Simultaneous production and co-mixing of microparticles of nevirapine with excipients by supercritical antisolvent method for dissolution enhancement.
Microparticles of a poorly water-soluble model drug, nevirapine (NEV) were prepared by supercritical antisolvent (SAS) method and simultaneously deposited on the surface of excipients such as lactose and microcrystalline cellulose in a single step to reduce drug-drug particle aggregation. In the proposed method, termed supercritical antisolvent-drug excipient mixing (SAS-DEM), drug particles were precipitated in supercritical CO(2) vessel containing excipient particles in suspended state. Drug/excipient mixtures were characterized for surface morphology, crystallinity, drug-excipient physico-chemical interactions, and molecular state of drug. In addition, the drug content uniformity and dissolution rate were determined. A highly ordered NEV-excipient mixture was produced. The SAS-DEM treatment was effective in overcoming drug-drug particle aggregation and did not affect the crystallinity or physico-chemical properties of NEV. The produced drug/excipient mixture has a significantly faster dissolution rate as compared to SAS drug microparticles alone or when physically mixed with the excipients.
Sanganwar
Ganesh P
GP
Department of Chemical Engineering, Auburn University, Auburn, AL 36849-5127, USA.
Sathigari
Sateeshkumar
S
Babu
R Jayachandra
RJ
Gupta
Ram B
RB
D002626:Chemistry, Pharmaceutical / Q000379:methods*; D025924:Chromatography, Supercritical Fluid / Q000379:methods*; D003460:Crystallization / Q000379:methods; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods*; D005079:Excipients / Q000737:chemistry*; D008863:Microspheres; D019829:Nevirapine / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility; D013499:Surface Properties
D004337:Drug Carriers; D005079:Excipients; D019829:Nevirapine