Amidon GE, He X, and Hageman MJ. Physicochemical Characterization and Principles of Oral Dosage Form Selection. In: Abraham DJ. Burger's Medicinal Chemistry and Drug Discovery, 6th Ed. John Wiley & Sons, NY, 2003, Chapt 18

Bagwe RP, Kanicky JR, Palla BJ, Patanjali PK, and Shah DO. Improved Drug Delivery Using Microemulsions: Rationale, Recent Progress, and New Horizons. Critical Rev Therap Drug Carrier Syst 2001;18:77-140

Basit AW, Newton JM, Short MD, Waddington WA, Ell PJ, and Lacey LF. The Effect of Polyethylene Glycol 400 on Gastrointestinal Transit: Implications for the Formulation of Poorly-Water Soluble Drugs. Pharm Res 2001; 18(8):1146-1150

Benita S, and Levy MY. Submicron Emulsions as Colloidal Carriers for Intravenous Administration: Comprehensive Physicochemical Characterization. J Pharm Sci 1993; 82(11):1069-1079

Bihanzadeh M, Mahmoudian M, Zolfaghari ME, Gouya MM, Kazinia T, and Khosravi A. The Influence of Particle Size and Dissolution Rate on Bioavailability of Two Indomethacin Capsules, J of the School of Pharmacy, Tehran Univ. of Medical Sciences and Health Services 1996; 5(1&2):14-24

Bohets H, Annaert P, Mannens G, van Beijsterveldt L, Anciaux K, Verboven P, Meuldermans W, and Lavrijsen K. Strategies for Absorption Screening in Drug Dscovery and Development. Curr Top Med Chem 2001; 1:367-383

Borchardt RT, Kerns EH, Lipinski CA, Thakker, DR, and Wang B. Pharmaceutical Profiling in Drug Discovery for Lead Selection. (Proceedings of the Workshop held 19-21 May 2003 in Whippany, NJ) [In: Biotechnol Pharm Aspects, 2004, 1]. 2004, 482 p

Caldwell GW. Compound Optimization in Early- and Late-Phase Drug Discovery: Acceptable Pharmacokinetic Properties Utilizing Combined Physicochemical, In Vitro and In Vivo Screens. Curr Opin Drug Dis Develop 2000; 3:30-41

Camenisch G, Folkers G, and van de Waterbeemd H. Review of Theoretical Passive Drug Absorption Models: Historical Background, Recent Developments and Limitations. Pharm Acta Hel 1996; 71:309-327

Charman WN. Lipids, Lipophilic Drugs and Oral Drug Delivery - Some emerging concepts. J Pharm Sci 2000; 89:967-978

Cho M J, Chen F J, and Huczek DL. Effects of Inclusion Complexation on the Transepithelial Transport of a Lipophilic Substance In Vitro. Pharm Res 1995; 12(4):560-564

Collins-Gold LC, Lyons RT, and Bartholow LC. Parenteral Emulsions for Drug Delivery. Adv Drug Delivery Rev 1990; 5(3):189-208

Conradi RA, Burton PS, and Borchardt RT. Physico-chemical and Biological Factors that Influence a Drug's Cellular Permeability by Passive Diffusion in Methods and Principles in Medicinal Chemistry. In: Pliska V, Testa B, and van de Waterbeemd H. Lipophilicity in Drug Action and Toxicology VCH Publishers 1996; 233-252

Curatolo W. Physical Chemical Properties of Oral Drug Candidates in the Discovery and Exploratory Development Settings. Pharmaceutical Science & Technology Today 1998; 1(9):387-393

Dressman JB, Fleisher D, and Amidon GL. Physicochemical Model for Dose-Dependent Drug Absorption. J Pharm Sci 1984; 73(9):1274-1279

Dressman JB, Amidon GL, and Fleisher D. Absorption Potential: Estimating the Fraction Absorbed for Orally Administered Compounds. J Pharm Sci 1985; 74(5):588-589

Gao P, Rush RD, Pfund WP, Huang T, Bauer JM, Morozowich W, Kuo MT, and Hageman MJ. Development of a Supersaturatable SEDDS (S-SEDDS) Formulation of Paclitaxel With Improved Oral Bioavailability. J Pharm Sci 2003; 92:2395-2407

Gao P, Guyton ME, Huang T, Bauer JM, Stefanski KJ, and Lu Q. Enhanced Oral Bioavailability of a Poorly Water Soluble Drug PNU-91325 by Supersaturatable Formulations. Drug Dev Ind Pharm 2004; 30:221-229

Hamlin WE, Nothram JI, and Wagner JG. Relationship Between in vitro Dissolution Rates and Solubilities of Numerous Compounds Representative of Various Chemical Species. J Pharm Sci 1965; 54:1651-1653

Hancock BC, and Zografi G. Characteristics and Significance of the Amorphous State in Pharmaceutical Systems, J Pharm Sci 1997; 86:1-12

