Preparation and characterization of ibuprofen–cetyl alcohol beads by melt solidification technique: effect of variables

Ibuprofen (IBU) exhibits short half-life, poor compressibility, flowability and caking tendency. IBU melt has sufficiently low viscosity and exhibits interfacial tension sufficient to form droplet even at low temperature. A single step novel melt solidification technique (MST) was developed to produ...

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Bibliographic Details
Published in:	International journal of pharmaceutics Vol. 261; no. 1; pp. 57 - 67
Main Authors:	Maheshwari, Manish, Ketkar, Anant R, Chauhan, Bhaskar, Patil, Vinay B, Paradkar, Anant R
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier B.V 11-08-2003 Elsevier
Subjects:	Anti-Inflammatory Agents, Non-Steroidal - chemistry Biological and medical sciences Calorimetry, Differential Scanning Cetyl alcohol Chemistry, Pharmaceutical Delayed-Action Preparations Factorial design Fatty Alcohols - chemistry General pharmacology Hot Temperature Ibuprofen Ibuprofen - chemistry Kinetics Medical sciences Melt solidification technique Microscopy, Electron, Scanning Microspheres Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Response surface methodology Solubility Spectroscopy, Fourier Transform Infrared Surface Properties Cetyl alcohol Response surface methodology Factorial design Ibuprofen Melt solidification technique Bed Prostaglandin-endoperoxide synthase Melting Pharmaceutical technology Enzyme Enzyme inhibitor Solidification Arylpropionic acid derivatives Response surface Oxidoreductases
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Summary:	Ibuprofen (IBU) exhibits short half-life, poor compressibility, flowability and caking tendency. IBU melt has sufficiently low viscosity and exhibits interfacial tension sufficient to form droplet even at low temperature. A single step novel melt solidification technique (MST) was developed to produce IBU beads with lower amounts of excipient. Effect of variables was studied using a 3 2 factorial approach with speed of agitation and amount of cetyl alcohol (CA) as variables. The beads were evaluated using DSC, FT-IR and scanning electron microscope (SEM). Yield, micromeritic properties, crushing strength and release kinetics were also studied. Spherical beads with a method yield of above 90% were obtained. The data was analyzed by response surface methodology. The variables showed curvilinear relationship with yield in desired particle size range, crushing strength and, bulk and tap density. The drug release followed non-Fickian case II transport and the release rate decreased linearly with respect to amount of CA in the initial stages followed by curvilinearity at later stages of elution. The effect of changing porosity and tortuosity was well correlated.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0378-5173 1873-3476
DOI:	10.1016/S0378-5173(03)00292-8