Albumin nanoparticle preparation for anthracycline antitumor antibiotic oleic acid compound

A technology of albumin nanoparticles and oleic acid complex, applied in the field of medicine, can solve the problems of inability to prepare, have no stability, and have hydrophilicity, etc., and achieve the effects of prolonging the action time of the medicine, being beneficial to storage, and increasing the curative effect.

Active Publication Date: 2012-07-11
SICHUAN BAILI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, anthracycline antitumor antibiotic liposomes also have many disadvantages: most of the anthracycline antitumor antibiotics used in the market are in the form of salts, which are hydrophilic
The patent (ZL97199720.9) published by American Bioscience Co., Ltd. made paclitaxel drugs into a stable albumin nanoparticle preparation suitable for clinical needs, but our experiments showed that if the active ingredients of anthracycline antitumor antibiotics were not affinity Lipidation treatment, and without adding other surfactants except albumin, can not prepare albumin nanoparticles suitable for clinical needs, with high encapsulation efficiency, uniform particle size, and stable anthracycline antitumor antibiotics. Granules
[0012] In summary, it can be seen that there is no new preparation of anthracycline antitumor antibiotics with good stability, suitable for industrialized large-scale production, simple preparation method, and low production cost.

Method used

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  • Albumin nanoparticle preparation for anthracycline antitumor antibiotic oleic acid compound
  • Albumin nanoparticle preparation for anthracycline antitumor antibiotic oleic acid compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Take 50 mg of human serum albumin, add 9 ml of water for injection and dissolve to obtain a human serum albumin solution.

[0063] Take 5 mg of pirarubicin, add 5 μl of oleic acid dissolved in 6 ml of acetone at about 43°C and stir for 1 to 2 hours to obtain an orange-yellow clear solution. Remove the acetone by rotary evaporation to obtain the pirarubicin oleic acid complex, add egg yolk lecithin E80 20mg, dissolve it with 1ml of dichloromethane, mix it with the above human serum albumin solution, and ultrasonicate the probe 10 times to make a suspension , and then the suspension was milked 15 times in a high-pressure homogenizer, and it was rotary-evaporated to remove the organic solvent, and the lyoprotectant sucrose was added to prepare the pirarubicin oleic acid complex albumin containing 10% sucrose The nanoparticle aqueous solution can be freeze-dried under sterile conditions.

[0064] The obtained lyophilized powder was reconstituted with water for injection to...

Embodiment 2

[0066] Take 200 mg of human serum albumin, add 9 ml of water for injection to dissolve to obtain a human serum albumin solution, and add 10 mg of Maize 52 to the solution.

[0067] Take 5 mg of pirarubicin, add 5 μl of oleic acid dissolved in 6 ml of acetone at about 42°C and stir for 1 to 2 hours to obtain an orange-yellow clear solution. Remove the acetone by rotary evaporation to obtain the pirarubicin oleic acid complex, dissolve it with 1ml of dichloromethane, mix it with the above-mentioned human serum albumin solution, and ultrasonically probe the probe for 10 times to make a suspension, then place the suspension in Homogenize 15 times in a high-pressure homogenizer, spin it to remove the solvent, add sucrose as a freeze-drying protective agent to prepare an aqueous solution of pirarubicin oleic acid complex albumin nanoparticles containing 10% sucrose, and prepare it under sterile conditions. Then freeze dry.

[0068] The obtained lyophilized powder was reconstituted ...

Embodiment 3

[0070]Take 500 mg of human serum albumin, add 9 ml of water for injection and dissolve to obtain a human serum albumin solution.

[0071] Take 5 mg of pirarubicin hydrochloride, dissolve it in 1 ml of water, add 50 mg / ml of NaHCO 3 20ul of the solution was vortexed for one minute, 10ul of oleic acid was added, vortexed until the water layer was colorless, centrifuged at 7000r / min for 5min, and the complex was precipitated. Add 30mg of soybean lecithin for injection, dissolve it with 1ml of dichloromethane, and mix it with the above-mentioned human serum albumin solution. The probe is ultrasonicated 10 times to make a suspension, and then the suspension is homogenized in a high-pressure mixer for 15 The second time, it was rotary evaporated to remove the solvent, and the freeze-drying protective agent glucose was added to prepare an aqueous solution of pirarubicin oleic acid complex albumin nanoparticles containing 10% glucose, and freeze-dried under sterile conditions.

[007...

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Abstract

The invention provides a method for preparing an anthracycline antitumor antibiotic oleic acid compound and an oil-water double phase for preparing the compound and albumin, and the anthracycline antitumor antibiotic oleic acid compound is prepared into an albumin nanoparticle preparation. The albumin nanoparticle preparation prepared by the method is little in using amount of auxiliary materials, high in medicine-carrying dose and high in stability, and a preparation process is simple and is suitable for large-scale industrial production; and the albumin nanoparticle preparation has the tumor targeting and good clinical application value.

Description

technical field [0001] The invention relates to a highly stable anthracycline antitumor antibiotic oleic acid compound albumin nanoparticle preparation and a preparation method thereof, which can be widely used in industrial production, and relates to the technical field of medicine. Background technique [0002] Anthracycline anti-tumor antibiotics are effective broad-spectrum anti-tumor drugs, which are widely used in clinical treatment of various cancers, such as breast cancer, liver cancer, lung cancer, leukemia, lymphoma and many other solid tumors. Anthracycline anti-tumor antibiotics can produce a wide range of biochemical effects on the body and have strong cytotoxicity. Antitumor effect. Due to their quinone-hydroquinone functional groups, anthracyclines are also thought to be involved in the generation of free radicals that cause DNA damage. These drugs mainly include: Doxorubicin (ADM ), Daunorubicin (DNR ), Epirubicin (Epirubicin, EPI ), Pirarubicin (THP-ADM ),...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/48A61K47/42A61P31/00A61P35/00A61P39/02
Inventor 龚涛张志荣孙逊
Owner SICHUAN BAILI PHARM CO LTD
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