Bioavailability of cinnarizine in dogs: Effect of SNEDDS loading level and correlation with cinnarizine solubilization during in vitro lipolysis

Pharmaceutical Research

Volumn 30, Issue 12, 2013, Pages 3101-3113

  Larsen, Anne T ^a   Åkesson, Pernilla ^b   Juréus, Anna ^b   Saaby, Lasse ^c   Abu Rmaileh, Ragheb ^d   Abrahamsson, Bertil ^b   Østergaard, Jesper ^a   Müllertz, Anette ^c  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b ASTRAZENECA R AND D   (Sweden)

^c UNIVERSITY OF COPENHAGEN   (Denmark)

^d ASTRAZENECA   (United Kingdom)

Author keywords

bioavailability; cinnarizine; lipolysis; oral drug delivery; self nanoemulsifying drug delivery systems

Indexed keywords

CINNARIZINE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; AQUEOUS SOLUTION; AREA UNDER THE CURVE; ARTICLE; CORRELATION ANALYSIS; DOG; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DEGRADATION; DRUG DELIVERY SYSTEM; DRUG DISTRIBUTION; DRUG DOSAGE FORM; DRUG DOSAGE FORM COMPARISON; DRUG EXPOSURE; DRUG LOADING LEVEL; DRUG SOLUBILITY; DRUG STRUCTURE; IN VITRO STUDY; IN VIVO STUDY; LIPOLYSIS; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PHARMACOLOGICAL PARAMETERS; PLASMA CONCENTRATION-TIME CURVE; PRECIPITATION; PRIORITY JOURNAL; PROCESS MODEL; PROCESS OPTIMIZATION; SELF NANOEMULSIFYING DRUG DELIVERY SYSTEM; SOLUBILIZATION; STATISTICAL ANALYSIS; TIME TO MAXIMUM PLASMA CONCENTRATION; ULTRACENTRIFUGATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CACO-2 CELLS; CALCIUM CHANNEL BLOCKERS; CINNARIZINE; DOGS; DRUG CARRIERS; EMULSIONS; HUMANS; LIPIDS; LIPOLYSIS; MALE; SOLUBILITY;

EID: 84890568252     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-013-1145-x     Document Type: Article

References (34)

