Investigating high-concentration monoclonal antibody powder suspension in nonaqueous suspension vehicles for subcutaneous injection

Journal of Pharmaceutical Sciences

Volumn 101, Issue 12, 2012, Pages 4433-4443

  Bowen, Mayumi ^a   Armstrong, Nick ^a   Maa, Yuh Fun ^a  

^a GENENTECH INC   (United States)

Author keywords

Glide force; High concentration; Injectability; Monoclonal antibody (mAb); Prefilled syringe; Spray drying; Viscosity

Indexed keywords

EID: 84868207432     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23324     Document Type: Article

References (40)

1. Stockwin LH, Holmes S. 2003. Antibodies as therapeutic agents: Vive la renaissance! Expert Opin Biol Ther 3:1133-1152.
2. Shire SJ, Shahrokh Z, Liu J. 2004. Challenges in the development of high protein concentration formulations. J Pharm Sci 93:1390-1402.
3. Overcashier DE, Chan EK, Hsu CC. 2006. Technical considerations in the development of prefilled syringes for protein products. Am Pharm Rev 9:77-83.
4. Kanai S, Liu J, Patapoff TW, Shire SJ. 2005. Reversible self-association of a concentrated monoclonal antibody solution mediated by Fab-Fab interactions that impact solution viscosity. J Pharm Sci 97:4219-4227.
5. Alford JR, Kendrick BS, Carpenter JF, Randolph TW. 2008. High concentration formulations of recombinant human interleukin-1 receptor antagonist: II. Aggregation kinetics. J Pharm Sci 97:3005-3021.
6. Salinas BA, Sathish HA, Bishop SM, Harn N, Carpenter JF, Randolpg TW. 2010. Understanding and modulating opalescence and viscosity in a monoclonal antibody formulation. J Pharm Sci 99:82-93.
7. Sukumar M, Doyle BL, Combs JL, Pekar AH. 2004. Opalescent appearance of an IgG1 antibody at high concentrations and its relationship to noncovalent association. Pharm Res 21:1087-1093.
8. He F, Woods CE, Trilisky E, Bower KM, Litowski JR, Kerwin BA, Becker GW, Narhi LO, Razinkov VI. 2011. Screening of monoclonal antibody formulation based on high-throughput thermostability and viscosity measurements: Design of experiment and statistical analysis. J Pharm Sci 100:1330-1340.
9. Dani B, Platz R, Tzannis ST. 2007. High concentration formulation feasibility of human immunoglubulin G for subcutaneous administration. J Pharm Sci 96:1504-1517.
10. Yang MX, Shenoy B, Disttler M, Patel R, McGrath M, Pechenov S, Margolin AL. 2003. Crystalline monoclonal antibodies for subcutaneous delivery. Proc Natl Acad Sci USA 100:6934-6939.
11. Trilisky E, Gillespie R, Osslund TD, Vunnum S. 2011. Crystallization and liquid-liquid phase separation of monoclonal antibodies and Fc-fusion proteins: Screening results. Biotechnol Prog 27:1054-1067.
12. Floyd AG, Jain S. 1996. Injectable emulsions and suspensions. In Pharmaceutical dosage forms: Disperse systems; Lieberman HA, Rieger MM, Banker GS, Eds. Vol. 2. New York City, New York: Dekker, pp 261-318.
13. Akers MJ, Fites AL, Robison RL. 1987. Formulation design and development of parenteral suspensions. J Parenter Sci Technol 41:88-96.
14. Larsen SW, Ostergaad J, Friberg-Johansen H, Jessen MN, Larsen C. 2006. In vitro assessment of drug release rates from oil depot formulations intended for intra-articular administration. Eur J Pharm Sci 29:348-354.
15. Hirano K, Ichihashi T, Yamada H. 1982. Studies on the absorption of practically water-insoluble drugs following injection V: Subcutaneous absorption in rats from solutions in water immiscible oils. J Pharm Sci 71:495-500.
16. Salmerón MD, Hernandez PJ, Cerezo A. 1997. Encapsulation study of 6-methylprednisolone in liquid microspheres. Drug Dev Ind Pharm 23:133-136.
17. Karasulu HY, Karabulut B, Goker E, Guneri T, Gabor F. 2007. Controlled release of methotrexate from W/O microemulsion and its in vitro antitumor activity. Drug Deliv 14:225-233.
18. Santucci E, Alhaique F, Carafa M, Coviello T, Murtas E, Riccieri M. 1996. Gellan for the formulation of sustained delivery beads. J Control Release 42:157-164.
