Modified hydrophobic auxiliary material as well as preparation method and application thereof

Abstract

The invention relates to preparation of novel pharmaceutic auxiliary materials and drug-loaded fat emulsions, and provides a hydrophobic auxiliary material, the molecular formula of which is as follows: R is a hydrophobic natural compound or synthetic compound with one to three hydroxyl groups (n= 1-3); R1 is an alpha-amino protecting group, R2 is an amino acid side chain, m is equal to 0, and atthe moment, R reacts with the amino acid derivative with the protecting group through esterification to form a hydrophobic auxiliary material carrying the amino acid derivative with the protecting group; or m is equal to 1, at the moment, an amino acid connecting arm (l being equal to 1, 2, 4, and 6) with different chain lengths is introduced into R through an ester group, then an amino acid derivative with a protective group is introduced, and the hydrophobic auxiliary material carrying the amino acid derivative polypeptide with the protective group is formed. According to the method, the amino acid derivative with the aromatic or alkoxycarbonyl or acyl amino protecting group is introduced to the hydrophobic auxiliary material, so that the solubility of the drug in the hydrophobic auxiliary material is increased, and the stability of the drug-loaded fat emulsion is improved.

Description

technical field

[0001] The invention relates to the application field of preparation of pharmaceutical excipients and drug-loaded fat emulsion, more specifically, it relates to a modified hydrophobic excipient, its preparation method and its application. Background technique

[0002] Many drugs with poor water solubility need to increase water solubility by chemical or physical methods, and can be used after being prepared into injections. Drugs can be solubilized by chemical bonding with hydrophilic or amphiphilic excipients, and can also be used to form molecular inclusions with cyclodextrins, and to form micelles, nanodispersions, and liposomes with surfactants. The active agent and the oil phase form an emulsion, and formulation processes such as albumin encapsulation achieve solubilization.

[0003] Emulsion is a commonly used drug carrier, which is used to increase the solubility of poorly water-soluble drugs, while protecting the drug from rapid degradation, and chan...

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