Biorelevant dissolution media: Aggregation of amphiphiles and solubility of estradiol

Journal of Pharmaceutical Sciences

Volumn 95, Issue 2, 2006, Pages 248-255

  Ilardia Arana, David ^a,b   Kristensen, Henning G ^a   Müllertz, Anette ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b UNIVERSITY OF NAVARRA   (Spain)

Author keywords

Biorelevant dissolution media; Drug solubilization; Estradiol; Intestinal surfactants; Mixed micelles; Poorly water soluble drugs

Indexed keywords

AMPHOPHILE; BILE SALT; ESTRADIOL; GLYCEROL OLEATE; GLYCOCHOLATE SODIUM; OLEIC ACID; PHOSPHATIDYLCHOLINE;

ARTICLE; BIORELEVANT DISSOLUTION MEDIUM; CONCENTRATION RESPONSE; CORRELATION ANALYSIS; CULTURE MEDIUM; DIET RESTRICTION; DILUTION; DRUG SOLUBILITY; HUMAN; MICELLE;

EID: 32644443825     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.20494     Document Type: Article

References (16)

1. Dressman JB, Reppas C. 2000. In vitro-in vivo correlations for lipophilic, poorly water-soluble drugs. Eur J Pharm Sci 11:S73-S80.
2. Pedersen BL, Brondsted H, Lennernas H, Christensen FN, Mullertz A, Kristensen HG. 2000. Dissolution of hydrocortisone in human and simulated intestinal fluids. Pharm Res 17:183-189.
3. Pedersen BL, Mullertz A, Brondsted H, Kristensen HG. 2000. A comparison of the solubility of danazol in human and simulated gastrointestinal fluids. Pharm Res 17:891-894.
4. Zangenberg NH, Mullertz A, Kristensen HG, Hovgaard L. 2001. A dynamic in vitro lipolysis model II: Evaluation of the model. Eur J Pharm Sci 14:237-244.
5. Dressman JB, Amidon GL, Reppas C, Shah VP. 1998. Dissolution testing as a prognostic tool for oral drug absorption: Immediate release dosage forms. Pharm Res 15:11-22.
6. Galia E, Nicolaides E, Horter D, Lobenberg R, Reppas C, Dressman JB. 1998. Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs. Pharm Res 15:698-705.
7. Hjelm RP, Schteingart CD, Hofmann AF, Thiyagarajan P. 2000. Structure of conjugated bile salt-fatty acid-monoglyceride mixed colloids: Studies by small-angle neutron scattering. J Phys Chem B 104:197-211.
8. Kossena GA, Boyd BJ, Porter CJ, Charman WN. 2003. Separation and characterization of the colloidal phases produced on digestion of common formulation lipids and assessment of their impact on the apparent solubility of selected poorly water-soluble drugs. J Pharm Sci 92:634-648.
9. Egelhaaf SU, Schurtenberger P. 1994. Shape transformations in the lecithin bile salt system-From cylinders to vesicles. J Phys Chem 98:8560-8573.
10. Cohen DE, Thurston GM, Chamberlin RA, Benedek GB, Carey MC. 1998. Laser light scattering evidence for a common wormlike growth structure of mixed micelles in bile salt- and straight-chain detergent-phosphatidylcholine aqueous systems: Relevance to the micellar structure of bile. Biochemistry 37:14798-14814.
11. Mazer NA, Carey MC, Kwasnick RF, Benedek GB. 1979. Quasielastic light scattering studies of aqueous biliary lipid systems. Size, shape, and thermo-dynamics of bile salt micelles. Biochemistry 18: 3064-3075.
12. Mazer NA, Benedek GB, Carey MC. 1980. Quasi-elastic light-scattering studies of aqueous biliary lipid systems. Mixed micelle formation in bile salt-lecithin solutions. Biochemistry 19:601-615.
13. Pedersen JS. Egelhaaf SU, Schurtenberger P. 1995. Formation of polymer like mixed micelles and vesicles in lecithin bile salt solution-a small angle neutron scattering study. J Phys Chem 99:1299-1305.
14. Wiedmann TS, Liang W, Kamel L. 2002. Solubilization of drugs by physiological mixtures of bile salts. Pharm Res 19:1203-1208.
15. Luner PE, Babu SR, Radebaugh GW. 1994. The effects of bile salts and lipids on the physicochemical behavior of gemfibrozil. Pharm Res 11:1755-1760.
16. Sunesen VH, Pedersen BL, Kristensen HG, Mullertz A. 2005. In vitro in vivo correlations for a poorly soluble drug, danazol, using the flow-through dissolution method with biorelevant dissolution media. Eur J Pharm Sci 24:305-313.