Solubilization behavior of poorly soluble drugs with combined use of Gelucire 44/14 and cosolvent

Journal of Pharmaceutical Sciences

Volumn 93, Issue 6, 2004, Pages 1471-1479

  Kawakami, Kohsaku ^a   Miyoshi, Kyoko ^a   Ida, Yasuo ^a  

^a SHIONOGI AND CO LTD   (Japan)

Author keywords

Cosolvent; Dimethylacetoamide; Dimethylsulfoxide; Gelucire 44 14; Log linear model; Micelle; Solubility; Two phase model

Indexed keywords

DIMETHYL SULFOXIDE; EXCIPIENT; GELUCIRE; INDOMETACIN; N,N DIMETHYLACETAMIDE; PHENYTOIN; SOLVENT; WATER;

ARTICLE; DRUG SOLUBILITY; FLUORESCENCE; LIGHT SCATTERING; MATHEMATICAL ANALYSIS; MATHEMATICAL COMPUTING; MICELLE; SOLUBILIZATION; STRUCTURE ANALYSIS; SURFACE PROPERTY; SURFACE TENSION;

EID: 2642542630     PISSN: 00223549     EISSN: None     Source Type: Journal    
DOI: 10.1002/jps.20067     Document Type: Article

References (21)

1. Bittner B, Mountfield RJ. 2002. Intravenous administration of poorly soluble new drug entities in early drug discovery: The potential impact of formulation on pharmacokinetic parameters. Curr Opin Drug Dis Dev 5:59-71.
2. Bittner B, Mountfield RJ. 2002. Formulations and related activities for the oral administration of poorly water-soluble compounds in early discovery animal studies. Pharm Ind 64:800-807.
3. Seethala R, Fernandes PB, editors. 2001. Handbook of drug screening. New York: Marcel Dekker.
4. Pan L, Ho Q, Tsutsui K, Takahashi L. 2001. Comparison of chromatographic and spectroscopic methods used to rank compounds for aqueous solubility. J Pharm Sci 90:521-529.
5. Kerns EH. 2001. High throughput physicochemical profiling for drug discovery. J Pharm Sci 90:1838-1858.
6. Krishna G, Chen KJ, Lin CC, Nomeir AA. 2001. Permeability of lipophilic compounds in drug discovery using in-vitro human absorption model, Caco-2. Int J Pharm 222:77-89.
7. Roussin P, Laforêt JP. 1997. Gelucire® 44/14: A high-performance system to enhance bioavailability of poorly water soluble drugs. B T Gattefossé 90:51-58.
8. Damian F, Blaton N, Naesens L, Balzarini J, Kinget R, Augustijns P, Van den Mooter G. 2000. Physicochemical characaterization of solid dispersions of the antiviral agent UC-781 with polyethylene glycol 6000 and Gelucire 44/14. Eur J Pharm Sci 10:311-322.
9. Rubino JT, Yalkowsky SH. 1987. Cosolvency and deviations from log-linear solubilization. Pharm Res 4:231-236.
10. Grant DJW, Brittain HG. 1995. Solubility of pharmaceutical solids. In: Brittain HG, editor. Physical characterization of pharmaceutical solids. New York: Marcel Dekker. pp 321-386.
11. Millard JW, Alvarez-Núñez, Yalkowsky SH. 2002. Solubilization by cosolvents. Establishing useful constants for the log-linear model. Int J Pharm 245:153-166.
12. Bustamante P, Navarro J, Romero S, Escalera B. 2002. Thermodynamic origin of the solubility profiles of drugs showing one or two maxima against the polarity of aqueous and nonaqueous mixtures: Niflumic acid and caffeine. J Pharm Sci 91:874-883.
13. Florence AT, Attwood D. 1998. Physicochemical principles of pharmacy, 3rd ed. New York: Palgrave. pp 199-251.
14. Almgren M, Swarup S, Löfroth JE. 1985. Effect of formamide and other organic polar solvents on the micelle formation of sodium dodecyl sulfate. J Phys Chem 89:4621-4626.
15. Aveyard R, Binks BP, Cooper P, Fletcher PDI. 1990. Incorporation of hydrocarbons into surfactant monolayers. Adv Colloid Interface Sci 33:59-77.
16. Israelachvili JN. 1991. Intermolecular and surface forces, 2nd ed. New York: Academic Press, Chapt 16.
17. Aguiar J, Carpena P, Molina-Bolívar JA, Ruiz CC. 2003. On the determination of the critical micelle concentration by the pyrene 1:3 ratio method. J Colloid Interface Sci 258:116-122.
18. Kawakami K, Nishihara Y, Hirano K. 1999. Liposome/emulsion transition induced by α-tocopheryl acetate. Langmuir 15:7454-7460.
19. Florence AT, Attwood D. 1998. Physicochemical principles of pharmacy, 3rd ed. New York: Palgrave. pp 84-85.
20. Shin DN, Wijnen JW, Engberts JBFN, Wakisaka A. 2001. On the origin of microheterogeneity: A mass spectroscopic study of dimethyl sulfoxide-water binary mixture. J Phys Chem B 105:6759-6762.
21. Shin DN, Wijnen JW, Engberts JBFN, Wakisaka A. 2002. On the origin of microheterogeneity: A mass spectroscopic study of acetonitrile-water and dimethyl sulfoxide-water binary mixtures (part 2). J Phys Chem B 106:6014-6020.