Assessing the performance of amorphous solid dispersions

Journal of Pharmaceutical Sciences

Volumn 101, Issue 4, 2012, Pages 1355-1377

  Newman, Ann ^a   Knipp, Gregory ^b   Zografi, George ^c  

^a Seventh Street Development Group   (United States)

^b PURDUE UNIVERSITY   (United States)

^c UNIVERSITY OF WISCONSIN MADISON   (United States)

Author keywords

Absorption; Amorphous; Bioavailability; Dissolution; In vitro in vivo correlation (IVIVC); Polymers; Solid dispersion; Solid dosage form; Stabilization

Indexed keywords

5 [5 (4,6 DIPHENYL 2 PYRIDYLOXY) 1,1 DIMETHYLPENTYL]TETRAZOLE; ALBENDAZOLE; CYCLOSPORIN A; ESOMEPRAZOLE; EUDRAGIT; FENOFIBRATE; FUROSEMIDE; GELUCIRE; HALOFANTRINE; INDOMETACIN; ITRACONAZOLE; KETOCONAZOLE; LONIDAMINE; LOPINAVIR; MACROGOL; MACROGOL STEARATE; N [4 [6 [4 (TRIFLUOROMETHYL)PHENYL] 4 PYRIMIDINYLOXY]BENZOTHIAZOL 2 YL]ACETAMIDE; NIFEDIPINE; NIMODIPINE; NITRENDIPINE; PHOSPHATIDYLCHOLINE; PHOSPHOLIPID; POLYMER; POLYSORBATE 80; PRANLUKAST; RITONAVIR; SORBITAN LAURATE; TACROLIMUS; TOLBUTAMIDE; UNINDEXED DRUG;

AMORPHOUS SOLID DISPERSION; CULTURE MEDIUM; DISPERSION; DRUG ABSORPTION; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; DRUG SOLUBILITY; HUMAN; IN VITRO STUDY; IN VIVO STUDY; NONHUMAN; NOTE; PARTICLE SIZE; PH; STOMACH JUICE;

EID: 84857506982     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23031     Document Type: Note

References (138)

1. Serrajuddin ATM. 1999. Solid dispersions of poorly water-soluble drugs: Early promises, subsequent problems, and recent breakthroughs. J Pharm Sci 88:1058-1066.
2. Brouwers J, Brewster ME, Augustijns P. 2009. Supersaturating drug delivery systems: Answer to solubility-limited oral bioavailability. J Pharm Sci 98:2549-2572.
3. Bhugra C, Pikal MJ. 2008. Role of thermodynamic, molecular and kinetic factors in crystallization from the amorphous state. J Pharm Sci 97:1329-1349.
4. Alonzo DE, Zhang GGZ, Zhou D, Gao Y, Taylor LS. 2010. Understanding behavior of amorphous pharmaceutical systems during dissolution. Pharm Res 27:608-618.
5. Padden BE, Mill JM, Robbins T, Zocharski PD, Prasad L, Spence JK, LaFountaine J. 2011. Amorphous solid dispersions as enabling formulations for discovery and early development. Amer Pharm Rev 1:66-73.
6. Dobry DE, Settell DM, Baumann JM, Ray RJ, Graham LJ, Beyerinck RA. 2009. A model-based methodology for spray-drying process development. J Pharm Innov 4:133-142.
7. Breitenbach J. 2002. Melt extrusion: From process to drug delivery technology. Eur J Pharm Biopharm 54:107-117.
8. Shamblin SL, Taylor LS, Zografi G. 1998. Mixing behavior of colyophilized binary systems. J Pharm Sci 87:694-701.
9. Newman A, Engers D, Bates S, Ivanisevic I, Kelly RC, Zografi G. 2008. Characterization of amorphous API-polymer mixtures using X-ray powder diffraction. J Pharm Sci 97:4840-4856.
10. 1relaxation measurements. Mol Pharm 7:1667-1691.
11. Ta J, Sun Y, Zhang GGZ, Yu L. 2009. Solubility of small molecule crystals in polymers: d-Mannitol in PVP, indomethacin in PVP/VA, and nifedipine in PVP/VA. Pharm Res 26:855-864.
