Method of avoiding phenomenon of accelerating blood clearance by continuously and repeatedly injecting polyethylene glycol (PEG) lipidosome of epirubicin hydrochloride

A kind of epirubicin hydrochloride, a technology for accelerating blood clearance, applied in the field of tissue distribution

Inactive Publication Date: 2013-06-19
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is worth noting that continuous low-dose injection of liposomes may lead to the generation of ABC phenomenon

Method used

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  • Method of avoiding phenomenon of accelerating blood clearance by continuously and repeatedly injecting polyethylene glycol (PEG) lipidosome of epirubicin hydrochloride
  • Method of avoiding phenomenon of accelerating blood clearance by continuously and repeatedly injecting polyethylene glycol (PEG) lipidosome of epirubicin hydrochloride
  • Method of avoiding phenomenon of accelerating blood clearance by continuously and repeatedly injecting polyethylene glycol (PEG) lipidosome of epirubicin hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Example 1 Preparation of epirubicin hydrochloride liposomes

[0066] The prescription is:

[0067] HSPC 3.0g

[0068] CH 1.0g

[0069] MPEG 2000 -DSPE 1.0 g

[0070] The preparation process is:

[0071] At 65 °C, dissolve the prescribed amount of membrane material with 5% ethanol (v / v), inject 60 mL of hydration medium (200 mmol L -1 (NH 4 ) 2 SO 4 solution), incubated for 20 min to obtain the primary liposome, which was treated by micro-fluidization (pressure of 14000 psi) to reduce the particle size to 100 nm, and passed through microporous membranes of 0.8, 0.45 and 0.22 μm in sequence, namely Obtain blank liposomes.

[0072] Gradient establishment: take blank liposomes, mix with mixed resin (the mixing ratio of 732 sodium cation exchange resin and 717 chloride anion exchange resin is 1:2 according to the wet volume) and let it stand for 5 minutes, then centrifuge at 2000 rpm for 4 minutes , to build the gradient.

[0073] Drug loading: add epirubicin hy...

Embodiment 2

[0074] Example 2 Effect of the first injection of blank liposomes and epirubicin hydrochloride liposomes on the ABC phenomenon of the second injection of epirubicin hydrochloride liposomes

[0075] 1 Processing of plasma and tissue samples

[0076] 1.1 Processing of plasma samples: Take 0.1 mL of rat plasma, put it in a 7 mL tube, add 0.3 mol·L -1 HCl methanol-water (50:50, v / v) solution 4.9 mL, vortex 30 s to mix. The suspension was centrifuged at 10,000 rpm for 10 min, and the supernatant was taken to measure the fluorescence value.

[0077] 1.2 Treatment of tissue samples: Take 0.5 g of tissue in a 7 mLEp tube, add 1 mL of normal saline for high-speed dispersion and homogenate, pipette 0.2 mL of tissue homogenate precisely, add 0.3 mol·L -1 HCl methanol-water (50:50, v / v) solution 4.8 mL, vortex 30 s to mix. The suspension was centrifuged at 10,000 rpm for 10 min, and the supernatant was taken to measure the fluorescence value.

[0078] 2 Establishment of in vivo ...

Embodiment 3

[0089] Example 3 Determination of IgM content of anti-PEG in serum

[0090] Refer to the method of Ichihara et al. (Ichihara M, Shimizu T, et al. Anti-PEG IgM Response against PEGylated Liposomes in Mice and Rats[J]. Pharmaceutics, 2011, 3: 1–11) to determine the content of anti-PEG IgM in serum Determination. The specific process is as follows: the MPEG 2000 -DSPE was prepared with absolute ethanol to a concentration of 0.2 mmol L -1 solution, take 50 μL and add it to a 96-well plate. After the 96-well plate is completely dry at room temperature, add Tris buffer containing 1% BSA (50 mmol L -1 Tris, 0.14 mmol L -1 NaCl, pH 8.0) 100 μL for blocking for 1 h, and then successively washed three times with Tris buffer containing 0.05% Tween20. Serum samples were diluted 100 times, 100 μL was added to each well, incubated at room temperature for 1 h, washed five times with Tris buffer containing 0.05% Tween20, and 1 μg / mL horseradish peroxidase-linked goat antibody was adde...

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Abstract

The invention belongs to the field of medical technology, relates to a method of avoiding a phenomenon of accelerating blood clearance by continuously and repeatedly injecting polyethylene glycol (PEG) lipidosome of epirubicin hydrochloride, and particularly relates to the influences of the pharmacokinetics behavior of the epirubicin hydrochloride in the second injection of the PEG epirubicin hydrochloride lipidosome by the first injection of blank lipidosome and PEG epirubicin hydrochloride lipidosome and the phenomenon of accelerating blood clearance by continuously and repeatedly injecting the PEG lipidosome. Dosage of PEG epirubicin hydrochloride lipidosome is provided to relieve or avoid the acceleration of the blood clearance on the mentioned basis. By changing the dosage of the epirubicin hydrochloride of the first injection or the continuous injection, the method reaches the purpose of preventing drugs from releasing from the lipidosome and relieving or eliminating the acceleration of the blood clearance.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and specifically relates to the influence of the first injection of blank liposomes and epirubicin hydrochloride liposomes on the pharmacokinetic behavior of epirubicin hydrochloride in the second injection of epirubicin hydrochloride liposomes, and Accelerated blood clearance (ABC) phenomenon of continuous multiple injections of PEGylated liposomes, and the administration dose of epirubicin hydrochloride liposomes for reducing or avoiding the ABC phenomenon. Background technique: [0002] Conventional ordinary (classic / traditional) intravenous drug delivery systems, such as ordinary liposomes, are easily phagocytized by the mononuclear macrophage system (MPS), and quickly distributed to liver, spleen and other organs after intravenous injection, resulting in blood circulation of liposomes Short time and poor targeting. In order to solve such problems, researchers use polyethylene glycol (PE...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61K9/127A61P35/00A61P31/04
Inventor 邓意辉杨强宋艳志佘振南
Owner SHENYANG PHARMA UNIVERSITY
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