Recent advances and novel strategies in pre-clinical formulation development: An overview

Journal of Controlled Release

Volumn 156, Issue 3, 2011, Pages 281-296

  Shah, Amit K ^a   Agnihotri, Sunil A ^b  

^a Product Development   (United States)

^b Frontage Laboratories Inc   (United States)

Author keywords

Formulation; In vivo models; Physico chemical properties; Preclinical; Stability

Indexed keywords

BASIC CONCEPTS; BIOPHARMACEUTICS; CLASSIFICATION SYSTEM; CLINICAL OUTCOME; COSOLVENTS; DRUG CANDIDATES; DRUG SUBSTANCES; FORMULATION; FORMULATION DEVELOPMENT; IN VIVO MODELS; IN-VIVO; NEW CHEMICAL ENTITIES; NOVEL STRATEGIES; OPTIMUM PH; PHYSICOCHEMICAL PROPERTY; PRECLINICAL; PRECLINICAL DEVELOPMENT; PRECLINICAL STUDIES; REGULATORY REQUIREMENTS; SELECTED EXAMPLES; SOLUBILIZERS; STUDY DESIGN;

CHEMICAL PROPERTIES; CHEMICAL STABILITY; CONVERGENCE OF NUMERICAL METHODS; STRATEGIC PLANNING; SURFACE ACTIVE AGENTS;

DRUG PRODUCTS;

ANTIDIABETIC AGENT; ANTIHYPERTENSIVE AGENT; ANTINEOPLASTIC AGENT; ANTIVIRUS AGENT; CYCLODEXTRIN; ENDOTOXIN; PARENTERAL SOLUTION; SODIUM CHLORIDE; SURFACTANT; WATER;

AQUEOUS SOLUTION; COMPLEX FORMATION; DIFFERENTIAL SCANNING CALORIMETRY; DISSOCIATION CONSTANT; DOSE RESPONSE; DRUG CLASSIFICATION; DRUG DECOMPOSITION; DRUG DEVELOPMENT; DRUG FORMULATION; DRUG LEGISLATION; DRUG MECHANISM; DRUG PENETRATION; DRUG SCREENING; DRUG SOLUBILITY; DRUG STABILITY; DRUG STERILITY; DRUG STRUCTURE; GLASS TRANSITION TEMPERATURE; IN VITRO STUDY; IN VIVO STUDY; INTRAPERITONEAL DRUG ADMINISTRATION; INTRAVENOUS DRUG ADMINISTRATION; MELTING POINT; MICROSCOPY; NONHUMAN; ORAL DRUG ADMINISTRATION; PARTITION COEFFICIENT; PH; PHARMACOKINETICS; PHARMACOLOGY; PKA; PRACTICE GUIDELINE; PRIORITY JOURNAL; REVIEW; SPECIES DIFFERENCE; TEMPERATURE; TOXICOLOGY; X RAY DIFFRACTION;

ANIMALS; CHEMISTRY, PHARMACEUTICAL; DRUG ADMINISTRATION ROUTES; DRUG EVALUATION, PRECLINICAL; HUMANS; PHARMACEUTICAL PREPARATIONS;

EID: 82755182842     PISSN: 01683659     EISSN: 18734995     Source Type: Journal    
DOI: 10.1016/j.jconrel.2011.07.003     Document Type: Review

References (133)