19. Pena LE, Possert PL, Stearns JF, Lee BL, Hageman MJ. 1995. Rheological characterization of rbSt oil suspensions. Int J Pharm 113:89-96.
20. Newell HE, Buckton G, Buttler DA, Thielmann F, Williams DR. 2001. The use of inverse gas chromatography to measure the surface energy of crystalline, amorphous, and recently milled lactose. Pharm Res 18:662-666.
21. Grimsey IM, Feeley JC, York P. 2002. Analysis of the surface energy of pharmaceutical powders by inverse gas chromatography. J Pharm Sci 91:571-583.
22. Newell HE, Buckton G. 2004. Inverse gas chromatography: Investigating whether the technique preferentially probes high energy sites for mixture of crystalline and amorphous lactose. Pharm Res 21:1440-1444.
23. Saleem I, Smyth H. 2008. Prediction of dry powder inhaler formulation performance from surface energetics and blide dynamics. Drug Dev Ind Pharm 34:1002-1010.
24. Panzer U, Schreiber HP. 1992. On the evaluation of surface interactions by inverse gas chromatography. Macromolecules 25:3633-3637.
25. Thielmann F. 2006. Inverse gas chromatography: Characterization of alumina and related surfaces. In Encyclopedia of surface and colloid science; Somasundaran P., Ed. Vol. 4. Boca Raton, Florida: CRC Press, pp 3009-3031.
26. Thielmann F, Butler D. 2007. Heat of sorption on microcrystalline cellulose by pulse inverse gas chromatography at infinite dilution. Surface measurement services application note 203. Accessed May 14, 2012, at: http://www.thesorptionsolution.com/Information_Application_Notes_IGC.php#Aps.
27. Avastin® (bevacizumab) highlights of prescribing information. Accessed May 14, 2012, at: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/125085s0168lbl.pdf.
28. Herceptin® (trastuzumab) highlights of prescribing information. Accessed May 14, 2012, at: http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/103792s5256lbl.pdf.
29. Rituxan® (rituximab) highlights of prescribing information. Accessed May 14, 2012, at: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/103705s5344lbl.pdf.
30. Lee GWJ. 2002. Spray drying of proteins. In Rational protein formulation: Theory and practice (Pharmaceutical Biotechnology Series); Carpenter J, Manning M, Borchardt R, Eds. New York City, New York: Plenum Press, pp 135-158.
31. Maury M, Murphy K, Kumar S, Shi L, Lee GWJ. 2005. Effects of process variables on the powder yield of spray-dried trehalose on a laboratory spray-dryer. Eur J Pharm Biopharm 59:566-573.
32. Maa YF, Nguyen PA, Sit K, Hsu CC. 1998. Spray-drying performance of a bench-top spray dryer for protein aerosol powder preparation. Biotechnol Bioeng 60:301-309.
33. Maa YF, Nguyen PA, Hsu CC. 1998. Spray drying of air-sensitive recombinant human growth hormone. J Pharm Sci 87:152-159.
34. Maa YF, Costantino HR, Nguyen PA, Hsu CC. 1997. The effect of operating and formulation variables on the morphology of spray-dried protein particles. Pharm Dev Technol 2:213-223.
35. Einstein A. 1911. A new determination of molecular dimensions. Annalen der Physik 34:591-592.
36. Mahjour M, Mauser BE, Rashidbaigi ZA, Fawzi MB. 1999. Effects of propylene glycol diesters of caprylic and capric acids (Miglyol® 840) and ethanol binary systems on in vitro skin permeation of drugs. Int J Pharm 95:161-169.
37. Seniro WJ. 1999. Final report on the safety assessment of propylene glycol (PG) dicaprylate, PG dicaprylate/dicaprate, PG dicocoate, PG dipelargonate, PG isostearate, PG laurate, PG myristate, PG oleate, PG oleate SE, PG dioleate, PG dicaprate, PG diisostearate, and PG dilaurate. Int J Toxicol 18:35-52.
38. Spiegel AJ, Noseworthy MM. 1963. Use of nonaqueous solvents in parenteral products. J Pharm Sci 52:917-927.
39. Mottu F, Laurent A, Rufenacht DA, Doelker E. 2000. Organic solvents for pharmaceutical parenterals and embolic liquids: A review of toxicity data. PDA J Pharm Sci Technol 54:456-469.
40. Toda K, Furuse H. 2006. Extension Of Einstein's viscosity equation to that for concentrated dispersions of solutes and particles. J Biosci Bioeng 102:524-528.