Antitumor preparation and preparation method for same

An anti-tumor and preparation technology, applied in the field of anti-tumor preparations and their preparation, can solve problems such as large side effects, and achieve the effects of reducing the dosage of medicine, reducing the cost of medicine and having a wide range of sources.

Active Publication Date: 2016-10-05
XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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  • Application Information

AI Technical Summary

Problems solved by technology

However, due to poor stability in vivo and pleiotropic effects, continuous infusion or frequent administration is required to obtain the desired therapeutic effect. In animal experiments, the dosage of each PD-1 antibody is usually 250ug / mice, and each time Dosing once every two days to maintain the efficacy of the drug, such a high dose causes side effects during systemic treatment, such as immune enteritis and severe autoimmune diseases, which limits its application

Method used

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  • Antitumor preparation and preparation method for same

Examples

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Effect test

Embodiment 1

[0038] Example 1. Preparation of the anti-tumor preparation of the present invention.

[0039] can follow as figure 1 The scheme shown prepares the antineoplastic formulations of the present invention.

[0040] Step (1), prepare 10-40mg / mL high molecular weight (SLG100, Mw=200,000–300,000g / mol) and low molecular weight (SLG20, Mw=75,000–220,000g / mol) respectively with physiological saline, FMC Biopolymer Company, USA Philadelphia) alginate solution, stirred overnight at 4° C. with a magnetic stirrer, and sterilized by filtration with a filter with a pore size of 0.22 μm. Take high and low molecular weight alginate solutions and mix them in a ratio of 1:3 and mix well;

[0041] Step (2)-a, weighing 3.75-7.5 mg of celecoxib powder (LC Laboratory, LC Laboratories, Massachusetts, USA) per milliliter of alginate solution, and mixing;

[0042] In step (2)-b, use a probe-type ultrasonic instrument (QSONICA, USA) to sonicate for 60 seconds with a power of 60W, so that the celecoxib...

Embodiment 2

[0050] Example 2: The sustained release effect and drug effect extension effect of the anti-tumor preparation provided by the present invention in vivo

[0051] 1. Prepare the anti-tumor preparation according to the same method as in Example 1, so that each milliliter of the anti-tumor preparation contains 500 ug of PD-1 blocking antibody and 3125 ug of celecoxib.

[0052] C57BL / 6 mice were purchased from Beijing Huafukang Biotechnology Co., Ltd., each weighing about 25 grams. B16-F10 melanoma cells were purchased from the American Type Culture Collection.

[0053] 2. Construction of mouse B16 melanoma model.

[0054] B16-F10 melanoma cells are recognized as the tumor cells with the strongest invasive ability, and each C57BL / 6 mouse was subcutaneously injected with 2.5×10 4 After a single B16-F10 melanoma cell, a well-formed melanoma in situ can be generated after 1 week, and then grow rapidly and cause the death of the mouse. The C57BL / 6 mouse melanoma model is a mature an...

Embodiment 3

[0069] Example 3 The anti-tumor preparation of the present invention can promote the production of active CD8 T cells

[0070] 1. Prepare the anti-tumor preparation according to the same method as in Example 1, so that each milliliter of the anti-tumor preparation contains 500 ug of PD-1 blocking antibody and 3125 ug of celecoxib.

[0071] 2. Construct the same mouse melanoma model as in Example 2.

[0072] One week after C57BL / 6 mice were inoculated with melanoma cells, set up the following 4 groups of mice:

[0073]

[0074] After each group of mice was treated as above, the percentage of active CD8 cells in the tumor microenvironment was detected by flow cytometry one week later.

[0075] Figure 3A with Figure 3B The detection results of CD8 T cells that can effectively kill tumor cells in the tumor microenvironment are shown. It shows that the administration of the anti-tumor preparation group of the present invention (formed by encapsulating PD-1 antibody and celec...

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Abstract

The invention provides an antitumor preparation and a preparation method for the same. The antitumor preparation is an injection and is in the form of a hydrogel which is formed from an alginate water solution in which active components including a PD-1 blocking antibody and celecoxib are dispersed. The antitumor preparation has excellent in-vivo stability and prolonged sustained-release effect, has significantly improved inhibition effects on growth and migration of tumor cells, and has enlarged anti-tumor spectrum.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to an anti-tumor preparation and a preparation method thereof. Background technique [0002] Tumor is one of the greatest enemies that threaten human health and life. According to the report of the World Health Organization, in 2012, 14.1 million people worldwide suffered from cancer, and the death toll reached 8.2 million, exceeding the total number of deaths from AIDS, malaria and tuberculosis. The number of new cancer cases in my country ranks first in the world, and cancer has become the number one cause of death among Chinese residents, with 2.07 million people dying of cancer every year. At present, in clinical practice, the treatment methods of tumors are mainly surgical resection, chemotherapy and radiotherapy. When treating malignant tumors, surgical methods are almost impossible to completely remove the spreading tumor cells, resulting in re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K39/395A61K47/36A61K9/06A61P35/00A61P35/02A61K31/635
CPCA61K9/00A61K31/635A61K39/395
Inventor 王琳李永奎方敏王征张剑宋煜石洁徐妞妞王健
Owner XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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