Impact of polymer type on bioperformance and physical stability of hot melt extruded formulations of a poorly water soluble drug

International Journal of Pharmaceutics

Volumn 505, Issue 1-2, 2016, Pages 107-114

  Mitra, Amitava ^a   Li, Li ^a   Marsac, Patrick ^a,b   Marks, Brian ^a   Liu, Zhen ^a   Brown, Chad ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b University of Kentucky   (United States)

Author keywords

Anti nucleation; Dissolution; Hot melt extrusion; Pharmacokinetics; Solid dispersion; Stability

Indexed keywords

DRUG; HYDROXYPROPYLMETHYLCELLULOSE; POLYMER; DRUG CARRIER; HYDROXYPROPYLMETHYLCELLULOSE ACETATE SUCCINATE; METHYLCELLULOSE; POLY(VINYLPYRROLIDONE-CO-VINYL-ACETATE); PYRROLIDINE DERIVATIVE; VINYL DERIVATIVE; WATER;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; DIFFERENTIAL SCANNING CALORIMETRY; DISPERSION; DOG; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG SOLUBILITY; DRUG STABILITY; LIQUID CHROMATOGRAPHY; MALE; MAXIMUM PLASMA CONCENTRATION; MOISTURE; NONHUMAN; PRIORITY JOURNAL; TANDEM MASS SPECTROMETRY; TEMPERATURE; TIME TO MAXIMUM PLASMA CONCENTRATION; X RAY DIFFRACTION; ANALOGS AND DERIVATIVES; ANIMAL; BIOAVAILABILITY; CHEMISTRY; COMPARATIVE STUDY; MEDICINAL CHEMISTRY; METABOLISM; PROCEDURES; SOLUBILITY;

ANIMALS; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; DOGS; DRUG CARRIERS; DRUG COMPOUNDING; DRUG STABILITY; MALE; METHYLCELLULOSE; PHARMACEUTICAL PREPARATIONS; POLYMERS; PYRROLIDINES; SOLUBILITY; VINYL COMPOUNDS; WATER;

EID: 84962886767     PISSN: 03785173     EISSN: 18733476     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2016.03.036     Document Type: Article

References (29)

