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Anticancer medicinal composition of loaded taxane and its synergist

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

Inactive Publication Date: 2007-08-01
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 release drugs 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 provincial toxic reactions like conventional injections

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0130]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 paclitaxel, 10mg doxorubicin, 10mg paclitaxel and 10mg doxorubicin respectively, shake up again and prepare 10% paclitaxel, 10% doxorubicin, and 10% paclitaxel and 10 % doxorubicin injection microspheres. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 100cp-200cp (at 20°C-30°C). 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

[0132] 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:

[0133] (1) 5-30% paclitaxel or docetaxel;

[0134] (2) 1-40% of arubicin, doxorubicin, epirubicin, idarubicin, pirarubicin, valrubicin, mitomycin C, actinomycin D or epirubicin Doxorubicin; or

[0135] (3) 5-30% taxane or docetaxel and 5-30% 1-40% arubicin, doxorubicin, epirubicin, edarubicin, pirarubicin, Combinations of valrubicin, mitomycin C, actinomycin D, or epirubicin.

Embodiment 3

[0137] 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 docetaxel, 30mg of epirubicin, 15mg of docetaxel and 15mg of epirubicin, re-shake and use spray drying method to prepare 30% docetaxel, 30% epirubicin, 15% polyene Paclitaxel and 15% epirubicin 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 release time of the slow-release injection in physiological saline in vitro is 55-65 days, and the release time in mice subcutaneously is about 60 days.

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PUM

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Abstract

Disclosed is a slow release injection agent of anticancer composition containing taxone and synergistic agent, which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the anticancer active constituents include taxone and / or taxone synergistic agent selected from anticancer antibiotics and / or tetrazine medicaments, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer of polyphosphate ester with polylactic acid, Polifeprosan, di-aliphatic acid and sebacylic acid, copolymer or blend of poly(erucic aciddipolymer-sebacylic acid) or poly(fumaric acid-sebacylic acid). The anticancer composition can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a period of effective concentration maintenance over 40 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing taxanes and / or taxane synergists, belonging to the technical field of medicines. Specifically, the invention relates to a sustained-release preparation capable of stably releasing taxanes and / or taxane synergists locally in solid tumors, mainly sustained-release implants and sustained-release injections, which can prolong drug release time and can increase 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 uneve...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/337A61K45/06A61K47/34A61P35/00A61K47/26
Inventor 孙娟邹会凤刘恩祥张婕
Owner JINAN KANGQUAN PHARMA TECH
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