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Anticancer medicament and synergist simultaneously carrying anticancer sustained release agent

A technology for anticancer drugs and sustained-release agents, applied in the field of anti-cancer sustained-release agents, can solve the problems of increased tolerance of anticancer drugs, treatment failure and the like

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

[0161] Put 80mg of polystyrene (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) 20:80) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, add 10mg of angstrom The phomycin D and leuprolide were shaken again and then spray-dried to prepare injection microspheres containing 10% epothilone D and 10% leuprolide. Then the microspheres were suspended in physiological saline containing 15% mannitol to prepare the corresponding suspension type sustained-release injection with a viscosity of 20cp-300cp (at 20°C-30°C). The release time of the sustained-release injection in vitro in physiological saline is 24-30 days, and the release time under the skin of mice is about 25-32 days.

Embodiment 2

[0163] The process of processing into a sustained-release injection is the same as in Example 1, but the difference is that the p-CPP:SA in polystyrene is 50:50, and the anti-cancer active ingredients and their weight percentages are:

[0164] (1) 5% epothilone B or isoepothilone D and 15% cyclophosphamide, melphalan, leuconin, ifosfamide, 4H-peroxycyclophosphamide, norcantharidin A combination of Su, metopepa, uritepa or azatepa;

[0165] (2) 15% Epothilone D or BMS-247550 and 5% Cyclophosphamide, Melphalan, Lyukonine, Ifosfamide, 4H Peroxycyclophosphamide, Norcantharidin, Meto A combination of tippa, uritepa or azatepa; or

[0166] (3) 10% of epothilone Aza, epothilone furanolide D or BMS-310705 and 5% of cyclophosphamide, melphalan, leuconin, ifosfamide, 4H-peroxy ring Combinations of phosphoramide, norcantharidin, metotepa, uritepa or azatepa. The viscosity of the prepared sustained-release injection is 80cp-600cp (at 20℃-30℃).

Embodiment 3

[0168] Put 70mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 20000-40000 into the container, add 100ml of dichloromethane, dissolve and mix well, add 15mg of epothilone B and 15mg of melphalan, and shake again After homogenization, the organic solvent was removed by vacuum drying. The dried drug-containing solid composition was freeze-pulverized into a micropowder containing 15% epothilone B and 15% melphalan, and then suspended in physiological saline containing 1.5% sodium carboxymethyl cellulose to prepare the corresponding The suspension type sustained-release injection, the viscosity is 200cp-380cp (20℃-30℃). The release time of the sustained-release injection in vitro in physiological saline is 28-35 days, and the release time under the skin of mice is about 30-40 days.

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Abstract

Disclosed is an anti-cancer slow release agent in the form of slow release injection or slow release implantation agent carrying both anti-cancer drugs and synergistic agent, the slow release injection 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 suspending agent is selected from carboxymethylcellulose, the viscosity of the suspension adjuvant is 80-3000cp (at room temperature). The anticancer active constituent being the combination of alkylating agent such as Melphalan and isoendoxan, purine analogues such as 06-BG and / or hormone group anti-cancer drugs selected from Triptorelin, Goserelin Leuprorelin and Epothilone and its derivatives (Epothilone A-F), the slow release auxiliary materials are selected from polylactic acid and its copolymer, Polifeprosan, polylactic acid copolymer or mixture, sebacylic acid copolymer or mixture. The slow release injection and slow release implanting agent can be used independently for effectively suppressing tumor accretion, or used in combination with non-operative methods such as chemotherapy and / or radiotheraphy with the function of improving their treatment effects.

Description

(1) Technical field [0001] The invention relates to an anti-cancer slow-release agent containing a synergist, which belongs to the technical field of medicines. Specifically, the present invention provides a sustained-release injection or sustained-release implant containing a synergist and an anticancer drug, wherein the anticancer drug is an alkylating agent, a purine derivative and / or a hormone anticancer drug . (2) Background technology [0002] The treatment of cancer 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 on the tumor. The effect is poor and the toxicity is high. Simply increasing the dose of drugs or radiation is limited by systemic toxicity. See Ko...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K31/427A61P35/00
Inventor 孔庆新刘恩祥贺润平
Owner JINAN SHUAIHUA PHARMA TECH
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