Anticancer sustained release agent containing epothilone

A technology of epothilone and isoepothilone, which is applied in the field of anticancer sustained-release agents, can solve the problems of treatment failure, increased tolerance of anticancer drugs, etc., and achieves the advantages of reducing costs, facilitating drug injection, and reducing toxicity. Effect

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 resist

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0160] Put 80mg of polyphenylpropane (p-CPP: 20:80 of sebacic acid (SA)) copolymer into a container, add 100ml of dichloromethane, 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 step of being processed into sustained-release injection is the same as that of Example 1, but the difference is that polyphenylene is 50:50, and the contained anticancer active ingredient and weight percentage thereof 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-hydroxycamptothecin , shake again and dry in vacuo to remove the organic solvent. 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-420ep (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

Disclosed is an anti-cancer drugs slow release agent containing Epothilone which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active constituents include Epothilone, Epothilone derivatives, Epothilone B, Epothilone D and combination of anti-cancer drugs selected from phosphoinositide-3-kinase inhibitor, of pyrimidine analogues and/or DNA restoring enzyme inhibitor, the slow release auxiliary materials include polylactic acid and its copolymer, polyethylene glycol, PLA-COOH copolymer, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid), poly(fumaric acid-sebacylic acid), Polifeprosan, polylactic acid and other biocompatible high polymers, the viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose. The anticancer active constituents and the slow release microspheres can also be prepared into slow release implanting agent for intra-tumor or around-tumor injection or placement for the effective suppression of tumor growth and for the appreciable enhancement for curative effects of non-operative treatments such as chemotherapy.

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): A61K9/00A61K31/427A61K45/06A61K47/34A61P35/00A61K47/10A61K47/14A61K47/24A61K47/26A61K47/42
Inventor 孙娟张婕邹会凤
Owner JINAN SHUAIHUA PHARMA TECH
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