Process optimization and characterization of poloxamer solid dispersions of a poorly water-soluble drug |
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Authors: | Tejal J Shah Avani F Amin Jolly R Parikh Rajesh H Parikh |
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Institution: | (1) Institute of Pharmacy, Nirma University of Science & Technology, Ahmedabad, Gujarat, India;(2) A. R. College of Pharmacy & G. H. Patel Institute of Pharmacy, Vallabh Vidyanagar, Gujarat, India;(3) Principal, Ramanbhai Patel College of Pharmacy, Education Campus, 388 421 Changa, Ta: Petlad, Dist: Anand, Gujarat, India |
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Abstract: | The objective of the present investigation was to improve the dissolution rate of Rofecoxib (RXB), a poorly water-soluble
drug by solid dispersion technique using a water-soluble carrier, Poloxamer 188 (PXM). The melting method was used to prepare
solid dispersions. A 32 full factorial design approach was used for optimization wherein the temperature to which the melt-drug mixture cooled (X
1) and the drug-to-polymer ratio (X
2) were selected as independent variables and the time required for 90% drug dissolution (t90) was selected as the dependent variable. Multiple linear regression analysis revealed that for obtaining higher dissolution
of RXB from PXM solid dispersions, a low level ofX
1 and a high level ofX
2 were suitable. The differential scanning calorimetry and x-ray diffraction studies demonstrated that enhanced dissolution
of RXB from solid dispersion might be due to a decrease in the crystallinity of RXB and PXM and dissolution of RXB in molten
PXM during solid dispersion preparation. In conclusion, dissolution enhancement of RXB was obtained by preparing its solid
dispersions in PXM using melting technique. The use of a factorial design approach helped in identifying the critical factors
in the preparation and formulation of solid dispersion.
Published: April 13, 2007 |
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Keywords: | Solid dispersion factorial design poloxamer poorly water-soluble drug |
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