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Anticancer composition containing taxane medicament and bortezomib

A technology of bortezomib and taxanes, applied in the direction of drug combination, boron compound active ingredients, medical preparations containing active ingredients, etc., can solve the problems of ineffective killing of tumor cells, sudden release of drugs, toxic reactions, etc.

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 taxane medicament and bortezomib
  • Anticancer composition containing taxane medicament and bortezomib
  • Anticancer composition containing taxane medicament and bortezomib

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0108] Put 90, 90 and 80 mg of PLGA (50:50) copolymers into three containers of A, B and C respectively, then add 100 ml of dichloromethane to each, dissolve and mix well, then add 10 mg of paclitaxel and 10 mg of boron Tezomib, 10 mg paclitaxel and 10 mg bortezomib were re-shaken and spray-dried to prepare microspheres for injection containing 10% paclitaxel, 10% bortezomib, and 10% paclitaxel 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 44-55 days, and the release time in mice subcutaneously is more than 55 days.

Embodiment 2

[0110] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that used adjuvant is the PLGA of 75: 25, containing anticancer active ingredient and weight percent thereof are:

[0111] (1) A combination of 20% paclitaxel, epipaclitaxel, docetaxel or deacetylpaclitaxel and 10% bortezomib;

[0112] (2) Combination of 15% paclitaxel or docetaxel and 5% bortezomib;

[0113] (3) A combination of 10% paclitaxel or docetaxel and 2.5% 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 docetaxel, 30mg bortezomib, 15mg docetaxel and 15mg bortezomib, re-shake and use spray drying method to prepare 30% docetaxel, 30% bortezomib, 15% docetaxel and 15 % Bortezomib Microspheres for Injection. 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 taxanes 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 effective anti-tumor ingredient comprises the anti-metabolite drug and / or the combination thereof; the taxanes drug is selected from Taxol, Docetaxel, EPI-Taxol or Hydroxy-Taxol; the sustained-release excipient is selected from polyphosphonate copolymer like p(LAEG-EOP)or p(DAPG-EOP), PLA, PLGA, polyphosphonate with PLA, polifeprosan and 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 taxane drugs and bortezomib, which belongs to the technical field of medicines. Specifically, the invention relates to a sustained-release preparation capable of stably releasing taxanes 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] Despite extensive research, the pathogenesis of cancer is not well understood. 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%. 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 patie...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/337A61K31/69A61K47/30A61P35/00
Inventor 孙亮孙忠先张伟
Owner 济南基福医药科技有限公司
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