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Medicine composition containing both anticancer medicine and its synergist

A technology of anticancer drugs and compositions, which is applied in drug combinations, antineoplastic drugs, and drug delivery, and can solve problems such as treatment failure, tumor chemotherapy obstacles, and enhanced tumor cell tolerance

Pending Publication Date: 2007-06-06
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above factors greatly limit the effective diffusion of drugs into solid tumors and tumors, thus constituting the main obstacle to tumor chemotherapy.
[0007] Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapeutic drugs, which often leads to the enhancement of tumor cell resistance to anticancer drugs, especially single drugs, resulting in treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0155] 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 rayon Pamycin and leuprolide, after re-shaking, microspheres for injection containing 10% rapamycin and 10% leuprolide were prepared by spray-drying method. 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 release time of the slow-release injection in physiological saline in vitro is 30-35 days, and the release time in mice subcutaneous is about 30-40 days.

Embodiment 2

[0157] The method step of being processed into sustained-release injection is the same as that of Example 1, but the difference is that p-CPP:SA is 50:50 in polyphenylpropanol, and the contained anticancer active ingredient and its weight percentage are: 0.5-10% rapamycin with 5-15% cyclophosphamide, melphalan, cyclophosphamide, ifosfamide, 4H-peroxycyclophosphamide, norcantharidin, methotepa, uretepa Or the combination of azatepa, the viscosity of the sustained-release injection is 180cp-450cp (at 20°C-30°C).

Embodiment 3

[0159] 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 rapamycin and 15 mg of melphalan, and shake again Then dry in vacuo to remove the organic solvent. The dried drug-containing solid composition was frozen and pulverized to make a micropowder containing 15% rapamycin and 15% melphalan, and then suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding Suspension-type sustained-release injection with a viscosity of 220cp-340cp (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 medicine composition with both anticancer medicine and its synergist is one kind of slow releasing injection comprising slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material. The solvent is special solvent containing suspending agent. The effective anticancer component is composition of sirolimus, alkylating agent, purine medicine and / or hormone anticarcinogen. The slow releasing supplementary material is selected from polylactic acid, lactic acid copolymer, polifeprosan, etc; the suspending agent is selected from carboxymethyl cellulose, etc and has viscosity of 80cp-3000cp. The medicine composition may be also prepared into slow releasing implant. Using rapamycin and other anticancer medicine can result in synergistic effect.

Description

(1) Technical field [0001] The invention relates to a pharmaceutical composition loaded with anticancer drugs and their synergists, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release injection or slow-release implant loaded with rapamycin and anticancer drugs, wherein the anticancer drugs are alkylating agents, purine derivatives and / or hormone anticancer drugs drug. (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. ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K31/436A61K47/34A61P35/00
Inventor 孔庆忠张婕
Owner SHANDONG LANJIN PHARMA
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