12. Sun Y, Tao Y, Zhang GGZ, Yu L. 2010. Solubilities of crystalline drugs in polymers: An improved analytical method and comparisons of solubilities of indomethacin and nifedipine in PVP, PVP/VA and PVAc. J Pharm Sci 99:4023-4031.
13. Matsumoto T, Zografi G. 1999. Physical properties of solid molecular dispersions of indomethacin with poly(vinyl pyrrolidone) and poly(vinyl pyrrollidone-co-acetate) in relation to indomethacin crystallization. Pharm Res 16:1722-1728.
14. Taylor LS, Zografi G. 1997. Spectroscopic characterization of interactions between PVP and indomethacin in amorphous molecular dispersions. Pharm Res 14:1691-1698.
15. Hancock BC, Shamblin S, Zografi G. 1995. Molecular mobility of amorphous pharmaceutical solids below their glass transition temperature. Pharm Res 12:799-806.
16. Friesen DT, Shanker R, Crew M, Smithey DT, Curatolo WJ, Nightingale JAS. 2008. Hydroxypropyl methylcellulose acetate succinate-based spray-dried dispersions: An overview. Mol Pharm 5:1003-1019.
17. Curatolo W, Nightingale JA, Herbig SM. 2009. Utility of hydroxypropylmethylcellulose acetate succinate (HPMCAS) for initiation and maintenance of drug supersaturation in the GI milieu. Pharm Res 26:1419-1431.
18. Rowland M, Towser TN. 1995. Clinical pharmacokinetics: Concepts and applications. 3rd Ed. Philadephia, Pennsylvania: Lippincott Williams & Wilkins, pp 2-6, 57-60, 95, and 99.
19. Elmquist WF. 2005. Targeted bioavailability: A fresh look at pharmacokinetic and pharmacodynamic issues in drug delivery. In Drug delivery: Principles and practices; Wang B, Siahaan T, Soltero R, Eds. Hoboken: John Wiley and Sons, Inc., pp 73-82.
20. Kalaiselvan R, Mohanta GP, Madhusadan S, Manna PK, Manavaian R. 2007. Enhancement of bioavailability and antihelmintic efficacy of albendazole by solid dispersions and cyclodextrin complexation techniques. Pharmazie 62:604-607.
21. Kalaiselvan R, Mohanta GP, Manavaian R. 2006. The inhibition of albendazole solid molecular dispersions. Pharmazie 61:618-624.
22. Kohri N, Yamayoshi Y, Xin H, Iseki K, Sato N, Todo S, Miyazaki K. 1999. Improving the oral bioavailability of albendazole in rabbits by the solid dispersion technique. J Pharm Pharmacol 51:159-164.
23. Kennedy M, Hu J, Ga P, Li L, Ali-Reynolds A, Chai B, Gupta V, Ma C, Mahajan N, Akrami A, Surapaneni S. 2008. Enhanced bioavailability of a poorly soluble VR1 antagonsit using an amorphous solid dispersion approach: A case study. Mol Pharm 5:981-993.
24. Joshi HN, Tejwani W, Jemal M, Bathala MS, Varia SA, Serajuddin ATM. 2004. Bioavailability enhancement of a poorly water soluble drug by solid dispersion in a polyetyleneglycol-polysorbate 80 mixture. Int J Pharm 269:251-258.
25. Lakshman JP, Cao Y, Kowalski J, Serajuddin ATM. 2008. 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 5:994-1002.
26. Liu C, Wu J, Shi B, Zhang Y, Gao T, Pei Y. 2006. Enhancing the bioavailability of cyclosporine A using solid dispersion containing polyethylene (40) stearate. Drug Dev Ind Pharm 32:115-123.
27. Kushida I, Ichikawa M, Asakawa N. 2002. Improvement of dissolution and oral absorption of WR-34122, a poorly water soluble dual 5-lipoxygenase/cyclooxygenase inhibitor with anti-inflammatory activity by preparing solid dispersion. J Pharm Sci 91:258-266.
28. Xie Y, Xie P, Song X, Tang X, Song H. 2008. Preparation of esomeprazole zinc solid dispersion and study on its pharmacokinetics. Int J Pharm 360:53-57.
