Publication: Formation of inhalable rifampicin-poly(l-lactide) microparticles by supercritical anti-solvent process
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Issued Date
2008
Resource Type
File Type
application/pdf
ISSN
15309932
Other identifier(s)
2-s2.0-63649113410
Rights Holder(s)
มหาวิทยาลัยศรีนครินทรวิโรฒ
Bibliographic Citation
AAPS PharmSciTech. Vol 9, No.4 (2008), p.1119-1129
Suggested Citation
Patomchaiviwat V., Paeratakul O., Kulvanich P. Formation of inhalable rifampicin-poly(l-lactide) microparticles by supercritical anti-solvent process. AAPS PharmSciTech. Vol 9, No.4 (2008), p.1119-1129. doi:10.1208/s12249-008-9152-7 Retrieved from: https://hdl.handle.net/20.500.14740/3856
Author(s)
Abstract
Formation of inhalable microparticles containing rifampicin and poly(L-lactide) (L-PLA) by using supercritical anti-solvent process (SAS) was investigated. The solutions of drug and polymer in methylene chloride were sprayed into supercritical carbon dioxide. The effect of polymer content and operating conditions, temperature, pressure, carbon dioxide molar fraction, and concentration of solution, on product characteristics were studied. The prepared microparticles were characterized with respect to their morphology, particle size and size distribution, drug content, drug loading efficiency, and drug release characteristic. Discrete, spherical microparticles were obtained at high polymer:drug ratios of 7:3, 8:2, and 9:1. The shape of L-PLA microparticles became more irregular and agglomerated with decreasing polymer content. Microparticles with polymer content higher than 60% exhibited volumetric mean diameter less than 5 μm, but percent drug loading efficiency was relatively low. Drug-loaded microparticles containing 70% and 80% L-PLA showed a sustainable drug release property without initial burst release. Operating temperature level influenced on mean size and size distribution of microparticles. The operating pressure and carbon dioxide molar fraction in the range investigated were unlikely to have an effect on microparticle formation. An increasing concentration of feed solution provided larger size microparticles. Rifampicin-loaded L-PLA microparticles could be produced by SAS in a size range suitable for dry powder inhaler formulation. © American Association of Pharmaceutical Scientists 2008.
Subject(s)
Carbon dioxide
Dichloromethane
Polylactide
Rifampicin
Microsphere
Polyester
Polylactide
Rifampicin
Solvent
Aerosol
Article
Drug release
Dry powder
Particle size
Pressure
Process design
Supercritical fluid
Temperature
Chemistry
High performance liquid chromatography
Inhalational drug administration
Scanning electron microscopy
Administration, Inhalation
Chromatography, High Pressure Liquid
Microscopy, Electron, Scanning
Microspheres
Particle Size
Polyesters
Rifampin
Solvents
Dichloromethane
Polylactide
Rifampicin
Microsphere
Polyester
Polylactide
Rifampicin
Solvent
Aerosol
Article
Drug release
Dry powder
Particle size
Pressure
Process design
Supercritical fluid
Temperature
Chemistry
High performance liquid chromatography
Inhalational drug administration
Scanning electron microscopy
Administration, Inhalation
Chromatography, High Pressure Liquid
Microscopy, Electron, Scanning
Microspheres
Particle Size
Polyesters
Rifampin
Solvents