1. P. Augustijns, and M.E. Brewster Supersaturating drug delivery systems: fast is not necessarily good enough J. Pharm. Sci. 101 2012 7 9
2. J. Brouwers, M.E. Brewster, and P. Augustijns Supersaturating drug delivery systems: the answer to solubility-limited oral bioavailability? J. Pharm. Sci. 98 2009 2549 2572
3. M.M. Crowley, F. Zhang, M.A. Repka, S. Thumma, S.B. Upadhye, S.K. Battu, J.W. McGinity, and C. Martin Pharmaceutical applications of hot-melt extrusion: part I Drug Dev. Ind. Pharm. 33 2007 909 926
4. W. Curatolo, J.A. Nightingale, and S.M. Herbig Utility of hydroxypropyl methyl cellulose acetate succinate (HPMCAS) for initiation and maintenance of drug supersaturation in the GI milieu Pharm. Res. 26 2009 1419 1431
5. D.T. Friesen, R. Shanker, M. Crew, D.T. Smithey, W.J. Curatolo, and J.A. Nightingale Hydroxypropyl methylcellulose acetate succinate-based spray-dried dispersions: an overview Mol. Pharm. 5 2008 1003 1019
6. H.R. Guzmán, M. Tawa, Z. Zhang, P. Ratanabanangkoon, P. Shaw, C.R. Gardner, H. Chen, J.P. Moreau, O. Almarsson, and J.F. Remenar Combined use of crystalline salt forms and precipitation inhibitors to improve oral absorption of celecoxib from solid oral formulations J. Pharm. Sci. 96 2007 2686 2702
7. N. Hasiwa, J. Bailey, P. Clausing, M. Daneshian, M. Eileraas, S. Farkas, I. Gyertyán, R. Hubrecht, W. Kobel, G. Krummenacher, M. Leist, H. Lohi, A. Miklósi, F. Ohl, K. Olejniczak, G. Schmitt, P. Sinnett-Smith, D. Smith, K. Wagner, J.D. Yager, J. Zurlo, and T. Hartung Critical evaluation of the use of dogs in biomedical research and testing in Europe ALTEX 28 2011 326 340
8. H. He, R. Yang, and X. Tang In vitro and in vivo evaluation of fenofibrate solid dispersion prepared by hot melt extrusion Drug Dev. Ind. Pharm. 36 2010 681 687
9. G.A. Ilevbare, H. Liu, K.J. Edgar, and L.S. Taylor Understanding polymer properties important for crystal growth inhibition impact of chemically diverse polymers on solution crystal growth of ritonavir Cryst. Growth Des. 12 2012 3133 3143
10. G.A. Ilevbare, H. Liu, K.J. Edgar, and L.S. Taylor Impact of polymers on crystal growth rate of structurally diverse compounds from aqueous solution Mol. Pharm. 10 2013 2381 2393
11. S.W. Jang, and M.J. Kang Improved oral absorption and chemical stability of everolimus via preparation of solid dispersion using solvent wetting technique Int. J. Pharm. 473 2014 187 193
12. T. Kararli Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals Biopharm. Drug Dispos. 16 1995 351 380
13. H. Konno, T. Handa, D.E. Alonzo, and L.S. Taylor Effect of polymer type on the dissolution profile of amorphous solid dispersions containing felodipine Eur. J. Pharm. Biopharm. 70 2008 493 499
14. J.P. Lakshman, Y. Cao, J. Kowalski, and A.T. Serajuddin Application of melt extrusion in the development of a physically and chemically stable high-energy amorphous solid dispersion of a poorly water-soluble drug Mol. Pharm. 5 2008 994 1002
15. B. Lang, J.W. McGinity, and R.O. Williams 3rd Hot-melt extrusion-basic principles and pharmaceutical applications Drug Dev. Ind. Pharm. 40 2014 1133 1155
16. D.A. Miller, J.M. Keen, C. Brough, D.J. Ellenberger, M. Cisneros, R.O. Williams 3rd, and J.W. McGinity Bioavailability enhancement of a BCS IV compound via an amorphous combination product containing ritonavir J. Pharm. Pharmacol. 2015 1 14
17. A. Newman, G. Knipp, and G. Zografi Assessing the performance of amorphous solid dispersion J. Pharm. Sci. 101 2012 1355 1377
18. D.M. Oh, R.L. Curl, and G.L. Amidon Estimating the fraction dose absorbed from suspensions of poorly soluble compounds in humans: a mathematical model Pharm. Res. 10 1993 264 270
19. A. Paudel, Z.A. Worku, J. Meeus, S. Guns, and G. Van den Mooter Manufacturing of solid dispersions of poorly water soluble drugs by spray drying: formulation and process considerations Int. J. Pharm. 453 2013 253 284
20. M.A. Repka, S.K. Battu, S.B. Upadhye, S. Thumma, M.M. Crowley, F. Zhang, C. Martin, and J.W. McGinity Pharmaceutical applications of hot-melt extrusion: Part II Drug Dev. Ind. Pharm. 33 2007 1043 1057
21. A.C. Rumondor, L.A. Stanford, and L.S. Taylor Effects of polymer type and storage relative humidity on the kinetics of felodipine crystallization from amorphous solid dispersions Pharm. Res. 26 2009 2599 2606
22. A.L. Sarode, P. Wang, S. Obara, and D.R. Worthen Supersaturation, nucleation, and crystal growth during single and biphasic dissolution of amorphous solid dispersions: polymer effects and implications for oral bioavailability enhancement of poorly water soluble drugs Eur. J. Pharm. Biopharm. 86 2014 351 360
23. A.T. Serajuddin Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs J. Pharm. Sci. 88 1999 1058 1166
24. F. Tajarobi, A. Larsson, H. Matic, and S. Abrahmsén-Alami The influence of crystallization inhibition of HPMC and HPMCAS on model substance dissolution and release in swellable matrix tablets Eur. J. Pharm. Biopharm. 78 2011 125 133
25. J.M. Ting, T.S. Navale, S.D. Jones, F.S. Bates, and T.M. Reineke Deconstructing HPMCAS: excipient design to tailor polymer-drug interactions for oral drug delivery ACS Biomater. Sci. Eng. 1 2015 978 990
26. K. Ueda, K. Higashi, K. Yamamoto, and K. Moribe Inhibitory effect of hydroxypropyl methylcellulose acetate succinate on drug recrystallization from a supersaturated solution assessed using nuclear magnetic resonance measurements Mol. Pharm. 10 2013 3801 3811
27. K. Ueda, K. Higashi, K. Yamamoto, and K. Moribe The effect of HPMCAS functional groups on drug crystallization from the supersaturated state and dissolution improvement Int. J. Pharm. 464 2014 205 213
28. L. Yin, and M.A. Hillmyer Preparation and performance of hydroxypropyl methylcellulose esters of substituted succinates for in vitro supersaturation of a crystalline hydrophobic drug Mol. Pharm. 11 2014 175 185
29. X. Zheng, R. Yang, Y. Zhang, Z. Wang, X. Tang, and L. Zheng Part II: bioavailability in beagle dogs of nimodipine solid dispersions prepared by hot-melt extrusion Drug Dev. Ind. Pharm. 33 2007 783 789