By Alex Avdeef(auth.)

Explains the way to practice and research the result of the most recent physicochemical methods

With this e-book as their advisor, readers have entry to all of the present info had to completely examine and effectively ensure a compound's pharmaceutical homes and their results on drug absorption. The ebook emphasizes oral absorption, explaining the entire physicochemical tools used this day to investigate drug applicants. in addition, the writer offers specialist information to aid readers research the result of their stories on the way to decide on the main promising drug candidates.

This Second Edition has been completely up to date and revised, incorporating all of the most modern study findings, equipment, and assets, including:

  • Descriptions and functions of recent PAMPA versions, drawing on greater than thirty papers released by way of the author's learn group

  • Two new chapters studying permeability and Caco-2/MDCK and permeability and the blood-brain barrier

  • Expanded details and techniques to help pKa determination

  • New examples explaining the therapy of virtually insoluble attempt compounds

  • Additional case experiences demonstrating using the most recent physicochemical techniques

  • New, revised, and accelerated database tables through the book

Well over two hundred drawings aid readers larger comprehend tricky innovations and supply a visible advisor to advanced approaches. additionally, over 800 references function a gateway to the first literature within the box, facilitating additional learn into the entire issues lined within the book.

This Second Edition is suggested as a reference for researchers in pharmaceutical R&D in addition to in agrochemical, environmental, and different similar components of analysis. it's also steered 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 uncomplicated Approximations (pages 681–684):

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Additional resources for Absorption and Drug Development: Solubility, Permeability, and Charge State, Second Edition

Sample text

Curr. Topics Med. Chem. 1, 277–351 (2001). 3) The relevance of Eq. 2) (which predicts how quickly molecules pass through simple membranes) to solubility comes in the concentration terms. Consider “sink” conditions, where CR is essentially zero. 4) Flux depends on the product of membrane permeability of the solute times the concentration of the solute (summed over all charge state forms) at the water side of the donor surface of the membrane. This concentration ideally may be equal to the dose of the drug, unless the dose exceeds the solubility limit at the pH considered, in which case it is equal to the solubility.

Smith, D. ; Jones, B. C. Lipophilicity in PK design: Methyl, ethyl, futile. J. -Aided Molec. Design 15, 273–286 (2001). 29. ; Smith, D. ; Walker, D. K. Property-based design: Optimization of drug absorption and pharmacokinetics. J. Med. Chem. 44, 1313–1333 (2001). 2 TRANSPORT MODEL This chapter defines the relationship between ionization constants, solubility, and permeability as a function of pH, using the framework of Fick’s laws of diffusion. In simplest terms, the flux across a membrane barrier is a product function of solubility and permeability in saturated solutions.

The tight junctions and the basement membrane appear to be slightly ion-selective (lined with some negatively charged groups) [29, 30, 33]. [Reprinted from Avdeef, A. Curr. Topics Med. Chem. 1, 277–351 (2001). ] The intestinal cells are joined at the tight junctions [19, 29]. These junctions have pores that can allow small molecules (MW < 200 Da) to diffuse through in aqueous solution. In the jejunum, the pores are about 7–9 Å in size. , dimensions of mannitol) [19]. 5). 7:1 [19]. The half-life of these proteins is about 6–12 h, whereas the epithelial cells last 2–3 days.

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