The invention discloses papaverine
hydrochloride sustained-release microspheres for injection and a preparation method of the papaverine
hydrochloride sustained-release microspheres, and relates to the technical field of pharmaceutical preparations. The sustained-release
microsphere comprises an
active component, a composite carrier, a composite stabilizer and a freeze-
drying protective agent. The composite carrier is a compound formed by
grafting a
polylactic acid-
glycolic acid copolymer and
hyaluronic acid, the composite stabilizer is a mixture of an
antioxidant and an
amino acid compound, the freeze-
drying protective agent is a mixture of
polyol and saccharides, and the surface of the
microsphere is provided with a hydrophilic-hydrophobic gradient
coating composed of a hydrophobic layer, an amphiphilic layer and a hydrophilic layer. The preparation method comprises the steps of primary
emulsion preparation, multiple
emulsion preparation, step-by-step curing,
surface modification and freeze-
drying treatment, and adopts the processes of gradient emulsification, step-by-step curing, layer-by-layer
grafting, gradient cooling and segmented sublimation. According to the technical scheme, the
drug encapsulation efficiency and the
drug loading capacity are effectively improved, the burst release rate is reduced, long-acting stable slow release is realized, the storage stability and the
biocompatibility are enhanced, and a safe and effective
drug administration choice is provided for treatment of ischemic diseases.