29. He H, Yang R, Tang X. 2010. In vitro and in vivo evaluation of fenofibrate solid dispersion prepared by hot-melt extrusion. Drug Dev Ind Pharm 36:681-687.
30. Doherty C, York P. 1998. The in vitro pH-dissolution dependence and in vivo bioavailability of frusemide-PVP solid dispersions. J Pharm Pharmacol 41:73-78.
31. Doherty C, York P. Mechanisms of dissolution of frusemide/PVP solid dispersions. Int J Pharm 34:197-205.
32. Doherty C, York P. Accelerated stability of an X-ray amorphous frusemide-polyvinylpyrrolidone solid dispersion. Drug Dev Ind Pharm 15:1969-1987.
33. Khoo S-M, Porter CJH, Charman WN. 2000. The formulation of halofantrine as either non-solubilising PEG 6000 or solubilising lipid based solid dispersions: Physical stability and absolute bioavailability assessment. Int J Pharm 205:65-78.
34. Chokshi RJ, Zia H, Sandhu HK, Shah NH, Malick WA. 2007. Improving the dissolution rate of poorly water soluble drug by solid dispersion and solid solution-Pros and cons. Drug Del 14:33-45.
35. Chowdary KPR, Babu KVVS. 1994. Dissolution, bioavailability and ulcerogenic studies on solid dispersions of indomethacin in water soluble cellulose polymers. Drug Dev Ind Pharm 20:799-813.
36. Ohnishi N, Yokoyama T, Umeda T, Kiyohara Y, Kuroda T, Kita Y, Kuroda K. 1986. Preparation of sustained-release suppositories of indomethacin using a solid dispersion system and evaluation of bioavailability in rabbits. Chem Pharm Bull 34:2999-2304.
37. Ohnishi N, Kiyohara Y, Kita Y, Kuroda K, Yokoyama T. 1987. Effect of the molecular weight of polyethylene glycol on the bioavailability of indomethacin in sustained-release suppositories prepared with solid dispersions. Chem Pharm Bull 35:3511-3515.
38. DiNunzio JC, Brough C, Miller DA, Williams RO, McGinity JW. 2010. Fusion processing of itraconazole solid dispersions by KinetiSol dispersing: A comparative study to hot melt extrusion. J Pharm Sci 99:1239-1253.
39. DiNunzio JC, Miller DA, Yang W, McGinity JW, Williams RO. 2008. Amorphous compositions using concentration enhancing polymers for improved bioavailability of itraconazole. Mol Pharm 5:968-980.
40. Engers D, Teng J, Jimenez-Novoa J, Gent P, Hossack S, Campbell C, Thomson J, Ivanisevic I, Templeton A, Byrn S, Newman A. 2010. A solid-state approach to enable early development compounds: Selection and animal bioavailability studies of an itraconazole amorphous solid dispersion. J Pharm Sci 99:3901-3922.
41. Kapsi SG, Ayres JW. 2001. Processing factors in development of solid solution formulation of itraconazole for enhancement of drug dissolution and bioavailability. Int J Pharm 229:193-203.
42. Lee SL, Nam K, Kim MS, Jun SW, Park J-S, Woo JS, Hwang S-J. 2005. Preparation and characterization of solid dispersions of itraconazole by using aerosol solvent extraction system for improvement in drug solubility and bioavailability. Arch Pharm Res 28:866-874.
43. thAnnual Meeting, July 20-25, Seoul, South Korea.
44. Six K, Daems T, de Hoon J, Van Hecken A, Depre M, Bouche M-P, Prinsen P, Verreck G, Peeters J, Brewster ME, Van den Mooter G. 2005. Clinical study of solid dispersions of itraconazole prepared by hot-stage extrusion. Eur J Pharm Sci 24:179-186.
45. Six K, Leuner C, Dressman J, Verreck G, Peeters J, Blaton N, Augustjins P, Kinget R. 2002. Thermal properties of hot-stage extrudates of itraconazole and Eudragit E100. Phase separation and polymorphism. J Therm Anal Cal 68:591-601.
