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      Enhanced dissolution rate of celecoxib using PVP and/or HPMC-based solid dispersions prepared by spray drying method

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          Manufacturing of solid dispersions of poorly water soluble drugs by spray drying: formulation and process considerations.

          Spray drying is an efficient technology for solid dispersion manufacturing since it allows extreme rapid solvent evaporation leading to fast transformation of an API-carrier solution to solid API-carrier particles. Solvent evaporation kinetics certainly contribute to formation of amorphous solid dispersions, but also other factors like the interplay between the API, carrier and solvent, the solution state of the API, formulation parameters (e.g. feed concentration or solvent type) and process parameters (e.g. drying gas flow rate or solution spray rate) will influence the final physical structure of the obtained solid dispersion particles. This review presents an overview of the interplay between manufacturing process, formulation parameters, physical structure, and performance of the solid dispersions with respect to stability and drug release characteristics. Copyright © 2012 Elsevier B.V. All rights reserved.
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            Characterization of curcumin-PVP solid dispersion obtained by spray drying.

            Curcumin, a naturally occurring highly lipophilic molecule has wide range of pharmacological activities. However, its limited aqueous solubility and degradation at alkaline pH restricts its bioavailability. Solid dispersions of curcumin in different ratios with PVP were prepared by spray drying. Physical characterization by SEM, IR, DSC, and XRPD studies, in comparison with corresponding physical mixtures revealed the changes in solid state during the formation of dispersion and justified the formation of high-energy amorphous phase. Dissolution studies of curcumin and its physical mixtures in 0.1 N HCl showed negligible release even after 90 min. Whereas, solid dispersions showed complete dissolution within 30 min. This may aid in improving bioavailability and dose reduction of the drug.
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              Effect of polymer type on the dissolution profile of amorphous solid dispersions containing felodipine.

              Amorphous solid dispersions are used as a strategy to improve the bioavailability of poorly water-soluble compounds. When formulating with a polymer, it is important not only for the polymer to stabilize against crystallization in the solid state, but also to improve the dissolution profile through inhibiting crystallization from the supersaturated solution generated by dissolution of the amorphous material. In this study, the dissolution profiles of solid dispersions of felodipine formulated with poly(vinylpyrrolidone) (PVP), hydroxypropyl methylcellulose (HPMC) or hydroxypropyl methylcellulose acetate succinate (HPMCAS) were compared. In addition, concentration versus time profiles were evaluated for the supersaturated solutions of felodipine in the presence and absence of the polymers. HPMCAS was found to maintain the highest level of supersaturation for the greatest length of time for both the dissolution and solution crystallization experiments, whereas PVP was found to be the least effective crystallization inhibitor. All polymers appeared to reduce the crystal growth rates of felodipine at an equivalent supersaturation and this mechanism most likely contributes to the enhanced solution concentration values observed during dissolution of the amorphous solid dispersions.
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                Author and article information

                Journal
                Journal of Pharmaceutical Investigation
                Journal of Pharmaceutical Investigation
                Springer Science and Business Media LLC
                2093-5552
                2093-6214
                June 2013
                April 14 2013
                June 2013
                : 43
                : 3
                : 205-213
                Article
                10.1007/s40005-013-0067-2
                6c803994-1777-4f7f-8e7e-c182838f76d5
                © 2013
                History

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