Relationship between dissolution and bioavailability for nimodipine colloidal dispersions: The critical size in improving bioavailability

International Journal of Pharmaceutics

Volumn 427, Issue 2, 2012, Pages 358-364

  Fu, Qiang ^a   Kou, Longfa ^a   Gong, Cheng ^a   Li, Mo ^b   Sun, Jin ^a   Zhang, Dong ^a   Liu, Meina ^a   Sui, Xiaofan ^b   Liu, Kai ^c   Wang, Siling ^a   He, Zhonggui ^a  

^a SHENYANG PHARMACEUTICAL UNIVERSITY   (China)

^b Liaoning Institute for Food and Drug Control   (China)

^c Jiangsu Hengrui Medicine Co Ltd   (China)

Author keywords

Bioavailability; Dissolution; Nimodipine; Particle size

Indexed keywords

NANOCRYSTAL; NIMODIPINE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CRYSTAL; DOG; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG SOLUBILITY; LASER DIFFRACTION; MALE; NONHUMAN; PARTICLE SIZE; PRECIPITATION; PRIORITY JOURNAL; X RAY POWDER DIFFRACTION;

ALGORITHMS; ANIMALS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CALCIUM CHANNEL BLOCKERS; CHEMISTRY, PHARMACEUTICAL; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; COLLOIDS; CRYSTALLIZATION; DOGS; MALE; NANOPARTICLES; NIMODIPINE; PARTICLE SIZE; SOLUBILITY; X-RAY DIFFRACTION;

EID: 84862799613     PISSN: 03785173     EISSN: 18733476     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2012.02.022     Document Type: Article

References (27)

