The apparent solubilizing capacity of simulated intestinal fluids for poorly water-soluble drugs

Pharmaceutical Development and Technology

Volumn 16, Issue 3, 2011, Pages 278-286

  Schwebel, Hervé J ^a   Van Hoogevest, Peter ^a   Leigh, Mathew L S ^a   Kuentz, Martin ^b  

^a Phares AG   (Switzerland)

^b UNIVERSITY OF APPLIED SCIENCES AND ARTS NORTHWESTERN SWITZERLAND   (Switzerland)

Author keywords

apparent solubilizing capacity; biorelevant media; FaSSIF; FeSSIF; Poorly soluble drugs

Indexed keywords

ACID; BASE; CANDESARTAN; CARBAMAZEPINE; CELECOXIB; DEXAMETHASONE; FENOFIBRATE; FINASTERIDE; GRISEOFULVIN; MEVINOLIN; PHENYTOIN; WATER;

ARTICLE; DIET RESTRICTION; DISSOLUTION; DRUG SOLUBILITY; INTESTINE FLUID; LIQUID; MICELLE; POWDER; PRIORITY JOURNAL; SIMULATION; SOLUBILITY; SOLUBILIZATION;

BIOLOGICAL AVAILABILITY; FASTING; GASTROINTESTINAL CONTENTS; HUMANS; MICELLES; MODELS, MOLECULAR; NUTRITIONAL STATUS; PARTICLE SIZE; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS; SOLUBILITY; WATER;

EID: 79955682309     PISSN: 10837450     EISSN: 10979867     Source Type: Journal    
DOI: 10.3109/10837451003664099     Document Type: Article

References (36)