1. M.C. Rogge, and D.R. Taft The scope of preclinical drug development: an introduction and framework J. Swarbrick, preclinical drug development 2005 Taylor & Francis Group Boca Raton 1 6
2. C. Parkinson, and P. Grasso The use of the dog in toxicity testing of pharmaceutical compounds Hum. Exp. Toxicol. 12 1993 99 109 (Pubitemid 23121672)
3. J.G. Vos Immunotoxicity assessment screening and function studies Arch. Toxicol. 4 1980 95 108 (Pubitemid 11227805)
4. J.S. Penta, M. Rosencweig, and A.M. Guarino Mouse and large animal toxicology studies of 12 antitumor agents: relevance of starting doses for phase I clinical trials Cancer Chemother. Pharmacol. 3 1979 97 101 (Pubitemid 10225496)
5. J.C. Barbiarz, and D.J. Pisano Overview of FDA and drug development D.J. Pisano, D.S. Mantus, FDA Regulatory Affairs: A Guide for Prescription Drugs, Medical Devices, and Biologics 2008 Informa Healthcare USA, Inc. New York 1 33
6. A.A. Nomeir, P. Markham, and L.T. Burka Species differences in the disposition and metabolism of nalidixic acid J. Pharmacol. Exp. Ther. 279 1996 222 230 (Pubitemid 27166915)
7. http://www.accessdata.fda.gov/scripts/cdrh/cfdocs/cfcfr/CFRSearch.cfm? CFRPart=58 in 21 CFR Part 58
8. J. Maas, W. Kamm, and G. Hauck An integrated early formulation strategy - from hit evaluation to preclinical candidate profiling Eur. J. Pharm. Biopharm. 66 2007 1 10 (Pubitemid 46412973)
9. P. Baldrick Toxicokinetics in preclinical evaluation Drug Discov. Today 8 2003 127 133 (Pubitemid 36143982)
10. R.J. Bastin Salt selection and optimization procedures for pharmaceutical new chemical entities Org. Process. Res. Dev. 4 2000 427 435
11. B.D. Anderson, and R.A. Conradi Predictive relationship in the water solubility of salts of a nonsteroidal anti-inflammatory drug J. Pharm. Sci. 74 1985 815 820 (Pubitemid 15042168)
12. P.F. Dimond Using nanotechnologies in biotech and medicine Genetic Engineering and Biotechnology News 25 2005 21
13. S.N. Bhattachar Solubility: its not just for physical chemists Drug Discov. Today 11 2006 1012 1018 (Pubitemid 44572881)
14. T. Higuchi, and K.A. Connors Phase-solubility techniques Adv. Anal. Chem. Instrum. 4 1965 117 212
15. L. Kumar An overview of automated systems relevant in pharmaceutical salt screening Drug Discov. Today. 12 2007 1046 1053 (Pubitemid 350186130)
16. T.M. Chen Evaluation of a method for high throughput solubility determination using a multi-wavelength UV plate reader Comb. Chem. High Throughput Screening. 5 2002 575 581
17. X.Q. Chen, and S. Venkatesh Miniature device for aqueous and non-aqueous solubility measurements during drug discovery Pharm. Res. 21 2004 1758 1761 (Pubitemid 39390085)
18. C.A. Lipinski Drug-like properties and the causes of poor solubility and poor permeability J. Pharmacol. Toxicol. Methods. 44 2000 235 249 (Pubitemid 32239479)
19. G.M. Keseru, and G.M. Makara The influence of lead discovery strategies on the properties of drug candidates Nat. Rev. Drug Discovery. 8 2009 203 212
20. S. Yalkowsky Solubility and solubilization in aqueous media first ed. 1999 Oxford University Press New York
21. T. Sakeda, N. Okamuara, S. Nagata, T. Yagami, M. Horinouchi, K. Okumura, F. Yamazhita, and M. Hashida Molecular and pharmacokinetic properties of 222 commercially available oral drugs in humans Biol. Pharm. Bull. 24 2001 935 940 (Pubitemid 32750322)
22. C.A. Lipinski, F. Lombardo, B.W. Dominy, and P.J. Feeney Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings Adv. Drug Delivery Rev. 46 2001 3 26 (Pubitemid 33653411)
