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Compound anticancer sustained-release injection containing bendamustine

A technology for bendamustine and sustained-release injections, which can be applied in pharmaceutical formulations, anti-tumor drugs, drug combinations, etc., and can solve problems such as treatment failure and enhanced tolerance to anti-cancer drugs.

Inactive Publication Date: 2008-07-16
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, which often leads to the enhancement of tumor cell resistance to anticancer drugs, and the result is treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0138] Put 80mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg of benzene Damustine and 10 mg melphalan were re-shaken and spray-dried to prepare microspheres for injection containing 10% bendamustine and 10% melphalan. 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 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

[0140] The method steps for processing into sustained-release injections are the same as in Example 1, but the difference is that the anti-cancer active ingredients and their weight percentages are: 1-40% bendamustine and 1-40% cyclophosphamide , melphalan, tumor canning, ifosfamide, 4H-peroxycyclophosphamide, dephosphamide, phosphamide, pefosfamide, hexamethazine, cantharidin, norcantharidin, mannasulfan, Triosulfan, Ritrasufan, Inprosulfan, Etoglu, Piperbromane, Piposufan, Aining, Epoxypiperazine, Benzotip, Purimotepa, Metox combination of uretipa, uretepa or azatepa;

[0141] The excipients used are: racemic polylactic acid, racemic polylactic acid / glycolic acid copolymer, monomethyl polyethylene glycol / polylactic acid, monomethyl polyethylene glycol / polylactic acid copolymer, polyethylene glycol / polylactic acid, polyethylene glycol / polylactic acid copolymer, carboxyl-terminated polylactic acid or carboxyl-terminated polylactic acid / glycolic acid copolymer; the viscosity ...

Embodiment 3

[0143] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of bendamustine and 15 mg of cyclophosphamide, and re-shake Dry in vacuo to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 15% bendamustine and 15% cyclophosphamide, and then suspending 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 invention provides a compound anticancer drug sustained release agent containing bendamustine, which is a sustained release injection consisting of sustained release microspheres and solvent, wherein, the sustained release microspheres comprise effective anticancer components and sustained-release excipient, and the solvent is a special solvent containing a suspending agent. The effective anticancer components are bendamustine and the combination of bendamustine synergist chosen from alkylating agent and / or hormone anticarcinogen. The sustained-release excipient is chosen from one of or the combination of polylactic acid, copolymer thereof, monomethyl polyethylene glycol, polyethylene glycol, carboxyl end polylactide copolymer, dual fatty acid, sebacie acid copolymer, poly (erucic dimer- sebacie acid), poly (fumarate- sebacie acid), Polifeprosan, polylactide copolymer or mixture and EVAc. The suspending agent is chosen from carboxymethyl cellulose, etc., and the viscosity of the suspending agent is 80cp-3000cp (in the temperature of 20 DEG C-30 DEG C). The sustained release microspheres can also be produced into a sustained-release implant. The sustained-release implant and the sustained release injection is arranged around the tumor or injected in the tumor, which can obviously improve the curative effect if being applied independently or combined with chemotherapeutics and / or radiotherapeutics and other non-operative treatment.

Description

(1) Technical field [0001] The invention relates to a compound anticancer slow-release injection containing bendamustine, which belongs to the technical field of medicines. Specifically, the present invention provides a sustained-release injection or sustained-release implant loaded with bendamustine and its synergist, wherein the bendamustine synergist is an alkylating agent and / or a hormone class of anticancer drugs. (2) Background technology [0002] Currently, 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 to...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/08A61K31/4184A61K47/34A61P35/00A61K47/26
Inventor 孙中先
Owner JINAN SHUAIHUA PHARMA TECH
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