메뉴 건너뛰기




Volumn 41, Issue 1, 2010, Pages 23-30

The influence of aqueous content in small scale salt screening-Improving hit rate for weakly basic, low solubility drugs

Author keywords

Crystallization; High throughput; Low water solubility; Physical form selection; Salt screening

Indexed keywords

ATROPINE; CINNARIZINE; CLOTRIMAZOLE; ITRACONAZOLE; SODIUM CHLORIDE; DRUG; INORGANIC SALT; WATER;

EID: 77954759851     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejps.2010.05.009     Document Type: Article
Times cited : (22)

References (22)
  • 2
    • 0034345216 scopus 로고    scopus 로고
    • Salt selection and optimization procedures for pharmaceutical new chemical entities
    • Bastin R.J., Bowker M.J., Slater B.J. Salt selection and optimization procedures for pharmaceutical new chemical entities. Org. Proc. Res. Dev. 2000, 4:427-435.
    • (2000) Org. Proc. Res. Dev. , vol.4 , pp. 427-435
    • Bastin, R.J.1    Bowker, M.J.2    Slater, B.J.3
  • 4
    • 34249088975 scopus 로고    scopus 로고
    • Structure, solubility, screening, and synthesis of molecular salts
    • Black S.N., Collier E.A., Davey R.J., Roberts R.J. Structure, solubility, screening, and synthesis of molecular salts. J. Pharm. Sci. 2007, 96:1053-1068.
    • (2007) J. Pharm. Sci. , vol.96 , pp. 1053-1068
    • Black, S.N.1    Collier, E.A.2    Davey, R.J.3    Roberts, R.J.4
  • 5
    • 58149242453 scopus 로고    scopus 로고
    • Aqueous versus non-aqueous salt delivery strategies to enhance oral bioavailability of a mitogen-activated protein kinase-activated protein kinase (MK-2) inhibitor in rats
    • Chiang P.C., South S.A., Daniels J.S., Anderson D.R., Wene S.P., Albin L.A., Mourey R.J., Selbo J.G. Aqueous versus non-aqueous salt delivery strategies to enhance oral bioavailability of a mitogen-activated protein kinase-activated protein kinase (MK-2) inhibitor in rats. J. Pharm. Sci. 2009, 98:248-256.
    • (2009) J. Pharm. Sci. , vol.98 , pp. 248-256
    • Chiang, P.C.1    South, S.A.2    Daniels, J.S.3    Anderson, D.R.4    Wene, S.P.5    Albin, L.A.6    Mourey, R.J.7    Selbo, J.G.8
  • 6
    • 0035835965 scopus 로고    scopus 로고
    • Changing the salt, changing the drug
    • Davies G. Changing the salt, changing the drug. Pharm. J. 2001, 266:322-323.
    • (2001) Pharm. J. , vol.266 , pp. 322-323
    • Davies, G.1
  • 7
    • 8844219708 scopus 로고    scopus 로고
    • Drugs as materials: valuing physical form in drug discovery
    • Gardner C.R., Walsh C.T., Almarsson O. Drugs as materials: valuing physical form in drug discovery. Nat. Rev. Drug Discov. 2004, 3:926-934.
    • (2004) Nat. Rev. Drug Discov. , vol.3 , pp. 926-934
    • Gardner, C.R.1    Walsh, C.T.2    Almarsson, O.3
  • 8
    • 34447649709 scopus 로고    scopus 로고
    • Acidity of several polyprotic acids, amiodarone and quetiapine hemifumarate in pure methanol
    • Garrido G., de Nogales V., Rafols C., Bosch E. Acidity of several polyprotic acids, amiodarone and quetiapine hemifumarate in pure methanol. Talanta 2007, 73:115-120.
    • (2007) Talanta , vol.73 , pp. 115-120
    • Garrido, G.1    de Nogales, V.2    Rafols, C.3    Bosch, E.4
  • 9
    • 33751574252 scopus 로고    scopus 로고
    • Acid-base equilibria in nonpolar media. Absolute pKa scale of bases in tetrahydrofuran
    • Garrido G., Koort E., Rafols C., Bosch E., Rodima T., Leito I., Roses M. Acid-base equilibria in nonpolar media. Absolute pKa scale of bases in tetrahydrofuran. J. Org. Chem. 2006, 71:9062-9067.
    • (2006) J. Org. Chem. , vol.71 , pp. 9062-9067
    • Garrido, G.1    Koort, E.2    Rafols, C.3    Bosch, E.4    Rodima, T.5    Leito, I.6    Roses, M.7
  • 10
    • 33644890760 scopus 로고    scopus 로고
    • Acidity constants in methanol/water mixtures of polycarboxylic acids used in drug salt preparations-potentiometric determination of aqueous pKa values of quetiapine formulated as hemifumarate
    • Garrido G., Rafols C., Bosch E. Acidity constants in methanol/water mixtures of polycarboxylic acids used in drug salt preparations-potentiometric determination of aqueous pKa values of quetiapine formulated as hemifumarate. Eur. J. Pharm. Sci 2006, 28:118-127.
    • (2006) Eur. J. Pharm. Sci , vol.28 , pp. 118-127
    • Garrido, G.1    Rafols, C.2    Bosch, E.3
  • 11
    • 0023032232 scopus 로고
    • Salt selection for basic drugs
    • Gould P.L. Salt selection for basic drugs. Int. J. Pharm. 1986, 33:201-217.
    • (1986) Int. J. Pharm. , vol.33 , pp. 201-217
    • Gould, P.L.1
  • 17
    • 37349115571 scopus 로고    scopus 로고
    • Trends in active pharmaceutical ingredient salt selection based on analysis of the Orange Book database
    • Paulekuhn G.S., Dressman J.B., Saal C. Trends in active pharmaceutical ingredient salt selection based on analysis of the Orange Book database. J. Med. Chem. 2007, 50:6665-6672.
    • (2007) J. Med. Chem. , vol.50 , pp. 6665-6672
    • Paulekuhn, G.S.1    Dressman, J.B.2    Saal, C.3
  • 20
    • 34548032742 scopus 로고    scopus 로고
    • Salt formation to improve drug solubility
    • Serajuddin A.T.M. Salt formation to improve drug solubility. Adv. Drug Deliv. Rev. 2007, 59:603-616.
    • (2007) Adv. Drug Deliv. Rev. , vol.59 , pp. 603-616
    • Serajuddin, A.T.M.1
  • 22
    • 0031806352 scopus 로고    scopus 로고
    • In situ salt screening-a useful technique for discovery support and preformulation studies
    • Tong W.Q., Whitesell G. In situ salt screening-a useful technique for discovery support and preformulation studies. Pharm. Dev. Technol. 1998, 3:215-223.
    • (1998) Pharm. Dev. Technol. , vol.3 , pp. 215-223
    • Tong, W.Q.1    Whitesell, G.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.