Selection of oral bioavailability enhancing formulations during drug discovery

Drug Development and Industrial Pharmacy

Volumn 38, Issue 2, 2012, Pages 235-247

  Zheng, Weijia ^a   Jain, Akash ^b   Papoutsakis, Dimitris ^b   Dannenfelser, Rose Marie ^c   Panicucci, Riccardo ^b   Garad, Sudhakar ^b  

^a ASTRAZENECA   (United Kingdom)

^b NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

^c NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Bioavailability; Co crystal; High throughput screening; Lipid based delivery; Physical form; Solid dispersion

Indexed keywords

DRUG; LCQ 789; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; COMPUTER MODEL; DOG; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG FORMULATION; DRUG HALF LIFE; DRUG PENETRATION; DRUG SOLUBILITY; HIGH THROUGHPUT SCREENING; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PARTICLE SIZE; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; CRYSTALLIZATION; DOGS; DRUG CARRIERS; DRUG DISCOVERY; LIPIDS; PARTICLE SIZE; PERMEABILITY; PYRAZOLES; PYRIMIDINONES; RATS; SOLUBILITY;

EID: 84255167486     PISSN: 03639045     EISSN: 15205762     Source Type: Journal    
DOI: 10.3109/03639045.2011.602406     Document Type: Article

References (39)