46. Six K, Berghmans H, Leuner C, Dressman J, Van Werde K, Mullens J, Benoist L, Thimon M, Meublat L, Verreck G, Peeters J, Brewster M, Van den Mooter G. 2003. Characterization of solid dispersions of itraconazole and hydroxypropylmethylcellulose prepared by melt extrusion, Part II. Pharm Res 20:1047-1054.
47. Six K, Verreck G, Peeter J, Brewster M, Van den Mooter G. 2004. Increased physical stability and improved dissolution properties of itraconazole, a class II drug, by solid dispersions that combine fast- and slow-dissolving polymers. J Pharm Sci 93:124-131.
48. Heo M-Y, Piao S-S, Kim T-W, Cao Q-R, Kim A, Lee B-J. 2005. Effect of solubilizing and microemulsifying excipients in polyethylene glycol 6000 solid dispersions on enhanced dissolution and bioavailability of ketoconazole. Arch Pharm Res 28:604-611.
49. Matsunaga N, Nakamura K, Yamamoto A, Taguchi E, Tsunoda H, Takahashi K. 2006. Improvement by solid dispersions of the bioavailability of KRN633, a selective inhibitor of vegf receptor-2 tryosine kinase, and identification of its potential therapeutic window. Mol Cancer Ther 5:80-88.
50. Palmieri FP, Cantalamessa F, Martino PD, Nasuti X, Martelli S. 2002. Lonidamine solid dispersions: In vitro and in vivo evaluation. Drug Dev Ind Pharm 28:1241-1250.
51. Kai T, Akayama Y, Nomura S, Sata M. 1996. Oral absorption improvement of poorly soluble drug using solid dispersion technique. Chem Pharm Bull 44:569-571.
52. Law SL, Lo WY, Lin FM, Chang CH. 1992. Dissolution and absorption of nifedipine in polyethylene glycol solid dispersion containing phosphatidylcholine. Int J Pharm 84:161-166.
53. Emara LH, Badr RM, Abd Elbary A. 2002. Improving the dissolution and bioavailability of nifedipine using solid dispersions and solubilizers. Drug Dev Ind Pharm 28:795-807.
54. Sugimoto I, Kuchiki A, Nakagawa H. 1981. Stability of nifedipine-polyvinylpyrrollidone coprecipitate. Chem Pharm Bull 29:1715-1723.
55. Sugimoto I, Kuchiki A, Nakagawa H, Tohgo K, Kondo S, Iwane I, Takahashi K. 1980. Dissolution and absorption of nifedipine from nifedipine-polyvinylpyrrollidone coprecipitate. Drug Dev Ind Pharm 6:137-160.
56. Uekama K, Uekama K, Ikegami K, Wang Z, Horiuchi Y, Hirayama F. 1992. Inhibitory effect of 2-hydroxypropyl-β-cyclodextrin on crystal growth of nifedipine during storage: Superior dissolution and oral bioavailability compared with polyvinyl pyrrolidone K-30. J Pharm Pharmacol 44:73-78.
57. Zheng X, Yang R, Zhang Y, Wang Z, Tang X, Zheng L. 2007. Part II: Bioavailability in Beagle dogs of nimodipine solid dispersions prepared by hot-melt extrusion. Drug Dev Ind Pharm 33:783-789.
58. Zheng X, Yang R, Tang X, Zheng L. 2007. Part I: Characterization of solid dispersions of nimodipine prepared by hot-melt extrusion. Drug Dev Ind Pharm 33:791-802.
59. Cui F, Yang M, Jiang Y, Cun D, Lin W, Fan Y, Kawashima Y. 2003. Design of sustained-release nitrendipine microspeheres having solid dispersion structure by quasi-emulsion solvent diffusion method. J Control Rel 91:375-384.
60. Chono S, Takeda E, Seki T, Morimoto K. 2008. Enhancement of the dissolution rate and gastrointestinal absorption of prankulast as a model poorly water-soluble drug by grinding with gelatin. Int J Pharm 347:71-78.
61. Verrek G, Vandecruys R, De Conde V, Baert L, Peeters J, Brewster M. 2004. The use of three different solid dispersion formulations-melt extrusions, film-coated beads, and a glass thermoplastic system-to improve the bioavailability of a novel microsomal triglyceride transfer protein inhibitor. J Pharm Sci 93:1217-1228.
