Main Article Content

Abstract

Celecoxib (CLX) is a drug that has low solubility and high permeability and belongs to BCS class II. The low solubility of CLX results in the bioavailability of CLX being only 40%, so it is necessary to increase the dissolution using a solid dispersion (DP) technique. This study aims to determine the dissolution profile of CLX in DP with a carrier combination of HPMC and PEG 6000. DP CLX were prepared by solvent evaporation method using drug-HPMC-PEG 6000 ratios were (1:1:1), (1:1:2) and (1:2:1). Pure CLX, physical mixture (CF) at the same ratio and DP were tested for dissolution in tribasic sodium phosphate 0.04 M (pH 12) and 1% sodium lauryl sulfate (SLS). The data from the dissolution test in the form of Q45 and DE60 values were analyzed statistically using non-parametric test. Overall Q45 DP CLX value > 75% and significantly different from pure CLX and CF. DE60 CLX value in DP ratio (1:1:1) 59.13±0.44%; ratio (1:1:2) 60.77±0.09%; ratio (1:2:1) 60.47±0.42%. Solid dispersion with a combination of HPMC polymer and PEG 6000 was able to increase the dissolution of celecoxib compared to the physical mixture and pure celecoxib.

Keywords

celecoxib dissolution HPMC PEG 6000 solid dispersion

Article Details

Author Biography

Danang Novianto Wibowo, Fakultas Farmasi Universitas Wahid Hasyim

Farmasetika dan Teknologi Farmasi

References

  1. British Pharmacopoeia Assosiation, 2007, British Pharmacopoeia, The Stationery Office, London, 3, 1516.
  2. Costa, A. R. M., Flavia, S. M., Mirela, M. O. L.V., Bruno, A. R., Paula, C. P. B., Pedro, L. M., Amaral., Hernane, S. B., Andresa, Ap., dan Berreta, S., 2011, Quercetin-PVP K25 solid dispersions, Journal of Thermal Analysis and Calorimetry, 104:273–278.
  3. Depkes RI, 1995, Farmakope Indonesia Edisi IV, Departemen Kesehatan Republik Indonesia, Jakarta.
  4. Dhirendra, K., Lewis, S., Udupa, N., and Atin, K., 2009, Solid Dispersion: Review, manipal collage of pharmaceutical sciences, 22(2), pp. 234–246.
  5. Dixit, M., Ashwini, G. K., and Parthasarthi, K. K., 2011, Enhancing Solubility and Dissolution of Celecoxib by Spray Drying Using Pluronic F 127, Indian Journal of Pharmaceutical Education and Research, 45, 346-347.
  6. Dixit, R. P., and Negarsenker, M. S., 2007, in vitro and in vivo advantage of celecoxib surface solid dispersion and dosage form development, Indian Journal of Pharmaceutical Sciences, PP. 370–377.
  7. Food Drug and Administration, 2010, Dissolution Methods, dalam https://www.accessdata.fda.gov/scripts/cder/dissolution/dsp_SearchResults.cfm diakses pada 12 Agustus 2020.
  8. Gandjar, I. G. and Rohman, A., 2007, Kimia Farmasi Analisis. Yogyakarta: Pustaka Pelajar.
  9. Goldenberg, M. M., 1999, Celecoxib, a selective cyclooxygenase-2 inhibitor for the treatment of rheumatoid arthritis and osteoarthritis. Clinical therapeutics, 21 (9), 1497-1513.
  10. Janssens, S., Armas, H. N. D., Roberts, C. J., Mooter, G. V. D., 2007, Characterization of Ternary solid Dispersions of Itraconazole, PeG 6000, and HPMC 2910 E5. Journal Of Pharmaceutical Sciences, 97 (6), 2110-2120.
  11. Kemenkes RI, 2020, Farmakope Indonesia Edisi VI, Kementrian Kesehatan Republik Indonesia, Jakarta.
  12. Lee, J. K., Kim, M. J.,Yoon, H., Shim, C. R., Ko, H. A., Cho, S. A., Lee, D., and Khang, G., 2013, Enhanced dissolution rate of celecoxib using PVP and/or HPMC based solid dispersions prepared by spray drying method, Journal of Pharmaceutical Investigation, 43, 205-213.
  13. Motallae, S., Azade, T., and Alireza, H., 2018, Preparation and characterization of solid dispersions of celecoxib obtained by spray-drying ethanolic suspensions containing PVP-K30 or isomalt, Journal of Drug Delivery Science and Technology, 46, 188–196.
  14. Vasconcelos, T., Saemento, B., dan Costa, P., 2007, Solid Dispersions as Strategy to Improve Oral Bioavailability of Poor Water Soluble Drugs, Drug Discover Today, 12 (23-24), 1068-1075.
  15. Wibowo, D. N., Ikhsan, M. N., dan Kartalina, E., 2020, Studi Sistem Dispersi Padat Celecoxib dengan Polimer HPMC-PEG 6000 dalam Peningkatan Kelarutan Obat, Jurnal Ilmiah Cendekia Eksakta, 2528-5912.