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Doxorubicin hydrochloride-docetaxel or paclitaxel liposome preparation and preparation method thereof

A technology of doxorubicin hydrochloride and liposome preparation, which is applied in the field of doxorubicin hydrochloride-docetaxel or paclitaxel liposomes, can solve problems such as large toxic and side effects, instability, etc., and achieve the effect of enhancing therapeutic function. Effect

Active Publication Date: 2014-03-12
常州金远药业制造有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the existence of surfactants and organic solvents in the common preparations of docetaxel or paclitaxel, there are unstable factors when compounding with doxorubicin hydrochloride, and the toxicity and side effects are large.

Method used

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  • Doxorubicin hydrochloride-docetaxel or paclitaxel liposome preparation and preparation method thereof
  • Doxorubicin hydrochloride-docetaxel or paclitaxel liposome preparation and preparation method thereof
  • Doxorubicin hydrochloride-docetaxel or paclitaxel liposome preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Preparation prescription:

[0032]

[0033] The preparation process is as follows:

[0034] Dissolve phospholipids, paclitaxel, cholesterol and vitamin E in chloroform according to the formula and mix evenly; use a rotary evaporator to remove the chloroform in the solution under reduced pressure to form a lipid film; prepare a 0.3M citric acid solution and hydrate with the citric acid solution Lipid film, the hydration temperature is 55°C, to obtain paclitaxel liposome suspension; after hydration is complete, use a high-pressure homogenizer to prepare liposomes to an average particle size of 120 ± 10nm, for liposome particle size and uniformity Multi-angle nanoparticle analyzer to detect; dissolve doxorubicin hydrochloride in 9% sucrose aqueous solution and heat to 50°C; adjust the pH of the empty paclitaxel liposome suspension to 7.5±0.3 with 0.5M anhydrous sodium carbonate aqueous solution ; Doxorubicin hydrochloride solution and basic paclitaxel liposome suspensi...

Embodiment 2

[0036] Preparation prescription:

[0037]

[0038]

[0039] Preparation Process:

[0040] Dissolve paclitaxel, phospholipids, cholesterol and vitamin E in chloroform according to the formula and mix them evenly; use a rotary evaporator to remove the chloroform in the solution under reduced pressure to form a lipid film; prepare 0.3M ammonium sulfate solution and hydrate with ammonium sulfate solution Lipid film, the hydration temperature is 40°C, to obtain paclitaxel-containing liposome suspension; after hydration is complete, use a high-pressure homogenizer to prepare liposomes to an average particle size of 120 ± 10nm, liposome particle size and uniformity Use a multi-angle nanoparticle analyzer to detect; use cross-flow technology to remove ammonium sulfate outside the liposome; dissolve doxorubicin hydrochloride in 9% lactose aqueous solution and heat to 40°C; add anhydrous sodium carbonate powder in the formula amount Adjust the pH of the paclitaxel-containing lipo...

Embodiment 3

[0042] Preparation prescription:

[0043]

[0044] Preparation Process:

[0045] Dissolve paclitaxel, phospholipids, cholesterol and vitamin E in chloroform according to the formula and mix them evenly; use a rotary evaporator to remove the chloroform in the solution under reduced pressure to form a lipid film; prepare 0.3M ammonium sulfate solution and hydrate with ammonium sulfate solution Lipid film, hydration temperature is between 70 ℃, obtains paclitaxel-containing liposome suspension; After hydration is complete, prepare liposomes with a high-pressure homogenizer until the average particle size is 120 ± 10nm, and the liposome particle size and The uniformity is detected by a multi-angle nanoparticle analyzer; the ammonium sulfate outside the liposome is removed by cross-flow technology; doxorubicin hydrochloride is dissolved in 9% lactose aqueous solution and heated to 40°C; Sodium powder adjusts the pH of the paclitaxel-containing liposome suspension to 7.5±0.3; mi...

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Abstract

The invention adopts the technical scheme that a doxorubicin hydrochloride-docetaxel or paclitaxel liposome preparation is provided. According to the technical scheme adopted by the invention, a water-soluble medicine and a fat-soluble medicine are encapsulated by liposome simultaneously; the water-soluble medicine is wrapped with the inner environment of the liposome; the fat-soluble medicine is wrapped between double layers of phospholipid membranes of the liposome; the water-soluble medicine is doxorubicin hydrochloride; and the fat-soluble medicine is docetaxel or paclitaxel. The doxorubicin hydrochloride-docetaxel or paclitaxel liposome preparation has the benefits that experiments prove that the toxic or side effect of the doxorubicin hydrochloride-docetaxel or paclitaxel liposome is obviously reduced and the anti-tumor therapy function of the doxorubicin hydrochloride-docetaxel or paclitaxel liposome is enhanced; the medicine encapsulation ratio of the liposome can reach 90% above; the result of the two-year stability experiment of the freeze-dried powder of the liposome at 2 to 8 DEG C below shows that the change rate of the average grain size is less than 6% and the change rate of the medicine encapsulation ratio is less than 5%, and shows excellent stability of the doxorubicin hydrochloride-docetaxel or paclitaxel liposome preparation.

Description

technical field [0001] The invention relates to a drug liposome, in particular to a doxorubicin hydrochloride-docetaxel or paclitaxel liposome. Background technique [0002] Doxorubicin hydrochloride (DOX-HCL) is the hydrochloride salt of anthracycline broad-spectrum antitumor antibiotic doxorubicin hydrochloride. Synthesis and Mitosis. Doxorubicin hydrochloride has a broad-spectrum anti-experimental tumor effect, and also has an inhibitory effect on topoisomerase, which can be applied to acute leukemia, malignant lymphoma, multiple myeloma, lung cancer, breast cancer, bladder cancer, testicular Carcinoma, thyroid cancer, soft tissue tumor, osteosarcoma, neuroblastoma, etc. It can also be used for gastric cancer, colorectal cancer, liver cancer, esophageal cancer, ovarian cancer, cervical cancer, etc. Although doxorubicin hydrochloride has a broad anti-tumor spectrum and good curative effect, it has severe side effects after intravenous injection, mainly including nausea, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/704A61P35/00A61K31/337
Inventor 贺明贺欣朱瑶俊代光玉
Owner 常州金远药业制造有限公司
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