Antitumor lymphatic metastasis function of mitoxantrone and pharmaceutical preparation of mitoxantrone

A technology for mitoxantrone and pharmaceutical preparations, applied in the field of medicine, can solve problems such as toxic and side effects, and achieve the effects of reducing toxic and side effects, reducing the risk of tumor recurrence, and inhibiting tumor lymphatic metastasis

Inactive Publication Date: 2019-05-07
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Like many other antineoplastic drugs, mitoxantrone can cause severe toxic side effects when administered systemically

Method used

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  • Antitumor lymphatic metastasis function of mitoxantrone and pharmaceutical preparation of mitoxantrone
  • Antitumor lymphatic metastasis function of mitoxantrone and pharmaceutical preparation of mitoxantrone
  • Antitumor lymphatic metastasis function of mitoxantrone and pharmaceutical preparation of mitoxantrone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1, the preparation of solution

[0025] This embodiment provides a mitoxantrone solution, and the proportion of the raw materials per 100ml of the drug is as follows: 0.5% mitoxantrone, 0.01% sodium acetate, 0.02% sodium metabisulfite, 0.092% acetic acid, and 0.8% sodium chloride. The preparation process is as follows: 0.01% sodium acetate, 0.02% sodium pyrosulfite, 0.092% acetic acid and 0.8% sodium chloride are dissolved in 100ml of pure water to obtain a solution for injection. Add 0.5% mitoxantrone to the solution for injection, stir magnetically at 50 rpm at room temperature for 25 minutes, then add medicinal charcoal, stir magnetically at 50°C and 50 rpm for 20 minutes to obtain a mitoxantrone solution. The mitoxantrone solution was filtered through a 0.22 μm microporous membrane, and sterilized at 121° C. for 15 minutes to obtain a sterilized mitoxantrone solution.

[0026] In this embodiment 1, in order to further verify the beneficial effects of the...

Embodiment 2

[0044] Embodiment 2, the preparation of microcrystalline gel

[0045] The present embodiment provides a mitoxantrone microcrystalline gel, and the ratio of each raw material per 10 g of the medicine is as follows: 10 mg of mitoxantrone, 5 mg of mitoxantrone hydrochloride, 2 g of poloxamer 407, and 2 g of poloxantrone Mu 188 0.5g, 7.49ml distilled water. The preparation process is as follows: accurately weigh 10 mg of mitoxantrone and 5 mg of mitoxantrone hydrochloride after grinding and sieving (200 mesh), add 2 g of Poloxamer 407, 0.5 g of Poloxamer 188, and 7.49 ml of distilled water , stirred magnetically at 30 rpm in an ice-water bath for 6 hours until the particles were completely dissolved, and placed at 4°C for 24 hours to obtain mitoxantrone microcrystalline gel.

[0046] In order to verify that the microcrystalline gel in Example 2 can reduce the drug toxicity of systemic administration of mitoxantrone after local administration, this example investigated the tissue ...

Embodiment 3

[0047] Embodiment 3, the preparation of liposome

[0048] This embodiment provides a mitoxantrone liposome, and the ingredients of each 10ml drug are formulated as follows: mitoxantrone 10mg, soybean lecithin 0.4g, cholesterol 0.04g, and glucose 1.5g. The preparation process is as follows: add 10 mg of mitoxantrone, 0.4 g of soybean lecithin, and 0.04 g of cholesterol solution to an appropriate amount of absolute ethanol to obtain a clear solution. Add 1.5 g of glucose powder to the clear solution, shake well, and sonicate to a milky white suspension. Ethanol was removed from the milky white suspension by rotary evaporation at 50°C to obtain a liposome film. Add 10ml of distilled water to the liposome film and hydrate at 50°C until all the solids are dissolved. The probe is sonicated for 10 minutes, and the mitoxantrone liposome is obtained by passing through a 0.45 μm filter membrane.

[0049] In order to verify that the liposomes in Example 3 can reduce the drug toxicity o...

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Abstract

The present invention relates to the technical field of medicine and particularly relates to an antitumor lymphatic metastasis function of mitoxantrone and a pharmaceutical preparation of the mitoxantrone. The mitoxantrone is administered locally, such as intratumoral administration and peritumoral and tumor subcutaneous administration. The mitoxantrone can be prepared into the clinically acceptable pharmaceutical preparation with a pharmaceutically acceptable carrier. The pharmaceutical preparation is a parenteral administration preparation. The parenteral administration preparation is selected from a solution, a liposome, a dendritic macromolecule, a nanoparticle, a nanocrystal, a microcrystal, a microsphere and a gel agent. The mitoxantrone is used for local chemotherapy to increase anti-tumor activity, reduces toxic and side effects, targets a lymphatic system, inhibits tumor lymphatic metastasis, can reduce tumor volume and is convenient for subsequent surgical resection when usedfor neoadjuvant chemotherapy, can also kills tumor cells metastasized in lymphatic vessels, reduces risks of postoperative tumor recurrence, and improves quality of life of patients.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the anti-tumor lymphatic metastasis effect of mitoxantrone and its pharmaceutical preparation. Background technique [0002] Tumor metastasis is a key factor in the death of patients with certain solid tumors, and breast cancer has a higher probability of metastasis. Usually the initial site of metastasis is the peritumoral lymph nodes. For the vast majority of tumors, the lymphatic system is the main and only way for tumor metastasis. Lymph nodes can funnel all exfoliated tumor cells into the reticular fibers of the marginal sinuses and subsequently proliferate in situ. More and more clinical and experimental data show that tumor metastasis is more common than sarcoma. The first indicator that cancer cells have spread is the presence of tumor cells in the lymph nodes. Therefore, it is very important to prevent lymphatic metastasis of tumor cells. The current clinical metho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/136A61K9/06A61K47/10A61P35/04
Inventor 韩诗雅白瑞雪刘珺王淑君闫格陈荟伊刘永睿叶田田
Owner SHENYANG PHARMA UNIVERSITY
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