Designing biorelevant dissolution tests for lipid formulations: Case example - Lipid suspension of RZ-50

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 69, Issue 2, 2008, Pages 776-785

  Jantratid, Ekarat ^a   Janssen, Niels ^a   Chokshi, Hitesh ^b   Tang, Kin ^b   Dressman, Jennifer B ^a  

^a GOETHE UNIVERSITY   (Germany)

^b HOFFMANN LA ROCHE INC   (United States)

Author keywords

Bio Dis method; Biorelevant; Curve comparisons; Dissolution; IVIVC; Lipid dosage forms; Paddle method

Indexed keywords

DRUG; GELATIN; LIPID; RZ 50;

ACIDITY; ANALYTIC METHOD; ANIMAL EXPERIMENT; APPARATUS; ARTICLE; CONTROLLED DRUG RELEASE; CONTROLLED STUDY; DISPERSION; DOG; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CAPSULE; DRUG DISTRIBUTION; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUBILITY; EMULSION; FEMALE; HYDRODYNAMICS; IN VITRO STUDY; IN VIVO STUDY; INTERMETHOD COMPARISON; NONHUMAN; PREDICTION; SUSPENSION;

ALGORITHMS; CHEMISTRY, PHARMACEUTICAL; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DATA INTERPRETATION, STATISTICAL; INTESTINE, SMALL; LIPIDS; POSTPRANDIAL PERIOD; SOLUBILITY; SOLVENTS; STOMACH; SUSPENSIONS;

EID: 43249097007     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2007.12.010     Document Type: Article

References (43)

