Improved oral absorption and chemical stability of everolimus via preparation of solid dispersion using solvent wetting technique

International Journal of Pharmaceutics

Volumn 473, Issue 1-2, 2014, Pages 187-193

  Jang, Sun Woo ^a   Kang, Myung Joo ^b  

^a Dong A Pharmaceutical Company   (South Korea)

^b Dankook University   (South Korea)

Author keywords

Everolimus; Oral absorption; Solid dispersion; Solvent wetting technique; Stability

Indexed keywords

ALCOHOL; EVEROLIMUS; HYDROXYPROPYLMETHYLCELLULOSE; DICHLOROMETHANE; IMMUNOSUPPRESSIVE AGENT; RAPAMYCIN; SOLVENT; TABLET;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; BEAGLE; BLOOD SAMPLING; DISPERSION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG RELEASE; DRUG SOLUBILITY; DRUG SOLUTION; DRUG STABILITY; DRUG SYNTHESIS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; IN VIVO STUDY; LIQUID CHROMATOGRAPHY; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PARTICLE SIZE; PHYSICAL CHEMISTRY; POWDER; PRECIPITATION; PRIORITY JOURNAL; SCANNING ELECTRON MICROSCOPY; SOLID STATE; SOLVENT WETTING TECHNIQUE; TABLET FORMULATION; TANDEM MASS SPECTROMETRY; TIME TO MAXIMUM PLASMA CONCENTRATION; WETTABILITY; X RAY POWDER DIFFRACTION; ANALOGS AND DERIVATIVES; ANIMAL; BIOAVAILABILITY; BLOOD; CHEMISTRY; DOG; INTESTINE ABSORPTION; MEDICINAL CHEMISTRY; ORAL DRUG ADMINISTRATION; POWDER DIFFRACTION; TABLET; X RAY DIFFRACTION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; DOGS; DRUG STABILITY; ETHANOL; HYPROMELLOSE DERIVATIVES; IMMUNOSUPPRESSIVE AGENTS; INTESTINAL ABSORPTION; MALE; METHYLENE CHLORIDE; MICROSCOPY, ELECTRON, SCANNING; PARTICLE SIZE; POWDER DIFFRACTION; SIROLIMUS; SOLVENTS; TABLETS; X-RAY DIFFRACTION;

EID: 84904309126     PISSN: 03785173     EISSN: 18733476     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2014.06.006     Document Type: Article

References (16)

1. D.Q.M. Craig The mechanism of drug release from solid dispersion in water-soluble polymers Int. J. Pharm. 231 2002 131 144 (Pubitemid 34033673)
2. EMEA, 2009. CHMP assessment report for Afinitor.
3. J.L. Ford The current status of solid dispersions Pharm. Acta Helv. 61 1986 69 88 (Pubitemid 16134014)
4. Guitard, P., Haeberlin, B., Link, R., Richter, F., 1997. Pharmaceutical compositions. WO 1997/03654.
5. ICH Harmonized tripartite guideline Impurities: guideline for residual solvents The Fourth International Conference on Harmonization 17 1997
6. E.J. Kim, M.K. Chun, J.S. Jang, I.H. Lee, K.R. Lee, and H.K. Choi Preparation of a solid dispersion of felodipine using a solvent wetting method Eur. J. Pharm. Biopharm. 64 2006 200 205
7. M. Kobayashi, N. Sada, M. Sugawara, K. Iseki, and K. Miyazaki Development of a new system for prediction of drug absorption that takes into account drug dissolution and pH change in the gastrointestinal tract Int. J. Pharm. 221 2001 87 94 (Pubitemid 32524038)
8. N. Kohri, Y. Yamayoshi, H. Xin, K. Iseki, N. Sato, S. Todo, and K. Miyazaki Improving the oral bioavailability of albendazol in rabbits by the solid dispersion technique J. Pharm. Pharmacol. 51 1999 159 164 (Pubitemid 29131308)
9. C. Leuner, and J. Dressman Improving drug solubility for oral delivery using solid dispersions Eur. J. Pharm. Biopharm. 50 2000 47 60 (Pubitemid 30326688)
10. R.J. Motzer, B. Escudier, S. Oudard, T.E. Hutson, C. Porta, S. Bracarda, V. Grünwald, J.A. Thompson, R.A. Figlin, N. Hollaender, G. Urbanowitz, W.J. Berg, A. Kay, D. Lebwohl, and A. Ravaud Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial Lancet 372 2008 449 456
11. B.C. Sallustio, B.D. Noll, and R.G. Morris Comparison of blood sirolimus, tacrolimus and everolimus concentrations measured by LC-MS/MS, HPLC-UV and immunoassay methods Clin. Biochem. 44 2011 231 236
12. L. Shargel Applied Biopharmaceutics and Pharmacokinetics 2nd ed. 1993 Appleton & Lange Norwalk, CT
13. J. Swarbrick Encyclopedia of Pharmaceutical Technology vol. III 1990 Marcel Dekker New York, NY
14. K. Yamashita, T. Nakate, K. Okimoto, A. Ohike, Y. Tokunaga, R. Ibuki, K. Higaki, and T. Kimura Establishment of new preparation method for solid dispersion formulation of tacrolimus Int. J. Pharm. 267 2003 79 91 (Pubitemid 37352952)
15. R. Yuan, A. Kay, W.J. Berg, and D. Lebwohl Targeting tumorigenesis: development and use of mTOR inhibitors in cancer therapy J. Hematol. Oncol. 2 2009 45 54
16. G.M. Williams, C.X. Wang, and M.J. Iatropoulos Toxicity studies of butylated hydroxyanisole and butylated hydroxytoluene. II. Chronic feeding studies Food Chem. Toxicol. 28 1990 799 806