23. C. Hansch, and T. Fujita A method for the correlation of biological activity and chemical structure J. Am. Chem. Soc. 86 1964 1616 1626
24. J. Sangster Octanol-water partition coefficients: fundamentals and physical chemistry 1997 John Wiley & Sons
25. C.e.a. Hansch Toward a quantitative comparative toxicology of organic compounds Crit. Rev. Toxicol. 19 1989 185 226
26. N. Gulyaeva, A. Zaslavsky, P. Lechner, M. Chelenov, O. McConnell, A. Chait, V. Kipnis, and B. Zaslavsky Relative hydrophobicity and lipophilicity of drug measured by aqueous two-phase partitioning, octanol-buffer partitioning and HPLC. A simple method for predicting blood-brain distribution Eur. J. Med. Chem. 38 2003 391 396 (Pubitemid 36577189)
27. C. Yamagami, K. Kawase, and K. Iwaki Hydrophobicity parameters determined by reversed-phase liquid chromatography. XV: optimal conditions for prediction of log P (oct) by using RP-HPLC procedures Chem. Pharm. Bull. 50 2002 1578 1583 (Pubitemid 41694843)
28. D. Bemporad, and J. Essex Permeation of small molecules through a lipid bilayer: a computer simulation study J. Phys. Chem. B. 108 2004 4875 4884
29. I.J. Hidalgo Assessing the absorption of new pharmaceuticals Curr. Top. Med. Chem. 1 2001 385 401
30. J. Mass, W. Kamm, and G. Hauck An integrated early formulation strategy - from hit evaluation to preclinical candidate profiling Eur. J. Pharm. Biopharm. 66 2007 1 10 (Pubitemid 46412973)
31. M.J. Hageman Preformulation design to enable discovery and assess developability Comb. Chem. High Throughput Screening. 13 2010 90 100
32. Z. Jia, T. Ramstad, and M. Zhong Medium-throughput pKa screening of pharmaceuticals by pressure-assisted capillary electrophoresis Electrophoresis 22 2001 1112 1118 (Pubitemid 32409380)
33. Y. Ishihama, M. Nakamura, T. Miwa, T. Kajima, and N. Asakawan A rapid method for pKa determination of drugs using pressure assisted capillary electrophoresis with photodiode array detection in drug discovery J. Pharm. Sci. 91 2002 933 942 (Pubitemid 34640917)
34. in Tufts Center for the Study of Drug Development, Tufts Unversity: Boston, MA, USA http://csdd.tufts.edu/files/uploads/how-new-drugs-move.pdf
35. http://www.phrma.org/files/attachments/RD%20Brochure%20022307.pdf, in (Eds.), Pharmaceutical Research and Manufacturers of AmericaWashington, DC, USA
36. S.C. Gad Preclinical Development Handbook: ADME and Biopharmaceutical Properties first ed. 2008 John Wiley & Sons, Inc. Hoboken, NJ
37. Sciencelab.com MSDS, Secondary Sciencelab.com MSDS, 2010.
38. BASF Technical Information Secondary BASF Technical Information 2008
39. Transcutol product profile, Gattefosse, Secondary Transcutol product profile, Gattefosse, 2011.
40. JTBaker MSDS, Secondary JTBaker MSDS, 2005.
41. W.J. Krasavage, and C.J. Terhaar d-a-Tocopheryl polyethylene glycol 1000 succinate, acute toxicity, subchronic feeding, reproduction and teratologic studies in rat J. Agric. Food Chem. 25 1977 273 278
42. R.J. Lewis Sax's Dangerous Properties of Industrial Materials, New York 2004
43. S. Wu, and W. Hopkins Characterization of D-a tocopheryl PEG 1000 succinate for applications as an absorption enhancer in drug delivery systems Pharm. Technol. 23 1999 52 68 (Pubitemid 29503108)
44. L. Yu, A. Bridgers, J. Polli, A. Vicerks, S. Long, A. Roy, R. Winnike, and M. Coffin Vitamin E-TPGS increases absorption flux of an HIV protease inhibitor by enhancing its solubility and permeability Pharm. Res. 16 1999 1812 1817 (Pubitemid 30040695)
