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Anticancer composition containing nitrosourea medicament and bortezomib

A technology of bortezomib and nitrosourea, applied in the field of anticancer compositions, can solve the problems of inability to effectively kill tumor cells, slow drug release, toxic reactions and the like

Inactive Publication Date: 2008-11-12
济南基福医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the sustained-release excipients used in the existing above-mentioned and other pharmaceutical preparations more or less cause sudden release or uneven release of the drug when the drug is released.
Some drugs are released too slowly, which is not enough to obtain effective drug concentration in the local area, so they cannot effectively kill tumor cells; some release drugs too fast, often causing burst release, which is likely to cause systemic toxic reactions like conventional injections

Method used

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  • Anticancer composition containing nitrosourea medicament and bortezomib
  • Anticancer composition containing nitrosourea medicament and bortezomib
  • Anticancer composition containing nitrosourea medicament and bortezomib

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0108] Put 90, 90 and 80mg p(BHET-EOP / TC), BHET-EOP: TC is 80:20) copolymer into three containers of A, B and C respectively, and then add 100 ml of dichloromethane to each , after dissolving and mixing, add 10mg carmustine, 10mg bortezomib, 10mg carmustine and 10mg bortezomib respectively, re-shake and use spray drying method to prepare 10% carmustine, 10% boron Tezomib, and microspheres for injection with 10% carmustine and 10% bortezomib. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The release time of the slow-release injection in physiological saline in vitro is 40-50 days, and the release time in mice subcutaneously is more than 50 days.

Embodiment 2

[0110] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that used auxiliary material is the p(BHET-EOP / TC) of 50: 50, containing anticancer active ingredient and weight percent thereof are:

[0111] (1) A combination of 10% estramustine, samustine, semustine, lomustine or methyllomustine and 10% bortezomib;

[0112] (2) Combination of 5% carmustine or nimustine and 15% bortezomib;

[0113] (3) Combination of 15% carmustine or nimustine and 10% bortezomib.

Embodiment 3

[0115] Put 70 mg of p(LAEG-EOP) with a peak molecular weight of 10,000-25,000 into three containers of A, B, and C, respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well, and pour into the three containers respectively Add 30mg of nimustine, 30mg of bortezomib, 15mg of nimustine and 15mg of bortezomib, re-shake and use the spray drying method to prepare 30% nimustine, 30% bortezomib, 15% Injectable microspheres of statin and 15% bortezomib. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The drug release time of the sustained release injection in physiological saline in vitro is 50-65 days, and the drug release time in mice subcutaneous is about 60 days.

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Abstract

The invention provides a sustained-release injection which is an anti-tumor composite containing nitrosoureas drug and bortezomib. The sustained-release injection comprises a sustained-release microsphere and a solution medium, wherein the sustained-release microsphere comprises effective anti-tumor ingredient and sustained-release excipient, the solution medium is a common solution medium or a special solution medium containing a suspending drug. The suspending drug has the viscosity between 100cp and 3000cp (under twenty centi degrees to thirty centi degrees) and is selected from sodium carboxymethylcellulose and others; the nitrosoureas drug is selected from nimustine,bendamustine,carmustine,galamustine,fotemustine,ranimustine,samustine or lomustine; the sustained-release excipient is selected from polyphosphonate copolymer like p(LAEG-EOP)or p(DAPG-EOP), PLA, PLGA, polyphosphonate with PLA, polifeprosan, the polymer or blending polymer of ( erucic acid dipolymer-sebacic acid) or poly(boletic acid-sebacic acid); the anti-tumor composite can also be prepared to be a sustained-release implant which can maintain the effective concentration of drug over forty days for intratumor or tumor circumference injection or placement, can also reduce general reaction obviously and enhance the treatment effect of non-operative therapeutics such as chemotherapy and radiotherapy.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing nitrosourea drugs and bortezomib, which belongs to the technical field of medicines. Specifically, the invention relates to a sustained-release preparation capable of stably releasing nitrosourea drugs and bortezomib locally in solid tumors, mainly sustained-release implants and sustained-release injections, which can prolong the drug release time and Can increase drug sensitivity. (2) Background technology [0002] Statistics show that in less than 20 years, the incidence of cancer in my country has increased by 69%, and the death rate has increased by 29.4%. The latest data show that in 2006, 3 million people died of cancer in my country. The incidence of cancer is increasing year by year and tends to be younger. According to the latest statistics from the World Health Organization, the global incidence of cancer will increase by 50% by 2020, and the number of patients will increase ...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/69A61K47/30A61P35/00
Inventor 侯洪春刘慧敏孙启明
Owner 济南基福医药科技有限公司
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