Pharmaceutical composition with palmitoyl ascorbate and antitumor medicine in synergism

An anti-tumor drug, palmitoyl ester technology, used in anti-tumor drugs, drug combinations, active ingredients of heterocyclic compounds, etc., can solve problems such as poor targeting and large systemic side effects

Inactive Publication Date: 2016-11-23
陈西敬
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0034] The purpose of the present invention is to provide a novel drug with definite curative effect and little side effect for the current clinical treatment of cancer, especially the

Method used

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  • Pharmaceutical composition with palmitoyl ascorbate and antitumor medicine in synergism
  • Pharmaceutical composition with palmitoyl ascorbate and antitumor medicine in synergism
  • Pharmaceutical composition with palmitoyl ascorbate and antitumor medicine in synergism

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0486] Example 1: Vitamin C palmitoyl ester liposomes for injection

[0487]

[0488] Weigh the prescription amount of vitamin C palmitoyl ester, soybean phospholipid and cholesterol, dissolve it in dichloromethane, and place it in a rotary evaporator to dry under reduced pressure to form a uniform lipid film, and place it in a vacuum drying oven to dry overnight. , Add water for injection to hydrate, ultrasonic to make the film fall off, after probe ultrasonic treatment or high-pressure homogenization treatment, and finally filtered through 0.22μm microporous filter membrane to obtain.

Example Embodiment

[0489] Example 2: Compound liposomes for injection

[0490]

[0491] Weigh the prescription amount of vitamin C palmitoyl ester, docetaxel, phospholipid and cholesterol, dissolve it in dichloromethane, and place it in a rotary evaporator to dry under reduced pressure to form a uniform lipid film and place it in a vacuum drying oven After drying overnight, add water for injection to hydrate, ultrasound to make the film fall off, ultrasonic treatment with probe or high-pressure homogenization treatment, and finally filtered through 0.22μm microporous filter membrane to obtain the product.

Example Embodiment

[0492] Example 3: Vitamin C palmitoyl ester nanoparticles for injection

[0493]

[0494] Dissolve PLGA in acetone to form PLGA acetone solution, add vitamin C palmitoyl ester and PLGA acetone solution as the oil phase, dissolve soybean phospholipids in ethanol solution, add poloxamer, DSPE-PEG-BIOTIN, water bath to remove organic The solvent is used as the water phase, and the oil phase is added dropwise to the water phase with constant temperature stirring. After the addition is complete, stirring is continued to remove the organic solvent. After adding it to a dialysis bag for dialysis overnight, adding mannitol to freeze-dry it to obtain.

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Abstract

The invention relates to a medicine for treating malignant tumors, in particular to an L-palmitoyl ascorbate antitumor medicine applied in the way of intravenous injection or oral administration or intratumor injection or the like. The pharmaceutically acceptable medicine applied in an injection or oral administration dosage form is prepared from L-palmitoyl ascorbate or/and one or more kinds of other chemotherapeutic medicine in combination. The medicine has high physicochemical stability and a definite antitumor effect; in-vitro cell tests and tumor-bearing mouse tests show that the medicine or a composition thereof has an effect on various malignant tumors such as breast cancer, liver cancer, lung cancer, stomach cancer, pancreatic cancer, cervical cancer, gliomas, prostatic cancer and colorectal cancer.

Description

technical field [0001] The invention relates to a medicine for treating malignant tumors, especially vitamin C palmitoyl ester anti-cancer drugs for intravenous injection, oral administration or intratumoral injection. and two other chemotherapeutic drugs, prepared into a pharmaceutically acceptable injection or oral dosage form for administration. The medicine of the present invention has excellent physical and chemical stability and definite anti-tumor effect. In vitro cell tests and tumor-bearing mouse tests show that the medicine or its composition is effective against breast cancer, liver cancer, lung cancer, gastric cancer, pancreatic cancer, cervical cancer, Cancer, glioma, prostate cancer, colorectal cancer and other malignant tumors are effective. Background technique [0002] Vitamin C (Vitamin C) is also called ascorbic acid (Ascorbic acid), the chemical formula is C 6 h 8 o 6 . It was first isolated and reported by Hungarian scientist and Nobel Prize winner ...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/375A61K31/704A61K31/337A61K31/475A61K31/4745A61K31/282A61K33/24A61K31/7068A61K31/44A61P35/00
CPCA61K31/282A61K31/337A61K31/375A61K31/44A61K31/4745A61K31/475A61K31/704A61K31/7068A61K33/24A61K45/06A61K2300/00
Inventor 卢杨王子厚杨越陈西敬赵娣李宁陈琪马恩龙张玲
Owner 陈西敬
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