of fluorouracil, 6-mercaptopurine, methotrexate, flumethhotrexate, calcium levofolinate, calcium folinate, carmofur, substitute A combination of fluoride, eufurdine, topotecan, topotecan hydrochloride, cytarabine, cyclocytidine, or hydroxyurea.

Embodiment 3

[0155] Put 80mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 1mg of radish Pamycin and 19 mg of fluorouracil were re-shaken and spray-dried to prepare microspheres for injection containing 1% rapamycin and 19% fluorouracil. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 20cp-300cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 15-25 days, and the drug release time in mice subcutaneous is about 30-40 days.

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Abstract

The invention provides a sustained-release injection containing a chemotherapeutic drug and a synergist thereof for treating solid tumors. The sustained-release injection comprises sustained-release microspheres and solvents. The sustained-release microspheres comprise an anticancer-active component and a sustained-release adjuvant, wherein the anticancer-active component is the combination of a chemotherapy synergist and an anticancer drug selected from antitumor antibiotics and / or antimetabolites. The solvents are special solvents containing a suspending agent. The chemotherapy synergist ispreferably rapamycin. The sustained-release adjuvant is selected from polylactic acid, monomethyl polyethylene glycol / polylactic acid, polyethylene glycol / polylactic acid, glycolic acid copolymer, and fatty acid-sebacic acid copolymer. The viscosity of the suspending agent ranges from 80cp to 3000cp (at a temperature ranging from 20 DEG C to 30 DEG C). The suspending agent is preferably carboxymethyl cellulose. The sustained-release microspheres can be also available in the form of sustained-release implant which is administered by intratumoral or local injection or implantation. The local drug release lasts from 30 days to 50 days. The sustained-release preparation is administered alone to achieve the effects of inhibiting tumor growth and promoting drug diffusion inside the tumor, or isadministered in combination with non-operative treatments such as chemotherapy and / or radiotherapy, to enhance the curative effect of non-operative treatments.

Description

(1) Technical field [0001] The invention relates to an anti-solid tumor slow-release agent, which belongs to the technical field of medicines. Specifically, the present invention provides a slow-release injection and a slow-release implant containing a chemotherapeutic synergist. The chemotherapeutic synergist in the anti-cancer sustained-release agent can effectively inhibit or destroy the solid tumor stroma and tumor blood vessels, not only can inhibit the neovascularization of tumors, but also effectively reduce the tension, interstitial pressure, and interstitial viscosity in the tumor. Improving the interstitial fluid conductance is conducive to the effective diffusion of drugs into solid tumors and tumors, and can also increase the sensitivity of tumors to chemotherapy drugs. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, surgical treatment cannot remove scattered tumor cells, so it often recurs...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/427A61K31/704A61K31/407A61K9/10A61K38/08A61K31/436A61K47/34A61K47/30A61P35/00
Inventor 刘玉燕孔庆忠
Owner SHANDONG LANJIN PHARMA