62. Law D, Schmitt EA, Marsh KC, Everitt EA, Wang W, Fort JJ, Krill SL, Qiu Y. 2004. Ritanovir-PEG 8000 amorphous solid dispersions: In vitro and in vivo evaluations. J Pharm Sci 93:563-570.
63. Law D, Krill SL, Schmitt EA, Fort JJ, Qiu Y, Wang W, Porter WR. 2001. Physicochemical considerations in the preparation of amorphous ritanovir-poly(ethylene glycol) 8000 solid dispersions. J Pharm Sci 90:1015-1025.
64. Klein C E, Chiu Y-L, Awni W, Zhu T, Heuser RS, Doan T, Breitenbach J, Morris JB, Brun SC, Hanna GJ. 2007. The tablet formulation of lopinavir/ritanovir provides similar bioavailability to the soft-gelatin capsule formulation with less pharmacokinetic variability and diminished food effect. J Acquir Immune Defic Syndr 44:401-410.
65. Sheen P-C, Khetarpal VK, Cariola CM, Rowlings CE. 1995. Formulation studies of a poorly water-soluble drug, in solid dispersions to improve bioavailability. Int J Pharm 118:221-227.
66. Yamashita K, Nakate T, Okimoto K, Ohike A, Tkunaga Y, Ibuki R, Higaki K, Kimura T. 2003. Establishment of new preparation method for solid dispersion formulation of tacrolimus. Int J Pharm 267:79-91.
67. Kedzierewicz F, Zinutti C, Hoffman M, Maindent P. 1993. Bioavailability study of tolbutamide g-cyclodextrin inclusion compounds. Solid dispersions and bulk powder. Int J Pharm 94:69-74.
68. Kedzierewicz F, Hoffman M, Maincent F. 1990. Comparison of tolbutamide β-cyclodextrin inclusion compounds and solid dispersions. Int J Pharm 58:221-227.
69. Kimura K, Hirayama F, Arima H, Uekama K. 2000. Effects of aging on crystallization, dissolution and absorption characteristics of amorphous tolbutamide-2-hydroxypropyl-β-cyclodextrin complex. Chem Pharm Bull 48:646-650.
70. Brown CK, Chokshi HP, Nickerson B, Reed RA, Rohrs BR, Shah PA. 2004. Acceptable analytical practices for dissolution testing of poorly soluble compounds. Pharm Tech. December issue: 56-64.
71. Food and Drug Administration. 2000. Guidance for industry: Waiver of in vivo bioavailability and bioequivalence studies for immediate release solid oral dosage forms based on a Biopharmaceutics Classification System. Rockville, Maryland.
72. Food and Drug Administration. 1997. Guidance for industry: Extended release oral dosage forms: Development, evaluation, and application of in vitro/in vivo correlations. Rockville, Maryland.
73. Loebenberg R, Amidon GL. 2000. Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards. Eur J Pharm Biopharm 5:3-12.
74. Xia D, Cui F, Piao H, Cun D, Piao H, Jiang Y, Ouyang M, Quan P. 2010. Effect of crystal size on the in vitro dissolution and oral absorption of nitrendipine in rats. Pharm Res 27:1965-1976.
75. Jantratid E, Janssen N, Reppas C, Dressman J. 2008. Dissolution media simulating conditions in the proximal human gastrointestinal tract: An update. Pharm Res 25:1663-1676.
76. Mudie DM, Amidon GL, Amidon GE. 2010. Physiological parameters for oral delivery and in-vitro testing. Mol Pharm 7:1388-1405.
77. Bevernage J, Fortier T, Brouwers J, Tack J, Annaert P, Augustijns P. 2011. Excipient-mediated supersaturation stabilization in human intestinal fluids. Mol Pharm 8:564-570.
78. Paul SM, Mytelka DS, Dunwiddie CT, Persinger CC, Munos BH, Lindborg SR, Schacht AL. 2010. How to improve R & D productivity: The pharmaceutical industry's grand challenge. Nat Rev Drug Discov 9:203-214.
