메뉴 건너뛰기




Volumn 33, Issue 1, 2008, Pages 29-41

Absorption-excipient-pH classification gradient maps: Sparingly soluble drugs and the pH partition hypothesis

Author keywords

Absorption; Absorption excipient pH; Double sink PAMPA; Excipients; HP CD; Low solubility; NMP; PEG400; Propylene glycol; Sodium taurocholate

Indexed keywords

2 HYDROXYPROPYL BETA CYCLODEXTRIN; 2 PYRROLIDONE DERIVATIVE; ALBENDAZOLE; AMIODARONE; ASTEMIZOLE; BUTACAINE; CLOTRIMAZOLE; DIPYRIDAMOLE; EXCIPIENT; GLIBENCLAMIDE; GRISEOFULVIN; MACROGOL 400; MEFENAMIC ACID; METHYL 2 PYRROLIDONE; NAPROXEN; POTASSIUM CHLORIDE; PROGESTERONE; PROPYLENE GLYCOL; TAUROCHOLIC ACID; UNCLASSIFIED DRUG;

EID: 36849018496     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejps.2007.09.009     Document Type: Article
Times cited : (43)

References (42)
  • 1
    • 36849047492 scopus 로고    scopus 로고
    • Advanced Chemistry Development Inc., Toronto, Canada. ACD/Solubility DB computer program (www.acdlabs.com, last accessed 15 September 2006).
  • 2
    • 0028948839 scopus 로고
    • A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability
    • Amidon G.L., Lennernäs H., Shah V.P., and Crison J.R. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 12 (1995) 413-420
    • (1995) Pharm. Res. , vol.12 , pp. 413-420
    • Amidon, G.L.1    Lennernäs, H.2    Shah, V.P.3    Crison, J.R.4
  • 3
    • 0002311366 scopus 로고    scopus 로고
    • High-throughput measurements of solubility profiles
    • Testa B., van de Waterbeemd H., Folkers G., and Guy R. (Eds), Verlag Helvetica Chimica Acta: Zürich and Wiley - VCH, Weinheim
    • Avdeef A. High-throughput measurements of solubility profiles. In: Testa B., van de Waterbeemd H., Folkers G., and Guy R. (Eds). Pharmacokinetic Optimization in Drug Research (2001), Verlag Helvetica Chimica Acta: Zürich and Wiley - VCH, Weinheim 305-326
    • (2001) Pharmacokinetic Optimization in Drug Research , pp. 305-326
    • Avdeef, A.1
  • 6
    • 36849025584 scopus 로고    scopus 로고
    • HT solubility and permeability: MAD-PAMPA analysis
    • Krämer S.D., Folkers G., and Testa B. (Eds), Wiley-VCH, Weinheim
    • Avdeef A. HT solubility and permeability: MAD-PAMPA analysis. In: Krämer S.D., Folkers G., and Testa B. (Eds). Physicochemical and Biological Profiling in Drug Research (2006), Wiley-VCH, Weinheim 221-241
    • (2006) Physicochemical and Biological Profiling in Drug Research , pp. 221-241
    • Avdeef, A.1
  • 9
    • 0036809320 scopus 로고    scopus 로고
    • Physicochemical profiling in drug research: a brief state-of-the-art of experimental techniques
    • Avdeef A., and Testa B. Physicochemical profiling in drug research: a brief state-of-the-art of experimental techniques. Cell. Mol. Life Sci. 59 (2003) 1681-1689
    • (2003) Cell. Mol. Life Sci. , vol.59 , pp. 1681-1689
    • Avdeef, A.1    Testa, B.2
  • 10
    • 84906468942 scopus 로고    scopus 로고
    • Dissolution - Solubility: pH, Buffer, Salt, Dual-Solid, and Aggregation Effects
    • Testa B., and van de Waterbeemd H. (Eds), Elsevier, Oxford, UK
    • Avdeef A., Voloboy D., and Foreman A. Dissolution - Solubility: pH, Buffer, Salt, Dual-Solid, and Aggregation Effects. In: Testa B., and van de Waterbeemd H. (Eds). Comprehensive Medicinal Chemistry II, Vol. 5 ADME-TOX Approaches (2007), Elsevier, Oxford, UK 399-423
    • (2007) Comprehensive Medicinal Chemistry II, Vol. 5 ADME-TOX Approaches , pp. 399-423
    • Avdeef, A.1    Voloboy, D.2    Foreman, A.3
  • 13
    • 3242717497 scopus 로고    scopus 로고
    • Accuracy of calculated pH-dependent aqueous drug solubility
    • Bergström C.A.S., Luthman K., and Artursson P. Accuracy of calculated pH-dependent aqueous drug solubility. Eur. J. Pharm. Sci. 22 (2004) 387-398
    • (2004) Eur. J. Pharm. Sci. , vol.22 , pp. 387-398
    • Bergström, C.A.S.1    Luthman, K.2    Artursson, P.3
  • 15
    • 0031741846 scopus 로고    scopus 로고
    • Physical chemical properties of oral drug candidates in the discovery and exploratory development settings
    • Curatolo W. Physical chemical properties of oral drug candidates in the discovery and exploratory development settings. Pharm. Sci. Tech. Today 1 (1998) 387-393
    • (1998) Pharm. Sci. Tech. Today , vol.1 , pp. 387-393
