Increased Solubility, Dissolution and Physicochemical Studies of Curcumin- Polyvinylpyrrolidone K-30 Solid Dispersions

Solid dispersions (SD) of curcuminpolyvinylpyrrolidone in the ratio of 1:2, 1:4, 1:5, 1:6, and 1:8 were prepared in an attempt to increase the solubility and dissolution. Solubility, dissolution, powder X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) of solid dispersions, physical mixtures (PM) and curcumin were evaluated. Both solubility and dissolution of curcumin solid dispersions were significantly greater than those observed for physical mixtures and intact curcumin. The powder X-ray diffractograms indicated that the amorphous curcumin was obtained from all solid dispersions. It was found that the optimum weight ratio for curcumin:PVP K-30 is 1:6. The 1:6 solid dispersion still in the amorphous from after storage at ambient temperature for 2 years and the dissolution profile did not significantly different from freshly prepared.

Authors:

• Nattha Kaewnopparat
• Sanae Kaewnopparat
• Amaravadee Jangwang
• Daungkhae Maneenaun
• Thitima Chuchome
• Pharkphoom Panichayupakaranant

Keywords:

• Curcumin
• polyvinylpyrrolidone K-30
• solid dispersion
• dissolution
• physicochemical.

References:

[1] H.P.T. Ammon, and M.A. Wahl, "Pharmacology of curcumin," Planta.
Med., vol. 57, pp. 1-7, 1991.
[2] V. Ravindranath, and N. Chandrasekhara, "Absorption and tissue
distribution of curcumin in rats," Toxicology, vol. 16(3), pp. 259-265,
1980.
[3] S. Okonogi, T. Oguchi, E. Yonemochi, S. Puttipipatkhachorn and K.
Yamamoto, "Improved dissolution of ofloxacin via solid dispersion,"
Int. J. Pharm., vol. 156, pp.175-180, 1997.
[4] M. Franco, G. Trapani, A. Latrofa, C. Tullio, M.R. Provenzano, M.
Serra, M. Muggironi, et al., "Dissolution properties and anticonvulsant
activity of phenytoin-polyethylene glycol 6000 and
polyvinylpyrrolidone K-30 solid dispersions," Int. J. Pharm., vol. 225,
pp. 63-73, 2001.
[5] R.N. Pan, J.H. Chen, and R.R. Chen, "Enhancement of dissolution and
bioavailability of piroxicam in solid dispersion systems," Drug. Dev.
Ind. Pharm., vol 26(9), pp. 989-994, 2000.
[6] N. Kohri, Y. Yamayoshi, H. Xin, K. Iseki, N. Sato, S. Todo, and
K. Miyazaki, "Improving the Oral Bioavailability of Albendazole in
Rabbits by the Solid dispersion Technique," J. Pharm. Pharmacol., vol.
51(2), pp. 159-164, 1999.
[7] W.L. Chiou, and S. Riegleman, "Pharmaceutical Applications of Solid
Dispersions Dispersion Systems," J. Pharm. Sci., vol 60(9), pp. 1281-
1302, 1971.
[8] A.T.M. Serajuddin, "Solid dispersion of poorly water-soluble drugs:
early promises, subsequent problems and recent breakthroughs," J.
Pharm. Sci., vol. 88, pp. 1058-1066, 1999.
[9] M.T. Marin, M.V. Margarit, and G.E. Salcedo, "Characterization and
solubility study of solid dispersions of flunarizine and
polyvinylpyrrolidone," II Farmaco., vol. 57, pp. 723-727, 2002.
[10] V. Tantishaiyakul, N. Kaewnopparat, and S. Ingkatawornwong,
"Properties of solid dispersions of piroxicam in polyvinylpyrrolidone,"
Int. J. Pharm., 181, pp. 143-151, 1999.
[11] H.H. Tonnesen, "Solubility, chemical and photochemical stability of
curcumin in surfactant solutions," Pharmazie, vol. 57(12), pp. 820-824,
2002.
[12] J.M. Gines, M.J. Arias, M.A. Holgado, M.F. Arevalo, and A.M.
Rabasco, "Dissolution rate study of triamterene-urea solid dispersions,"
Drug Dev. Ind. Pharm., vol. 20, pp. 2729-2740, 1994.
[13] H. Sekikawa, M. Nakano, and T. Arita, "Inhibitory effect of
polyvinylpyrrolidone on the crystallization of drugs," Chem. Pharm.
Bull., vol. 6, pp. 118-126, 1978.
[14] V. Tantishaiyakul, N. Kaewnopparat, and S. Ingkatawornwong,
"Properties of solid dispersions of piroxicam in polyvinylpyrrolidone
K-30," Int. J. Pharm., vol. 143, pp. 59-66, 1996.
[15] Mooter, G., Wuyts, M., Blaton, N., Busson, R., Grobet, P., Augustijns,
P., Kinget, R., "Physical stabilisation of amorphous ketoconazole in
solid dispersions with polyvinylpyrrolidone K 25,". Eur. J. Pharm. Sci.
vol. 12, pp. 261-269, 2001.
[16] L.P. Ruan, B.Y. Yu, G.M. Fu, and D. Zhu, "Improving the solubility of
ampelopsin by solid dispersions and inclusion complexes," J.
Pharm. Biomed. Anal., vol. 38(3), pp. 457-464, 2005.
[17] G.P. Bettinetti, P. Mura, F. Giordano, and M. Setti, "Thermal behavior
and physicochemical properties of naproxen in mixtures with
polyvinylpyrrolidone," Thermochimica. Acta., vol. 199, pp. 165-171,
1992.
[18] M. Moneghini, A. Carcano, G. Zingone, B. Perissutti, "Studies in
Dissolution Enhancement of Atenolol: Part I," Int. J. Pharm., vol. 175,
pp. 177-183, 1998.
[19] J.L. Ford, "The current status of solid dispersions," Pharm. Acta. Helv.,
vol. 61(3), pp. 69-88, 1986.
[20] J. Akbuga, A. Gursoy, and E. Kendi, "The preparation and stability of
fast release furosemide-PVP solid dispersion," Drug Dev. Ind. Pharm.,
vol. 14, pp. 1439-1464, 1988.