By Alex Avdeef(auth.)
Explains how you can practice and study the result of the newest physicochemical methods
With this booklet as their advisor, readers have entry to all of the present details had to completely examine and properly be sure a compound's pharmaceutical homes and their results on drug absorption. The publication emphasizes oral absorption, explaining the entire physicochemical equipment used this day to research drug applicants. additionally, the writer offers specialist tips to aid readers research the result of their experiences so one can decide on the main promising drug candidates.
This Second Edition has been completely up-to-date and revised, incorporating the entire most up-to-date examine findings, tools, and assets, including:
Descriptions and functions of recent PAMPA types, drawing on greater than thirty papers released by way of the author's study group
Two new chapters analyzing permeability and Caco-2/MDCK and permeability and the blood-brain barrier
Expanded details and strategies to aid pKa determination
New examples explaining the remedy of virtually insoluble try compounds
Additional case experiences demonstrating using the newest physicochemical techniques
New, revised, and increased database tables during the book
Well over two hundred drawings aid readers higher comprehend tough strategies and supply a visible advisor to advanced approaches. furthermore, over 800 references function a gateway to the first literature within the box, facilitating additional study into all of the issues lined within the book.
This Second Edition is usually recommended as a reference for researchers in pharmaceutical R&D in addition to in agrochemical, environmental, and different similar parts of study. it's also instructed as a supplemental textual content for graduate classes in pharmaceutics.
Chapter 1 creation (pages 1–11):
Chapter 2 shipping version (pages 12–30):
Chapter three pKa selection (pages 31–173):
Chapter four Octanol–Water Partitioning (pages 174–219):
Chapter five Liposome–Water Partitioning (pages 220–250):
Chapter 6 Solubility (pages 251–318):
Chapter 7 Permeability—PAMPA (pages 319–498):
Chapter eight Permeability: Caco?2/MDCK (pages 499–574):
Chapter nine Permeability: Blood–Brain Barrier (pages 575–680):
Chapter 10 precis and a few easy Approximations (pages 681–684):
Read Online or Download Absorption and Drug Development: Solubility, Permeability, and Charge State, Second Edition PDF
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Additional resources for Absorption and Drug Development: Solubility, Permeability, and Charge State, Second Edition
Pharm. Sci. 94, 1–16 (2005). 17. Bergström, C. A. ; Artursson, P. Accuracy of calculated pH-dependent aqueous drug solubility. Eur. J. Pharm. Sci. 22, 387–398 (2004). 18. ; Kansy, M. Solubility—Excipient classiﬁcation gradient maps. Pharm. Res. 24, 530–545 (2007). 19. Avdeef, A. Solubility of sparingly-soluble drugs. [Dressman, J; Reppas, C. ). Special issue: The Importance of Drug Solubility]. Adv. Drug Deliv. Rev. 59, 568–590 (2007). 20. ; Fischer, H. Advances in screening for membrane permeability: High-resolution PAMPA for medicinal chemists.
Eur. J. Pharm. Sci. 24, 333–349 (2005). 22. Avdeef, A. The rise of PAMPA. Expert Opinion Drug Metab. Toxicol. 1, 325–342 (2005). 23. ; Yamauchi, Y. PAMPA—A useful tool in drug discovery. J. Pharm. Sci. 96, 2893–2909 (2007). 24. ; Ecker, G. ; Senner, F. Coexistence of passive and active carrier-mediated uptake processes in drug transport: A more balanced view. Nature Rev. Drug Discov. 9, 597–614 (2010). REFERENCES 11 25. Lipinski, C. A. Avoiding investment in doomed drugs—Is solubility an industry wide problem?
J. Pharm. Sci. 24, 333–349 (2005). 22. Avdeef, A. The rise of PAMPA. Expert Opinion Drug Metab. Toxicol. 1, 325–342 (2005). 23. ; Yamauchi, Y. PAMPA—A useful tool in drug discovery. J. Pharm. Sci. 96, 2893–2909 (2007). 24. ; Ecker, G. ; Senner, F. Coexistence of passive and active carrier-mediated uptake processes in drug transport: A more balanced view. Nature Rev. Drug Discov. 9, 597–614 (2010). REFERENCES 11 25. Lipinski, C. A. Avoiding investment in doomed drugs—Is solubility an industry wide problem?