    • Curatolo, W.1
  • 16
    • 0022070123 scopus 로고
    • Absorption potential: estimating the fraction absorbed for orally administered compounds
    • Dressman J.B., Amidon G.L., and Fleisher D. Absorption potential: estimating the fraction absorbed for orally administered compounds. J. Pharm. Sci. 74 (1985) 588-589
    • (1985) J. Pharm. Sci. , vol.74 , pp. 588-589
    • Dressman, J.B.1    Amidon, G.L.2    Fleisher, D.3
  • 17
    • 0003110845 scopus 로고    scopus 로고
    • Physicochemical parameters as tools in drug discovery and lead optimization
    • Testa B., van de Waterbeemd H., Folkers G., and Guy R. (Eds), Verlag Helvetica Chimica Acta, Zürich and Wiley - VCH, Weinheim
    • Faller B., and Wohnsland F. Physicochemical parameters as tools in drug discovery and lead optimization. In: Testa B., van de Waterbeemd H., Folkers G., and Guy R. (Eds). Pharmacokinetic Optimization in Drug Research (2001), Verlag Helvetica Chimica Acta, Zürich and Wiley - VCH, Weinheim 257-274
    • (2001) Pharmacokinetic Optimization in Drug Research , pp. 257-274
    • Faller, B.1    Wohnsland, F.2
  • 18
    • 0037448408 scopus 로고    scopus 로고
    • Bioavailability and efficacy characteristics of two different oral liquid formulations of albendazole
    • Garcia J.J., Bolás F., and Torrado J.J. Bioavailability and efficacy characteristics of two different oral liquid formulations of albendazole. Int. J. Pharm. 250 (2003) 351-358
    • (2003) Int. J. Pharm. , vol.250 , pp. 351-358
    • Garcia, J.J.1    Bolás, F.2    Torrado, J.J.3
  • 19
    • 12244263506 scopus 로고    scopus 로고
    • Comparison of a miniaturized shake-flask solubility method with automated potentiometric acid/base titrations and calculated solubilities
    • Glomme A., März J., and Dressman J.B. Comparison of a miniaturized shake-flask solubility method with automated potentiometric acid/base titrations and calculated solubilities. J. Pharm. Sci. 94 (2005) 1-16
    • (2005) J. Pharm. Sci. , vol.94 , pp. 1-16
    • Glomme, A.1    März, J.2    Dressman, J.B.3
  • 20
    • 36849094590 scopus 로고    scopus 로고
    • Guidance for Industry, Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System, FDA, Washington, DC, USA, August 2000.
  • 22
    • 0020540853 scopus 로고
    • Drug absorption by the rat jejunum perfused in situ. Dissociation from the pH-partition theory and the role of microclimate-pH and unstirred layer
    • Högerle M.L., and Winne D. Drug absorption by the rat jejunum perfused in situ. Dissociation from the pH-partition theory and the role of microclimate-pH and unstirred layer. Naunyn-Schmiedeberg's Arch. Pharmacol. 322 (1983) 249-255
    • (1983) Naunyn-Schmiedeberg's Arch. Pharmacol. , vol.322 , pp. 249-255
    • Högerle, M.L.1    Winne, D.2
  • 23
    • 0000845392 scopus 로고
    • Drug transport across gastrointestinal epithelia
    • Johnson L.R. (Ed), Raven Press, New York
    • Jackson M.J. Drug transport across gastrointestinal epithelia. In: Johnson L.R. (Ed). Physiology of the Gastrointestinal Tract. second ed. (1987), Raven Press, New York 1597-1621
    • (1987) Physiology of the Gastrointestinal Tract. second ed. , pp. 1597-1621
    • Jackson, M.J.1
  • 24
    • 0030444550 scopus 로고    scopus 로고
    • Guidance in the setting of drug particle size specifications to minimize variability in absorption
    • Johnson K., and Swindell A. Guidance in the setting of drug particle size specifications to minimize variability in absorption. Pharm. Res. 13 (1996) 1795-1798
    • (1996) Pharm. Res. , vol.13 , pp. 1795-1798
    • Johnson, K.1    Swindell, A.2
  • 25
    • 13244271270 scopus 로고    scopus 로고
    • Advances in screening for membrane permeability: high-resolution PAMPA for medicinal chemists
    • Kansy M., Avdeef A., and Fischer H. Advances in screening for membrane permeability: high-resolution PAMPA for medicinal chemists. Drug Discov. Today: Technol. 1 (2005) 349-355
    • (2005) Drug Discov. Today: Technol. , vol.1 , pp. 349-355
    • Kansy, M.1    Avdeef, A.2    Fischer, H.3
  • 26
    • 0034461768 scopus 로고    scopus 로고
    • Drug-like properties and the causes of poor solubility and poor permeability