45. B. Rege, J. Kao, and J. Polli Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers Eur. J. Pharm. Sci. 16 2002 237 246
46. E.D. Hugger, B.L. Novak, P.S. Burton, K.L. Audus, and R.T. Borchardt A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro J. Pharm. Sci. 91 2002 1991 2002 (Pubitemid 36254935)
47. A.W. Basit, F. Podczeck, J.M. Newton, W.A. Waddlington, P.J. Eli, and L.F. Lacey Influence of polyethylene glycol 400 on the gastrointestinal absorption of ranitidine Pharm. Res. 19 2002 1368 1374
48. ™ as pharmacokinetic simulation tool and a statistical screening design applied to dog study Eur. J. Pharm. Biopharm. 27 2006 91 99 (Pubitemid 41728259)
49. N.H. Shah, M.T. Carvajal, C.I. Patel, and M.H. Infeld M.A. W., Self-emulsifying drug delivery systems (SEDDS) with polyglycolysed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs Int. J. Pharm. 106 1994 15 23 (Pubitemid 24110060)
50. M.J. Groves The self-emulsifying action of mixed surfactants in oil Acta. Pharm. Suec. 13 1976 361 372
51. J.H. Schulman, and J.B. Montagne Formation of microemulsions by amino alkyl alcohols Ann. N. Y. Acad. Sci. 92 1961 366 371
52. A.R. Patel, and P.R. Vavia Preparation and in-vivo evaluation of SMEDDS (Self-Microemulsifying drug delivery system) containing Fenofibrate AAPS J. 9 2007 E344 E352
53. T.R. Kommuru, B. Gurley, M.A. Khan, and I.K. Reddy Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment Int. J. Pharm. 212 2001 233 246 (Pubitemid 32119449)
54. P. Patil, J. Joshi, and J. Paradkhar Effect of formulation variables on preparation and evaluation of gelled self-emulsifying drug delivery system (SEDDS) of ketoprofen AAPS Pharm. Sci. Tech. 5 2004 34 42
55. P. Patil, P. Vandana, and P. Paradkhar Formulation of self emulsifying drug delivery system for oral delivery of simvastatin: in vitro and in vivo evaluation Acta Pharma. 57 2007 111 122 (Pubitemid 46361952)
56. R. Sachan, K. Khatri, and S.B. Keasture Self-emulsifying drug delivery system a novel approach for enhancement of bioavailability Int. J. Pharm. Tech. Res. 2 2010 1738 1745
57. B. Bittner, R.C.B. Gonzales, I. Walter, and J. Huwyler Impact of oral administration of the surface-active excipient solutol HS15 on the pharmacokinetics of intravenously administered colchicines Lett. Drug Des. Discov. 2 2005 193 195 (Pubitemid 40694846)
58. R.C.B. Gonzales, J. Huwyler, F. Boess, I. Walter, and B. Bittner In vitro investigation on the impact of the surface-active excipients Cremophor EL, Tween 80 and Solutol HS 15 on the metabolism of midazolam Biopharm. Drug Dispos. 25 2004 37 49 (Pubitemid 38159262)
59. A.J. Tije, J. Verweij, W.J. Loos, and A. Sparreboom Pharmacological effects of formulation vehicles: implications for cancer chemotherapy Clin. Pharmacokinet. 42 2003 665 685 (Pubitemid 36936530)
60. M. Kuentz, P. Egloff, and D. Rothlisberger A technical feasibility study of surfactant-free drug suspensions using octenyl succinate-modified starches Eur. J. Pharm. Biopharm. 63 2006 37 43
61. B. Rabinow Nanosuspensions in drug delivery Nat. Rev. Drug Discovery. 3 2004 785 796 (Pubitemid 39242830)
62. S. Pace, G. Pace, I. Parikh, and A. Mishra Novel injectable formulations of insoluble drugs Pharm. Technol. 23 1999 116 134 (Pubitemid 29135950)
63. F. Kesisoglou, S. Panami, and Y. Wu Oral formulation development and biopharmaceutical evaluation Adv. Drug Delivery Rev. 59 2007 631 644 (Pubitemid 47285408)
64. C.M. Keck, and R.H. Muller Drug nanocrystals of poorly soluble drugs produced by high pressure homogenization Eur. J. Pharm. Biopharm. 62 2006 3 16 (Pubitemid 41736019)