79. General Chapters <711>, "Dissolution" and <724> "Drug Release." 2004. In The United States Pharmacopeia 27-National Formulary 22. United States Pharmacopeial Convention, Inc., Rockville, Maryland, pp 2303-2304and 2305-2312.
80. Yu LX, Wang JT, Hussain AS. 2002. Evaluation of USP apparatus 3 for dissolution testing of immediate- release products. AAPS PharmSci 4, 1-5.
81. Carino SR, Sperry DC, Hawley M. 2010. Relative bioavailability of three different solid forms of PNU-141659 as determined with the artificial stomach-duodenum model. J Pharm Sci 99:3923-3930.
82. Gao Y, Carr A, Spence JK, Wang WW, Turner TM, Lipari JM, Miller JM. 2010. A pH-dilution method for estimation of biorelevant drug solubility along the gastrointestinal tract: Application to physiologically based pharmacokinetic modeling. Mol Pharm 7:1516-1526.
83. Polster CS, Stassi F, Wu S-Y, Sperry DC. 2010. Use of artificial stomach-duodenum model for investigation of dosing fluid effect on clinical trial variability. Mol Pharm 7:1533-1538.
84. General Chapter <1092>. 2006. The dissolution procedure: Development and validation. In The United States 41Pharmacopeia 34-National Formulary 29. United States Pharmacopeial Convention, Inc., Rockville, Maryland.
85. Supplementary Chapter I E. 1998. Dissolution of solid oral dosage forms." In British Pharmacopeia1998, Vol. II, pp A327-A331.
86. Fadda HM, Sousa T, Carlsson AS, Abrahamsson B, Williams JG, Kumar D, Basit AW. 2010. Drug solubility in luminal fluids from different regions of the small and large intestine of humans. Mol Pharm 7:1527-1532.
87. Fadda HM, McConnell EL, Short MD, Basit AW. 2009. Meal-induced acceleration of tablet transit through the human small intestine. Pharm Res 26:356-360.
88. Selen A. 2009. Biorelevant dissolution testing: Characterizing the product for the patient. short course #3: developing biorelevant dissolution test methods with an emphasis on QbD. Los Angeles, California: American Association of Pharmaceutical Scientists.
89. Schiller C, Frohlich CP, Giessmann T, Siegmund W, Monnikes H, Hosten N, Weitschies W. 2005. Intestinal fluid volumes and transit of dosage forms as assessed by magnetic resonance imaging. Aliment Pharmacol Ther 22:971-979.
90. Weitschies W, Wedemeyer RS, Kosch O, Fach K, Nagel S, Söderlind E. 2005. Impact of the intragastric location of extended rlease tablets on food interactions. J Control Release 108:375-85.
91. Minekus M, Marteau P, Havenaar R, Huis In T Veld J. 1995. A multicomparmental dynamic computer-controlled model simulating the stomach and small intestine. Altern Lab Animals 23:197-209.
92. Minekus M, Smeets-Peeters M, Bernalier A, Marol-Bonnin S, Havenaar R, Marteau P, Alric M, Fonty G, Huis In T Veld JH. 1995. A computer-controlled system to simulate conditions of the large intestine with peristaltic mixing, water absorption and absorption of fermentation products. Appl Microbiol Biotechnol 53:108-114.
93. Garbacz G, Wedemeyer R-S, Nagel S, Giessmann T, Mönnikes H, Wilson CG. 2008. Irregular absorption profiles observed from diclofenac extended release tablets can be predicted using a dissolution test apparatus that mimics in vivo physical stresses. Eur J Pharm Biopharm 70:421-428.
94. D'Arcy DM, Corrigan OI, Healy AM. 2006. Evaluation of hydrodynamics in the basket dissolution apparatus using computational fluid dynamics-dissolution rate implications. Eur J Pharm Sci 27:259-267.
95. Wei JD, Ho HO, Chen CH, Ke WT, Chen ET, Sheu MT. 2010. Characterisation of fenofibrate dissolution delivered by a self-microemulsifying drug-delivery system. J Pharm Pharmacol 62:1685-1696.