1. G.L. Amidon, H. Lennernäs, V.P. Shah, and J.R. Crison A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability Pharm. Res. 12 1995 413 420
2. P. Bernatchez, A. Sharma, P.M. Bauer, E. Marin, and W.C. Sessa A noninhibitory mutant of the caveolin-1 scaffolding domain enhances eNOS-derived NO synthesis and vasodilation in mice J. Clin. Invest. 121 2011 3747 3755
3. T.M. Cardoso, P.O. Rodriguesm, H.K. Stulzer, M.A. Segatto Silva, and J. do Rosário Matos Physical-chemical characterization and polymorphism determination of two nimodipine samples deriving from distinct laboratories Drug Dev. Ind. Pharm. 31 2005 631 637
4. W.N.A. Charman, and V.J. Stella Effect of lipid class and lipid vehicle volume on the intestinal lymphatic transport of DDT Int. J. Pharm. 33 1986 165 172
5. Fu, Q., Sun, J., Ai, X., Kou, L., Gong, C., He, Z. What accounts for unfavoured in vitro in vivo correlation of nimodipine nanocrystals and solid dispersions: molecular form versus crystal form, under review.
6. L. Gao, D. Zhang, M. Chen, T. Zheng, and S. Wang Preparation and characterization of an oridonin nanosuspension for solubility and dissolution velocity enhancement Drug Dev. Ind. Pharm. 33 2007 1332 1339
7. A. Grunenberg, B. Keil, and J.-O. Henck Polymorphism in binary mixtures, as exemplified by nimodipine Int. J. Pharm. 118 1995 11 21
8. Z. He, D. Zhong, X. Chen, X. Liu, X. Tang, and L. Zhao Development of a dissolution medium for nimodipine tablets based on bioavailability evaluation Eur. J. Pharm. Sci. 21 2004 487 491
9. J. Jinno, N. Kamada, M. Miyake, K. Yamada, T. Mukai, M. Odomi, H. Toguchi, G.G. Liversidge, K. Higaki, and T. Kimura Effect of particle size reduction on dissolution and oral absorption of a poorly water-soluble drug, cilostazol, in beagle dogs J. Control. Release 111 2006 56 64
10. N. Kaneniwa, N. Watari, and H. Iijima Dissolution of slightly soluble drugs. V. Effect of particle size on gastrointestinal drug absorption and its relation to solubility Chem. Pharm. Bull. (Tokyo) 26 1978 2603 2614
11. Y. Kawabata, K. Wada, M. Nakatani, S. Yamada, and S. Onoue Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: basic approaches and practical applications Int. J. Pharm. 420 2011 1 10
12. M.L. Lind, J. Jacobsen, R. Holm, and A. Müllertz Intestinal lymphatic transport of halofantrine in rats assessed using a chylomicron flow blocking approach: the influence of polysorbate 60 and 80 Eur. J. Pharm. Sci. 35 2008 211 218
13. G.G. Liversidge, and K.C. Cundy Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: I. Absolute oral bioavailability of nanocrystalline danazol in beagle dogs Int. J. Pharm. 125 1995 91 97
14. M.E. Matteucci, M.A. Hotze, K.P. Johnston, and R.O. Williams Drug nanoparticles by antisolvent precipitation: mixing energy versus surfactant stabilization Langmuir 22 2006 8951 8959
15. X. Ning, J. Sun, X. Han, Y. Wu, Z. Yan, J. Han, and Z. He Strategies to improve dissolution and oral absorption of glimepiride tablets: solid dispersion versus micronization techniques Drug Dev. Ind. Pharm. 37 2011 727 736
16. V.B. Patravale, A.A. Date, and R.M. Kulkarni Nanosuspensions: a promising drug delivery strategy J. Pharm. Pharmacol. 56 2004 827 840
17. M. Perrut, J. Jung, and F. Leboeuf Enhancement of dissolution rate of poorly-soluble active ingredients by supercritical fluid processes. Part I: Micronization of neat particles Int. J. Pharm. 288 2005 3 10
18. E. Roger, F. Lagarce, E. Garcion, and J.P. Benoit Biopharmaceutical parameters to consider in order to alter the fate of nanocarriers after oral delivery Nanomedicine (Lond.) 5 2010 287 306
19. G. Sahay, D.Y. Alakhova, and A.V. Kabanov Endocytosis of nanomedicines J. Control. Release 145 2010 182 195
20. R. Shegokar, and R.H. Müller Nanocrystals: industrially feasible multifunctional formulation technology for poorly soluble actives Int. J. Pharm. 399 2010 129 139
21. K. Sigfridsson, A.J. Lundqvist, and M. Strimfors Particle size reduction for improvement of oral absorption of the poorly soluble drug UG558 in rats during early development Drug Dev. Ind. Pharm. 35 2009 1479 1486
22. K. Sigfridsson, A. Nordmark, S. Theilig, and A. Lindahl A formulation comparison between micro- and nanosuspensions: the importance of particle size for absorption of a model compound, following repeated oral administration to rats during early development Drug Dev. Ind. Pharm. 37 2011 185 192
23. W. Sun, S. Mao, Y. Shi, L.C. Li, and L. Fang Nanonization of itraconazole by high pressure homogenization: stabilizer optimization and effect of particle size on oral absorption J. Pharm. Sci. 100 2011 3365 3373
24. B. Van Eerdenbrugh, G. Van den Mooter, and P. Augustijns Top-down production of drug nanocrystals: nanosuspension stabilization, miniaturization and transformation into solid products Int. J. Pharm. 364 2008 64 75
25. C.Y. Wu, and L.Z. Benet Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system Pharm. Res. 22 2005 11 23
26. Y. Wu, A. Loper, E. Landis, L. Hettrick, L. Novak, K. Lynn, C. Chen, K. Thompson, R. Higgins, U. Batra, S. Shelukar, G. Kwei, and D. Storey The role of biopharmaceutics in the development of a clinical nanoparticle formulation of MK-0869: a beagle dog model predicts improved bioavailability and diminished food effect on absorption in human Int. J. Pharm. 285 2004 135 146
27. D. Xia, F. Cui, H. Piao, D. Cun, H. Piao, Y. Jiang, M. Ouyang, and P. Quan Effect of crystal size on the in vitro dissolution and oral absorption of nitrendipine in rats Pharm. Res. 27 2010 1965 1976