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 Development and Industrial Pharmacy

Volumn 37, Issue 2, 2011, Pages 185-192

  Sigfridsson, Kalle ^a   Nordmark, Anna ^b   Theilig, Stefanie ^b   Lindahl, Anders ^b  

^a ASTRAZENECA R AND D   (Sweden)

^b ASTRAZENECA R AND D   (Sweden)

Author keywords

Absorption; in vivo exposure; nanosuspension; pharmacokinetic; poorly soluble; rat; saturated elimination; suspensions

Indexed keywords

DRUG; MODEL COMPOUND; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CRYSTALLIZATION; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG EXPOSURE; DRUG FORMULATION; DRUG HALF LIFE; DRUG MEGADOSE; DRUG SOLUBILITY; DRUG STABILITY; IN VIVO STUDY; LIPOPHILICITY; LOW DRUG DOSE; MALE; MAXIMUM PLASMA CONCENTRATION; MICROSUSPENSION; NANOSUSPENSION; NONHUMAN; PARTICLE SIZE; RAT; REPEAT PROCEDURE; SUSPENSION; TIME TO MAXIMUM PLASMA CONCENTRATION; ZETA POTENTIAL;

EID: 79952922229     PISSN: 03639045     EISSN: 15205762     Source Type: Journal    
DOI: 10.3109/03639045.2010.504209     Document Type: Article

References (37)

