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Anticancer composition loaded with anti-metabolism medicine fluorouracil and synergist thereof

A technology of fluorouracil and composition, which is applied in the field of anti-cancer composition, and can solve the problems of toxic reaction, inability to effectively kill tumor cells, burst release, etc.

Inactive Publication Date: 2009-03-25
JINAN KANGQUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] 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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] Put 90, 90 and 80 mg of p(BHET-EOP / TC), BHET-EOP: TC is 80:20) copolymers into three containers of A, B and C respectively, and then add 100 ml of dichloromethane to each , after dissolving and mixing, add 10mg fluorouracil, 10mg epirubicin, 10mg fluorouracil and 10mg epirubicin respectively, re-shake and prepare 10% fluorouracil, 10% epirubicin, and 10% Microspheres for Injection of Fluorouracil and 10% Epirubicin. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The release time of the sustained-release injection in physiological saline in vitro is 50-70 days, and the release time in mouse subcutaneous colon cancer is more than 60 days.

Embodiment 2

[0114] The method step of being processed into sustained release injection is the same as Example 1, but the difference is that the adjuvant used is the p(BHET-EOP / TC) of 50:50, containing anticancer active ingredient and its weight percentage is:

[0115] (1) 5-30% fluorouracil, tegafur or pemetrexed;

[0116] (2) 5-30% epirubicin, doxorubicin, pirarubicin, valrubicin, or epirubicin; or

[0117] (3) A combination of 5-30% fluorouracil or pemetrexed and 5-30% epirubicin, doxorubicin, pirarubicin, valrubicin or epirubicin.

Embodiment 3

[0119] 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 pemetrexed, 30mg of doxorubicin, 15mg of pemetrexed and 15mg of doxorubicin, re-shake and use the spray drying method to prepare Microspheres for Injection of Trecet and 15% Doxorubicin. 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 55-65 days, and the drug release time in mouse subcutaneous lung cancer is about 60 days.

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PUM

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Abstract

Disclosed is an anticancer, which contains antimetabolics fluorouracil and the synergist thereof, and is a sustained-release injection. The anti-cancer combination is composed of sustained-release microspheres and solvent; wherein, the sustained-release microsphere contains effective anticancer ingredients and auxiliary material; the solvent is common solvent or special solvent which contains suspending agent. The viscosity of the suspending agent is 100cp-3000cp (20 DEG C-30 DEG C) and is selected from carboxymethyl cellulose; the antimetabolics is selected from methotrexate, fluorouracil, carmofur, tegafur, decitabine, capecitabine or gemcitabine; the synergist is tetrazine medicine or anticancer antibiotics; the auxiliary material is selected from p(LAEG-EOP), p(DAPG-EOP), or polyphosphate copolymer, or copolymer or mixture of polyphosphate, polylactic acid, polifeprosan, sebacic acid and PLGA; the anticancer combination also can be made into sustained-release implants which can be injected or implanted in tumor or the periphery of tumor with the effective medicine concentration maintained for more than 50 days; meanwhile, the systemic reaction of the medicine is obviously reduced; the treatment effects of the non-operative treatments such as chemotherapy or radiation treatment are selectively enhanced.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing anti-metabolism drugs and synergists, belonging to the technical field of medicines. Specifically, the invention relates to a slow-release preparation that can stably release anti-metabolite drugs and synergists locally in solid tumors, mainly slow-release implants and slow-release injections, which can prolong the drug release time and can Increased drug sensitivity. (2) Background technology [0002] Local application of chemotherapeutic drugs, especially local sustained release, has become the current research direction and focus of solid tumor chemotherapy. 参见(中国专利申请号200510042234.3、03148624.X、200510042236.2、96116041.1、97107078.4、200510042260.6、200510042261.0、200510042262.5、200510042263.X;美国专利US5651986,RE37410)。 [0003] However, the sustained-release excipients used in the above-mentioned and other existing pharmaceutical preparations more or less cause sudden release or uneven rele...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/08A61K31/513A61K31/704A61K47/30A61K45/00A61P35/00
Inventor 孙娟张红军俞建江邹会风
Owner JINAN KANGQUAN PHARMA TECH
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