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Composition liposome of ascorbyl palmitate and adriamycin

A technology of ascorbyl palmitate and ascorbyl ester, which is applied in the field of compound liposome preparation of ascorbyl palmitate and doxorubicin, can solve the problem of failure to achieve synergistic effect, low content of ascorbyl palmitate, and obvious Doxorubicin particles and other issues

Inactive Publication Date: 2016-08-24
陈西敬
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Professor Rambhau Devraj of India's Kakatiya University (Kakatiya University) has reported a compound liposome preparation of ascorbyl palmitate and doxorubicin, and its ascorbyl palmitate: the ratio of doxorubicin is 0.6: 1 (w / w), wherein the content of ascorbyl palmitate is relatively low, failing to reach the purpose of synergistic effect; the mass ratio of adriamycin is 15%, and research of the present invention shows that it is difficult to encapsulate medicine in liposomes under this ratio , obvious doxorubicin particles appeared during the preparation process, and doxorubicin liposomes could not be prepared

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  • Composition liposome of ascorbyl palmitate and adriamycin
  • Composition liposome of ascorbyl palmitate and adriamycin
  • Composition liposome of ascorbyl palmitate and adriamycin

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Effect test

Embodiment 1

[0110] Embodiment 1: a kind of composition liposome formulation of compound ascorbyl palmitate / doxorubicin and its preparation are as follows:

[0111] Experimental method: The liposome preparation process of the compound ascorbyl palmitate / doxorubicin is: dissolving doxorubicin, ascorbyl palmitate, dimyristate phosphatidylcholine, and cholesterol in 15 mL of chloroform , vortexed until completely dissolved, then added to a 500mL eggplant-shaped flask, evaporated under reduced pressure at 70°C to remove the organic solvent, and prepared a uniform lipid film on the wall of the bottle, dried overnight at 75°C in a vacuum oven, then added 15mL of distilled water, after the lipid film was washed off by ultrasonication, the probe was ultrasonicated for 2 cycles in an ice-water bath (30%, 20s, ultrasonication for 1s and off for 1s).

[0112] Liposome evaluation method:

[0113] The measurement of the particle diameter of liposome: adopt laser particle size analyzer to measure.

[...

Embodiment 2

[0122] Embodiment 2: a kind of composition liposome formulation of compound ascorbyl palmitate / doxorubicin and its preparation are as follows:

[0123] Experimental method: the liposome preparation process of the compound ascorbyl palmitate / doxorubicin is as follows: adriamycin, ascorbyl palmitate, soybean lecithin, and sitosterol are dissolved in 15mL of chloroform, vortexed to complete After dissolving, add it to a 500mL eggplant-shaped flask, remove the organic solvent by rotary decompression evaporation at 60°C, and obtain a uniform lipid film on the wall of the bottle, place it in a vacuum drying oven at 35°C to dry overnight, add 15mL of distilled water, and ultrasonically After the lipid film was washed off, the probe was ultrasonicated for 4 cycles in an ice-water bath (80%, 50 s, ultrasonic 1 s off 1 s), and the product was obtained.

[0124] Experimental results: see Table 2.

[0125] Table 2. The experimental result of embodiment 2

[0126]

[0127] Doxorubicin...

Embodiment 3

[0129] Embodiment 3: a kind of composition liposome formulation of compound ascorbyl palmitate / doxorubicin and its preparation are as follows:

[0130] Experimental method: the liposome preparation process of the compound ascorbyl palmitate / doxorubicin is: dissolving doxorubicin, ascorbyl palmitate, dipalmitate phosphatidylcholine, cholesterol hemisuccinate in 15mL three In methyl chloride, vortex until completely dissolved, then add to a 500mL eggplant-shaped flask, remove the organic solvent by rotary evaporation under reduced pressure at 70°C, prepare a uniform lipid film on the bottle wall, and dry in a vacuum oven at 75°C overnight Finally, add 15mL of distilled water, ultrasonically wash off the lipid film, and perform 6 cycles of ultrasound with the probe in an ice-water bath (30%, 60s, ultrasonication for 1s and stop for 1s).

[0131] Experimental results: see Table 3.

[0132] Table 3. The experimental result of embodiment 3

[0133]

[0134] Doxorubicin: DOX, As...

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Abstract

The invention relates to a composition liposome preparation used for medicines for treating tumors by injection drug administration and in particular relates to a preparation method of a compound composition liposome of ascorbyl palmitate and adriamycin. By combining the ascorbyl palmitate and the adriamycin, in-vivo and in-vitro experiments show that the anti-tumor drug function of the adriamycin can be remarkably enhanced, so that the adriamycin can express the drug effect under an extremely low dosage; the adriamycin is administrated in manners of vein drug administration, artery drug administration, muscle drug administration, subcutaneous drug administration, abdominal cavity drug administration and the like and is particularly used for interventional drug administration including intravenous infusion or intratumoral injection and the like, so that the effectiveness and safety of clinical application of the adriamycin are improved. The preparation method provided by the invention is simple in process and low in cost; prepared liposomes are uniform in particle diameter and high in entrapment efficiency and the drug releasing property is good; compared with a single liposome of the ascorbyl palmitate and the adriamycin, the effects of inhibiting the growth of the tumors in vitro and resisting proliferation of the tumors in vivo of the composition are remarkably enhanced.

Description

technical field [0001] The invention relates to a composition liposome preparation for injecting drugs for treating tumors, in particular to a method for preparing a composition liposome of compound ascorbyl palmitate and doxorubicin. Background technique [0002] Doxorubicin (Doxorubicin, DOX, see formula 1 for chemical structure formula) is currently the first-line broad-spectrum anti-tumor drug in clinical practice, with a clear anti-tumor mechanism, mainly inhibiting the synthesis of RNA and DNA. It was approved for clinical application in the United States in 1974 for the treatment of various malignant tumors, such as breast cancer, liver cancer, ovarian cancer, bladder cancer, lung cancer, lymphoma, neurocytoma, acute and chronic leukemia, etc. After injection, it is widely distributed in the heart, liver, spleen, lung, and kidney, and disappears rapidly in plasma, and has many adverse reactions, the most serious being dose-dependent cardiotoxicity and neurotoxicity, w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61K31/375A61K9/127A61K47/24A61K47/28A61P35/00
CPCA61K9/0019A61K9/127A61K31/375A61K31/704A61K47/24A61K47/28A61K2300/00
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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