1. Ogunbona F.A., Smith I.F., and Olawoye O.S. Fat contents of meals and bioavailability of griseofulvin in man. J. Pharm. Pharmacol. 37 (1985) 283-284
2. Bramer S.L., and Forbes W.P. Relative bioavailability and effects of a high fat meal on single dose cilostazol pharmacokinetics. Clin. Pharmacokinet. 37 (1999) 13-23
3. Aungst B.J., Nguyen N.H., Taylor N.J., and Bindra D.S. Formulation and food effects on the oral absorption of a poorly water soluble, highly permeable antiretroviral agent. J. Pharm. Sci. 91 (2002) 1390-1395
4. Fleisher D., Li C., Zhou Y., Pao L.H., and Karim A. Drug, meal and formulation interactions influencing drug absorption after oral administration. Clinical implications. Clin. Pharmacokinet. 36 (1999) 233-254
5. Charman W.N., Porter C.J., Mithani S., and Dressman J.B. Physicochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH. J. Pharm. Sci. 86 (1997) 269-282
6. Julianto T., Yuen K.H., and Noor A.M. Improved bioavailability of vitamin E with a self emulsifying formulation. Int. J. Pharm. 200 (2000) 53-57
7. Hong J.Y., Kim J.K., Song Y.K., Park J.S., and Kim C.K. A new self-emulsifying formulation of intraconazole with improved dissolution and oral absorption. J. Control. Release 110 (2006) 332-338
8. Alhamami O.M., Aljanabi N.H., and Shalan N.M. Biopharmaceutic and pharmacokinetic studies following the oral administration of sodium salicylate in oily and aqueous vehicles to rabbit. Int. J. Pharm. 311 (2006) 63-68
9. Odeberg J.M., Kaufmann P., Kroon K.G., and Hoglung P. Lipid drug delivery and rational formulation design for lipophilic drugs with low oral bioavailability, applied to cyclosporine. Eur. J. Pharm. Sci. 20 (2003) 375-382
10. Wei L., Sun P., Nei S., and Pan W. Preparation and evaluation of SEDDS and SMEDDS containing carvedilol. Drug Dev. Ind. Pharm. 31 (2005) 785-794
11. Kommuru T.R., Gurley B., Khan M.A., and Reddy I.K. Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment. Int. J. Pharm. 212 (2001) 233-246
12. Sek L., Boyd B.J., Charman W.N., and Porter C.J. Examination of the impact of a range of Pluronic surfactants on the in-vitro solubilisation behaviour and oral bioavailability of lipidic formulations of atovaquone. J. Pharm. Pharmacol. 58 (2006) 809-820
13. Wu W., Wang Y., and Que L. Enhanced bioavailability of silymarin by self-microemulsifying drug delivery system. Eur. J. Pharm. Biopharm. 63 (2006) 288-294
14. Pouton C.W. Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system. Eur. J. Pharm. Sci. 29 (2006) 278-287
15. Pouton C.W. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems. Eur. J. Pharm. Sci. 11 (2000) S93-S98
16. Porter C.J., and Charman W.N. In vitro assessment of oral lipid based formulations. Adv. Drug Deliv. Rev. 50 (2001) S127-S147
17. Stuchlik M., and Zak S. Lipid-based vehicle for oral drug delivery. Biomed. Pap. Med. Fac. Univ. Palacky Olomouc Czech. Repub. 145 (2001) 17-26
18. Charman W.N. Lipids, lipophilic drugs, and oral drug delivery-some emerging concepts. J. Pharm. Sci. 89 (2000) 967-978
19. Caliph S.M., Charman W.N., and Porter C.J. Effect of short-, medium-, and long-chain fatty acid-based vehicles on the absolute oral bioavailability and intestinal lymphatic transport of halofantrine and assessment of mass balance in lymph-cannulated and non-cannulated rats. J. Pharm. Sci. 89 (2000) 1073-1084
20. Devani M., Ashford M., and Craig D.Q. The emulsification and solubilisation properties of polyglycolysed oils in self-emulsifying formulations. J. Pharm. Pharmacol. 56 (2004) 307-316
21. Humberstone A.J., and Charman W.N. Lipid-based vehicles for the oral delivery of poorly water soluble drugs. Adv. Drug Deliv. Rev. 25 (1997) 103-128
22. Taha E.I., Al-Saidan S., Samy A.M., and Khan M.A. Preparation and in vitro characterization of self-nanoemulsified drug delivery system (SNEDDS) of all-trans-retinol acetate. Int. J. Pharm. 285 (2004) 109-119
23. Dressman J., Schamp K., Beltz K., and Alsenz J. Characterizing release from lipid-based formulations. In: Hauss D.J. (Ed). Oral Lipid-Based Formulations: Enhancing the Bioavailability of Poorly Water-Soluble Drugs (2007), Informa Healthcare USA, Inc., New York 241-256
24. Galia E., Nicolaides E., Hörter D., Löbenberg R., Reppas C., and Dressman J.B. Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs. Pharm. Res. 15 (1998) 698-705
25. Nicolaides E., Galia E., Efthymiopoulos C., Dressman J.B., and Reppas C. Forecasting the in vivo performance of four low solubility drugs from their in vitro dissolution data. Pharm. Res. 16 (1999) 1876-1882
26. Dressman J.B., and Reppas C. In vitro-in vivo correlations for lipophilic, poorly water-soluble drugs. Eur. J. Pharm. Sci. 11 (2000) S73-S80
27. Sunesen V.H., Pedersen B.L., Kristensen H.G., and 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. Sci. 24 (2005) 305-313
28. Wei H., and Löbenberg R. Biorelevant dissolution media as a predictive tool for glyburide a class II drug. Eur. J. Pharm. Sci. 29 (2006) 45-52
29. Nicolaides E., Symillides M., Dressman J.B., and Reppas C. Biorelevant dissolution testing to predict the plasma profile of lipophilic drugs after oral administration. Pharm. Res. 18 (2001) 380-388
30. Vertzoni M., Dressman J., Butler J., Hempenstall J., and Reppas C. Simulation of fasting gastric conditions and its importance for the in vivo dissolution of lipophilic compounds. Eur. J. Pharm. Biopharm. 60 (2005) 413-417
31. N. Janssen, E. Jantratid, J. Dressman, Biorelevant media to simulate postprandial conditions in the proximal gut, in: 2007 AAPS Annual Meeting and Exposition, San Diego, CA.
32. 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
33. Reppas C., and Nicolaides E. Analysis of drug dissolution data. In: Dressman J.B., and Lennernäs H. (Eds). Oral Drug Absorption: Prediction and Assessment (2000), Marcel Dekker, New York 229-254
34. Derendorf H., Gramatte T., and Schäfer H.G. Bioverfügbarkeit und Bioäquivalenz. In: Derendorf H., Gramatte T., and Schäfer H.G. (Eds). Pharmakokinetik: Einführung in die Theorie und Relevanz für die Arzneimitteltherapie (2002), Wissenschaftliche Verlagsgesellschaft mbH, Stuttgart 125-154
35. USP 29/NF 24, The United State Pharmacopeia/The National Formulary, United States Pharmacopeial Convention Inc., Rockville, USA, 2006.
36. Dressman J.B., Amidon G.L., Reppas C., and Shah V.P. Dissolution testing as a prognostic tool for oral drug absorption: immediate release dosage forms. Pharm. Res. 15 (1998) 11-22
37. Kalantzi L., Persson E., Polentarutti B., Abrahamsson B., Goumas K., Dressman J.B., and Reppas C. Canine intestinal contents vs. simulated media for the assessment of solubility of two weak bases in the human small intestinal contents. Pharm. Res. 23 (2006) 1373-1381
38. Kalantzi L., Goumas K., Kalioras V., Abrahamsson B., Dressman J.B., and Reppas C. Characterization of the human upper gastrointestinal contents under conditions simulating bioavailability/bioequivalence studies. Pharm. Res. 23 (2006) 165-176
39. Rossi R.C., Dias C.L., Donato E.M., Martins L.A., Bergold A.M., and Fröehlich P.E. Development and validation of dissolution test for ritronavir soft gelatin capsules based on in vivo data. Int. J. Pharm. 338 (2007) 119-124
40. Al-Hammami O.M., and Richards J.H. Effects of excipients on the bioavailability of sodium salicylate from orally administered, oily suspensions. Pharm. Acta Helv. 71 (1996) 297-303
41. Kim J.Y., and Ku Y.S. Enhanced absorption of indomethacin after oral or rectal administration of a self-emulsifying system containing indomethacin to rats. Int. J. Pharm. 194 (2000) 81-89
42. Armand M., Borel P., Pasquier B., Dubois C., Senft M., Andre M., Peyrot J., Salducci J., and Lairon D. Physicochemical characteristics of emulsions during fat digestion in human stomach and duodenum. Am. J. Physiol. 271 (1996) G172-G183
43. Armand M. Lipases and lipolysis in the human digestive tract: Where do we stand?. Curr. Opin. Clin. Nutr. Metab. Care 10 (2007) 156-164