Discovery pharmaceutics - Challenges and opportunities

AAPS Journal

Volumn 8, Issue 2, 2006, Pages

  Chen, Xue Qing ^a   Antman, Melissa D ^a   Gesenberg, Christoph ^a   Gudmundsson, Olafur S ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

Physicochemical properties; Preformulation; Solubility; Stability

Indexed keywords

DIMETHYL SULFOXIDE; DRUG; DRUG VEHICLE;

CONTROLLED STUDY; DRUG DEGRADATION; DRUG DOSAGE FORM; DRUG FORMULATION; DRUG INDUSTRY; DRUG RESEARCH; DRUG SOLUBILITY; DRUG SOLUTION; DRUG STABILITY; IONIZATION; LIGHT EXPOSURE; LIPOPHILICITY; OXIDATION; PH; PHYSICAL CHEMISTRY; SHORT SURVEY; SOLID STATE; SUSPENSION; TOXICITY TESTING;

BIOPHARMACEUTICS; DRUG INDUSTRY; DRUG THERAPY; FORECASTING; LIPIDS; PHARMACEUTICAL PREPARATIONS; SOLUBILITY; SURFACE PROPERTIES;

EID: 33745070265     PISSN: 15507416     EISSN: None     Source Type: Journal    
DOI: 10.1208/aapsj080246     Document Type: Short Survey

References (33)

1. Florence AT. Attwood D. Physicochemical Principles of Pharmacy: London. UK: Macmillan Press: 1998.
2. Gudmundsson OS. Venkatesh S. Strategies for in silico and experimental screening of physicochemical properties. In: Borchardt RT. Kerns EH. Lipinski CA. Thakker DR. Wang B. eds. Pharmaceutical Pro ling in Drug Discovery for Lead Selection. Arlington. VA: AAPS Press: 2004:393-412.
3. Kerns E. High throughput physicochemical pro ling for drug discovery. J Pharm Sci. 2001:90:1838-1858.
4. Di L. Kerns EH. Pro ling drug-like properties in discovery research. Curr Opin Chem Biol. 2003:7:402-408.
5. Hageman MJ. Solubility. solubilization. and dissolution in drug delivery during lead optimization. AAPS Workshop of Optimization of Drug-Like Properties During Lead Optimization: September 19-22. 2004: Parsippany. NJ.
6. Lipinski CA. Lombardo F. Dominy BW. Feeney PJ. Experimental and computational approaches to estimate solubility and permeability in drug discover and development settings. Adv Drug Deliv Rev. 2001:46:3-26.
7. Bevan CD. Lloyd RSA. High-throughput screening method for the determination of aqueous drug solubility using laser nephelometry in microtiter plates. Anal Chem. 2000:72:1781-1787.
8. Di L. Kerns EH. Pro ling drug-like properties in discovery research. Curr Opin Chem Biol. 2003:7:402-408.
9. Hancock BC. Parks M. What is the true solubility advantage for amorphous pharmaceuticals? Pharm Res. 2000:17:397-404.
10. Pudipeddi M. Serajuddin ATM. Trends in solubility of polymorphs. J Pharm Sci. 2005:94:929-939.
11. Huang LF. Tong WQ. Impact of solid state properties on developability assessment of drug candidates. Adv Drug Deliv Rev. 2004:56:321-334.
12. Jia Z. Ramstad T. Zhong M. Medium-throughput pKa screening of pharmaceuticals by pressure-assisted capillary electrophoresis. Electrophoresis. 2001:22:1112-1118.
13. Albert A. Serjeant EP. The Determination of Ionization Constants: A Laboratory Manual, London: Chapman & Hall: 1984.
14. Comer J. Tam K. Lipophilicity pro les: theory and measurement. In: Testa B. van de Waterbeemd H. Folkers G. Guy R. eds. Pharmacokinetic Optimization in Drug Research: Biological, Physicochemical, and Computational Strategies. Zurich. Switzerland: VCHA and Wiley-VCH: 2001:275-304.
15. Yamagami C. Recent advances in reversed-phase-HPLC techniques to determine lipophilicity. In: Testa B. van de Waterbeemd H. Folkers G. Guy R. eds. Pharmacokinetic Optimization in Drug Research: Biological, Physicochemical, and Computational Strategies. Zurich. Switzerland: VCHA and Wiley-VCH: 2001.
16. Kodavanti UP. Mehendale HM. Cationic amphiphilic drugs and phospholipid storage disorder. Pharmacol Rev. 1990:42:327-354.
17. Adamson AW. Gast AP. Physical Chemistry of Surfaces. New York. NY: John Wiley and Sons: 1997.
18. ICH. Stability Testing of New Drug Substances and Products. Geneva. Switzerland: IFPMA: 2003.
19. Fiese EF. General pharmaceutics - the new physical pharmacy. J Pharm Sci. 2003:92:1331-1342.
20. Bakshi M. Singh S. Development of validated stability-indicating assay methods - critical review. J Pharm Biomed Anal. 2002:28:1011-1040.
21. Shah KP. Zhou J. Lee R. et al. Automated analytical systems for drug development studies. I: a system for the determination of drug stability. J Pharm Biomed Anal. 1994:12:993-1001.
22. Sims JL. Roberts JK. Bateman AG. Carreira JA. Hardy MJ. An automated workstation for forced degradation of active pharmaceutical ingredients. J Pharm Sci. 2002:91:884-892.
23. Bakshi M. Singh S. ICH guidance in practice: establishment of inherent stability of seenidazole and development of a validated stability-indicating high-performance liquid chromatographic assay method. J Pharm Biomed Anal. 2004:36:769-775.
24. Byrn SR. Xu W. Newman AW. Chemical reactivity in solid-state pharmaceuticals: formulation implications. Adv Drug Deliv Rev. 2001:48:115-136.
25. Hovorka S. Schoneich C. Oxidative degradation of pharmaceuticals: theory. mechanisms and inhibition. J Pharm Sci. 2001:90:253-269.
26. Waterman KC. Adami RC. Alsante KM. et al. Stabilization of pharmaceuticals to oxidative degradation. Pharm Dev Technol. 2002:7:1-32.
27. Simon P. Veverka M. Oluliar J. New screening method for the determination of stability of pharmaceuticals. Int J Pharm. 2004:270:21-26.
28. Tonnesen HH. Formulation and stability testing of photolabile drugs. Int J Pharm. 2001:225:1-14.
29. Rourick RA. Volk KJ. Klohr E. Spears T. Kerns EH. Lee MS. Predictive strategy for the rapid structure elucidation of drug degradants. J Pharm Biomed Anal. 1996: 14:1743-1752.
30. Rowe RC. Sheskey PJ. Weller PJ. Handbook of Pharmaceutical Excipients. London. UK: Pharmaceutical Press: 2003.
31. Sweetana S. Akers MJ. Solubility principles and practices for parenteral drug dosage form development. PDA J Pharm Sci Technol. 1996:50:330-342.
32. Simamora P. Pinsuwan S. Alvarez JM. Myrdal PB. Yalkowsky SH. Effect of pH on injection phlebitis. J Pharm Sci. 1995:84:520-522.
33. Johnson JLH. He Y. Yalkowsky SH. Prediction of precipitation-induced phlebitis: a statistical validation of an in vitro model. J Pharm Sci. 2003:92:1574-1581.