Back to Search
Start Over
Preparation and Evaluation of Solid Dispersion of Atorvastatin Calcium with Soluplus® by Spray Drying Technique
- Source :
- Chemical and Pharmaceutical Bulletin. 62:545-551
- Publication Year :
- 2014
- Publisher :
- Pharmaceutical Society of Japan, 2014.
-
Abstract
- The aim of the present study was to investigate the effect of Soluplus® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus® increases the aqueous solubility of atorvastatin calcium. Several solid dispersion formulations of atorvastatin calcium with Soluplus® were prepared at various drug : carrier ratios by spray drying. Physicochemical analysis demonstrated that atorvastatin calcium is amorphous in each solid dispersion, and the 2 : 8 drug : carrier ratio provided the highest degree of sustained atorvastatin supersaturation. Pharmacokinetic analysis in rats revealed that the 2 : 8 dispersion significantly improved the oral bioavailability of atorvastatin. This study demonstrates that spray-dried Soluplus® solid dispersions can be an effective method for achieving higher atorvastatin plasma levels.
- Subjects :
- Male
Atorvastatin
Administration, Oral
Biological Availability
Polyethylene Glycols
Rats, Sprague-Dawley
Atorvastatin calcium
health services administration
Drug Discovery
medicine
Animals
Pyrroles
heterocyclic compounds
cardiovascular diseases
Desiccation
Solubility
Supersaturation
Chromatography
Chemistry
Water
nutritional and metabolic diseases
General Chemistry
General Medicine
Rats
Bioavailability
Amorphous solid
Heptanoic Acids
Spray drying
Polyvinyls
lipids (amino acids, peptides, and proteins)
Dispersion (chemistry)
medicine.drug
Subjects
Details
- ISSN :
- 13475223 and 00092363
- Volume :
- 62
- Database :
- OpenAIRE
- Journal :
- Chemical and Pharmaceutical Bulletin
- Accession number :
- edsair.doi.dedup.....518bbf92573a00fd3b090a752b1ea62e
- Full Text :
- https://doi.org/10.1248/cpb.c14-00030