Particle size reduction and pharmacokinetic evaluation of a poorly soluble acid and a poorly soluble base during early development

Drug Development and Industrial Pharmacy

Volumn 37, Issue 3, 2011, Pages 243-251

  Sigfridsson, Kalle ^a   Lundqvist, Anders J ^a   Strimfors, Marie ^a  

^a ASTRAZENECA R AND D   (Sweden)

Author keywords

Dissolution rate; nanosuspension; pharmacokinetic; poorly soluble; suspension

Indexed keywords

AC 88; ACID; BA 99; BASE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG FORMULATION; FEMALE; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; MICROSUSPENSION; NANOSUSUPENSION; NONHUMAN; PARTICLE SIZE; RAT; SOLUBILITY; STOMACH ABSORPTION; STOMACH PH; SUSPENSION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ACIDS; ADMINISTRATION, ORAL; ANIMALS; AREA UNDER CURVE; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; MICROTECHNOLOGY; NANOPARTICLES; PARTICLE SIZE; PHARMACEUTICAL PREPARATIONS; RATS; RATS, SPRAGUE-DAWLEY; SOLUBILITY; SUSPENSIONS;

EID: 79952950073     PISSN: 03639045     EISSN: 15205762     Source Type: Journal    
DOI: 10.3109/03639045.2010.505927     Document Type: Article

References (26)

1. Lipinski CJ. (2001). Avoiding investment in doomed drugs. Is poor solubility an industry wide problem? Curr Drug Dis, 4:17-9.
2. Lipinski CJ. (2002). Poor aqueous solubility-an industry wide problem in drug discovery. Am Pharm Rev, 5:82-5.
3. Lennernäs H. (1998). Human intestinal permeability. J Pharm Sci, 87:403-10. (Pubitemid 28175799)
4. Lennernäs H. (2007). Animal data: the contributions of the using chamber and perfusion systems to predicting human oral drug delivery in vivo. Adv Drug Deliv Rev, 59:1103-20. (Pubitemid 47615203)
5. Nernst W, Brunner E. (1904). Theorie der reaktionsgeschwind-igkeit in heterogenen systemen. Z Physik Chemie, 47:52-110.
6. Liversidge GG, Cundy K. (1995). Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: I. Absolute oral bioavailability of nanocrystalline danazol in beagle dogs. Int J Pharm, 125:91-7.
7. Patravale VB, Date AA, Kulkarni RM. (2004). Nanosuspensions: A promising drug delivery strategy. J Pharm Pharmacol, 56:827-40. (Pubitemid 38885975)
8. Wu Y, Loper A, Landis E, Hettrick L, Novak L, Lynn K, et al. (2004). The role of biopharmaceutics in the development of a clinical nanoparticle formulation of MK-0869: A beagle dog model predits improved bioavailability and diminished food effect on absorption in human. Int J Pharm, 285:135-46. (Pubitemid 39361543)
9. Li X, Gu L, Xu Y, Wang Y. (2009). Preparation of fenofibrate nano-suspension and study of its pharmacokinetic behavior in rats. Drug Dev Ind Pharm, 35:827-33.
10. Kamiya S, Kurita T, Miyagishima A, Arakawa M. (2009). Prepara-tion of griseofulvin nanoparticle suspension by high-pressure homogenization and preservation of the suspension with sac-charides and sugar alcohols. Drug Dev Ind Pharm, 35:1022-8.
11. Muller RH, Jacobs C, Kayser O. (2001). Nanosuspensions as particulate drug formulations in therapy. Rationale for develop-ment and what we can expect for the future. Adv Drug Deliv Rev, 47:3-19. (Pubitemid 32209229)
12. Jia L, Wong H, Wang Y, Garza M, Weitman SD. (2003). Carbendazim: disposition, cellular permeability, metabolite identification, and pharmacokinetic comparison with its nano-particle. J Pharm Sci, 92:161-72. (Pubitemid 36042307)
13. Merisko-Liversidge E, Liversidge GG, Cooper ER. (2003). Nanosizing: A formulation approach for poorly-water-soluble compounds. Eur J Pharm Biopharm, 18:113-20. (Pubitemid 36184748)
14. Hecq J, Deleers M, Fanara D, Vranckx H, Boulanger P, Le lamer S, et al. (2006). Preparation ad in vitro/in vivo evaluation of nano-sized crystals for dissolution rate enhancement of ucb-35440-3, a highly dosed poorly water-soluble weak base. Eur J Pharm Biopharm, 64:360-8. (Pubitemid 44585201)
15. Keck CM, Muller RH. (2006). Drug nanocrystals of poorly soluble drugs produced by high pressure homogenisation. Eur J Pharm Biopharm, 62:3-16. (Pubitemid 41736019)
16. Kesisoglou F, Panmai S, Wu Y. (2007). Nanosizing-Oral formu-lation development and biopharmaceutical evaluation. Adv Drug Deliv Rev, 59:631-44. (Pubitemid 47285408)
17. Rabinow BE. (2004). Nanosuspensions in drug delivery. Nat Rev Drug Discov, 3:785-96. (Pubitemid 39242830)
18. Amidon GL, Lennernäs H, Shah VP, Crison JR. (1995). A theoret-ical basis for a biopharmaceutic drug classification: The correla-tion of in vitro drug product dissolution and in vivo bioavailability. Pharm Res, 12:413-20.
19. Yu LX, Amidon GL, Polli JE, Zhao H, Mehta MU, Conner DP, et al. (2002). Biopharmaceutics classification system: The scientific basis for biowaiver extensions. Pharm Res, 19:921-5. (Pubitemid 34804232)
20. Ziller KH, Rupprecht HH. (1990). Control of crystal growth in drug suspensions. Part II: influence of polymers on dissolution and crystallization during temperature cycling. Pharm Ind, 52:1017-22. (Pubitemid 20330148)
21. Sigfridsson K, Forssen S, Holländer P, Skantze U, de Verdier J. (2007). A formulation comparison, using solution and different nanosuspensions of a poorly soluble compound. Eur J Pharm Biopharm, 67:540-7. (Pubitemid 47225040)
22. Liversidge GG, Conzentino P. (1995). Drug particle reduction for decreasing gastric irritancy and enhancing absorption of naproxen in rats. Int J Pharm, 125:309-13.
23. Jia L, Wong J, Cerna C, Weitman S. (2002). Effect of nanonization on absorption of 301029: Ex vivo and in vivo pharmacokinetic correlations determined by liquid chromatography/mass spectrometry. Pharm Res, 19:1091-6. (Pubitemid 34984991)
24. Dressman JB, Reppas C (2000). In vitro-in vivo correlations for lipophilic, poorly water-soluble drugs. Eur J Pharm Sci, 11:73-80.
25. Mouton JW, van Peer A, de Beule K, van Vliet A, Donnelly JP, Soons PA. (2006). Pharmacokinetics of intraconazole and hydroxyitraconazole in healthy subjects after single and multi-ple doses of a novel formulation. Antimicrob Agents Chemother, 50:4096-102. (Pubitemid 44865154)
26. Xiong R, Lu W, Li J, Wang P, Xu R, Chen T. (2008). Preparation and characterization of intravenously injectable nimodipine nanosuspension. Int J Pharm, 350:338-43.