By Alex Avdeef

ISBN-10: 0471423653

ISBN-13: 9780471423652

Time and again medicines paintings superb whilst verified outdoors the physique, but if they're demonstrated within the physique they fail. one of many significant purposes a drug fails is that it can't be take up via the physique in how to have the impact it used to be meant to have. Permeability, Solubility, Dissolution, and Charged nation of Ionizable Molecules:

  • Helps drug discovery pros to dispose of poorly absorbable molecules early within the drug discovery method, that could shop drug businesses thousands of dollars.
  • Extensive tabulations, in appendix layout, of homes and constructions of approximately 2 hundred normal drug molecules.

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Additional info for Absorption and Drug Development: Solubility, Permeability, and Charge State

Example text

1a represents a strong acid–base titration, containing no sample species. The curve on the right side of Fig. 1a is that of morphine-6! XHÆ ! XHÀ ! X2À) glucuronide (M6G), which has three pKa values (XHþ 2 3 [151]. 5 and 10 in the right curve). 5). 8 in the morphine metabolite curve). At such a point the molecule is present in two states of protonation of equal concentration (pH ¼ pKa ), unless two or more overlapping pKa values are in the buffer region. So by inspection of Fig. 8. ) Where are the other pKa values of M6G?

5 and 10 in the right curve). 5). 8 in the morphine metabolite curve). At such a point the molecule is present in two states of protonation of equal concentration (pH ¼ pKa ), unless two or more overlapping pKa values are in the buffer region. So by inspection of Fig. 8. ) Where are the other pKa values of M6G? Unfortunately, a titration curve does not always reveal all the pKa values that a molecule may have. To reveal the other two pKa values of M6G and to test for overlapping pKa values, it is necessary to transform the titration curves into Bjerrum plots [112,116,118,153,163–165].

The left curve in Fig. 1a represents a strong acid–base titration, containing no sample species. The curve on the right side of Fig. 1a is that of morphine-6! XHÆ ! XHÀ ! X2À) glucuronide (M6G), which has three pKa values (XHþ 2 3 [151]. 5 and 10 in the right curve). 5). 8 in the morphine metabolite curve). At such a point the molecule is present in two states of protonation of equal concentration (pH ¼ pKa ), unless two or more overlapping pKa values are in the buffer region. So by inspection of Fig.

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Absorption and Drug Development: Solubility, Permeability, and Charge State by Alex Avdeef


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