1. Lipinski CA. (2002). Poor aqueous solubility-an industry wide problem in drug discovery. Am Pharm Rev, 5: 82-5.
2. Saxena V, Panicucci R, Joshi Y, Garad S. (2009). Developability assessment in pharmaceutical industry: An integrated group approach for selecting developable candidates. J Pharm Sci, 98:1962-1979.
3. Chemburkar SR, Bauer J, Deming K, Spiwek H, Patel K, Morris J, et al. (2000). Dealing with the impact of ritonavir polymorphs on the late stages of bulk drug process development. Org Process Res Dev, 4:413-17.
4. Miller JM, Collman BM, Greene LR, Grant DJ, Blackburn AC. (2005). Identifying the stable polymorph early in the drug discoverydevelopment process. Pharm Dev Technol, 10:291-297. (Pubitemid 40677449)
5. Fakes MG, Vakkalagadda BJ, Qian F, Desikan S, Gandhi RB, Lai C et al. (2009). Enhancement of oral bioavailability of an HIVattachment inhibitor by nanosizing and amorphous formulation approaches. Int j Pharm, 370:167-174.
6. Ganta S, Paxton JW, Baguley BC, Garg S. (2009). Formulation and pharmacokinetic evaluation of an asulacrine nanocrystalline suspension for intravenous delivery. Int j Pharm, 367:179-186.
7. Attama AA, Reichl S, Müller-Goymann CC. (2008). Diclofenac sodium delivery to the eye: In vitro evaluation of novel solid lipid nanoparticle formulation using human cornea construct. Int J Pharm, 355:307-313.
8. Sigfridsson K, Forssén S, Holl'nder 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, 67:540-547. (Pubitemid 47225040)
9. Ning X, Sun J, Han X, Wu Y, Yan Z, Han J et al. (2011). Strategies to improve dissolution and oral absorption of glimepiride tablets: Solid dispersion versus micronization techniques. Drug Dev Ind Pharm, 37:727-736.
10. Zhang ZL, Le Y, Wang JX, Chen JF. (2011). Preparation of stable micron-sized crystalline irbesartan particles for the enhancement of dissolution rate. Drug Dev Ind Pharm Posted Online on 6 May 2011:1-8.
11. Chhabra G, Chuttani K, Mishra AK, Pathak K. (2011). Design and development of nanoemulsion drug delivery system of amlodipine besylate for improvement of oral bioavailability. Drug Dev Ind Pharm Posted Online on 14 May 2011:1-10
12. Sigfridsson K, Lundqvist AJ, Strimfors M. (2011). Particle size reduction and pharmacokinetic evaluation of a poorly soluble acid and a poorly soluble base during early development. Drug Dev Ind Pharm, 37:243-251.
13. Sigfridsson K, Nordmark A, Theilig S, Lindahl A. (2011). 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, 37:185-192.
14. 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, 35:1479-1486.
15. Hickey MB, Peterson ML, Scoppettuolo LA, Morrisette SL, Vetter A, Guzmán H et al. (2007). Performance comparison of a co-crystal of carbamazepine with marketed product. Eur J Pharm Biopharm, 67:112-119. (Pubitemid 46991320)
16. Trask AV, Motherwell WD, Jones W. (2006). Physical stability enhancement of theophylline via cocrystallization. Int J Pharm, 320:114-123. (Pubitemid 44128714)
17. Morissette SL, Almarsson O, Peterson ML, Remenar JF, Read MJ, Lemmo AV et al. (2004). High-throughput crystallization: polymorphs, salts, co-crystals and solvates of pharmaceutical solids. Adv Drug Deliv Rev, 56:275-300. (Pubitemid 38201426)
18. McNamara DP, Childs SL, Giordano J, Iarriccio A, Cassidy J, Shet MS et al. (2006). Use of a glutaric acid cocrystal to improve oral bioavailability of a low solubility API. Pharm Res, 23:1888-1897. (Pubitemid 44200553)
19. Bak A, Gore A, Yanez E, Stanton M, Tufekcic S, Syed R et al. (2008). The co-crystal approach to improve the exposure of a water-insoluble compound: AMG 517 sorbic acid co-crystal characterization and pharmacokinetics. J Pharm Sci, 97:3942-3956.
20. Pouton CW. (2000). Lipid formulations for oral administration of drugs: Non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems. Eur J Pharm Sci, 11 Suppl 2:S93-S98.
21. O'Driscoll CM. (2002). Lipid-based formulations for intestinal lymphatic delivery. Eur J Pharm Sci, 15:405-415. (Pubitemid 34567104)
22. Porter CJ, Trevaskis NL, Charman WN. (2007). Lipids and lipidbased formulations: optimizing the oral delivery of lipophilic drugs. Nat Rev Drug Discov, 6:231-248. (Pubitemid 46344627)
23. Wu Z, Guo D, Deng L, Zhang Y, Yang Q, Chen J. (2011). Preparation and evaluation of a self-emulsifying drug delivery system of etoposide-phospholipid complex. Drug Dev Ind Pharm, 37:103-112.
24. Wu X, Xu J, Huang X, Wen C. (2011). Self-microemulsifying drug delivery system improves curcumin dissolution and bioavailability. Drug Dev Ind Pharm, 37:15-23.
25. Shao B, Tang J, Ji H, Liu H, Liu Y, Zhu D et al. (2010). Enhanced oral bioavailability of Wurenchun (Fructus Schisandrae Chinensis extracts) by self-emulsifying drug delivery systems. Drug Dev Ind Pharm, 36:1356-1363.
26. Sakai K, Yoshimori T, Obata K, Maeda H. (2010). Design of self-microemulsifying drug delivery systems using a highthroughput formulation screening system. Drug Dev Ind Pharm, 36:1245-1252.
27. Attivi D, Ajana I, Astier A, Demoré B, Gibaud S. (2010). Development of microemulsion of mitotane for improvement of oral bioavailability. Drug Dev Ind Pharm, 36:421-427.
28. Chen Y, Zhang GG, Neilly J, Marsh K, Mawhinney D, Sanzgiri YD. (2004). Enhancing the bioavailability of ABT-963 using solid dispersion containing Pluronic F-68. Int J Pharm, 286:69-80. (Pubitemid 39410474)
29. Joshi HN, Tejwani RW, Davidovich M, Sahasrabudhe VP, Jemal M, Bathala MS et al. (2004). Bioavailability enhancement of a poorly water-soluble drug by solid dispersion in polyethylene glycolpolysorbate 80 mixture. Int J Pharm, 269:251-258. (Pubitemid 38032837)
30. Sugimoto M, Okagaki T, Narisawa S, Koida Y, Nakajima K. (1998). Improvement of dissolution characteristics and bioavailability of poorly water-soluble drugs by novel cogrinding method using water soluble polymer. Int J Pharm, 160:11-19. (Pubitemid 28059925)
31. Konno H, Handa T, Alonzo DE, Taylor LS. (2008). Effect of polymer type on the dissolution profile of amorphous solid dispersions containing felodipine. Eur J Pharm Biopharm, 70: 493-499.
32. Miller DA, DiNunzio JC, Yang W, McGinity JW, Williams RO 3rd. (2008). Targeted intestinal delivery of supersaturated itraconazole for improved oral absorption. Pharm Res, 25:1450-1459.
33. Vogt M, Kunath K, Dressman JB. (2008). Dissolution improvement of four poorly water soluble drugs by cogrinding with commonly used excipients. Eur j Pharm Biopharm, 68:330-337.
34. DiNunzio JC, Miller DA, Yang W, McGinity JW, Williams RO 3rd.(2008). Amorphous compositions using concentration enhancing polymers for improved bioavailability of itraconazole. Mol Pharm, 5:968-980.
35. Ranzani LS, Font J, Galimany F, Santanach A, Gomez-Gomar AM, Casadevall G et al. (2011). Enhanced in vivo absorption of CB-1 antagonist in rats via solid solutions prepared by hot-melt extrusion. Drug Dev Ind Pharm, 37:694-701.
36. Palanisamy M, Khanam J. (2011). Solid dispersion of prednisolone: Solid state characterization and improvement of dissolution profile. Drug Dev Ind Pharm, 37:373-386.
37. Jijun F, Lishuang X, Xiaoli W, Shu Z, Xiaoguang T, Xingna Z et al. (2011). Nimodipine (NM) tablets with high dissolution containing NM solid dispersions prepared by hot melt extrusion. Drug Dev Ind Pharm Posted Online 21 Mar 2011:1-11.
38. DiNunzio JC, Hughey JR, Brough C, Miller DA, Williams RO 3rd, McGinity JW. (2010). Production of advanced solid dispersions for enhanced bioavailability of itraconazole using KinetiSol Dispersing. Drug Dev Ind Pharm, 36:1064-1078.
39. Shanbhag A, Rabel S, Nauka E, Casadevall G, Shivanand P, Eichenbaum G et al. (2008). Method for screening of solid dispersion formulations of low-solubility compounds-miniaturization and automation of solvent casting and dissolution testing. Int J Pharm, 351:209-218. (Pubitemid 351186860)