Influence of Storage Humidity on the in Vitro Inhalation Properties of Salbutamol Sulfate Dry Powder with Surface Covered Lactose Carrier

Abstract

The influence of storage humidity on the in vitro inhalation properties of salbutamol sulfate dry powder with surface covered lactose carrier was investigated. In the present study, drug/carrier powder mixtures were prepared consisting of micronized salbutamol sulfate and lactose carriers with different particle surface conditions prepared by surface covering. Lactose carrier surfaces were covered with vegetable magnesium stearate (Mg-St-V) by a high-speed elliptical-rotor-type powder mixer (Theta-Composer ® ). These powder mixtures were aerosolized by a Jethaler ® , and the in vitro inhalation properties of salbutamol sulfate were evaluated by a twin impinger. Compared with the powder mixed with uncovered lactose carrier, the in vitro inhalation properties of the powder mixture prepared using the surface covered lactose carrier were little decreased with increased in relative humidity (RH), showing that the in vitro inhalation properties of salbutamol sulfate were improved at high RH. Using this surface covering technique would thus be valuable for storage humidity of dry powder inhalation (DPI) with lactose carrier particles.Key words dry powder inhalation; storage humidity; salbutamol sulfate; lactose carrier particle; vegetable magnesium stearate 444 Notes Chem.

Influence of Humidity on the Electrostatic Charge and Aerosol Performance of Dry Powder Inhaler Carrier based Systems

“…For example, at elevated humidities, condensation between salbutamol sulphate and lactose carrier may result in increased capillary forces and reduced drug liberation during inhalation. Previous studies using salbutamol sulphate/carrier systems have suggested elevated humidity above 60% RH to result in a significant reduction in aerosolisation performance (7,8). Furthermore, similar studies conducted on drug only systems suggested salbutamol sulphate aerosolisation performance to decrease when the humidity was above 60% RH (5,6).…”

Evolution of Granule Structure and Drug Content During Fluidized Bed Granulation by X-Ray Microtomography and Confocal Raman Spectroscopy

“…Apparently, ibuprofen particles become incorporated into granules as easily as lactose monohydrate and MCC, despite the fact that ibuprofen has significantly higher contact angle. [49][50][51][52] The high contact angle prevents binder droplets, which impact with the ibuprofen particles from spreading over the particle surface. As the likelihood for successful coalescence depends on the availability of the liquid layer at the contact point, the ibuprofen particles have a lower probability of forming liquid bridges, compared with lactose monohydrate and MCC particles with their lower contact angles.…”

Mechanical Methods for Dry Particle Coating Processes and Their Applications in Drug Delivery and Development

“…No effect of rotation speed (3500-4500rpm) on melting point and particle density was observed [65]. Coating of lactose with magnesium stearate by theta-composer ® showed increased humidity resistance when subjected to different relative humidity (RH) conditions (33,53,75, and 84 %) which was due to increase in contact angle and hydrophobicity of lactose [66]. Begat et al 2005 suggested conditioning of drug rather than carrier lactose to achieve best performance of DPI by showing effect of FCAs (leucine, lecithin and magnesium stearate) on the interfacial properties of salbutamol sulfatelactose DPI formulations by mechanofusion of lactose (<10μm size).…”