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
View PDF11 Cites 19 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, single-agent chemotherapy often leads to increased resist

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0159] Example 1.

[0160] Put 80mg of polyphenylpropanine (p-carboxyphenylpropane (p-CPP): Sebacic acid (SA) 20:80) copolymer into the container, add 100ml of dichloromethane, dissolve and mix well, add 10mg Epothilone B and 10mg 7-hydroxyoxy-staurosporin, shake well and spray-dry to prepare injection containing 10% epothilone B and 10% 7-hydroxyoxy-staurosporin Microspheres. Then the microspheres are suspended 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 sustained-release injection in physiological saline in vitro is 18-25 days, and the release time under the skin of mice is about 20-30 days.

Example Embodiment

[0161] Example 2.

[0162] The method of processing into a sustained-release injection is the same as in Example 1, but the difference is that the polyphenylprotease is 50:50, and the anti-cancer active ingredients and their weight percentages are: 5% epothilone, epothilone Epothilone A, Epothilone B, Epothilone C, Epothilone D, Epothilone D, Epothilone E, Epothilone F, ixabepilone (BMS-247550), Aza Epothilone B, Epothilone furan D or BMS-310705 and 15% of 7-hydroxyoxy-staurosporin, 7-O-alkyl-staurosporin, β-methoxy astrospore A combination of hormone, alkyl phosphocholine or hexadecyl phosphocholine,

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

Example Embodiment

[0164] Example 3.

[0165] Put 70mg of polylactic acid (PLA) with a peak molecular weight of 10000-20000 into the container, add 100ml of dichloromethane, dissolve and mix well, add 20mg of epothilone D and 10mg of 7-ethyl-10-hydroxycamptotheca Alkali, shake well and vacuum dry to remove organic solvents. The dried drug-containing solid composition was freeze-pulverized into a micropowder containing 20% ​​epothilone D and 10% 7-ethyl-10-hydroxycamptothecin, and then suspended in 1.5% sodium carboxymethyl cellulose In normal saline, the corresponding suspension type sustained-release injection was prepared. The viscosity of the injection is 240cp-420cp (at 20°C-30°C), the release time of the sustained-release injection in physiological saline in vitro is 20-35 days, and the release time under the skin of mice is about 35-50 days.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Viscosityaaaaaaaaaa
Viscosityaaaaaaaaaa
Viscosityaaaaaaaaaa
Login to view more

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K9/10A61K31/427A61K45/00A61K47/30A61K47/34A61K47/32A61P35/00
Inventor 孙娟邹会凤
Owner JINAN SHUAIHUA PHARMA TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap