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Epirubicin hydrochloride liposome and preparation thereof

A technology of epirubicin hydrochloride fat and epirubicin hydrochloride, which is applied in the field of epirubicin hydrochloride liposome and its preparation, can solve the problems of strong toxicity and side effects, reduce toxicity, reduce production costs, and be suitable for industrial The effect of production

Inactive Publication Date: 2008-09-17
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in clinical application, it is found that there are still strong toxic and side effects

Method used

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  • Epirubicin hydrochloride liposome and preparation thereof
  • Epirubicin hydrochloride liposome and preparation thereof
  • Epirubicin hydrochloride liposome and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Embodiment 1 prepares epirubicin liposome

[0049] Epirubicin 0.4mg

[0050]Hydrogenated Phospholipids 30mg

[0051] Cholesterol 11.5mg

[0052] Preparation method: Weigh the phospholipids and cholesterol in the above formula and dissolve them in an appropriate amount of chloroform / methanol solution to obtain a lipid solution. Evaporate under reduced pressure on a rotary evaporator to remove the organic solvent, and form a uniform lipid on the bottle wall. film, add 150mM ammonium sulfate solution to the lipid film, shake for 2h until the lipid film is completely hydrated, prepare blank liposomes with a micro squeezer, and elute the blank liposome solution with 10% sucrose solution through Replace the outer water phase with Sephadex G50 gel column, add the formulated amount of epirubicin hydrochloride sucrose solution, mix, put it in a water bath at 65°C and keep it warm for 20 minutes to obtain the product. It was determined that the encapsulation efficiency of the ...

Embodiment 2

[0053] Embodiment 2 prepares epirubicin liposome

[0054] Epirubicin 0.4mg

[0055] Soy Lecithin 30mg

[0056] DSPG 6mg

[0057] Cholesterol 11.5mg

[0058] Preparation method: Weigh the phospholipids and cholesterol in the above formula and dissolve them in an appropriate amount of chloroform / methanol solution to obtain a lipid solution. Evaporate under reduced pressure on a rotary evaporator to remove the organic solvent, and form a uniform lipid on the bottle wall. For thin film, add 150mM ammonium sulfate solution to the lipid film, shake for 2 hours until the lipid film is completely hydrated, use ultrasonic probe to reduce the particle size, and pass through the filter membranes with 0.22 μm and 0.15 μm pore sizes twice to obtain the liposome mixture. For the suspension, the blank liposome solution was eluted with 10% sucrose solution and passed through a Sephadex G50 gel column to replace the outer water phase, and the formula amount of epirubicin hydrochloride sucro...

Embodiment 3

[0059] Embodiment 3 prepares epirubicin liposome

[0060] Epirubicin 0.4mg

[0061] Yolk Lecithin 30mg

[0062] Dimyristate Phosphatidylglycerol 6mg

[0063] PEG 2000 -DSPE 7mg

[0064] Cholesterol 11.5mg

[0065] Preparation method: Weigh the phospholipids and cholesterol in the above formula and dissolve them in an appropriate amount of chloroform / methanol solution to obtain a lipid solution. Evaporate under reduced pressure on a rotary evaporator to remove the organic solvent, and form a uniform lipid on the bottle wall. film, add 150mM ammonium sulfate solution to the lipid film, shake for 2h until the lipid film is completely hydrated, prepare blank liposomes with a micro squeezer, and elute the blank liposome solution with 10% sucrose solution through Replace the outer water phase with the Sephadex G50 gel column, add the prescribed amount of epirubicin hydrochloride sucrose solution, mix, place in a water bath at 65°C for 20 minutes, and obtain the product. The en...

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Abstract

The invention belongs to the medicine technical field, relates to epirubicin hydrochloride liposome and a preparation method. The liposome comprises epirubicin hydrochloride and neutral phospholipid and cholesterol and / or negative charge phospholipids and / or long-circulating phospholipids and buffer solution, and actively carries drug with a PH gradient method or an ammonium sulphate gradient method; the entrapment rate of the achieved liposome is more than 90%, to make smaller volume contain more main drug component of epirubicin. Compared with the exiting techniques, the epirubicin hydrochloride liposome and the preparation method has the advantages of high drug content, high bioavailability, long internal circulation time, low toxic and side effect and other advantages; besides, the production cost can be reduced obviously, the epirubicin hydrochloride liposome is more suitable for industrial production after being made into lyophilized preparation. The liposome is clinically suitable for the tumor therapy, in particular to the tumor therapy for children.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to epirubicin hydrochloride liposome and a preparation method thereof. Background technique [0002] Epirubicin (epirubicin, 4'-epiadriamycin, epidoxorubicin, EPI), is an anthracycline antitumor antibiotic synthesized by Italian scholar Arcamone in 1975 through a semi-synthetic route, and is an isomer of doxorubicin. The difference is that the hydroxyl group at the 4' position of the amino sugar changes from cis to trans. The mechanism of action of epirubicin is to directly insert DNA bases, inhibit the activity of topoisomerase II, generate oxygen and drug free radicals, and chelate metal ions. At present, it is mainly used for the treatment of breast cancer, malignant lymphoma, soft tissue sarcoma, lung cancer, pleural mesothelioma, gastrointestinal cancer, head and neck cancer, ovarian cancer, prostate cancer, metastatic bladder cancer and other tumors. [0003] Af...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/704A61K47/24A61P35/00
Inventor 方晓玲郭洁张志文潘振华吴江
Owner FUDAN UNIV
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