Solid dispersions naproxen

Hirasawa and coworkers prepared a naproxen solid dispersion by melting, followed by rapid cooling with liquid nitrogen using lactose as a carrier. The dissolution studies of naproxen indicated that the dissolution rate was markedly increased in solid dispersions compared with physical mixtures and pure drugs. 

Hirasawa, N. Danjo, K. Haruna, M. Otsuka, A. Physio-chemical characterization and drug release studies of naproxen solid dispersions using lactose as a carrier. Chem. Pharm. Bull. 1998, 46 (6), 1027-1030. 

Research was undertaken to develop a controlled release tablet of naproxen using ethylcellulose and both methods of wet granulation and solid dispersion were compared for effectiveness. Naproxen level was kept constant at 16% while ethylcellulose content was varied from 6% to 28% in the formulations. While both methods were successful at producing formulations with drug release profiles of at least 12 hours, the amount of ethylcellulose required to prepare such formulations was 33% less using the solid dispersion method. While none of the formulations released 100% of the drug, a cumulative 88% of naproxen was released from the solid dispersion formulation, compared with 84% from the wet granulation formulation (50). 

Iqbal Z, Babar A. Ashraf M. Controlled-release naproxen using micronized ethyl cellulose by wet-granulation and solid-dispersion method. Drug Dev Ind Pharm 2002 28... 

Mura, R Faucci, M.T. Manderioli, A. Bramanti, G. Parrini, P. Thermal behavior and dissolution properties of naproxen from binary and ternary solid dispersion. Drug Dev. Ind. Pharm. 1999, 25 (3), 257-264. 

II. Theoretical demonstration. J Non-Cryst Solids 320(l-3) 9-20 Ayenew Z, Paudel A, Van den Mooter G (2012) Can compression induce demixing in amorphous solid dispersions A case study of naproxen-PVP K25. Eur J Pharm Biopharm 81(1) 207-213 Babu NJ, Nangia A (2011) Solubility advantage of amorphous dmgs and pharmaceutical cocrystals. Cryst Growth Design 11(7) 2662-2679... 

Paudel A, Mooter G (2012) Influence of solvent composition on the miscibility and physical stability of naproxen/PVP K 25 solid dispersions prepared by cosolvent spray-drying. Pharm Res 29 251-270... 

Paudel A, Nies E, Van den Mooter G (2012) Relating hydrogen-bonding interactions with the phase behavior of naproxen/PVP K 25 solid dispersions evaluation of solution-cast and quench-cooled films. Mol Pharm 9 3301-3317... 

Paudel A, Loyson Y, Van den Mooter G (2013b) An investigation into the effect of spray drying temperature and atomizing conditions on miscibility, physical stability, and performance of naproxen-PVP K 25 solid dispersions. J Pharm Sci 102 1249-1267 Pavia DL, Lampman GM, Kriz GS (2001) Infrared spectroscopy in Introduction to spectroscopy a guide for students of organic chemistry, 3rd edn. WB Saunders Co., Philadelphia... 

Yoshihashi Y, lijima H, Yonemochi E, Terada K (2006) Estimation of physical stability of amorphous solid dispersion using differential scamiing calorimetry. J Therm Anal Caloiim 85 689-692 Yoshihashi Y, Yonemochi E, Maeda Y, Terada K (2010) Prediction of the induction period of crystallization of naproxen in solid dispersion using differential scanning calorimetry. J Therm Anal Calorim 99 15-19... 

Mura P, Maestrelli F, Cirri M (2003) Ternary systems of naproxen with hydroxypropyl-p-cyclodextrin and aminoacids. Int J Pharm 260 293-302 Mura P, Bettinetti GP, Cirri M, Maestrelli F, Sorrenti M, Catenacci L (2(X)5) Solid-state chtirac-terization and dissolution properties of Naproxen-Arginine-Hydroxypropyl-[beta]-cyclodextrin ternary system. Eur J Pharm Biopharm 59 99-106 Newman A, Knipp G, Zografi G (2012) Assessing the performance of amorphous solid dispersions. J Pharm Sci 101 1355-1377... 

The results of this study illustrate how much more rapidly a poorly water-soluble drug can be orally absorbed when formulated in nanoparticulate form instead of conventional micronized form. Furthermore, the closely similar pharmacokinetic profiles of the two nanoparticulate test articles confirm that the benefits of small particles (high surface area and rapid dissolution) can be realized from solid products as well as liquid dispersions. The application of fine particle technology to other poorly water-soluble analgesics such as naproxen and ketoprofen can be expected to produce qualitatively similar results. 

---