Pharmaceutical composition containing sunitinib as well as preparation and application of pharmaceutical composition

A technology of sunitinib and pharmaceutical preparations, which is applied in the field of tumor treatment, can solve the problems of serious drug resistance, reduce treatment effect, reduce sunitinib drug resistance, etc., achieve significant killing efficiency, broad market prospects, reduce The effect of clinical dosage

Active Publication Date: 2020-08-21
SUN YAT SEN UNIV CANCER CENT
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In view of the above problems and deficiencies, the present invention provides a pharmaceutical composition containing sunitinib to solve the problem of severe drug resistance caused by the use of conventional doses of sunitinib in the prior art and after reducing the therapeutic dose The problem of significantly reduced therapeutic effect, so as to obtain more significant clinical therapeutic effect and reduce sunitinib drug resistance and side effects

Method used

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  • Pharmaceutical composition containing sunitinib as well as preparation and application of pharmaceutical composition
  • Pharmaceutical composition containing sunitinib as well as preparation and application of pharmaceutical composition
  • Pharmaceutical composition containing sunitinib as well as preparation and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Cell Proliferation Inhibition Experiment in Vitro

[0041] (1) Take 786-O cells in the logarithmic growth phase and plant them in a 96-well plate at a certain density (1500-2000 / well);

[0042] (2) Discard the old medium after 24 hours, divide the cells into 5 groups of 1-5 for use, add medium containing different drug concentrations, set 3 duplicate wells for each group, and add sunitinib alone to group 1 Sunitinib and 10 μM apatinib were added to group 2, sunitinib and 10 μM apatinib were added to group 3, DMSO was added to group 4, and group 5 was used as a blank group;

[0043] (3) After culturing for 48 hours, discard the drug solution, add medium containing 5% CCK-8, incubate at 37°C for 3 hours, and then use a microplate reader to detect the OD value at 450nm.

[0044] Based on the DMSO group, the cell survival rate = (OD value of the drug-dosed group - OD value of the blank group) / (OD value of the DMSO group - OD value of the blank group) × 100%, co...

Embodiment 2

[0048] Example 2 In vitro anti-tumor synergy experiment

[0049] In this experiment, on the basis of the in vitro cell proliferation inhibition experiment stated in Example 1, by measuring the 786-O cells at 10%, 30%, 50%, 70% and 90% inhibition rate, single drug (Apa Apatinib, Axitinib, or Sunitinib) and the drug concentration required for combination therapy (Apatinib + Sunitinib or Axitinib + Sunitinib), so as to calculate the combination index using the formula (Combination Index, CI), make a Fa-CI curve: where the CI calculation formula is as follows:

[0050] CI = D 1x / D 1 + D 2x / D 2 +( D 1x · D 2x ) / ( D 1 · D 2 ).

[0051] D 1x : The concentration of the first drug when the combination group reaches a certain cell inhibition rate; D 2x : The concentration of the second drug when the combination group reaches a certain cell inhibition rate; D 1 : The concentration of the first drug when the single-drug group reaches a certain cell inhibition ...

Embodiment 3

[0056] Example 3 In vitro anti-tumor synergistic compatibility experiment

[0057] (1) The 786-O, A498 and Caki-1 cells in the logarithmic growth phase were planted in a 96-well plate at a certain density (1500-2000 / well);

[0058] (2) Discard the old medium after 24 hours, add drugs containing different compatible forms to continue the culture, and set 3 duplicate wells for each group;

[0059] (3) After culturing for 48 hours, discard the cell culture medium, add a medium containing 5% CCK-8, incubate at 37°C for 3 hours, and then use a microplate reader to detect the OD value at 450nm.

[0060] Based on the DMSO group, the corresponding synergistic effect evaluation was carried out on the inhibition rate, and the combined drug effect was analyzed by King's formula (Q value):

[0061] Q=E (A+B) / (E A +E B -E A ×E B ), that is, E (A+B) : Inhibition rate of combination drug, E A : Inhibition rate of drug A alone, E B : Inhibition rate of drug B alone. When Q>1.15, it...

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Abstract

The invention provides a pharmaceutical composition containing sunitinib as well as a preparation and an application of the pharmaceutical composition. On the basis of the original sunitinib, at leastone tyrosine kinase receptor inhibitor, especially apatinib and / or axitinib, is further added to generate a very significant synergistic effect with the sunitinib, so that the proliferation of cancercells is obviously inhibited, and the sunitinib has very significant killing efficiency on the cancer cells. The pharmaceutical composition provided by the invention can obviously improve the problemof serious drug resistance caused by singly adopting sunitinib in the prior art and the problem of obviously reduced treatment effect when the conventional use amount of sunitinib is reduced; clinical treatment efficiency is greatly improved, treatment toxic and side effects of a patient are reduced, a new scheme is provided for clinical treatment, and the traditional Chinese medicine compositionhas very wide market prospects and extremely important social significance.

Description

technical field [0001] The invention belongs to the technical field of tumor treatment, and in particular relates to a pharmaceutical composition containing sunitinib and its preparation and application. Background technique [0002] Sunitinib is a highly effective, multi-target tyrosine kinase receptor inhibitor, its targets include vascular endothelial cell growth factor receptor 1, 2, 3 (VEGF Receptor, VEGFR-1, 2,3), platelet growth factor receptor α, β (PDGF Receptor, PDGFR-α, β), c-KIT and so on. According to the existing research results, sunitinib mainly exerts anti-tumor effects through three ways: inhibiting tumor angiogenesis, destroying tumor blood vessels and directly killing tumor cells. Currently, sunitinib is approved for the treatment of advanced metastatic renal cell carcinoma and imatinib-resistant gastrointestinal stromal tumor (Gastrointestinal Stromal Tumor, GIST). Corresponding research and clinical trials are also underway in other cancers such as no...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/404A61K31/444A61K31/4439A61P35/00A61P35/04A61P35/02
CPCA61K45/06A61K31/404A61K31/444A61K31/4439A61P35/00A61P35/04A61P35/02A61K2300/00
Inventor 岳欣刘然义刘听雨
Owner SUN YAT SEN UNIV CANCER CENT
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