Hann MM, and Oprea TI. Pursuing the Leadlikeness Concept in Pharmaceutical Research. Current Opinion in Chemical Biology 2004; 8(3):255-263

Hilgers AR, Conradi RA, and Burton PS. Caco-2 Cell Monolayersas a Model for Drug Transport Across the Intestinal Mucosa. Pharm Res 1990; 7:902-909

Hilgers AR, Smith DP, Biermacher JJ, Day JS, Jensen JL, Sims SM, Adams WJ, Friis JM, Palandra J, Hosley JD, Shobe EM, and Burton PS. Predicting Oral Absorption of Drugs: A Case with a Novel Class of Antimicrobial Agents. Pharm Res 2003; 20:1149-1155

Higuchi T. Physical Chemical Analysis of the Percutaneous Absorption Process. J

Soc Cosmetic Chemists 1960; 11:85-97

Higuchi WI, and Hiestand EN. Dissolution Rates of Finely Divided Drug Powders: I. Effect of Distribution of Particle Sizes in a Diffusion-Controlled Process. J Pharm Sci 1963; 52:67-71

Humberstone AJ, and Charman WN. Lipid-based Vehicles for Oral Delivery of Poorly Soluble drugs. Adv Drug Deliv Rev 1997; 25:103-128

Iervolino M, Raghavan RL, and Hadgraft J. Membrane Penetration Enhancement of Ibuprofen using Supersaturation. Int J Pharm 2000; 198:229-238

Jindal KC, Chaudhary RS, Singal AK, Gangwal SS, and Khanna S. Effect of Particle Size on the Bioavailability and Dissolution Rate of Rifampicin. Indian Drugs 1995; 32(3):100-107

Johnson KC, and Swindell AC. Guidance in the Setting of Drug Particle Size Specification to Minimize Variability in Absorption. Pharm Res 1996; 13:17951798

Kennedy T. Managing the Drug Discovery/Development Interface. Drug Discov Today 1997; 2:436-444

Klang SH, Parnas M, and Benita S. Emulsions as Drug Carriers. Possibilities, Limitations and Future Perspectives. In: Muller RH, Benita S, and Bohm BHL

Emulsions and Nanosuspensions for the Formulation of Poorly Soluble Drugs, Medpharm Publ., Stuttgart, Germany, 1998; pp 31-65

Koeplinger KA, Raub TJ, Padbury GE, and Zhao Z. Equilibrium Distribution of HIV Antiviral Drugs into Human Peripheral Blood Mononuclear Cells (PBMC) is Controlled by Free Drug Concentration in the Extracellular Medium. J. Pharm. Biomed. Anal. 1999; 19(3-4):399-411

Kola I, and Landis J. Opinion: Can the Pharmaceutical Industry Reduce Attrition Rates? Nature Reviews Drug Discovery 2004; 3(8):711-716

Kubinyi H. Opinion: Drug Research: Myths, Hype and Reality. Nature Reviews Drug Discovery 2003; 2(8):665-668

Leuner C, and Dressman J. Improving Drug Solubility for Oral Delivery Using Solid Dispersions. Eur J Pharm Biopharm 2000; 50:47-60

Levy G. Effect of Particle Size on Dissolution and Gastrointestinal Absorption Rates of Pharmaceuticals. Am J Pharm 1963; 135:78-92

Lipinski CA, Lombardo F, Dominy BW, Feeney PJ. Experimental and Computational Approaches to Estimate Solubility and Permeability in Drug Discovery and Development Settings. Adv Drug Delivery Rev 2001; 46(1-3):3-26

Megrab NA, Williams AC, and Barry BW. Oestradiol Permeation Through Human Skin Silastic Membrane: Effects of Propylene Glycol and Supersaturation. J

Control Rel 1995; 36:277-294

McGovern SL, Caselli E, Grigorieff N, and Shoichet BK. A Common Mechanism Underlying Promiscuous Inhibitors from Virtual and High-Throughput Screening. J Med Chem 2002; 45(8):1712-1722

Mithani SD, Bakatselou V TenHoor CN, and Dressman JB. Estimation of the Increase in Solubility of Drugs as a Function of Bile Salt Concentration. Pharm Res 1996; 13(1):163-167

Mooney KG, Mintun MA, Himmelstein KJ, and Stella VJ. Dissolution Kinetics of Carboxylic Acids I: Effect of pH Under Unbuffered Conditions. J Pharm Sci 1981a; 70(1):13-22

Mooney KG, Mintun MA, Himmelstein KJ, and Stella VJ. Dissolution Kinetics of Carboxylic Acids II: Effect of Buffers. J Pharm Sci 1981b; 70(1):22-32

