The invention discloses
salicylic acid sustained-release microspheres prepared by a
cyclodextrin inclusion technology and a preparation method of the
salicylic acid sustained-release microspheres, and belongs to the technical field of pharmaceutical preparations. The method aims to solve the problems of poor
solubility, low
drug loading capacity and lack of sustained-release capability of traditional
cyclodextrin inclusion
salicylic acid. The core of the method is that two brand new functional compounds, namely
quaternary ammonium salt
hydroxypropyl beta cyclodextrin and
nicotinamide poloxamer covalent conjugates, are firstly prepared; when the microspheres are prepared, the two compounds are dissolved in a mixed
solvent of
ethanol and water, then salicylic acid and
nicotinamide are added, a supramolecular inclusion solution is formed through stirring, and finally a
microsphere product is obtained through
spray drying and screening. Wherein the affinity with the
skin is enhanced by the cationic
cyclodextrin derivative, the
nicotinamide conjugate and salicylic acid form a stable compound through
intermolecular interaction, and efficient inclusion and loading of salicylic acid are realized through synergism of the cationic
cyclodextrin derivative and the nicotinamide conjugate. The dissolvability, the solution transparency and the storage stability of salicylic acid are remarkably improved, the
microsphere wrapping amount is high, a good slow-release effect is achieved, and the salicylic acid
microsphere is suitable for the field of
skin external preparations.