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Anti cancer controlled release agent of carried interstitial hydrolytic agent and derivative of Epothilone

A technology of epothilone and hydrogen epothilone, which is applied in the direction of antineoplastic drugs, drug combination, and drug delivery, and can solve problems such as enhanced epothilone tolerance, limitation of effective drug diffusion, and obstacles to tumor chemotherapy , to achieve the effect of facilitating penetration and diffusion, improving interstitial fluid conductivity, and promoting penetration and diffusion

Inactive Publication Date: 2007-05-09
JINAN SHUAIHUA PHARMA TECH
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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 leads to the enhancement of tumor cell resistance to epothilone, and the result is treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0156] Put 40 mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymer and 40 mg of PLGA (50:50, MW20000) into a container, add 100 ml of dichloro methane, after dissolving and mixing, add 10 mg epothilone D and 10 mg collagenase, re-shake and prepare microspheres for injection containing 10% epothilone D and 10% collagenase by spray drying method. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare a corresponding suspension type sustained-release injection with a viscosity of 280cp-560cp (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 22-35 days.

Embodiment 2

[0158]The method step of being processed into sustained-release injection is the same as that of Example 1, but the difference is that the p-carboxyphenyl propane of the sustained-release auxiliary material polyphenylpropane: sebacic acid is 50:50, PLGA is 75:250, and MW is 40000 ;Contains 5% rapamycin, epothilone, epothilone A, epothilone B, epothilone C, epothilone D, isopothilone D , epothilone E, epothilone F, BMS-247550, azaepothilone B, furan epothilone D, or the combination of BMS-310705 and 15% gefitinib; viscosity of extended-release injection It is 300cp-580cp (at 20°C-30°C).

Embodiment 3

[0160] Put 40mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymer and 40mg of PLA (MW20000) into the container, add 100 ml of dichloro Methane, after dissolving and mixing, add 5 mg hyaluronidase and 15 mg rapamycin, shake again, and then vacuum dry to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 5% hyaluronidase and 15% rapamycin, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding Suspension-type sustained-release injections with a viscosity of 200cp-420cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 20-35 days, and the drug release time in mice subcutaneous is about 30-40 days.

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PUM

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Abstract

A slowly-release anticancer medicine in the form of injection or implant is disclosed. Said slowly-release injection is composed of a special solvent containing suspending aid and the slowly-release microballs consisting anticance medicine, iterstitial hydrolyte and slowly-releasing auxiliary. Said anticancer medicine is chosen from Epothilone A, Epothilone B, etc. Said interstitial hydrolyte is chosen from collagenase, relaxin, etc. Said slowly-releasing auxiliary is chosen from p(BHET-EOP / TC), p(LAEG-EOP), polyethanediol, etc.

Description

(1) Technical field [0001] The invention relates to an anti-solid tumor composition containing an interstitial hydrolyzing agent, which is an anti-cancer slow-release agent and belongs to the technical field of medicines. Specifically, the invention provides a sustained-release injection and a sustained-release implant containing an interstitial hydrolyzing agent. The anti-cancer slow-release agent can effectively inhibit or destroy the solid tumor stroma and tumor blood vessels, and can inhibit tumor angiogenesis, effectively reduce the tension in the tumor, interstitial pressure, and interstitial viscosity, thereby improving its interstitial fluid conduction. The rate is conducive to the effective diffusion of drugs into solid tumors and tumors. (2) Background technology [0002] Cancer surgical treatment cannot remove scattered tumor cells, so it often recurs or causes tumor cells to spread and metastasize due to surgical stimulation; radiotherapy and traditional chemoth...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K38/46A61K47/34A61P35/00
Inventor 孙娟刘玉燕孔庆新
Owner JINAN SHUAIHUA PHARMA TECH
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