65. E. Merisko-Liversidge, G.G. Loversidge, and E.R. Cooper Nanosizing: a formulation approach for poorly-water-soluble compounds Eur. J. Pharm. Sci. 18 2003 113 120 (Pubitemid 36184748)
66. R.H. Muller, C. Jacobs, and O. Kayser Nanosuspensions as particulate drug formulation in therapy. Rationale for development and what we can expect for the future Adv. Drug Delivery Rev. 47 2001 3 19 (Pubitemid 32209229)
67. F. Gonzales-Caballero J. de Dios Garcia Lopez-Duran, Suspension formulation F. Niellout, G. Marti-Mestres, Pharmaceutical Emulsions and Suspensions, Drugs and the Pharmaceutical Science 2000 Marcel Dekker, Inc. New York 127 190
68. J. Wong, A. Brugger, A. Khare, M. Chaubal, P. Papadopoulos, B. Rainbow, J. Kipp, and J. Ning Suspension for intravenous (IV) injection: A review of development, preclinical and clinical aspects Adv. Drug Delivery Rev. 60 2008 939 954
69. J. Swarbirck, J. Rubino, and O. Rubino Coarse dispersion D. Troy, Remington: The Science and Practice of Pharmacy 2006 Lippincott Williams & Wilkins Baltimore 319
70. B. Eerdenbrugh, G. Mooter, and P. Augustijns Top-down production of drug nanocrystals: nanosuspension stabilization, miniaturization and transformation into solid products Int. J. Pharm. 364 2008 64 75
71. J.L. Lach, and J. Cohen Interaction of pharmaceuticals with Schardinger dextrins II: Interaction with selected compounds J. Pharm. Sci. 52 1963 137 142
72. K. Uekama, T. Fujina, F. Hirayama, M. Otagiri, and M. Yamasaki Inclusion complexes of steroid hormones with cyclodextrins in water and in solid phases Int. J. Pharm. 10 1982 1 15 (Pubitemid 12145049)
73. H.M. Marques, J. Hadgraft, and I.J. Kellaway Studies of cyclodextrin inclusion complexes I. The salbutamol-cyclodextrin complex as studied by phase solubility and DSC Int. J. Pharm. 63 1990 259 266
74. X. Liu, H. Lin, J.C. Thenmozhiyal, S.Y. Chan, and P.C. Ho Inclusion of acitretin into cyclodextrins: phase solubility, photostability and physicochemical characterization J. Pharm. Sci. 92 2003 2449 2457 (Pubitemid 37484771)
75. T. Loftsson, and M.E. Brewester Pharmaceutical applications of cyclodextrins I: drug solubilization and stabilization J. Pharm. Sci. 85 1996 1017 1025 (Pubitemid 26338912)
76. Y.L. Loukas, V. Vraka, and G. Gregoriadis Drugs in cyclodextrins in liposomes: a novel approach to the chemical stability of drugs sensitive to hydrolysis Int. J. Pharm. 162 1998 137 142 (Pubitemid 28166099)
77. E. Antoniadou-Vyaza, G. Buckton, S.G. Michaleas, Y.L. Loukas, and M. Efentakis The formulation of an inclusion complex of methocarbamol wiht hydroxypropyl-B-cyclodextrin: the effect on chemical stability, solubility and dissolution rate Int. J. Pharm. 158 1997 233 239 (Pubitemid 28012910)
78. S. Rawat, and S.K. Jain Rofecoxib-B-cyclodextrin inclusion complex for solubility enhancement Pharmazie 58 2003 639 641 (Pubitemid 37187426)
79. M. Nakamura, K. Tokihiro, M. Yukihisa, S. Nishide, and S. Yokohama Potential use of cyclodextrins to enhance the solubility of YM466 in aqueous solution Drug Dev. Ind. Pharm. 29 2003 903 908 (Pubitemid 37203692)
80. H. Choi, D. Kim, H.W. Jun, and B. Yoo Improvement of dissolution and bioavailability of nitrendipine by inclusion in hydroxypropyl-B-cyclodextrin Drug Dev. Ind. Pharm. 29 2003 1085 1094 (Pubitemid 37499544)
81. K. Fromming, and J. Szejtli Cyclodextrins J.E.D. Davies, Cyclodextrins in Pharmacy 1993 Kluwer Academic Publishers Dordrecht 1 17
82. J. Szejtli Cyclodextrins in drug formulations Pharm. Tech. 15 1991 36 44
