Nano Spray-dried Formulations for Pulmonary Delivery of Salbutamol Salphate
|School||Liaoning Normal University|
|Keywords||Salbutamol Sulfate Nano Spray-Dried Powders Pulmonary Drug Delivery Excipients Formula Fine Particle Fraction|
Salbutamol sulfate can relax bronchial smooth muscle, reduce capillary permeability,increase airway epithelial cilia clearance function, eliminate bronchial smooth muscle spasm,and therefore quickly relieve asthma symptoms. The main diseases that salbutamol sulfatecan effectively treat are bronchial asthma, wheezing bronchitis, pneumonia and otherrespiratory diseases, and the inhaled aerosols is a major pharmaceutical formulation ofsalbutamol sulfate on the market. With salbutamol sulfate as the effective ingredient, thispaper screened the best supplementary material formula, mist pulmonary inhaled salbutamolsulfate powder preparation, and its properties were improved.Methods:1) Nano spray drying was used to prepare the salbutamol sulfate dry powders,and a series of carbohydrates were used as excipients to modify the physiochemical propertiesof nano spray-dried powders. The quality assessment methods were established to evaluatethe physiochemical properties and in-vitro lung deposition of nano spray-dried powders.2) Leucine was used as dispersibility enhancers to improve the lung depositon. A series ofleucine contents (10%,20%,30%and50%) were used and optimized in the dry powderformulations, with the aim to improve the dispersibility and aerosolisation performance ofnano spray-dried powders.3) Ammonium bicarbonate was added in the spray-dryingsolutions at different concentrations of0.2g,0.4g,0.6g,0.8g and1.0g to generate theporous nano spray-dried particles. These porous nano spray-dried powders wereinvestigated in their physiochemical properties including the porosity, morphology, particlesize and in-vitro lung deposition. The optimized content of ammonium bicarbonate wassubsequently selected to generate the ultralight powders for efficient pulmonary drugdelivery.Results:1) the lactose hygroscopicity strong, easy to reunite adhesion between particles,the starch solubility is poorer, trehalose and cyclodextrin with good solubility, low moistureabsorption, spray drying is the size of the particle size distribution is appropriate, effectivelung deposition rate were43.37%and43.86%respectively.2) with the increase of leucine inthe supplementary material proportion, particle surface concave fold, lower density, particlesize and distribution is appropriate, can improve the dispersion. When the dosage of leucinein the supplementary material is30%, lung deposition rate can reach68.79%.3) with theincrease of the amount of ammonium bicarbonate, powder particle volume, lower density, powder particles minimum tap density of0.01g/cm3. When the amount of ammoniumbicarbonate was0.6g, lung deposition rate can reach78.7%.Conclusion: the trehalose and cyclodextrin mist can be used as a good powdermaterials formula, the drug have the effect of dilution dispersion, acted as the carrier of drugand excipients. For hydrophobic amino acid leucine, reduce drug hygroscopicity, and formthe surface of hollow microsphere, improve powder mist dispersion, improve lung depositionrate effectively. Ammonium bicarbonate in the supplementary material formula have theeffect of raising agent, can reduce drug particles density, improve powder mist dispersion,improve lung deposition rate effectively.