Method of producing hepatic targeting drug microcapsule

A technology of liver targeting and microcapsules, which is applied in the field of preparation of drug microcapsules, can solve the problems of inability to precisely control drug sustained release, lack of tissue targeting, and normal tissue toxicity and side effects, and achieve a simple, efficient and easy-to-use copolymerization method Operation, high efficacy

Inactive Publication Date: 2008-02-27
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there is no report on the formation of microcapsules directly assembled layer by layer on the surface of solid drug particles, and the general layer-by-layer assembly microcapsules that have been reported so far are not grafted with targeting groups and do not have tissue (liver) targeting. Toxic and side effects similar to conventional drugs on normal tissues
The reported drug-carrying systems containing

Method used

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  • Method of producing hepatic targeting drug microcapsule
  • Method of producing hepatic targeting drug microcapsule
  • Method of producing hepatic targeting drug microcapsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 Synthesis of Galactose Vinyl Ester Monomer

[0045] Put 16g of divinyl adipate, 4g of galactose, and 1g of subtilisin into a 250mL Erlenmeyer flask, add 40mL of pyridine, ultrasonically mix, and react on a shaker at 50°C at 200rpm for 3 days. The solid was removed by filtration, the crude product was isolated, and distilled under reduced pressure to obtain a galactose vinyl ester monomer containing a double bond. The infrared spectrogram of galactose vinyl ester monomer is shown in Figure 1 (upper curve), and the characteristic peaks of vinyl ester C=C double bond and sugar C-O characteristic peaks are obvious, indicating that galactose vinyl ester monomer was successfully prepared.

Embodiment 2

[0046] Example 2 Synthesis of sugar-containing polycations (1)

[0047] After vacuum-drying the galactose vinyl ester monomer, place it in a desiccator and dry slowly for 20 days, take 0.4g galactose vinyl ester and 0.7g methacryloyloxyethyltrimethylammonium chloride (DMC) in a 25mL small flask In, add 1.4ml of distilled water to dissolve, at the same time add 1ml of potassium persulfate solution with a concentration of 10mg / ml. Vacuumize the nitrogen repeatedly for 3 times, the polymerization solution is stirred and reacted at 70°C for 24 hours under the protection of nitrogen, pour into acetone to precipitate the polymer, dissolve it with 10mL water, put it in a dialysis bag with a molecular weight cut-off of 3500kD, and dialyze against water for one day. The solution in the bag was freeze-dried, and the infrared spectrum of the obtained sugar-containing polycation was shown in Figure 1 (lower curve). The characteristic peak of the C=C double bond disappeared, the characteri...

Embodiment 3

[0048] Example 3 Synthesis of sugar-containing polycations (2)

[0049] Using the method of Example 2, 0.1 g of galactose vinyl ester monomer was copolymerized with 0.7 g of DMC to finally obtain a sugar-containing polycation with a grafted sugar molar ratio of 5%. The H NMR spectrum characterization is shown in Figure 2b.

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Abstract

The invention discloses a method for preparing a medicine with liver target taxis for slow-releasing the nanometer microcapsule. The method comprises the following steps: proceeding with enzymatic reaction of liver target taxis gene with sugar monomer of cerebrose residue and ethylated carboxylate; copolymerizing vinyl ester with glycosyl and unsaturated cationic or anion; getting liver target taxis polyelectrolyte; getting the medicinal microcapsule with liver target taxis by multilayer packaging polyelectrolyte on the surface of medicine by electrostatic action, wherein the deactivation speed of microcapsule medicine can be controlled. The polymerization method is simple, high effective and non-toxicity. The coating method has the high efficient, the simple operation and the mild technology, which can cycle several times. The preparing medicine can save for a long time, which can release step by step, can accumulate in the liver, improves the medicinal effect of disease portion, reduces the toxic effect of the other healthy organ, and has the good application prospect.

Description

technical field [0001] The invention relates to a preparation method of drug microcapsules. technical background [0002] Drugs in conventional dosage forms are distributed throughout the body after intravenous, oral or local injection, and the amount of drugs that actually reach the treatment target area is only a small part of the dose, and the distribution of most drugs in non-target areas not only has no therapeutic effect, It can also cause toxic side effects. In response to the above problems, a new type of drug dosage form - targeted drug delivery system has been developed, which can concentrate and localize the drug in diseased tissues, organs, cells or cells. Targeted preparations have the advantages of high curative effect, less drug dosage, and less toxic and side effects. An ideal targeted drug delivery system can release the drug in the target organ or the site of action, and at the same time, the systemic uptake is small, so that the curative effect can be im...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K45/00A61K47/36A61K31/513A61K31/522A61K31/573A61K31/704A61K31/7056B01J13/10
Inventor 林贤福张馥陈志春许建明
Owner ZHEJIANG UNIV
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