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Method for preparing vesicle medicinal nanoparticles

A technology of nano-suspension and capsule core, which is applied in the field of medicine and can solve the problems of insoluble drugs in organic solvents and limited use of drugs

Inactive Publication Date: 2015-04-15
NANJING LAKESEN BIOPHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] According to statistics, at least 40% of the drugs are currently limited in use due to water solubility, and some drugs are even difficult to dissolve in organic solvents

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation of Hydroxycamptothecin Capsule-nucleus Suspension

[0028] The present invention contains the following components in every 100ml hydroxycamptothecin capsule nucleus formula nanosuspension:

[0029] Hydroxycamptothecin 500mg, dimethyl sulfoxide 1.5ml, stabilizer 0.2g, isotonic regulator 2.2g, and the rest is water. The stabilizer is polyaspartic acid-chondroitin block copolymer, and the isotonic regulator is glycerol.

[0030] Preparation:

[0031] 1. Synthesis and process optimization of polyaspartic acid block (amphiphilic) copolymer

[0032] Protect aspartic acid with benzyl alcohol, then carry out N-carboxylic acid anhydride, and then synthesize polyaspartic acid by ring-opening polymerization, and use the aminated hydrophilic polymer compound chondroitin-NH 2 Terminate the reaction, synthesize polyaspartic acid-chondroitin block copolymers in two steps, remove the protecting group benzyl alcohol by alkaline hydrolysis, and finally use va...

Embodiment 2

[0040] Example 2 Preparation of paclitaxel capsule-core nanosuspension

[0041] The present invention contains the following components in every 100ml paclitaxel capsule-core nanosuspension:

[0042] Paclitaxel 0.3g, ethanol 6ml, stabilizer 0.1g, isotonic regulator 2.0g, and the rest is water. The stabilizer is polyglutamic acid-hyaluronic acid block copolymer and Anti-HER2 modified polyglutamic acid-hyaluronic acid block copolymer, and the isotonic regulator is glycerol.

[0043] Preparation:

[0044] 1. Synthesis and process optimization of polyglutamic acid block (amphiphilic) copolymer

[0045] Protect glutamic acid with benzyl alcohol, then carry out N-carboxylic acid anhydride, and then prepare polyglutamic acid by ring-opening polymerization, and terminate the reaction with hyaluronic acid, a hydrophilic polymer compound, to synthesize polyglutamic acid in two steps. Amino acid-hyaluronic acid copolymer, and then remove the protecting group benzyl alcohol by alka...

Embodiment 3

[0053] Example 3 Preparation of Oridonin A Capsule-nucleus Nanosuspension

[0054] The present invention contains the following components in every 100ml oridonin capsule-core nanosuspension:

[0055] Oridonin 1g, N-methylpyrrolidone 10ml, stabilizer 0.2g (including targeting stabilizer 50mg), isotonic regulator 2.0g, and the rest is water. The stabilizer is polyhistidine-chitosan block copolymer and polyhistidine-chitosan block copolymer modified by folic acid, and the isotonic regulator is mannitol.

[0056] 1. Synthesis and process optimization of polyhistidine block (amphiphilic) copolymer

[0057] Protect the amino group of L-histidine with benzyl chloroformate, and the resulting intermediate undergoes nucleophilic substitution reaction with 2,4-dinitrofluorobenzene under alkaline conditions to obtain compound N α -CBZ-N im -DNP-L-histidine, under the action of thionyl chloride, N α -CBZ-N im -DNP-L-histidine undergoes intramolecular condensation to generate anhyd...

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Abstract

The invention relates to the technical field of medicines, and relates to design, preparation and application of vesicle nanoparticles of insoluble medicines. The invention comprises the following aspects: (1) a model medicine is dissolved in a good solvent to form a medicinal solution, and a functional stabilizer is dissolved in another solvent to form a poor medicinal solution; and (2) the medicinal solution is mixed with the poor solvent, and vesicle nanocrystal suspension of which the average effective particle size of less than 1 mu m is formed through self-assembly. A micromolecular material with high compatibility is selected, and a macromolecular polymer stabilizer is synthesized by a covalent binding technology; by microsedimentation, self-assembly and surface modification technologies, the medicine is stabilized in the poor solvent in a form of pure nanocrystals, and a problem that the insoluble medicines are hardly prepared into solution preparations and the problems of dumping and passivity of the traditional nanoparticles are solved; and compared with the traditional preparations, the vesicle nanoparticles have the advantages that the adverse reaction is reduced, toxic and side effects are reduced, the bioavailability is improved, and the vesicle nanoparticles have controlled-release and active targeting functions, and are convenient to use.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a vesicular drug nanoparticle [0002] Preparation. Background technique [0003] According to statistics, currently at least 40% of drugs are limited in use due to water solubility, and some drugs are even difficult to dissolve in organic solvents. For BCS class 2 and 4 poorly soluble drugs, when used for intravenous administration, an aqueous medium must be used. In order to improve the water solubility and drug loading of drugs, non-aqueous solvents, solubilizers, etc. are often used in the prescription, which makes the problems of biotoxicity and biocompatibility quite prominent. For example, paclitaxel injection uses polyoxyethylated castor oil , Docetaxel injection uses Tween-80 and ethanol. In 1995, Müller et al proposed a new drug delivery system - nanosuspensions (nanosuspensions). Nanosuspension is a submicron colloidal dispersion system formed by dispersing "pure...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K9/51A61K9/10A61K47/34A61K47/42A61K47/36
Inventor 蒲晓辉袁琦杨浩赵辉刘伟芬李禄辉郭允
Owner NANJING LAKESEN BIOPHARM TECH CO LTD
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