A new solid self-microemulsifying formulation prepared by spray-drying to improve the oral bioavailability of poorly water soluble drugs

The objectives of the present work were, first, to develop a new solid self-microemulsifying drug delivery system (SMEDDS) for oral poorly water-soluble drugs such as nimodipine; and second, to evaluate its oral bioavailability in healthy rabbits. The liquid SMEDDS consisted of ethyl oleate, Labraso...

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Bibliographic Details
Published in:European journal of pharmaceutics and biopharmaceutics 2008-10, Vol.70 (2), p.439-444
Main Authors: Yi, Tao, Wan, Jiangling, Xu, Huibi, Yang, Xiangliang
Format: Article
Language:English
Subjects:
Absorption
Animals
Bioavailability
Biological and medical sciences
Biological Availability
Chemistry, Pharmaceutical
Drug Delivery Systems
Emulsions
General pharmacology
Male
Medical sciences
Nimodipine - administration & dosage
Nimodipine - chemistry
Nimodipine - pharmacokinetics
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Poorly soluble drugs
Rabbits
Self-microemulsifying
Solid dosage form
Solubility
Spray-drying
Technology, Pharmaceutical
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Summary:The objectives of the present work were, first, to develop a new solid self-microemulsifying drug delivery system (SMEDDS) for oral poorly water-soluble drugs such as nimodipine; and second, to evaluate its oral bioavailability in healthy rabbits. The liquid SMEDDS consisted of ethyl oleate, Labrasol ®, Cremophor ® RH 40 and nimodipine. The solid SMEDDS was prepared by spray-drying the liquid SMEDDS in a laboratory spray dryer, using dextran as solid carrier. The imaging of TEM and photo correlation spectroscopy revealed no difference in the droplet size of reconstituted microemulsion between both SMEDDS. Solid state characterization of the solid SMEDDS was performed by SEM, DSC, and X-ray powder diffraction. The same dose of nimodipine in the solid SMEDDS and in the liquid SMEDDS resulted in similar AUC and C max values, but the maximum absorption was retarded by the solid SMEDDS. AUC and C max after oral administration of the solid SMEDDS were 2.6- and 6.6-fold higher, respectively, compared with those of the conventional tablet. These results demonstrate that the solid SMEDDS may preserve an improved bioavailability with releasing microemulsion lipid droplets from the formulation in vivo. Thus, this solid self-microemulsifying system may provide a useful solid dosage form for oral poorly water-soluble drugs.
ISSN:0939-6411
1873-3441
DOI:10.1016/j.ejpb.2008.05.001