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Anticancer sustained release injection containing epothilone derivatives

A sustained-release injection, epothilone technology, applied in the field of medicine, can solve problems such as increased resistance to anticancer drugs and treatment failure

Inactive Publication Date: 2007-05-30
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

[0135] Put 80 mg of polystyrene (p-carboxyphenyl propane (p-CPP): sebacic acid (SA) as 20: 80) copolymer into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg Paclitaxel and 10 mg of epothilone B were shaken again to prepare microspheres for injection containing 10% paclitaxel and 10% epothilone B by spray drying. Then, the microspheres were suspended in physiological saline containing 15% mannitol to prepare a corresponding suspension type sustained-release injection with a viscosity of 220cp-460cp (at 20°C-30°C). The release time of the sustained-release injection in physiological saline in vitro is 10-15 days, and the release time of the sustained-release injection under the skin of mice is about 20-30 days.

Embodiment 2

[0137] The method steps of being processed into sustained-release injections are the same as those in Example 1, but the difference is that polystyrene is 20:80, and the anticancer active ingredients and the weight percent thereof are:

[0138] (a) 5% epothilone, epothilone A, epothilone B, epothilone C, epothilone D, isoepothilone D, epothilone E, epothilone Combination of mycin F, BMS-247550, azaepothilone B, furan epothilone D, or BMS-310705 with 25% paclitaxel or docetaxel;

[0139] (b) 20% epothilone, epothilone A, epothilone B, epothilone C, epothilone D, isoepothilone D, epothilone E, epothilone Mycin F, BMS-247550, Azaepothilone B, Furanepothilone D, or BMS-310705 with 10% carmustine, nimustine, bendamustine, gamustine , ramustine, fomaustine, comustine, lomustine, methyllomustine, uramustine, samustine, semustine, streptozocin, or mitozole a combination of amines; or

[0140] (c) 20% epothilone, epothilone A, epothilone B, epothilone C, epothilone D, isoepothilone ...

Embodiment 3

[0142] Put 70 mg of polylactic acid (PLGA, 75:25) with a molecular weight peak of 40000-65000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of epothilone D and 15 mg of nimustine, and reconstitute the solution. After shaking, the organic solvent was removed by vacuum drying. The dried drug-containing solid composition is frozen and pulverized to prepare micropowder containing 15% epothilone D and 15% nimustine, and then suspended in physiological saline containing 1.5% sodium carboxymethyl cellulose to prepare The corresponding suspension-type sustained-release injection has a viscosity of 300cp-400cp (at 20°C-30°C). The release time of the sustained-release injection in physiological saline in vitro is 10-15 days, and the release time of the sustained-release injection under the skin of mice is about 20-30 days.

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Abstract

Disclosed is an anti-cancer slow release injection containing Epothilone derivatives which comprises slow release microspheres and dissolvent, the slow release micro-balloons include anticancer drugs selected from Paclitaxel, alkyl agent and / or plant alkaloids, Epothilone derivatives and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The Epothilone derivatives are selected from Epothilone B, Epothilone D, Isoepothilone D, BMS-247550, azaepothilone B, furaepothilone D or BMS-310705. The slow release auxiliary material is selected from poly-D, L-lactic acid and its glycolic copolymer, polyethylene glycol and polylactic acid copolymer, PLA-COOH copolymer, aliphatic acid and sebacylic acid copolymer, the viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C), and is selected from sodium carboxymethylcellulose, The slow release microspheres can also be prepared into slow release implanting agent, for injection or placement in or around tumor with the period of local drug release can be about 40-50 days, as a result, the local medicinal concentration can be increased selectively, and the treatment effect of the non-operative treatment methods such as chemotherapy can be improved substancially.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection containing an epothilone derivative, belonging to the technical field of medicine. Specifically, the present invention provides a sustained-release injection and a sustained-release implant containing an epothilone derivative. (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 locally in the tumor, with poor effect and high toxicity. Simply increasing the drug or radiation dose is limited by systemic toxicity. See Kong et al. "Intratumoral placement of cisplatin plus systemic carmustine for brain tumors in rats" Journal of Surgical Oncol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/427A61K31/337A61K45/06A61K47/34A61P35/00A61K47/10A61K47/26A61K47/36
Inventor 孙娟刘玉燕孔庆新
Owner JINAN SHUAIHUA PHARMA TECH
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