83. B. Muller, and V. Brauns Solubilization of drugs by modified B-cyclodextrins Int. J. Pharm. 26 1985 77 88
84. M.S. Worthington, B.D. Glass, and L.J. Penkler Phase solubility analysis in studying the interaction of nifedipine with selected cyclodextrins in aqueous solutions J. Inclusion Phenom. Macrocyclic Chem. 25 1996 153 156
85. D.J. Eatough, J.J. Christensen, and R.M. Izatt Experiments in thermometric titrimetry and titration calorimetry rev. ed. 1974 Brigham Young University Publication Provo
86. E.V. Kovaleva, L.A. Zemnukhova, N.S. Lebedeva, and G.A. Fedorishcheva Complexation processes in KF-SbF3-H2O system studied by calorimetric titration Russ. J. Coord. Chem. 31 2005 156 158 (Pubitemid 40536793)
87. L. Liu, G. Weng, and Q. Guo Association constant prediction for the inclusion of alfa-cyclodextrin with benzene derivatives by an artificial neural network J. Inclusion Phenom. Macrocyclic Chem. 34 1999 291 298
88. M. Cirri, F. Maestrelli, S. Orlandini, S. Furlanetto, S. Pinzauti, and P. Mura Determination of stability constant values of fubliprofen-cyclodextrin complexes using different techniques J. Pharm. Biomed. Anal. 37 2005 995 1002 (Pubitemid 40614830)
89. C. Yanez, R. Salazar, L.J. Nunez-Vergara, and J.A. Squella Spectrophotometric and electrochemical study of the inclusion complex between beta-cyclodextrin and furnidipine J. Pharm. Biomed. Anal. 35 2004 51 56 (Pubitemid 38368859)
90. M. Casolaro, C. Anselmi, and G. Picciocchi The protonation thermodynamics of ferulic acid/gamma-cyclodextrin inclusion compounds Thermochim. Acta. 425 2005 143 147 (Pubitemid 40082681)
91. C.E. Dahlheim, M.M. Dali, V.H. Naringrekar, S.A. Miller, and R.B. Shukla Multidisciplinary investigation of atypical inclusion complexes of beta-cyclodextrin and a phospholipase-A2 inhibitor J. Pharm. Sci. 94 2005 409 422 (Pubitemid 40293336)
92. P. Malyala, and M. Singh Endotoxin limits in formulations for preclinical research J. Pharm. Sci. 97 2007 2041 2044
93. S. Mutalik, A. Naha, A.N. Usha, A.K. Ranjith, P. Musmade, K. Manoj, P. Anju, and S. Prasanna Preparation, in vitro, preclinical and clinical evaluations of once daily sustained release tablets of aceclofenac Arch. Pharmacal Res. 30 2007 222 234
94. D. Stepensky, W. Srour, M. Friedman, I. Raz, and A. Hoffman Dependency of metformin hypoglycemic effect on mode of administration in diabetic rats: measurement and kinetics of in vivo drug effects Advances in simultaneous pharmacokinetic/pharmacodynamic modeling. in 3rd International Symposium 1998 The Netherlands
95. D. Stepensky, M. Friedman, I. Raz, and A. Hoffman Pharmacokinetic- pharmacodynamic analysis of glucose-lowering effect of metformin in diabetec rats revelas first-pass pharmacodynamic effect Drug. Metab. Dispos. 30 2002 861 868 (Pubitemid 34815414)
96. N. Vidon, S. Chaussade, M. Noel, C. Franchisseur, B. Huchett, and J.J. Bernier Metformin in the digestive tract Diabetes Res. Clin. Pract. 4 1988 223 229 (Pubitemid 18080749)
97. P.H. Marathe, Y. Wen, J. Norton, D.S. Greene, R.H. Barbhaiya, and I.R. Wilding Effect of altered gastric emptying and gastrointestinal motility on bioavailability of metformin AAPS Annual Meeting 1999 New Orleans, LA
98. D. Stepensky, M. Friedman, W. Srour, I. Raz, and A. Hoffman Preclinical evaluation of pharmacokinetic-pharmacodynamix rationale for oral CR metformin formulation J. Controlled Release 71 2001 107 115 (Pubitemid 32195445)
99. P. Li, and L. Zhao Developing early formulations: practice and perspective Int. J. Pharm. 34 2007 1 29
