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Anti-tumor combined medicament

An anti-tumor and drug technology, applied in the directions of anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problem of the combined use of epirubicin and quercetin that is not reported in the literature, and achieve the goal of reducing toxicity and reversing drug resistance. Effect

Inactive Publication Date: 2012-10-03
CHENGDU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Currently, there are no literature reports on the combined use of epirubicin and quercetin

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1 The preparation of drug freeze-dried preparation of the present invention

[0048] Prescription: epirubicin 0.2g, quercetin 2g, PLGA100g, PVA2055g, mannitol 50g; 1000 tubes in total;

[0049] The specific steps are:

[0050] a. Prepare the EPI solution with a concentration of 1mg / ml with ethanol, and prepare the QC solution with a concentration of 10mg / ml in acetone for subsequent use;

[0051] b. Weigh PLGA, add dichloromethane and acetone solution to dissolve PLGA, then add ethanol solution to form the organic phase, the volume ratio of dichloromethane: acetone: ethanol is: 1: 0.4: 0.1, mix well, and mix with 2% PVA The water phase is mixed, and the 200W power probe is ultrasonicated for 3 minutes, and then placed in a round bottom flask. Under the conditions of 25 ° C and 50 r / min, the organic solvent is removed on a rotary evaporator under reduced pressure, and nanoparticles (EPI-QC compound nanoparticles) are obtained after 40 minutes. Add distilled ...

Embodiment 2

[0053] Example 2: Research on the Preparation Technology of Nanoparticles Simultaneously Encapsulating Epirubicin Hydrochloride and Quercetin

[0054] In terms of nanoparticle wrapping materials, the present invention selects the polylactic acid copolymer (PLGA) which has been approved abroad and has good biocompatibility and degradability. Circulation is transformed into water and carbon dioxide to be excreted from the body, non-irritating and non-toxic.

[0055] The selected model drugs of the present invention, epirubicin and quercetin, are quite different in their physical and chemical properties. The former is a water-soluble drug, while the latter is a water-insoluble and fat-insoluble drug, and there are great difficulties in the preparation process.

[0056] 1 Instruments and reagents

[0057] 1.1 Instrument

[0058]

[0059] 1.2 Reagents

[0060] PLGA Shandong Medical Device Research Institute

[0061] PVA Kuraray International Trading (Shanghai) Co., Ltd.

[...

Embodiment 3

[0146] Embodiment 3 EPI-QC compound nanoparticle quality research of the present invention and its freeze-drying process research

[0147] The morphology, particle size distribution and Zeta potential of the final formulation of EPI-QC compound nanoparticles were investigated, and the freeze-drying process was studied.

[0148] 1 Instruments and reagents

[0149] 1.1 Instrument

[0150] Malvern Zetasizer Nano ZS90 laser particle size analyzer Malvern UK

[0151] pHS-4C acidity meter Chengdu Ark Technology Development Co., Ltd.

[0152] ModulyoD freeze dryer American thermoelectric company

[0153] 1.2 Reagents

[0154] Epirubicin hydrochloride Jinan Weidu Chemical Co., Ltd.

[0155] Quercetin Gift from Chengdu Superman Phytochemical Co., Ltd.

[0156] EPI-QC compound nanoparticles were prepared according to the method of Example 1

[0157] Acetonitrile is chromatographically pure; other reagents are analytically pure.

[0158] 2 Experimental methods

[0159] 2.1 Appea...

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Abstract

The invention discloses applications of pharmorubicin and quercetin to preparation of an anti-tumor combined medicament. The invention further discloses a combined medicament. The pharmorubicin is taken as an anti-tumor medicament; the quercetin is taken as an MDR (Multiple Drug Resistance) reversal agent of the pharmorubicin; PLGA (Poly(Lactic-Co-Glycolic Acid)) is taken as nanoparticle copolymer material; compound nanoparticles of pharmorubicin and quercetin are entrapped during preparation, so that a certain entrapment efficiency and medicament loading amount are achieved; various indexes of the nanoparticles are used for evaluating the property of the medicament; and an in-vitro cell test is used for evaluating the reversed multi-medicament resistance effect of the medicament. EPI-QC (Epichlorohydrin-QC) compound nanoparticles are prepared by adopting an emulsified solvent evaporation method; and according to research on a comparison system, the EPI-QC compound nanoparticles can be used for reverting the medicament tolerance of tumor cells in a certain degree, and the toxicity on normal cells is lowered.

Description

technical field [0001] The invention relates to an anti-tumor combined drug. It belongs to the field of medicine. Background technique [0002] Malignant tumors have become an important cause of human death. In recent years, chemotherapy, like surgery and radiotherapy, has become an indispensable and important treatment for malignant tumors. Although people have made a lot of efforts in chemotherapy, researching new chemotherapy drugs and improving chemotherapy regimens, the therapeutic effect is still not satisfactory. On the one hand, most anti-tumor drugs lack selectivity to tumor cells. While killing cells, they also have toxic side effects on normal cells, resulting in serious systemic adverse reactions. Therefore, many patients cannot persist or even give up chemotherapy, which is clinically difficult. It is expected to obtain the desired effect by increasing the dose of drugs; on the other hand, the resistance of tumor cells to chemotherapy drugs is more likely to ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61K31/352A61P35/00A61P35/02A61K9/19
Inventor 孙毅毅钟玲林东尹佳
Owner CHENGDU MEDICAL COLLEGE
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