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Anticancer sustained-release agent containing epothilone

A technology of epothilone and hydroepothilone, which is applied in the field of anticancer sustained-release preparations, can solve the problems of treatment failure, increased tolerance of anticancer drugs, etc., so as to reduce costs, facilitate drug injection, and reduce complications Effect

Inactive Publication Date: 2009-05-20
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, single-agent chemotherapy often leads to increased resistance of tumor cells to anticancer drugs, with consequent treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0160] 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 Epothilone B and 10mg 7-hydroxyl-staurosporine, re-shake and spray-dry to prepare injection containing 10% epothilone B and 10% 7-hydroxyl-staurosporine Microspheres. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 200cp-400cp (at 20°C-30°C), the release time of the slow-release injection in physiological saline in vitro is 18-25 days, and the release time of the subcutaneous mouse is about 20-30 days.

Embodiment 2

[0162] The method steps of being processed into sustained-release injections are the same as in Example 1, but the difference is that polyphenylene is 50:50, and the contained anticancer active ingredients and their weight percentages are: 5% epothilone, epothilone Epothilone A, Epothilone B, Epothilone C, Epothilone D, Isopothilone D, Epothilone E, Epothilone F, ixabepilone (BMS-247550), aza Epothilone B, furan epothilone D or BMS-310705 with 15% of 7-hydroxy-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine Combinations of ketones, alkylphosphocholines, or hexadecylphosphorylcholines,

[0163] The viscosity of the injection is 200cp-400cp (at 20°C-30°C).

Embodiment 3

[0165] Put 70 mg of polylactic acid (PLA) with a peak molecular weight of 10,000-20,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, then add 20 mg of epothilone D and 10 mg of 7-ethyl-10-hydroxycamptotheca Alkali, shake again and dry in vacuo to remove organic solvents. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 20% ​​epothilone D and 10% 7-ethyl-10-hydroxycamptothecin, and then suspending in 1.5% sodium carboxymethylcellulose The corresponding suspension-type sustained-release injection was prepared in normal saline. The viscosity of the injection is 240cp-420cp (at 20°C-30°C), and the release time of the slow-release injection in physiological saline in vitro is 20-35 days, and the release time of the subcutaneous mouse is about 35-50 days.

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Abstract

The invention relates to anti-cancer drug slow release agent containing epothilone, which consists of slow release microspheres and solvent, wherein the slow release microspheres comprise anti-cancer effective components and slow release accessories; and the solvent is special solvent containing suspending agent. The anti-cancer effective components are combinations of epothilone, epothilone derivative, epothilone B, epothilone D and anticancer drugs selected from phosphoinositide 3-kinase inhibitor, pyrimidine analog and / or DNA repairase inhibitor, and the like; the slow release accessories are biocompatible high molecules such as polylactic acid and copolymer thereof, polyethylene glycol, terminal carboxyl polylactic acid copolymer, di-fatty acid and sebacic acid copolymer, poly (erucic acid dimmer-sebacic acid), poly (fumaric acid-sebacic acid), polifeprosan, polylactic acid, and the like; and the suspending agent is selected from sodium carboxymethyl cellulose and the like when the viscosity of the suspending agent is 100 to 3,000cp (at a temperature of between 20 and 30 DEG C). The anti-cancer effective components and the slow release microspheres can also be made into slow release implant agents, can effectively inhibit tumor growth through injection or placement and energy removal in tumor or tumor periphery, and can also remarkably enhance curative effect of non-operative treatment such as chemicotherapy and the like.

Description

(1) Technical field [0001] The invention relates to an anticancer sustained-release agent containing epothilone, which belongs to the technical field of medicines. Specifically, the invention provides a sustained-release injection and a sustained-release implant containing epothilone and its synergist. (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 or causes tumor cells to spread and metastasize due to surgical stimulation; radiotherapy and traditional chemotherapy are not selective, and it is difficult to form an effective drug concentration or therapeutic dose in the local tumor, resulting in poor efficacy and high toxicity. Simply increasing the dose of drugs or radiation is limited by systemic toxicity. See Kong et al. "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of rat brain tumors" "Journ...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/427A61K45/00A61K47/30A61K47/34A61K47/32A61P35/00
Inventor 孙娟邹会凤
Owner JINAN SHUAIHUA PHARMA TECH
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