External release testing method of liposome medicaments prepared by pH gradient active drug loading method

An active drug-loading method and testing method technology, which is applied in the testing field of liposome drugs, can solve problems such as the inability to simulate the in vivo and in vitro release relationship of drugs, the prolonged main release period of doxorubicin, and the indistinct details of the release curve. , to achieve enhanced differentiation, high reliability, and easy implementation

Active Publication Date: 2017-03-29
上海复旦张江生物医药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the detailed characteristics of the release curve obtained by this method are not obvious, and the main release period of doxorubicin cannot be lengthened to increase the differentiation between different formulations, and the in vivo and in vitro release relationship of the drug cannot be simulated.

Method used

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  • External release testing method of liposome medicaments prepared by pH gradient active drug loading method
  • External release testing method of liposome medicaments prepared by pH gradient active drug loading method
  • External release testing method of liposome medicaments prepared by pH gradient active drug loading method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1: Rotation - 52°C - 10% Resin - 33mM Ammonium Chloride

[0062] Steps A and B are the same as Comparative Examples 1 and 2.

[0063] C. In vitro release test

[0064] a. Add 5ml doxorubicin liposome dilution in the EPPENDORF centrifuge tube of 5ml;

[0065] b, adding ammonium chloride in the solution to form a mixed solution, so that the concentration of ammonium chloride is 33mM;

[0066] c. Add 0.5g (w / v=10%) cation exchange resin to the mixed solution;

[0067] d. Set the temperature of the molecular hybridization instrument at 52° C. and the rotation speed at 0 rpm, and add samples while preheating;

[0068] e. After sealing the centrifuge tube, fix it on the hybridization tube rack of the molecular hybridization instrument perpendicular to the rotation axis in a radial and centripetal manner;

[0069] f. Set the temperature of the molecular hybridization instrument at 52° C., and the rotational speed at 25 rpm, start to rotate and count.

[0070] g. T...

Embodiment 2

[0084] Example 2: 52°C - 10% resin - 48mM ammonium chloride

[0085] Steps A, B, and C are all the same as in Example 1. The difference is that the final concentration of ammonium chloride in the mixed solution is 48mM.

[0086] Samples were taken at the time points of 1h, 2h, 4h, 6h, and 8h, and 6 samples were taken at each time point, and the standard deviation (SD) was calculated. The test results are shown in Table 2.

[0087] 6 samples release rate of each time point in table 2, embodiment 2

[0088]

[0089] attached figure 2 It is a plot of the data in Table 2. It can be seen from the figure that the release rate of doxorubicin is very close in the 6 groups of investigations operated at the same time, and the repeatability of the method is very good.

[0090] (3) Investigate the influence of temperature and the pH value of PBS buffer on the release rate

Embodiment 3

[0091] Example 3: 37°C-10% resin-33mM ammonium chloride-pH5.5

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Abstract

The invention relates to a method for testing liposome medicaments, and especially relates to external release of liposome medicaments prepared by a pH gradient active drug loading method. A vertical displacement motion mode of a container is used for controlling rate of a release promoting agent for releasing compounds and dissolving balance of components in solution and air, indirectly controlling release rate of medicaments, and simulating dynamic action of internal blood circulation for medicaments. Addition, temperature or rotating speed and other parameters of the release promoting agent are controlled, in order to accurately adjust release speed. The method has the advantages of high controllability, operation convenience, and good repeatability. Ion exchange resin also can be added in order to adsorb released free drug, in order to simulate internal sink condition state effects.

Description

technical field [0001] The invention relates to a test method of liposome medicine, in particular to a test method for simulating the release process of liposome medicine in vitro after entering the body. Background technique [0002] Since the discovery of phospholipid bilayer membranes in the 1990s, the research on liposomes as drug delivery vehicles has made great progress. Liposomes are microvesicles formed by encapsulating drugs in lipid bilayers. When phospholipid molecules are in water, the hydrophilic head of the molecule is inserted into the water, and the hydrophobic tail extends to the air to form a spherical liposome with a lipid bilayer structure, and the particle size is usually 25-1000nm. [0003] The bilayer membrane structure of liposomes is similar to biological membranes and has good biocompatibility; the drugs encapsulated by liposomes have the advantages of targeting, long-acting, low toxicity and good encapsulation protection. Therefore, liposomes are...

Claims

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Application Information

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IPC IPC(8): G01N33/15
Inventor 唐海玲张金平毛文学苏勇
Owner 上海复旦张江生物医药股份有限公司
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