100. P. Bummer Interfacial phenomena D. Troy, Remington: The Science and Practice of Pharmacy 2006 Lippincott Williams & Wilkins Baltimore 280
101. R.L. Grant, C. Yao, D. Gabaldon, and D. Acosta Evaluation of surfactant cytotoxicity potential by primary cultures of ocular tissues: characterization of rabbit corneal epithelial cells and initial injury and delayed toxicity studies Toxicology 76 1992 153 156
102. L. Yu, and G. Amidon Saturable small intestinal drug absorption in humans: modeling and interpretation of cefatrizine data Eur. J. Pharm. Biopharm. 45 1998 199 203 (Pubitemid 28167747)
103. B. Agoram, W. Woltosz, and M. Bolger Predicting the impact of physiological and biochemical processes on oral drug bioavailability Adv. Drug Delivery Rev. 50 2001 S41 S67
104. W.B. Geho, H.C. Geho, J.R. Lau, and T.J. Gana Hepatic-derived vesicle insulin: a review of formulation development and preclinical evaluation J. Diabetes Sci. Technol. 3 2009 1451 1459
105. J.T. MacGregor, J.M. Collins, Y. Sugiyama, C.A. Tyson, J. Dean, L. Smith, M. Andersen, R.D. Curren, J.B. Houston, F.F. Kadlubar, G.L. Kedderis, K. Krishnan, A.P. Li, R.E. Parchment, K. Thummel, J.E. Tomaszewski, R. Ulrich, A. Vickers, and S.A. Wrington In-vitro human tissue models in risk assessment: report of a consensus-building workshop Toxicol. Sci. 59 2001 17 36 (Pubitemid 32117978)
106. http://www.outsourcing-pharma.com/Preclinical-Research/ Human-tissue-use-in-preclinical-development-could-cut-attrition-rates-says- Biopta, Secondary http://www.outsourcing-pharma.com/Preclinical-Research/Human- tissue-use-in-preclinical-development-could-cut-attrition-rates-says-Biopta
107. I. Nestorov Whole-body physiologically based pharmacokinetic models Expert Opin. Drug Metab. Toxicol. 3 2007 235 249 (Pubitemid 47321518)
108. D. Mager Quantitative structure-pharmacokinetic/pharmacodynamic relationships Adv. Drug Delivery Rev. 58 2006 1326 1356
109. E.L. Schuck, and H. Derendorf Pharmacokinetic/pharmacodynamic evaluation of anti-infective agents Expert Rev Anti Infect Ther. 3 2005 361 373 (Pubitemid 40872531)
110. Y. Sun, H. Lee, R. Almon, and W. Jusko A pharmacokinetic/pharmacodynamic model for recombinant human growth hormone effects on induction of insulin-like growth factor I in monkeys J. Pharmacol. Exp. Ther. 289 1999 1523 1532 (Pubitemid 29246686)
111. J. Gabrielsson, A. Green, and P. Van der Graff Optimizing in vivo pharmacology studies - practical PKPD consideration J. Pharmacol. Toxicol. Methods. 61 2010 146 156
112. M. Danhof, R. Van der Geest, T. Van Laar, and H. Bodde An integrated pharmacokinetic-pharmacodynamic approach to optimization of R-apomorphine delivery in Pharkinson's disease Adv. Drug Delivery Rev. 33 1998 253 263 (Pubitemid 28403627)
113. B. Meibohm, and H. Derendorf Pharmacokinetic/pharmacodynamic studies in drug product development J. Pharm. Sci. 91 2002 18 31 (Pubitemid 34074464)
114. J.K. Peterson, and P.J. Houghton Integrated pharmacology and in vivo cancer models in preclinical and clinical drug development Eur. J. Cancer. 40 2004 837 844 (Pubitemid 38519762)
115. P.J. Houghton, J.A. Houghton, L. Myers, P. Cheshire, J.J. Howbert, and G.B. Grindey Evaluation of N-(5-indanylsulfonyl)-N0-(4-chlorophenyl)-urea against xenografts of pediatric rhabdomyosarcoma Cancer Chemother. Pharmacol. 25 1989 84 88 (Pubitemid 20009432)
116. P.J. Houghton, P.J. Cheshire, and J.C. Hallman Evaluation of a novel bis-naphthalimide anticancer agent DMP-840 against human xenograft derived from adult, juvenile, and pediatric cancers Cancer Chemother. Pharmacol. 36 1994 45 52
