Encapsulation of poorly soluble basic drugs into enteric microparticles: A novel approach to enhance their oral bioavailability

International Journal of Pharmaceutics

Volumn 416, Issue 1, 2011, Pages 55-60

  Alhnan, Mohamed A ^a   Murdan, Sudaxshina ^a   Basit, Abdul W ^a  

^a UNIVERSITY OF LONDON   (United Kingdom)

Author keywords

Enteric polymers; IVIVC; Microspheres; o o emulsion solvent evaporation; pH responsive; Site specific; Wistar rats

Indexed keywords

CINNARIZINE; EUDRAGIT;

ACIDITY; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUBILITY; EMULSION; EVAPORATION; IN VITRO STUDY; INTESTINE; MALE; MAXIMUM PLASMA CONCENTRATION; MICROENCAPSULATION; NONHUMAN; PH; POWDER; PRIORITY JOURNAL; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CINNARIZINE; DRUG COMPOUNDING; HYDROGEN-ION CONCENTRATION; MALE; PARTICLE SIZE; POLYMETHACRYLIC ACIDS; RATS; RATS, WISTAR; SOLUBILITY; TABLETS, ENTERIC-COATED;

EID: 80051793571     PISSN: 03785173     EISSN: 18733476     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2011.05.079     Document Type: Article

References (22)

1. M.A. Alhnan, D. Cosi, S. Murdan, and A.W. Basit Inhibiting the gastric burst release of drugs from enteric microparticles: the influence of drug molecular mass and solubility J. Pharm. Sci. 99 2010 4576 4583
2. F. De Jaeghere, E. Allemann, F. Kubel, B. Galli, R. Cozens, E. Doelker, and R. Gurny Oral bioavailability of a poorly water soluble HIV-1 protease inhibitor incorporated into pH-sensitive particles: effect of the particle size and nutritional state J. Control. Release 68 2000 291 298 (Pubitemid 30488906)
3. H. Derendorf, C.P. VanderMaelen, R.S. Brickl, T.R. MacGregor, and W. Eisert Dipyridamole bioavailability in subjects with reduced gastric acidity J. Clin. Pharmacol. 45 2005 845 850 (Pubitemid 40875337)
4. G.B. Fregnan, and F. Berte Enhancement of specific biological activity of dipyridamole by complexation with beta-cyclodextrin Pharmacology 40 1990 96 102 (Pubitemid 20105230)
5. C.H. Gu, D. Rao, R.B. Gandhi, J. Hilden, and K. Raghavan Using a novel multicompartment dissolution system to predict the effect of gastric pH on the oral absorption of weak bases with poor intrinsic solubility J. Pharm. Sci. 94 2005 199 208 (Pubitemid 40116383)
6. R. Kendall, M.A. Alhnan, S. Nilkumhang, S. Murdan, and A.W. Basit Fabrication and in vivo evaluation of highly pH-responsive acrylic microparticles for targeted gastrointestinal delivery Eur. J. Pharm. Sci. 37 2009 284 290
7. G.A. Kossena, W.N. Charman, B.J. Boyd, and C.J. Porter A novel cubic phase of medium chain lipid origin for the delivery of poorly water soluble drugs J. Control. Release 99 2004 217 229 (Pubitemid 39222108)
8. E.S. Kostewicz, M. Wunderlich, U. Brauns, R. Becker, T. Bock, and J.B. Dressman Predicting the precipitation of poorly soluble weak bases upon entry in the small intestine J. Pharm. Pharmacol. 56 2004 43 51 (Pubitemid 38195327)
9. J.P. Krise, W.N. Charman, S.A. Charman, and V.J. Stella A novel prodrug approach for tertiary amines. 3. In vivo evaluation of two N-phosphonooxymethyl prodrugs in rats and dogs J. Pharm. Sci. 88 1999 928 932 (Pubitemid 29438958)
10. J.C. Leroux, R. Cozens, J.L. Roesel, B. Galli, F. Kubel, E. Doelker, and R. Gurny Pharmacokinetics of a novel HIV-1 protease inhibitor incorporated into biodegradable or enteric nanoparticles following intravenous and oral administration to mice J. Pharm. Sci. 84 1995 1387 1391
11. E.L. McConnell, A.W. Basit, and S. Murdan Measurements of rat and mouse gastrointestinal pH, fluid and lymphoid tissue, and implications for in-vivo experiments J. Pharm. Pharmacol. 60 2008 63 70
12. S. Nilkumhang, M.A. Alhnan, E.L. McConnell, and A.W. Basit Drug distribution in enteric microparticles Int. J. Pharm. 379 2009 1 8
13. H. Ogata, N. Aoyagi, N. Kaniwa, A. Ejima, N. Sekine, M. Kitamura, and Y. Inoue Gastric acidity dependent bioavailability of cinnarizine from two commercial capsules in healthy volunteers Int. J. Pharm. 29 1986 113 120 (Pubitemid 16102002)
14. C.J. Porter, C.W. Pouton, J.F. Cuine, and W.N. Charman Enhancing intestinal drug solubilisation using lipid-based delivery systems Adv. Drug Deliv. Rev. 60 2008 673 691
15. G. Ricevuti, A. Mazzone, D. Pasotti, E. Uccelli, F. Pasquali, G. Gazzani, and G.B. Fregnan Pharmacokinetics of dipyridamole-beta-cyclodextrin complex in healthy volunteers after single and multiple doses Eur. J. Drug Metab. Pharmacokinet. 16 1991 197 201
16. T.L. Russell, R.R. Berardi, J.L. Barnett, T.L. O'Sullivan, J.G. Wagner, and J.B. Dressman pH-related changes in the absorption of dipyridamole in the elderly Pharm. Res. 11 1994 136 143 (Pubitemid 24040777)
17. T. Stozek, and L. Krowczynski The bioavailability of dipyridamole in the form of liposomes Pharmazie 41 1986 645 647
18. G.L. Stracciari, J. Malvisi, P. Anfossi, and G.B. Fregnan Pharmacokinetics of dipyridamole-beta-cyclodextrin complex in dogs Arch. Int. Pharmacodyn. Ther. 300 1989 7 13
19. T. Tokumura, Y. Tsushima, K. Tatsuishi, M. Kayano, Y. Machida, and T. Nagai Evaluation of bioavailability upon oral administration of cinnarizine-beta-cyclodextrin inclusion complex to beagle dogs Chem. Pharm. Bull. (Tokyo) 33 1985 2962 2967 (Pubitemid 16258169)
20. T. Tokumura, H. Ueda, Y. Tsushima, M. Kasai, M. Kayano, I. Amada, and T. Nagai Inclusion complexes of cinnarizine with beta-cyclodextrin in aqueous solution and in the solid state Chem. Pharm. Bull. (Tokyo) 32 1984 4179 4184 (Pubitemid 15208368)
21. S.M. Wong, I.W. Kellaway, and S. Murdan Fast-dissolving microparticles fail to show improved oral bioavailability J. Pharm. Pharmacol. 58 2006 1319 1326 (Pubitemid 44580562)
22. I. Yamada, T. Goda, M. Kawata, and K. Ogawa Application of gastric acidity-controlled beagle dog to bioavailability study of cinnarizine Yakugaku Zasshi 110 1990 280 285 (Pubitemid 20190964)