1. Bakatselou V, Oppenheim RC, Dressman JB. Solubilization and wetting effects of bile salts on the dissolution of steroids. Pharm Res 1991;8:1461-1469.
2. Mithani SD, Bakatselou V, TenHoor CN, Dressman JB. Estimation of the increase in solubility of drugs as a function of bile salt concentration. Pharm Res 1996;13:163-167. (Pubitemid 26076314)
3. Dressman JB, Vertzoni M, Goumas K, Reppas C. Estimating drug solubility in the gastrointestinal tract. Adv Drug Deliv Rev 2007;59:591-602. (Pubitemid 47287780)
4. Amidon GL, Lennernaes H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995;12(3):413-420.
5. Kuentz M. Drug absorption modeling as a tool to define the strategy in clinical formulation development. AAPS J 2008;10(3):473-479.
6. Takano R, Sugano K, Higashida A, Hayashi Y, Machida M, Aso Y, Yamashida S. Oral absorption of poorly water-soluble drugs: Computer simulation of fraction absorbed in humans from a miniscale dissolution test. Pharm Res 2006;23(6):1144-1156. (Pubitemid 43946137)
7. Okumu A, DiMaso M, Löbenberg R. Dynamic dissolution testing to establish in vitro/in vivo correlations for montelukast sodium, a poorly soluble drug. Pharm Res 2008;25(12):2778-2785.
8. Sunesen VH, Pedersen BL, Kristensen HG, Müllertz A. In vivo in vitro correlations for a poorly soluble drug, danazol, using the flow-through dissolution method with biorelevant dissolution media. Eur J Pharm Biopharm 2005;24:305-313. (Pubitemid 40283513)
9. Galia E, Nicolaides E, Hörter D, Löbenberg R, Reppas C, Dressman JB. Evaluation of various dissolution media for predicting in vivo performance of Class I and II drugs. Pharm Res 1998;15(5):698-705. (Pubitemid 28275645)
10. Nicolaides E, Symillides M, Dressman J, Reppas Ch. Biorelevant dissolution testing to predict the plasma profile of lipophilic drugs after oral administration. Pharm Res 2001;18(3):380-388. (Pubitemid 32595828)
11. Jantratid E, Janssen N, Reppas Ch, Dressman JB. Dissolution media simulating conditions in the proximal human gastrointestinal tract: An update. Pharm Res 2008;25(7):1663-1676.
12. Jantratid E, Dressman JB. Biorelevant dissolution media simulating the proximal human gastrointestinal tract: An update. Diss Technol 2009;16:21-25.
13. Vertzoni M, Fotaki N, Kostewicz A, Stippler E, Leuner Ch Nicolaides E, Dressman J, Reppas Ch. Dissolution media simulating the intraluminal composition of the small intestine: Physiological issues and practical aspects. J Pharm Pharmacol 2004;56:453-462. (Pubitemid 38455610)
14. Boni JE, Brickl, RS, Dressman J, Pfefferle, ML. Instant FaSSIF and FeSSIF- biorelevance meets practicality. Dissolut Technol 2009;16(3):41-45.
15. Alsenz J, Kansy M. High throughput solubility measurement in drug discovery and development. Adv Drug Deliv Rev 2007;59:546-567. (Pubitemid 47285404)
16. Alsenz J, Meister E, Haenel E. Development of a partially automated solubility screening (PASS) assay for early drug development. J Pharm Sci 2007;96(7):1748-1762. (Pubitemid 47122953)
17. Bard B, Martel S, Carrupt PA. High throughput UV method for the estimation of thermodynamic solubility and the determination of the solubility in biorelevant media. Eur J Pharm Sci 2008;33:230-240.
18. Nielsen FS, Gibault E, Ljusberg-Wahren H, Arleth L, Pedersen JS, Müllertz A. Characterization of prototype self- nanoemulsifying formulations of lipophilic compounds. J Pharm Sci 2007;96(4):876-982.
19. Ertl P, Rohde B, Selzer P. Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties. J Med Chem 2000;43:3714-3717.
20. Van Krevelen DW. Properties of polymers: Their correlation with chemical structure; their numerical estimation and prediction from additive group contributions. Amsterdam: Elsevier; 1997:898.
21. Glomme A, Maerz J, Dressman JB. Comparison of a miniaturized shake-flask solubility method with automated potentionmetric acid/base titrations and calculated solubilities. J Pharm Sci 2005;94(1):1-16. (Pubitemid 40116365)
22. Lehto P, Aaltonen J, Tenho M, Rantanen J, Hirvonen J, Tanninen VP, Peltonen L. Solvent-mediated solid phase transformations of carbamazepine: Effects of simulated intestinal fluid and fasted state simulated intestinal fluid. J Pharm Sci 2009;98(3):985-996.
23. Agoram B, Woltosz W, Bolger M. Predicting the impact of physiological and biochemical processes on oral drug bioavailability. Adv Drug Deliv Rev 2001;50(S1):S41-67. (Pubitemid 32905355)
24. Willmann S, Schmitt W, Keldenich J, Lippert J, Dressman J. A physiological model for the estimation of the fraction dose absorbed in humans. J Med Chem 2004;47(16):4022-4031. (Pubitemid 38970963)
25. Jamei M, Turner D, Yang J, Neuhoff S, Polak S, Rostami-Hodjegan A, Tucker G. Population-based mechanistic prediction of oral drug absorption. AAPS J 2009;11(2):225-237.
26. Yang G, Jain N, Yalkowsky SH. Combined effects of SLS and (SBE)7M-â-CD on the solubilization of NSC-639829. Int J Pharm 2004;269:141-148. (Pubitemid 38035211)
27. Mazer NA, Benedek GB, Carey MC. Quasielastic light- scattering studies of aqueous biliary lipid systems. Mixed micelle formation in bile salt-lecithin solutions. Biochemistry 1980;19: 601-615.
28. Schurtenberger P, Mazer N, Känzig W. Micelle to vesicle transition in aqueous solutions of bile salt and lecithin. J Phys Chem 1985;89:1042-1049.
29. Dörfler HD. Chirality, twist and structures of micellar lyotropic cholesteric liquid crystals in comparison to the properties of chiralic thermotropic phases. Adv Coll Interf Sci 2002;98:285-340.
30. Reis S, Moutinho CG, Pereira E, Castro B, Gameiro P, Lima J. â-blockers and benzodiazepines location in SDS and bile salt micellar systems. An ESR study. J Pharm Biomed Anal 2007;45:62-69. (Pubitemid 47375000)
31. Glomme A. Biorelevante Löslichkeit schwerlöslicher Arzneistoffe. PhD Thesis, 2003. Johann Wolfgang Goethe-Universität Frankfurt, Germany. pp 134-139.
32. Ilardia-Arana D, Kristensen HG, Müllertz A. Biorelevant dissolution media: Aggregation of amphiphiles and solubility of estradiol. J Pharm Sci 2006;95(2):248-255. (Pubitemid 43241968)
33. Patel AR, Vavia PR. Preparation and in vivo evaluation of SMEDDS (self-microemulsifying drug delivery system) containing fenofibrate. AAPS J 2007;9(3):E344-352. (Pubitemid 351801762)
34. Sonet B, Vanderbist F, Streel, B, Houin G. Randomised crossover studies of the bioequivalence of two fenofibrate formulations after administration of a single oral dose in healthy volunteers. Belg Arzneimittel-Forschung 2002;52(3):200-204. (Pubitemid 34256400)
35. Tziomalos K, Athyros VG. Fenofibrate: A novel formulation (Triglide) in the treatment of lipid disorders: A review. Int J Nanomed 2006;1(2):129-147.
36. Guivarch PH, Vachon MG, Fordyce D. A new fenofibrate formulation: Results of six single-dose, clinical studies of bioavailability under fed and fasting conditions. Clin Therapeut 2004;26(9):1456-1469. (Pubitemid 39582714)