96. Garbacz G, Golke B, Wedemeyer R-S, Axell M, Söderlind E, Abrahamsson B. 2009. Comparison of dissolution profiles obtained from nifedipine extended release once a day products using different dissolution test apparatuses. Eur J Pharm Sci 38:147-155.
97. Webster J, Bollen P, Grimm H, Jennings M. 2010. Ethical implications of using the minipig in regulatory toxicology studies. J Pharmacol Toxicol Methods 62:160-166.
98. Curtis MJ. 2010. The RETHINK project: Impact of toxicity testing in the minipig as an alternative approach in regulatory toxicity testing. J Pharmacol Toxicol Methods 62(3):157-162.
99. Kimura T, Higaki K. 2002. Gastrointestinal transit and drug absorption. Biol Pharm Bull 25:149-164.
100. Collins PJ, Horowitz M, Cook DJ, Harding PE, Shearman DJC. 1983. Gastric emptying in normal subjects-A reproducible technique using a single scintillation camera and computer system. Gut 24:1117-1125.
101. McLaughlan G, Fullarton GM, Crean GP, McColl KE. 1989. Comparison of gastric body and antral pH: A 24 hour ambulatory study in healthy volunteers. Gut 30:573-578.
102. Washington N, Washington C, Wilson CG. 2001. Physiological pharmaceutics: Barriers to drug absorption, 2nd Ed. London, UK: Taylor and Francis.
103. Jamei M, Turner D, Yang J, Neuhoff S, Polak S, Rostami-Hodjegan A, Tucker G. 2009. Population-based mechanistic prediction of oral drug absorption. AAPS J 11:225-237.
104. Rostami-Hodjegan A, Tucker G. 2007. Simulation and prediction of in vivo drug metabolism in human populations from in vitro data. Nat Rev Drug Disc 6:140-148.
105. Huang W, Lee SL, Yu LX. 2009. Mechanistic approaches to predicting oral drug absorption. AAPS J 11:217-224.
106. Coupe AJ, Davis SS, Wilding IR. 1991. Variation in gastrointestinal transit of pharmaceutical dosage forms in healthy subjects. Pharm Res 8:360-364.
107. Podczeck F, Mitchell CL, Newton JM, Evans D, Short MB. 2007. The gastric emptying of food as measured by gamma-scintigraphy and electrical impedance tomography (EIT) and its influence on the gastric emptying of tablets of different dimensions. J Pharm Pharmacol 59(11):1527-1536.
108. McConnell EL, Fadda HM, Basit AW. 2008. Gut instincts: Explorations in intestinal physiology and drug delivery. Int J Pharm 364:213-226.
109. Yu LX, Amidon GL. 2002. Biopharmaceutics Classification System: The scientific basis for biowaiver extensions. Pharm Res 19(7):921-925.
110. Wu CY, Benet LZ. 2005. Predicting drug disposition via application of BCS: Transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res 22:11-23.
111. Ashiru DAI, Patel R, Basit AW. 2008. Polyethylene glycol 400 enhances the bioavailability of a BCS class III drug (ranitidine) in male subjects but not females. Pharm Res 25:2327-2333.
112. Kabanov AV, Okano T. 2003. Challenges in polymer therapeutics: State of the art and prospects of polymer drugs. Adv Exp Med Biol 519:1-27.
113. Vertzoni M, Diakidou A, Chatzilias M, Söderlind E, Abrahamsson B, Dressman JB, Reppas C. 2010. Biorelevant media to simulate fluids in the ascending colon of humans and their usefulness in predicting intracolonic drug solubility. Pharm Res 27:2187-2196.
114. Puri V, Dantuluri K, Bansal AK. 2011. Investigation of atypical dissolution behavior of an amorphous solid dispersion. J Pharm Sci 100:2640-2648.
115. Rolan P, Danhof M, Stanskic D, Peck C. 2007. Current issues relating to drug safety especially with regard to the use of biomarkers: A meeting report and progress update. Eur J Pharm Sci 30:107-112.
116. Jantratid E, Janssen N, Reppas C, Dressman J. 2008. Dissolution media simulating conditions in the proximal human gastrointestinal tract: An update. Pharm Res 25:1663-1676.