    • Lipinski C.A. Drug-like properties and the causes of poor solubility and poor permeability. J. Pharmacol. Toxicol. Methods 44 (2000) 235-249
    • (2000) J. Pharmacol. Toxicol. Methods , vol.44 , pp. 235-249
    • Lipinski, C.A.1
  • 27
    • 0020613211 scopus 로고
    • Determination of acid surface pH in vivo in rat proximal jejunum
    • Lucas M. Determination of acid surface pH in vivo in rat proximal jejunum. Gut 24 (1983) 734-739
    • (1983) Gut , vol.24 , pp. 734-739
    • Lucas, M.1
  • 29
    • 0033815655 scopus 로고    scopus 로고
    • Estimating log P with atom/fragments and water solubility with log P
    • Maylan W.M., and Howard P.H. Estimating log P with atom/fragments and water solubility with log P. Perspect. Drug Discov. Des. 19 (2000) 67-84
    • (2000) Perspect. Drug Discov. Des. , vol.19 , pp. 67-84
    • Maylan, W.M.1    Howard, P.H.2
  • 30
    • 0023747201 scopus 로고
    • The effect of Escherichia coli STa enterotoxin and other secretagogues on mucosal surface pH of rat small intestine in vivo
    • McEwan G.T.A., Daniel H., Fett C., Bergess M.N., and Lucas M.L. The effect of Escherichia coli STa enterotoxin and other secretagogues on mucosal surface pH of rat small intestine in vivo. Proc. R. Soc. London B. Biol. Sci. 234 (1988) 219-237
    • (1988) Proc. R. Soc. London B. Biol. Sci. , vol.234 , pp. 219-237
    • McEwan, G.T.A.1    Daniel, H.2    Fett, C.3    Bergess, M.N.4    Lucas, M.L.5
  • 31
    • 36849078972 scopus 로고    scopus 로고
    • Pharma Algorithms, 2006. Toronto, Canada. Algorithm Builder V1.8 and ADME Boxes V2.5 computer programs (www.ap-algorithms.com, last accessed 15 September 2006).
  • 32
    • 0000890758 scopus 로고
    • Transport of weak electrolytes
    • Schultz S.G. (Ed), The Gastrointestinal System, Am. Physiol. Soc, Bethesda, MD
    • Rechkemmer G. Transport of weak electrolytes. In: Schultz S.G. (Ed). Handbook of Physiology. Sec. 6. (1991), The Gastrointestinal System, Am. Physiol. Soc, Bethesda, MD 371-388
    • (1991) Handbook of Physiology. Sec. 6. , pp. 371-388
    • Rechkemmer, G.1
  • 33
    • 0018557299 scopus 로고
    • Mucin layer in the large intestine
    • Saikata T., and von Engelhardt W. Mucin layer in the large intestine. Ann. Rech. Vet. 10 (1979) 485-487
    • (1979) Ann. Rech. Vet. , vol.10 , pp. 485-487
    • Saikata, T.1    von Engelhardt, W.2
  • 34
    • 0031786697 scopus 로고    scopus 로고
    • Co-administration of a water-soluble polymer increases the usefulness of cyclodextrins in solid oral dosage forms
    • Savolainen J., Järvinen K., Taipale H., Jarho P., Loftsson T., and Järvinen T. Co-administration of a water-soluble polymer increases the usefulness of cyclodextrins in solid oral dosage forms. Pharm. Res. 15 (1998) 1696-1701
    • (1998) Pharm. Res. , vol.15 , pp. 1696-1701
    • Savolainen, J.1    Järvinen, K.2    Taipale, H.3    Jarho, P.4    Loftsson, T.5    Järvinen, T.6
  • 39
    • 0037433788 scopus 로고    scopus 로고
    • Prediction of human intestinal permeability using artificial membrane permeability
    • Sugano K., Nabuchi Y., Machida M., and Aso Y. Prediction of human intestinal permeability using artificial membrane permeability. Int. J. Pharm. 257 (2003) 245-251
    • (2003) Int. J. Pharm. , vol.257 , pp. 245-251
    • Sugano, K.1    Nabuchi, Y.2    Machida, M.3    Aso, Y.4
  • 40
    • 0028029150 scopus 로고
    • Transcellular transport of benzoic acid across Caco-2 cells by a pH-dependent and carrier-mediated transport mechanism
    • Tsuji A., Takanaga H., Tamai I., and Terasaki T. Transcellular transport of benzoic acid across Caco-2 cells by a pH-dependent and carrier-mediated transport mechanism. Pharm. Res. 11 (1994) 30-37
    • (1994) Pharm. Res. , vol.11 , pp. 30-37
    • Tsuji, A.1    Takanaga, H.2    Tamai, I.3    Terasaki, T.4
  • 41
    • 0035953319 scopus 로고    scopus 로고
    • Property-based design: optimization of drug absorption and pharmacokinetics
    • van de Waterbeemd H., Smith D.A., Beaumont K., and Walker D.K. Property-based design: optimization of drug absorption and pharmacokinetics. J. Med. Chem. 44 (2001) 1313-1333
    • (2001) J. Med. Chem. , vol.44 , pp. 1313-1333
    • van de Waterbeemd, H.1    Smith, D.A.2    Beaumont, K.3    Walker, D.K.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.