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Anti-cancer medicine composition carried with blood-vessel inhibiting agent and synergistic agent

A technology of vascular inhibitor and synergist, applied in the field of anti-cancer compositions, sustained-release implants and sustained-release injections, can solve problems such as unbalanced release, toxic reactions, inability to effectively kill tumor cells, etc. effect on tumor growth

Inactive Publication Date: 2007-08-29
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

[0120] 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 tipifarnib, 10mg doxorubicin, 10mg tipifarnib and 10mg doxorubicin respectively, shake up again and use spray drying method to prepare 10% tipifarnib, 10% adriamycin Mycin, and 10% tipifarnib 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

[0122] 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:

[0123] (1) 5-30% tipifarnib or lapatinib;

[0124] (2) 1-40% of arubicin, doxorubicin, epirubicin, idarubicin, pirarubicin, valrubicin, mitomycin C, actinomycin D or epirubicin Doxorubicin; or

[0125] (3) 5-30% lapatinib or tipifarnib and 1-40% arubicin, doxorubicin, epirubicin, edarubicin, pirarubicin, valrubicin Combinations of star, mitomycin C, actinomycin D, or epirubicin.

Embodiment 3

[0127] 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 lapatinib, 30mg epirubicin, 15mg lapatinib and 15mg epirubicin, shake up again and prepare with spray drying method containing 30% lapatinib, 30% epirubicin, 15 % lapatinib and 15% epirubicin injection microspheres. 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

The present invention relates to an anti-cancer medicine composition containing angiogenesis inhibitor and its synergist. It is formed from microsphere and solvent, in which the slow-release microsphere includes anti-cancer effective component and slow-release auxiliary material, and the solvent is general one or special one containing suspension adjuvant. The suspension adjuvant is selected from carboxymethylcellulose sodium, etc. and its viscosity is 100 cp-3000 cp (at 20 deg.C-30 deg.C). The slow-release auxiliary material is selected from polyphosphate copolymer of p(LAEG-EOP) and p(DAPG-EOP), etc. or polyphosphate and polylactic acid, difatty acid and sebacic acid copolymer, poly (erucidic acid dimmer-sebacic acid) or poly (fumaric acid-sebacic acid) copolymer or mixture. The anti-cancer effective component includes angiogenesis inhibitor and / or its synergist selected from anti-cancer antibiotic and / or tetrazine medicine. Said anti-cancer medicine composition also can be made into slow-release implantation.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing a blood vessel inhibitor and / or a blood vessel inhibitor synergist, belonging to the technical field of medicines. Specifically, the invention relates to a slow-release preparation capable of stably releasing vasopressors and / or vasopressor 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 mor...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K45/06A61K47/34A61K47/36A61K47/38A61K47/42A61K35/00
Inventor 孙娟刘玉燕孔庆新
Owner JINAN KANGQUAN PHARMA TECH
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