117. Volpe DA. 2010. Application of method suitability for drug permeability classification. AAPS J 12:670-678.
118. Volpe DA. 2008. Variability in Caco-2 and MDCK cell-based intestinal permeability assays. J Pharm Sci 97:712-725.
119. Yamashita S, Tachiki H. 2009. Analysis of risk factors in human bioequivalence study that incur bioinequivalence of oral drug products. Mol Pharm 6:48-59.
120. Abrahamsson B, Lennernas H. 2005.Application of the Biopharmaceutics Classification System now and in the future. Drug bioavailability: Estimation of solubility, permeability, absorption and bioavailability. In Methods and principles in medicinal chemistry; vanWaterbeemd H, Lennerhäs H, Artursson P, Eds. Vol. 18. Weinheim, Germany: Wiley-VCH.
121. Lennerhäs H. 1998. Human intestinal permeability. J Pharm Sci 87:403-410.
122. Maury J, Nicoletti C, Guzzo-Chambraud L, Maroux S. 1995. The filamentous brush border glycocalyx, a mucin-like marker of enterocyte hyper-polarization. Eur J Biochem 228:323-331.
123. Sutton SC. 2009. Role of physiological intestinal water in oral absorption. AAPS J 11:277-285.
124. Desso JM, Williams AL. 2008. Contrasting the gastrointestinal tracts of mammals: Factors that influence absorption. Ann Rep Med Chem 43:353-371.
125. Kararli TT. 1995. Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm Drug Dispos 16:351-380.
126. Grass GM, Sinko PJ. 2002. Physiologically-based pharmacokinetic simulation modeling. Adv Drug Deliv Rev 54:433-451.
127. Bode G, Clausing P, Gervais F, Loegsted J, Luft J, Nogues V, Sims J, and under the auspices of the Steering Group of the RETHINK Project. 2010. The utility of the Minipig as an animal model in regulatory toxicology. J Pharmacol Toxicol Methods 62:196-220.
128. Kagan L, Hoffman A. 2008. Systems for region selective drug delivery in the gastrointestinal tract: Biopharmaceutical considerations. Expert Opin Drug Deliv 5:681-692.
129. Johnson KC. 2003. Dissolution and absorption modeling: Model expansion to simulate the effects of precipitation, water absorption, longitudinally changing intestinal permeability, and controlled release on drug absorption. Drug Dev Ind Pharm 29:833-842.
130. Bolger MB, Lukacova V, Woltosz WS. 2009. Simulations of the nonlinear dose dependence for substrates of influx and efflux transporters in the human intestine. AAPS J 11:353-363.
131. Lukacova V, Woltosz WS, Bolger MB. 2009. Prediction of modified release pharmacokinetics and pharmacodynamics from in vitro, immediate release, and intravenous data. AAPS J 11:323-334.
132. Trevaskis NL, Charman WN, Porter CJ. 2008. Lipid-based delivery systems and intestinal lymphatic drug transport: A mechanistic update. Adv Drug Deliv Rev 60:702-716.
133. Porter CJ, Charman WN. 2001. Intestinal lymphatic drug transport: An update. Adv Drug Deliv Rev 50:61-80.
134. Aoki Y, Morishita M, Asai K, Akikusa B, Hosoda S, Takayama K. 2005. Region-dependent role of the mucous/glycocalyx layers in insulin permeation across rat small intestinal membrane. Pharm Res 22:1854-1862.
135. van Waterschoot RA, ter Heine R, Wagenaar E, van der Kruijssen CM, Rooswinkel RW, Huitema AD, Beijnen JH, Schinkel AH. 2010. Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. Br J Pharmacol 160:1224-1233.
136. ter Heine R, Van Waterschoot RA, Keizer RJ, Beijnen JH, Schinkel AH, Huitema AD. 2011. An integrated pharmacokinetic model for the influence of cyp3a4 expression on the in vivo disposition of lopinavir and its modulation by ritonavir. J Pharm Sci 100:2508-2515.
137. Benet LZ, Broccatelli F, Oprea TI. 2011. BDDCS applied to over 900 drugs. AAPS J 13:519-547.
138. Butler JM, Dressman JB. 2010. The developability classification system: Application of biopharmaceutics concepts to formulation development. J Pharm Sci 99:4940-4954.