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Anti-cancer sustained-released injection containing epothilone derivate

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

Inactive Publication Date: 2009-04-01
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 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 Paclitaxel and 10 mg epothilone B were re-shaken and spray-dried to prepare microspheres for injection containing 10% paclitaxel and 10% epothilone B. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 220cp-460cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

Embodiment 2

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

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

[0139] (b) 20% epothilone, epothilone A, epothilone B, epothilone C, epothilone D, isopothilone D, epothilone E, epothilone Mymycin F, BMS-247550, azaepothilone B, furan epothilone D or BMS-310705 with 10% carmustine, nimustine, bendamustine, garmustine , ramustine, formustine, mermustine, lomustine, methyllomustine, uramustine, samustine, semustine, streptozocin, or mitozole combinations of amines; or

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

Embodiment 3

[0142] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 40,000-65,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of epothilone D and 15 mg of nimustine, and re- Shake well and dry under vacuum to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 15% epothilone D and 15% nimustine, and then suspending in physiological saline containing 1.5% carboxymethylcellulose sodium to obtain The corresponding suspension-type sustained-release injection has a viscosity of 300cp-400cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

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Abstract

The invention relates to an anti-cancer sustained release injection containing epothilone derivative, consisting of sustained microspheres and menstruum. The sustained microspheres comprise anti-cancer drugs selected from taxane, alkylating agent and / or plant alkaloid and the like, the epothilone derivative and sustained release auxiliary material. The menstruum is a special menstruum containing suspending agent. The epothilone derivative is selected from epothilone B, epothilone D, iso-epothilone D, BMS-247550, azaepothilone B, furan epothilone D or BMS-310705. The sustained release auxiliary material is selected from poly-dl-lactide, the glycolic acid copolymer of the poly-dl-lactide, polyethyleneglycol, the polylactide copolymer of the polyethyleneglycol, carboxyl terminated polylactide copolymer, fatty acid and decanedioic acid copolymer, etc. The suspending agent is selected from carboxymethyl cellulose and the like with the viscosity of 100cp to 3000cp (under the temperature of 25 DEG C to 30 DEG C). The sustained release microsphere can also be made into a sustained release implant. The sustained release injection is injected or arranged in or around the tumour and can release drug at partial position for 40 days approximately, therefore, the sustained release injection improves the local drug concentration selectively and enhances the treatment effect of non-operative treatments, such as radiotherapy, chemotherapy and the like at the same time.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection containing epothilone derivatives, belonging to the technical field of medicines. Specifically, the present invention provides a sustained-release injection and a sustained-release implant containing epothilone derivatives. (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" "Jou...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/427A61K31/337A61K47/34A61P35/00
Inventor 孙娟刘玉燕孔庆新
Owner JINAN SHUAIHUA PHARMA TECH
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