Hydrophobic cyclodextrin clathrate and preparation and use thereof

Abstract

The present invention provides a hydrophobic cyclodextrin clathrate compound with a slow release effect, which is made by mixing a tert-butyl alcohol solution of hydrophobic cyclodextrin and a water phase solution containing hydrophilic medicine. The volume ratio of the tert-butyl solution to the water phase solution is 1 to 100:3. The mol mass ratio of the cyclodextrin to the hydrophilic medicine is 1 to 10:1. The present invention also discloses a method for preparing the clathrate compound. The method comprises the steps of: preparing the hydrophobic cyclodextrin tert-butyl alcohol solution and the water phase solution of the hydrophilic medicine; mixing both solutions into a single phase solution; and, drying, etc. The present invention also discloses an application of the cyclodextrin clathrate compound in pharmacy. Compared with the ordinary release preparations, the clathrate compound formed by the hydrophobic cyclodextrin and the water-soluble medicine is capable of reducing the solubility and digestion velocity of the water-soluble medicine and postponing the release of the medicine. The process is simple, convenient in operation, short in period, low in energy dissipation, and suitable for industrialized production, and has no residue of organic solvent.

Description

technical field The invention belongs to the field of pharmaceutical preparations in medical engineering, and in particular relates to a hydrophobic cyclodextrin inclusion compound with a slow-release effect and a preparation method and application thereof. Background technique In recent years, the continuous development of cyclodextrin (CD) derivatives has broadened the application of cyclodextrin in the field of pharmacy. There are a large number of primary and secondary hydroxyl groups in the cyclodextrin molecule. These hydroxyl groups (especially the 2, 3 and 6-position hydroxyl groups) can be used as chemical structure modification points, and groups with different properties (methyl, ethyl, etc.) can be replaced by substitution reactions. , hydroxypropyl, hydroxyethyl, acetyl, etc.) into the CD molecule, and the introduction of these groups does not affect the capacity of the central hole to accommodate guest molecules, but improves some of the physicochemical propert...

AI Technical Summary

Problems solved by technology

However, there is no research report on the hydrophobic cyclodextrin inclusion complex of tert-butanol / water co-solvent system for inclusion of hydrophilic drugs

Images