117. P.J. Houghton, P.J. Cheshire, J.D. Hallman, and J.A. Houghton Therapeutic efficacy of the cyclopropylpyrroloindole carzelesin against xenografts derived from adult childhood solid tumors Cancer Chemother. Pharmacol. 36 1995 45 52
118. P. Pouna, S. Bonoron-Adele, G. Gouverneur, L. Tariosse, P. Besse, and J. Robert Development of the model of rat isolated perfused heart for the evaluation of anthracycline cardiotoxicity and its circumvention Br. J. Pharmacol. 117 1996 1593 1599 (Pubitemid 26116789)
119. P.L. Black, M.A. Ussery, S. Barney, R. Wittrock, P. MDeMarsh, G.B. Dreyer, S.R. Petteway, P. Dalmonte, J. Baldoni, and D.M. Lambert Effect of SKF 108922, an HIV-1 protease inhibitor on retrovirus replication in mice Antiviral Res. 29 1996 175 186 (Pubitemid 26135176)
120. R. D'Souza, S. Mutalik, M. Venkatesh, S. Vidyasagar, and N. Udupa Nasal insulin gel as an alternate to parenteral insulin: formulation, preclinical, and clinical studies AAPS Pharm. Sci. Tech. 6 2005 E184 E189
121. M.J. Rathbone, R. Purvesh, F.A. Ghazail, and P.C. Ho In vivo techniques for studying the oral mucosal absorption characteristics of drug in animals and humans M.J. Rathbone, Oral mucosal drug delivery 1996 Marcel Dekker, Inc. New York 121 156
122. M.M. Dali, P.A. Moench, N.R. Mathias, P.I. Stetsko, C.L. Heran, and R.L. Smith A rabbit model for sublingual drug delivery: comparison with human pharmacokinetic studies of propranolol J. Pharm. Sci. 95 2006 37 44
123. A.P. Li Overview: hepatocytes and cryopreservation - a personal historical perspective Chem.-Biol. Interact. 121 1999 1 5 (Pubitemid 29240665)
124. Note for guidance on toxicokinetics: the assessment of systemic exposure in toxicity studies S3A in ICH Harmonized Tripartate Guideline 1994
125. FDA, Content and format of investigational new drug applications (INDs) for phase 1 studies of drugs, including well-characterized, therapeutic, biotechnology-derived products 1995 Center of Drug Evaluation and Research: Rockville, MD
126. FDA Good laboratory practice for nonclinical laboratory studies 21 Code Federal Regulations 58 2009 265
127. CPMP/SEP/1042 Note for guidance of repeated dose toxicity study http://www.emea.eu.int 2000
128. CPMP/ICH/286/95 Non-clinical safety studies for the conduct of human clinical trials and marketing authorization for pharmaceuticals http://www.emea.eu.int 2008
129. Challenging requirements for acute toxicity studies:workshop report Secondary Challenging requirements for acute toxicity studies:workshop report 2006
130. S. Robinson A European pharmaceutical company initiative challenging the regulatory requirement for acute toxicity studies in pharmaceutical drug development Regul. Toxicol. Pharmacol. 50 2008 345 352
131. M.T. Huizing, H. Rosing, F.P. Koopmans, and J.H. Beijene Influence of Cremophor EL on the quantification of paclitaxel in plasma using high-performance liquid chromatography with solid-phase extraction as sample treatment J. Chromatogr. B. 709 1998 161 165 (Pubitemid 28238431)
132. J.D. Perdue, P.J. Seaton, J.A. Tyrell, and D.R. DeVido The removal of Cremophor EL from paclitaxel for quantitative analysis by HPLC-UV J. Pharm. Biomed. Anal. 41 2006 117 123
133. D. Law, E.A. Schmitt, K.C. Marsh, E.A. Everitt, W. Wang, J. Fort, S.L. SKrill, and Y. Qui Ritonavir-PEG 8000 amorphous solid dispersions: in vitro and in vivo evaluations J. Pharm. Sci. 93 2003 563 570 (Pubitemid 38332289)