1. Attivi D, Ajana I, Astier A, Demore B, Gibaud S. Development of microemulsion of mitotane for improvement of oral bioavailability. Drug Dev Ind Pharm. 2010;36:421-7.
2. Dixit AR, Rajput SJ, Patel SG. Preparation and bioavailability assessment of SMEDDS containing valsartan. AAPS PharmSciTech. 2010;11:314-21.
3. Shafiq S, Shakeel F, Talegaonkar S, Ahmad FJ, Khar RK, Ali M. Design and development of oral oil in water ramipril nanoemulsion formulation: in vitro and in vivo assessment. J Biomed Nanotechnol. 2007;3:28-44.
4. Larsen AT, Ogbonna A, Abu-Rmaileh R, Abrahamsson B, Østergaard J, Mullertz A. SNEDDS containing poorly water soluble cinnarizine; development and in vitro characterization of dispersion, digestion and solubilization. Pharmaceutics. 2012;4:641-65.
5. Larsen AT, Ohlsson AG, Polentarutti B, Barker RA, Phillips AR, Abu-Rmaileh R, et al. Oral bioavailability of cinnarizine in dogs: relation to SNEDDS droplet size, drug solubility and in vitro precipitation. Eur J Pharm Sci. 2013;48:339-50.
6. Date AA, Nagarsenker MS. Design and evaluation of self-nanoemulsifying drug delivery systems (SNEDDS) for cefpodoxime proxetil. Int J Pharm. 2007;329:166-72.
7. Date AA, Desai N, Dixit R, Nagarsenker M. Self-nanoemulsifying drug delivery systems: formulation insights, applications and advances. Nanomedicine. 2010;5:1595-616.
8. Marasini N, Yan YD, Poudel BK, Choi HG, Yong CS, Kim JO. Development and optimization of self-nanoemulsifying drug delivery system with enhanced bioavailability by Box-Behnken design and desirability function. J Pharm Sci. 2012;101:4584-96.
9. Holm R, Tonsberg H, Jorgensen EB, Abedinpour P, Farsad S, Mullertz A. Influence of bile on the absorption of halofantrine from lipid-based formulations. Eur J Pharm Biopharm. 2012;81:281-7.
10. Thomas N, Holm R, Mullertz A, Rades T. In vitro and in vivo performance of novel supersaturated self-nanoemulsifying drug delivery systems (super-SNEDDS). J Control Release. 2012;160:25-32.
11. Thomas N, Holm R, Garmer M, Karlsson JJ, Mullertz A, Rades T. Supersaturated self-nanoemulsifying drug delivery systems (super-SNEDDS) enhance the bioavailability of the poorly water-soluble drug simvastatin in dogs. AAPS J. 2012;15:219-27.
12. Grove M, Pedersen GP, Nielsen JL, Mullertz A. Bioavailability of seocalcitol I: relating solubility in biorelevant media with oral bioavailability in rats - effect of medium and long chain triglycerides. J Pharm Sci. 2005;94:1830-8.
13. Kossena GA, Charman WN, Boyd BJ, Porter CJ. A novel cubic phase of medium chain lipid origin for the delivery of poorly water soluble drugs. J Control Release. 2004;99:217-29.
14. Larsen A, Holm R, Pedersen ML, Mullertz A. Lipid-based formulations for danazol containing a digestible surfactant, labrafil M2125CS: in vivo bioavailability and dynamic in vitro lipolysis. Pharm Res. 2008;25:2769-77.
15. Zangenberg NH, Mullertz A, Kristensen HG, Hovgaard L. A dynamic in vitro lipolysis model II: evaluation of the model. Eur J Pharm Sci. 2001;14:237-44.
16. Polentarutti B, Albery T, Dressman J, Abrahamsson B. Modification of gastric pH in the fasted dog. J Pharm Pharmacol. 2010;62:462-9.
17. Rautio J, Humphreys JE, Webster LO, Balakrishnan A, Keogh JP, Kunta JR, et al. In vitro P-glycoprotein inhibition assays for assessment of clinical drug interaction potential of new drug candidates: a recommendation for probe substrates. Drug Metab Dispos. 2006;34:786-92.
18. Kleberg K, Jacobsen F, Fatouros DG, Mullertz A. Biorelevant media simulating Fed State intestinal fluids: colloid phase characterization and impact on solubilization capacity. J Pharm Sci. 2010;99:3522-32.
19. Artursson P, Karlsson J. Correlation between oral-drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (caco-2) cells. Biochem Biophys Res Commun. 1991;175:880-5.
20. Amidon GL, Lennernas 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;12:413-20.
21. Fagerberg JH, Tsinman O, Sun N, Tsinman K, Avdeef A, Bergstrom CA. Dissolution rate and apparent solubility of poorly soluble drugs in biorelevant dissolution media. Mol Pharm. 2010;7:1419-30.
22. Constantinides PP, Wasan KM. Lipid formulation strategies for enhancing intestinal transport and absorption of P-glycoprotein (P-gp) substrate drugs: in vitro/in vivo case studies. J Pharm Sci. 2007;96:235-48.
23. Cornaire G, Woodley J, Hermann P, Cloarec A, Arellano C, Houin G. Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo. Int J Pharm. 2004;278:119-31.
24. Kariya S, Isozaki S, Uchino K, Suzuki T, Narimatsu S. Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996;19:1511-4.
25. Narimatsu S, Kariya S, Isozaki S, Ohmori S, Kitada M, Hosokawa S, et al. Involvement of Cyp2D6 in oxidative-metabolism of cinnarizine and Flunarizine in human liver-microsomes. Biochem Biophys Res Commun. 1993;193:1262-8.
26. Ingelman-Sundberg M. Genetic polymorphisms of cytochrome P450 2D6 (CYP2D6): clinical consequences, evolutionary aspects and functional diversity. Pharmacogenomics J. 2005;5:6-13.
27. Paulson SK, Engel L, Reitz B, Bolten S, Burton EG, Maziasz TJ, et al. Evidence for polymorphism in the canine metabolism of the cyclooxygenase 2 inhibitor, celecoxib. Drug Metab Dispos. 1999;27:1133-42.
28. Martignoni M, Groothuis GMM, de Kanter R. Species differences between mouse, rat, dog, monkey and human CYP-mediated drug metabolism, inhibition and induction. Expert Opin Drug Metab Toxicol. 2006;2:875-94.
29. Schmidt R, Baumann F, Hanschmann H, Geissler F, Preiss R. Gender difference in ifosfamide metabolism by human liver microsomes. Eur J Drug Metab Pharmacokinet. 2001;26:193-200.
30. Jarvinen T, Jarvinen K, Schwarting N, Stella VJ. Beta-cyclodextrin derivatives, Sbe4-beta-Cd and Hp-beta-Cd. Increase the oral bioavailability of cinnarizine in beagle dogs. J Pharm Sci. 1995;84:295-9.
31. Han SF, Yao TT, Zhang XX, Gan L, Zhu CL, Yua HZ, et al. Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione: effects of lipid composition and formulation. Int J Pharm. 2009;379:18-24.
32. Porter CJH, Kaukonen AM, Boyd BJ, Edwards GA, Charman WN. Susceptibility to lipase-mediated digestion reduces the oral bioavailability of danazol after administration as a medium-chain lipid-based microemulsion formulation. Pharm Res. 2004;21:1405-12.
33. Kossena GA, Charman WN, Wilson CG, O'Mahony B, Lindsay B, Hempenstall JM, et al. Low dose lipid formulations: effects on gastric emptying and biliary secretion. Pharm Res. 2007;24:2084-96.
34. Sassene PJ, Knopp MM, Hesselkilde JZ, Koradia V, Larsen A, Rades T, et al. Precipitation of a poorly soluble model drug during in vitro lipolysis: characterization and dissolution of the precipitate. J Pharm Sci. 2010;99:4982-91.