Anticancer sustained-release preparation loaded with anti-cancer medicine and synergist thereof

A technology of anti-cancer drugs and sustained-release agents, which is applied in the field of anti-cancer sustained-release agents, and can solve problems such as increased resistance to anti-cancer drugs and treatment failure

Inactive Publication Date: 2009-03-11
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 polyphenylene propane (p-CPP: sebacic acid (SA) 20:80) copolymer into a container, add 100ml dichloromethane, dissolve and mix well, then add 10mg Pothilone D and leuprolide were re-shaken to prepare microspheres for injection containing 10% epothilone D and 10% leuprolide by spray drying. Then suspend the microspheres 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 drug release time of the sustained-release injection in physiological saline in vitro is 24-30 days, and the drug release time in mice subcutaneously is about 2532 days.

Embodiment 2

[0163] The method steps of being processed into sustained-release injections are the same as in Example 1, but the difference is that p-CPP:SA is 50:50 in polyphenylene, and the anticancer active ingredients and their weight percentages are:

[0164] (1) 5% epothilone B or isopothilone D and 15% cyclophosphamide, melphalan, leucoridine, ifosfamide, 4H peroxycyclophosphamide, norcantharidin , Metutepa, Uretepa or Azatepa in combination;

[0165] (2) 15% epothilone D or BMS-247550 and 5% cyclophosphamide, melphalan, tumor canine, ifosfamide, 4H peroxycyclophosphamide, norcantharidin, metto a combination of tepa, uretepa, or azatepa; or

[0166] (3) 10% azaepothilone B, furan epothilone D or BMS-310705 and 5% cyclophosphamide, melphalan, tumor canine, ifosfamide, 4H-peroxycycline A combination of phosphoramide, norcantharidin, metutepa, uretepa, or azatepa. The prepared sustained-release injection has a viscosity of 80cp-600cp (at 20°C-30°C).

Embodiment 3

[0168] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 20,000-40,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of epothilone B and 15 mg of melphalan, and re-shake After homogenization, the organic solvent was removed by vacuum drying. The dried drug-containing solid composition was frozen and pulverized to make a micropowder containing 15% epothilone B and 15% melphalan, and then suspended in physiological saline containing 1.5% carboxymethylcellulose sodium to obtain the corresponding Suspension-type sustained-release injections with a viscosity of 200cp-380cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 28-35 days, and the drug release time in mice subcutaneous is about 30-40 days.

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Abstract

An anticarcinogenic slow release formulation carrying an anticancer drug and a synergist is a slow release injection or a slow release implant, and the slow release injection is made from slow release microspheres and a dissolvant. The slow release microspheres comprise anticancer active components and a slow adjuvant, and the dissolvant is a special dissolvant containing a suspending agent which is selected from sodium carboxymethyl cellulose and the like, and the viscosity of the suspending agent is 80cp-3,000cp (at room temperature). The anticancer active components are alkylating agents such as melphalan, ifosfamide and the like, purine analogues such as O6-BG and the like, and/or hormones anticancer drugs selected from triptorelin, goserelin, leuprorelin and a composition selected from epothilone (A-F) and derivatives thereof; the slow release adjuvant is chosen from one of or the copolymer or the mixture of polylactic acid and a copolymer thereof, polifeprosan and the copolymer or the mixture of polylactic acid and sebacic acid copolymer; the slow release implant and the slow release injection are injected or put in tumors or around the tumors, which is beneficial to diffusing the drug in the solid tumors, maintaining high concentration, reducing drug tolerance, being capable of mutual synergy and enhancing curative effects of chemotherapy and/or radiotherapy.

Description

(1) Technical field [0001] The invention relates to an anticancer slow-release agent containing a synergist, which belongs to the technical field of medicines. Specifically, the present invention provides a slow-release injection or slow-release implant loaded with synergists and anticancer drugs, wherein the anticancer drugs are alkylating agents, purine derivatives and / or hormonal anticancer drugs . (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. "Int...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K45/00A61K47/34A61K47/10A61K47/26A61K47/36A61K47/42A61P35/00
Inventor 孔庆新刘恩祥贺润平
Owner JINAN SHUAIHUA PHARMA TECH
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