Solubilization carrier for drug, its preparation method and application

A drug and carrier technology, applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, freeze-dried delivery, etc., can solve problems such as hemolysis, turbidity, dilution instability, etc.

Inactive Publication Date: 2006-10-04
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN 1439655 discloses a novel chitosan derivative N-long-chain alkyl-O-sulfonic acid chitosan, the reaction conditions are relatively harsh, and the chlorosulfonic acid used is a very active strong acid, which will explode when it meets water. Unsafe, the sulfonation process needs to be carried out at 10°C N 2 Hemolysis occurs when the final concentration of micelles>0.18mg / ml, the critical micellar concentration is higher, 450mg / L, the drug loading of paclitaxel is 25% (w / w), but the dilution is unstable, dilute to It can only be stable for 1.5h at 0.67mg / ml, and it will become cloudy immediately when diluted to 0.6mg / ml (Zhang, Can, Qineng, Ping, et al.Colloids and Surfaces B: Biointerfaces, 2004, 39(1-2), 69- 75)
CN 1698899 discloses a kind of modified chitosan directly with hydrophobic carbon chain, can form micelle in aqueous medium under suitable molecular weight and suitable degree of substitution, but lower to drug load, as paclitaxel only 6.7% (w / w)

Method used

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  • Solubilization carrier for drug, its preparation method and application
  • Solubilization carrier for drug, its preparation method and application
  • Solubilization carrier for drug, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0120] Preparation of 6-O-carboxymethyl-2-N-octyl chitosan (connecting hydrophilic group first and then hydrophobic group)

[0121] 1. Preparation of 6-O-carboxymethyl chitosan

[0122] Suspend 1g of chitosan in isopropanol, add 5g of NaOH, stir at 30°C for 12h, add 6g of chloroacetic acid in isopropanol, react at 35°C for 5h, pour off the supernatant, add a certain amount of water, and use Adjust the pH to 7 with NaOH aqueous solution, precipitate with methanol, filter, wash with 90% ethanol and dry in vacuum to obtain highly substituted 6-O-carboxymethyl chitosan as light yellow or white powder.

[0123] 2. Preparation of 6-O-carboxymethyl-2-N-octyl chitosan

[0124] A reacts with haloalkane

[0125] Disperse 1g of 6-O-carboxymethyl chitosan evenly in isopropanol, add 2g of NaOH, alkalinize at 35°C, add n-octyl chloride under stirring, react at 30°C for 8h, adjust pH to 7, add acetone to precipitate, filter, filter The cake was washed with ether, and the sample was vacuum...

Embodiment 2

[0131] Preparation of 6-O-carboxymethyl-2-N-octyl chitosan (first connect hydrophobic group and then connect hydrophilic group)

[0132] 1. Preparation of 2-N-octyl chitosan

[0133] The method is the same as in Example 1, 2, replacing 6-O-carboxymethyl chitosan with chitosan.

[0134] 2. Preparation of 6-O-carboxymethyl-2-N-octyl chitosan

[0135] Method is with embodiment 1 middle 1, replaces chitosan with 2-N-octyl chitosan

[0136] Elemental analysis showed that the deacetylation degree was 91.5%, the carboxymethyl substitution degree was 95%, and the octyl substitution degree was 48%.

Embodiment 3

[0138] Preparation of 6-O-carboxymethyl-2-N-decyl chitosan

[0139] Replace n-octyl chloride and n-octyl aldehyde in embodiments 1 and 2 with n-decyl chloride and n-decyl aldehyde, and the preparation method is the same as in embodiments 1 and 2.

[0140] Elemental analysis showed that the deacetylation degree was 91.5%, the carboxymethyl substitution degree was 98%, and the decyl substitution degree was 40%.

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Abstract

This invention discloses a drug solubilization carrier and its preparation method and use. The carrier is made by separately inducting hydrophilic carboxymethyl or hydroxyethyl and hydrophobilic alkyl or alkyonyl on the 6 location and 2 location of chitose framework to produce amphipathic chitose derivatives that can combine to nanomicelle naturally. The carrier has low critical gathering concentration, high load capacity, little toxicity, high encapsulating ratio and has stable nanomicelle; it can be used as carrier for indissoluble or micro-dissoluble drugs. For this invention has simple processing method and mature technics, it fits to large-scale series production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a drug solubilizing carrier using chitosan as a raw material, and also relates to a preparation method and application of the carrier. Background technique [0002] Both nanotechnology and biodegradable materials are currently hot research areas for the development of drug delivery systems. Polymer nanomicelle research combines the advantages of both, which can be biodegradable and form drug nanocarriers. Polymer nanomicelle has the following characteristics: [0003] 1. Hydrophilicity and flexibility: The polymer can spontaneously form micelles in water, and its hydrophobic parts are entwined with each other to form a "core", while the hydrophilic parts surround the outside to form a flexible hydrophilic "shell". The inner core acts as a drug carrier or reservoir to provide a stable microenvironment for hydrophobic drugs, and the hydrophilic outer shell enables nanomic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K9/19
Inventor 周建平霍美蓉魏彦张勇许向阳李玲张祖菲
Owner CHINA PHARM UNIV
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