Morris KR, Fakes MG, Thakur AB, Newman AW, Singh AK, Venit JJ, Sagnuolo CJ, and Serajuddin, ATM. An Integrated Approach to the Selection of Optimal Salt Form for a New Drug Candidate. Int J Pharm 1994; 105(3):209-217

Nerurkar MM, Burton PS, and Borchardt RT. The Use of Surfactants to Enhance the Permeability of Peptides Through Caco-2 Cells by Inhibition of an Apically Polarized Efflux system. Pharm Res 1996; 13(4):528-534

Oh D-M, Curl RL, and Amidon GL. Estimating the Fraction Dose Absorbed from Suspensions of Poorly Soluble Compounds in Humans: A Mathematical Model. Pharm Res 1993; 10(2):264-270

Oh D-M, Curl RL, Yong C-S, and Amidon GL. Effect of Micronization on the Extent of Drug Absorption from Suspensions in Humans. Arch Pharmacal Res 1995; 18(6):427-433

Olah MM, Bologa CG, and Oprea TI. Strategies for Compound Selection. Current Drug Discovery Technologies 2004; 1(3):211-220

Oprea TI. Current trends in lead discovery: Are We Looking for the Appropriate Properties? J Computer-Aided Molecular Design 2002; 16(5/6):325-334

Oprea TI, Davis AM, Teague SJ, and Leeson PD. Is There a Difference Between Leads and Drugs? A Historical Perspective. J Chemical Info Computer Sciences 2001; 41(5):1308-1315

Pellet MA, Davis AF, and Hadgraft J. Effect of Supersaturation on Membrane Transport: 2. Piroxicam. Int J Pharm 1994; 111:1-6

Pellet MA, Castellano S, Hadgraft J, and Davis AF. The Penetration of Supersaturated Solutions of Piroxicam Across Silicone Membranes and Human Skin In Vitro. J Control Rel 1997; 46:205-214

Poelma FGJ, Breas R, and Tukker JJ. Intestinal Absorption of Drugs. III. The Influence of Taurocholate on the Disappearance Kinetics of Hydrophilic and Lipophilic Drugs from the Small Intestine of the Rat. Pharm Res 1990; 7:392397

Pouton CW. Formulations of Self-Emulsifying Drug Delivery Systems. Adv Drug Delev Rev 1997; 25:47-48

Rajewski RA, and Stella VJ. Pharmaceutical Aplications of Cyclodextrins. 2. In Vivo Drug Delivery. J Pharm Sci 1996; 85(11):1142-1169

Ranson M, Howell A, Cheeseman S, and Margison J. Liposomal Drug Delivery.

Cancer Treat Rev 1996; 22(5):365-379

Raub T J; Barsuhn C L; Williams L R; Decker D E; Sawada G A; and Ho N F Use of a Biophysical-Kinetic Model to Understand the Roles of Protein Binding and Membrane Partitioning on Passive Diffusion of Highly Lipophilic Molecules Across Cellular Barriers. J Drug Targ 1993; 1(4):269-286

Raub TJ, Bauer JM, Goodman TG, Hageman MJ, and Bajt-Jaeschke ML unpublished results, Pharmacia & Upjohn 1999

Rishton GM. Nonleadlikeness and Leadlikeness in Biochemical Screening. Drug Discovery Today 2002, 2003; 8(2):86-96

Schulze JDR, Waddington WA, Ell PJ, Parsons GE, Coffin MD, and Basit, AW. Concentration-Dependent Effects of Polyethylene Glycol 400 on Gastrointestinal Transit and Drug Absorption. Pharm Res 2003; 20(12):1984-1988

Serajuddin ATM. Solid Dispersion of Poorly Water-soluble Drugs: Early Promises, Subsequent Problems, and Recent Breakthroughs. J Pharm Sci 1999; 88(10):1058-1066

Thompson DO. Cyclodextrins -Enabling Excipients: Their Present and Future Use in Pharmaceuticals. Crit Rev Therap Drug Carrier Syst 1997; 14:1-104

Tong WQ, and Whitesell G. In situ Salt Screening - A Useful Technique for Discovery Support and Preformulation Studies. Pharm Dev Tech 1998; 3(2):215-223

Wade A, and Weller PJ. Handbook of Pharmaceutical Excipients, 2nd ed., American Pharmaceutical Association, Washington, DC, 1994

Wang Y, Mesfin GM, Rodriguez CA, Slatter JG, Schuette MR, Cory AL, and Higgins MJ. Venous Irritation, Pharmacokinetics, and Tissue Distribution of Tirilazad in Rats Following Intravenous Administration of a Novel Supersaturated Submicron Lipid Emulsion. Pharm Res 1999; 16(6):930-938

Ware EC, and Lu DR. An Automated Approach to Salt Selection for New Unique Trazodone Salts. Pharm Res 2004; 21(1):177-184

Yalkowsky SH. Solubility and Solubilization in Aqueous Media Oxford Univ Press, New York, 1999

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