Investigations on the Humidity-Induced Transformations of Salbutamol Sulphate Particles Coated with l-Leucine

Raula, Janne; Thielmann, Frank; Kansikas, Jarno; Hietala, Sami; Annala, Minna; Seppälä, Jukka; Lähde, Anna; Kauppinen, Esko I.

doi:10.1007/s11095-008-9613-4

Cited by 41 publications

(20 citation statements)

References 44 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…1 shows particle morphologies. In consistent with the previous results (16,18), in this study the morphology of particles depended on the saturation conditions of L-leucine as follows, see Fig. 1.…”

Section: Particle Morphologysupporting

confidence: 93%

“…Particle preparation by the aerosol flow reactor has been discussed in detail in our previous work (12,18). Briefly, the solute droplets formed from the precursor solutions (ultrasonic nebulizer RBI Pyrosol 7901) containing salbutamol sulphate and L-leucine were dried to form solid microparticles in the gas phase.…”

Section: Particle Productionmentioning

confidence: 99%

“…Both layers were crystalline (16). The rough coating layer provided excellent powder aerosolization (17), whereas the encapsulating layer protected the particles against moisture (18).…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Structure and Dissolution of l-Leucine-Coated Salbutamol Sulphate Aerosol Particles

et al. 2012

Self Cite

View full text Add to dashboard Cite

Abstract. L-Leucine formed different crystalline coatings on salbutamol sulphate aerosol particles depending on the saturation conditions of L-leucine. The work emphasizes a careful characterization of powders where structural compartments such as crystal size and particle coating may affect the performance of drug when administered. The sublimation of L-leucine from the aerosol particles took place 90°C lower temperature than the bulk L-leucine which was attributed to result from the sublimation of L-leucine from nano-sized crystalline domains. The dissolution slowed down and initial dissolution rate decreased with increasing L-leucine content. Decreasing crystalline domains to nano-scale improve heat and mass transfer which was observed as the lowered decomposition temperature of the drug salbutamol sulphate and the sublimation temperature of surface material L-leucine as well as the altered dissolution characteristics of the drug. The structure of the coated drug particles was studied by means of thermal analysis techniques (DSC and TG), and the dissolution of salbutamol sulphate was studied as an on-line measurement in a diffusion cell.

show abstract

Section: Particle Morphologysupporting

confidence: 93%

Section: Particle Productionmentioning

confidence: 99%

See 1 more Smart Citation

Structure and Dissolution of l-Leucine-Coated Salbutamol Sulphate Aerosol Particles

et al. 2012

Self Cite

View full text Add to dashboard Cite

show abstract

“…[14][15][16][17] From the stand point of particle shape, the shape with a smaller surface contact area generally results in a higher dispersibility.…”

mentioning

confidence: 99%

“…[14][15][16][17] From the stand point of particle shape, the shape with a smaller surface contact area generally results in a higher dispersibility. 18) The particles prepared by the supercritical fluid antisolvent method presented various shapes as a function of materials and preparation conditions.…”

mentioning

confidence: 99%

Development of Dry Salbutamol Sulfate Powder with High Inhalation Performance Independent of Inhalation Patterns

Hira

Okuda

Ichihashi

et al. 2012

CHEMICAL & PHARMACEUTICAL BULLETIN

View full text Add to dashboard Cite

While dry powder inhalations are commonly used to treat pulmonary diseases, their clinical performance depends on patient inspiratory flow patterns. The purpose of this study was to develop a new powder with high and stable therapeutic performance for various patients. We applied the supercritical antisolvent (SCF) method to salbutamol sulfate (SS) to prepare a bulky SS particle (SS-SCF). Tests of in vitro inhalation performance with a human inspiratory flow simulator revealed SS-SCF to be less susceptible to inspiratory flow patterns than milled SS. When inspired, the unique structure seemed to be broken resulting in small fragments that could be delivered to the lungs. However, stability tests under physical stress showed tolerance for transportation and handling. In addition, optimization of the concentration of the SS solution applied to SCF method improved the in vitro inhalation performance of SS-SCF. These results indicated that a unique bulky SS powder prepared by the SCF method was useful for dry powder inhalation.Key words dry powder inhalation; inspiratory flow pattern; supercritical fluid drying; twin stage liquid impinger; inhalation performanceThe most common treatment for pulmonary diseases like asthma and chronic obstructive pulmonary disease (COPD) is inhalation therapy. Dry powder inhalants (DPIs) have become common in the field of inhalation therapy because they are free from environmentally damaging propellants and easy to use with small portable devices.1,2) With passive DPIs, because the aerosolization is activated by inhalation, handling is easier than that with pressurized metered dose inhalers (pMDIs). Many studies have investigated the therapeutic performance of dry powders influenced by particle size, morphology, surface roughness, crystallinity, and so on. [3][4][5] In addition, inspiratory flow patterns and inhalation devices have a significant impact on particle dispersion. [6][7][8] The clinical performance of inhalable drugs is susceptible to inspiratory patterns. 9,10) Numerous studies have shown the influence on inhalation performance of inspiratory patterns. 8,11,12) For stable therapeutic performance, not only drug administration guidance for patients but also the development of new formulations whose inhalation performance is independent of inspiratory flow patterns is needed.We previously constructed a human inspiratory flow simulator, and evaluated the influence of human inspiratory flow patterns and inhalation device type on the in vitro inhalation performance of dry salbutamol sulfate (SS) powders physically mixed with coarse lactose monohydrate powders, revealing that the effect of inspiratory flow patterns depended on the particle diameter of the active pharmaceutical ingredient (API).13) Peak flow rate (PFR) most affected in vitro inhalation performance among three critical parameters selected for the characterization of human inspiratory flow patterns; flow increase rate (FIR), inspiratory flow volume (area under the curve corresponding to inspiratory flow volume, AUC...

show abstract

Dry Powder Aerosols Generated by Standardized Entrainment Tubes From Drug Blends With Lactose Monohydrate: 1. Albuterol Sulfate and Disodium Cromoglycate

Mansour

Mulder³

et al. 2010

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Investigations on the Humidity-Induced Transformations of Salbutamol Sulphate Particles Coated with l-Leucine

Abstract: In order to preserve good flowability together with good physical stability, the best coating would contain two L-leucine layers, the inner layer being formed by diffusion (physical stability) and the outer layer by vapour deposition (flowability).

Cited by 41 publications

References 44 publications

Structure and Dissolution of l-Leucine-Coated Salbutamol Sulphate Aerosol Particles

Structure and Dissolution of l-Leucine-Coated Salbutamol Sulphate Aerosol Particles

Development of Dry Salbutamol Sulfate Powder with High Inhalation Performance Independent of Inhalation Patterns

Dry Powder Aerosols Generated by Standardized Entrainment Tubes From Drug Blends With Lactose Monohydrate: 1. Albuterol Sulfate and Disodium Cromoglycate

Contact Info

Product

Resources

About