1. Lipinski CJ. (2001). Avoiding investment in doomed drugs. Is poor solubility an industry wide problem? Curr Drug Discov, 4:17-9.
2. Lipinski CJ. (2002). Poor aqueous solubility-an industry wide problem in drug discovery. Am Pharm Rev, 5:82-5.
3. Loftsson T, Brewster ME. (1996). Pharmaceutical applications of cyclodextrins. J Pharm Sci, 85:1017-25.
4. Stella VJ, Rajewski RA. (1997). Cyclodextrins: Their future in drug formulation and delivery. Pharm Res, 14:556-67. (Pubitemid 27220271)
5. Akers MJ. (2002). Excipient-drug interactions in parenteral formulations. J Pharm Sci, 91:2283-300. (Pubitemid 35231192)
6. Rasheed A, Kumar ACK, Sravanthi VVNSS. (2008). Cyclodextrins as drug carrier molecules: A review. Sci Pharm, 76:567-98.
7. Floyd AG. (1999). Top ten considerations in the development of parenteral emulsions. Pharm Sci Technol Today, 4:134-43. (Pubitemid 29195746)
8. Lawrence MJ, Rees GD. (2000). Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev, 45:89-121.
9. Nakano M. (2000). Places of emulsions in drug delivery. Adv Drug Deliv Rev, 45:1-4.
10. Serajuddin ATM. (1999). Solid dispersion of poorly water-soluble drugs: Early promises, subsequent problems, and recent breakthroughs. J Pharm Sci, 88:1058-66.
11. Chokshi RJ, Zia H, Sandhu HK, Shah NH, Malick WA. (2007). Improving dissolution rate of poorly water soluble drug by solid dispersion and solid solution-Pros and cons. Drug Deliv, 14:33-45. (Pubitemid 44764457)
12. Serajuddin ATM. (2007). Salt formation to improve drug solubility. Adv Drug Deliv Rev, 59:603-16. (Pubitemid 47285406)
13. Van den Mooter GM, Wuyts N, Blaton R, Busson P, Grobet P. (2001). Physical stabilisation of amorphous ketoconazole in solid dispersions with polyvinylpyrrolidone K25. Eur J Pharm Sci, 12:261-9.
14. Hirasawa N, Ishise S, Miyata H, Danjo K. (2003). An attempt to stabilize nilvadipine solid dispersion by the use of ternary systems. Drug Dev Ind Pharm, 29:997-1004. (Pubitemid 37346101)
15. Weuts I, Kempen D, Verreck G, Decorte A, Heymans K, Peeters J, et al. (2005). Study of the physicochemical properties and stability of solid dispersions of loperamide and PEG6000 prepared by spray drying. Eur J Pharm Biopharm, 59:119-26. (Pubitemid 39573443)
16. Smikalla MM, Urbanetz NA. (2007). The influence of povidone K17 on the storage stability of solid dispersions of nimodipine and polyethylene glycol. Eur J Pharm Biopharm, 66:106-12. (Pubitemid 46412964)
17. Pudipeddi M, Serajuddin ATM. (2005). Trends in solubility of polymorphs. J Pharm Sci, 94:929-39. (Pubitemid 40780760)
18. Llinas A, Box KJ, Burley JC, Glen RC, Goodman JM. (2007). A new method for the reproducible generation of polymorphs: Two forms of sulindac with very different solubilities. J Appl Crystallogr, 40:379-81. (Pubitemid 46439141)
19. Jia L, Wong H, Cerna C, Weitman SD. (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)
20. Sigfridsson K, Forssen S, Holländer P, Skantze U, de Verdier J. (2007). A formulation comparison, using a solution and different nanosuspensions of a poorly soluble compound. Eur J Pharm Biopharm, 67:540-7. (Pubitemid 47225040)
21. Gao L, Zhang D, Chen M. (2008). Drug nanocrystals for the formulation of poorly soluble drugs and its application as a potential drug delivery system. J Nanopart Res, 10:845-62.
22. Mauludin R, Müller RH, Keck CM. (2009). Kinetic solubility and dissolution velocity of rutin nanocrystals. Eur J Pharm Biopharm, 36:502-10.
23. Sigfridsson K, Lundqvist AJ, Strimfors M. (2009). Particle size reduction for improvement of oral absorption of the poorly soluble drug UG558 in rats during early development. Drug Dev Ind Pharm, 35:1479-86.
24. Li X, Gu L, Xu Y, Wang Y. (2009). Preparation of fenofibrate nanosuspension and study of its pharmacokinetic behavior in rats. Drug Dev Ind Pharm, 35:827-33.
25. Kamiya S, Kurita T, Miyagishima A, Arakawa M. (2009). Preparation of griseofulvin nanoparticle suspension by high-pressure homogenization and preservation of the suspension with saccharides and sugar alcohols. Drug Dev Ind Pharm, 35:1022-8.
26. 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.
27. Peters K, Leitzke S, Diederichs JE, Borner K, Hahu H, Müller RH, et al. (2000). Preparation of a clofazimine nanosuspension for intravenous use and evaluation of its therapeutic efficacy in murine Mycobacterium avium infection. J Antimicrob Chemother, 45:77-83. (Pubitemid 30060237)
28. Pignatello R, Bucolo C, Ferrara P, Maltese A, Puleo A, Puglisi G. (2002). Eudragit RS100 nanosuspensions for the ophthalmic controlled delivery of ibuprofen. Eur J Pharm Sci, 16:53-61. (Pubitemid 34756782)
29. Jacobs C, Müller RH. (2002). Production and characterization of a budesonide nanosuspension for pulmonary administration. Pharm Res, 19:21-4.
30. Amidon GL, Lennernäs H, Shah VP, Crison JR. (1995). A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res, 12:413-20.
31. Muller RH, Jacobs C, Kayser O. (2001). Nanosuspensions as particulate drug formulations in therapy. Rationale for development and what we can expect for the future. Adv Drug Deliv Rev, 47:3-19. (Pubitemid 32209229)
32. Kararli TT. (1995). Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm Drug Dispos, 16:351-80.
33. de Zwart LL, Rompelberg CJM, Sips AJAM, Welink J, van Engelen JGM. (1999). Anatomical and physiological differences between various species used in studies on pharmacokinetics and toxicology of xenobiotics. Investigation performed by 'research for man and environment' at National Institute of Public Health and Environment, The Netherlands.
34. Ward FW, Coates ME. (1987). Gastrointestinal pH measurements in rats: Influence of microbial flora, diet, and fasting. Lab Anim, 21:216-22.
35. Noyes AA, Whitney WR. (1897). The rate of solution of solid substances in their own solutions. J Am Chem Soc, 19:930-4.
36. Sakaguchi E, Itoh H, Uchida S, Horigome T. (1987). Comparison of fibre digestion and digesta retention time between rabbits, guinea pigs, rats and hamsters. Br J Nutr, 58:149-58. (Pubitemid 17105572)
37. DeSesso JM, Jacobson CF. (2001). Anatomical and physiological parameters affecting gastrointestinal absorption in humans and rats. Food Chem Toxicol, 39:209-28. (Pubitemid 32244129)