Excipients for pulmonary formulations

Excipient Development for Pharmaceutical, Biotechnology, and Drug Delivery Systems

Volumn , Issue , 2006, Pages 225-249

  Smyth, Hugh ^a  

^a UNIVERSITY OF NEW MEXICO   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 80052211370     PISSN: None     EISSN: None     Source Type: Book    
DOI: None     Document Type: Chapter

References (95)

1. Clark A. Pulmonary delivery technology: recent advances and potential for the new millennium. In: Hickey AJ, ed. Pharmaceutical Inhalation Aerosol Technology. 2d ed. New York: Marcel Dekker, 2004.
2. Molina MJ, Rowland FS. Stratospheric sink for chlorofluoromethane: chlorine atom catalyzed destruction of ozone. Nature 1974; 274: 810-812.
3. Patton JS. Deep-lung delivery of therapeutic proteins. Chem Tech 1997; 27(12): 34-38.
4. Edwards DA. Delivery of biological agents by aerosols. AICHE J 2002; 48(1): 2-6.
5. Zeng XM, Martin AP, Marriott C. Particulate Interactions in Dry Powder Formulations for Inhalation. London: Taylor and Francis, 2001.
6. Crowder TM. Vibration technology for active dry-powder inhalers. Pharma Technol 2004; 52-61.
7. FDA. Guidance for industry metered dose inhaler (MDI) and dry powder inhaler (DPI) drug products. CDERGUIDj2180dft.wpd, Nov 1998, http://www.fda.gov/cder/guidance/2180dft.pdf, 1998.
8. Byron PR, Dalby RN, Hickey AJ. Optimized inhalation aerosols. I. The effects of spherical baffle size and position upon the output of several pressurized nonaqueous suspension formulations. Pharma Res 1989; 6(3): 225-229.
9. Dalby RN, Hickey AJ, Tiano SL. Medical devices for the delivery of therapeutic aerosols to the lungs. In: Hickey AJ, ed. Inhalation Aerosols. New York, New York: Marcel Dekker, Inc., 1996: 441-473.
10. Garcia-Contreras L, Smyth HDC. Dry-powder and liquid spray systems for inhaled delivery of peptide and proteins. Am J Drug Delivery 2005; 3(1): 29-45.
11. Crowder TM, Louey MD, Sethuraman VV, Smyth HDC, Hickey AJ. 2001: an odyssey in formulation and design. Pharm Technol 2001; 25(7): 99-113.
12. FDA. Guidance for industry: metered dose inhaler (MDI) and dry powder inhaler (DPI) drug products. Draft guidance 1998; www.fda.gov/cder/guidance/index.htm.
13. Tzou TZ. Aerodynamic particle size of metered-dose inhalers determined by the quartz crystal microbalance and the Andersen cascade impactor. Int J Pharm 1999; 186(1): 71-79.
14. Cheng YS, Fu CS, Yazzie D, Zhou Y. Respiratory deposition patterns of salbutamol pMDI with CFC and HFA-134a formulations in a human airway replica. J Aerosol Med 2001; 14(2): 255-266.
15. Wilkes W, Fink J, Dhand R. Selecting an accessory device with a metered-dose inhaler: variable influence of accessory devices on fine particle dose, throat deposition, and drug delivery with asynchronous actuation from a metered-dose inhaler. J Aerosol Med 2001; 14(3): 351-360.
16. Warren SJ, Farr SJ. Formulation of solution metered dose inhalers and comparison with aerosols emitted from conventional suspension systems. Int J Pharma 1995; 124: 195-203.
17. Stein SW. Size distribution measurements of metered dose inhalers using Andersen Mark II cascade impactors. Int J Pharma 1999; 186(1): 43-52.
18. Smyth HDC, Garcia-Contreras L, Cooney DJ, Garmise RJ, Jones LD, Hickey AJ. Medical and pharmaceutical aerosols. In: Ruzer LS, Harley NH, eds. Aerosols Handbook: Measurement, Dosimetry, and Health Effects. Boca Raton: CRC Press, 2005: 265-289.
19. Purewal TS. Formulation of metered dose inhalers. In: Purewal TS, Grant DJW, eds. Metered Dose Inhaler Technology. Buffalo Grove, Illnois: Interpharm, 1998.
20. Smyth HDC. The influence of formulation variables on the performance of alternative propellant-driven metered dose inhalers. Adv Drug Delivery Rev 2003; 55(7): 807-828.
21. Atkins P. Chlorofluorocarbon to hydrofluoroalkane formulations: an industry perspective. J Allergy Clin Immunol 1999; 104(6): S268-S270.
22. Ross DL, Gabrio BJ. Advances in metered dose inhaler technology with the development of a chlorofluorocarbon-free drug delivery system. J Aerosol Med 1999; 12(3): 151-160.
23. Johnson KA. Interfacial phenomena and phase behavior in metered-dose inhaler formulations. In: Hickey AJ, ed. Inhalation Aerosols. New York: Marcel Dekker, 1996: 385-415.
24. Vervaet C, Byron PR. Drug-surfactant-propellant interactions in HFA-formulations. Int J Pharm 1999; 186(1): 13-30.
25. Brambilla G, Ganderton D, Garzia R, Lewis D, Meakin B, Ventura P. Modulation of aerosol clouds produced by pressurized inhalation aerosols. Int J Pharm 1999; 186(1): 53-61.
26. McDonald KJ, Martin GP. Transition to CFC-free metered dose inhalers-into the new millennium. Int J Pharm 2000; 201(1): 89-107.
27. Gupta A, Stein SW, Myrdal PB. Balancing ethanol cosolvent concentration with product performance in 134a-based pressurized metered dose inhalers. J Aerosol Med 2003; 16(2): 167-174.
28. Tiwari D, Goldman D, Malick WA, Madan P. Formulation and evaluation of albuterol metered dose inhalers containing tetrafluoroethane (P134a), a non-CFC propellant. Pharma Dev Technol 1998; 3: 163-174.
29. DeStefano G, Kelash-Cannavo LJ, inventors; Boehringer Ingelheim Pharmaceuticals, Inc., U.S., assignee. Formulation for a Metered Dose Inhaler Using Hydrofluoroalkanes as Propellants. US Patent 2004184994, 2004.
30. Ashurst I, Malton A, Prime D, Sumby B. Latest advances in the development of dry powder inhalers. Pharm Sci Technol Today 2000; 3(7): 246-256.
31. Steckel H, Bolzen N. Alternative sugars as potential carriers for dry powder inhalations. Int J Pharma 2004; 270(1-2): 297-306.
32. Buskeyfield LJ, Jay GE, Wright P, inventors; Fisons, PLC, assignee. Pharmaceutical Inhalation Compositions. US Patent US 5,607,662, 4 Mar 1997.
33. Rowe RC, Sheskey PJ, Weller PJ. Handbook of Pharmaceutical Excipients. APhA Publications, 2003.
34. Asmus MJ, Sherman J, Hendeles L. Bronchoconstrictor additives in bronchodilator solutions. J Allergy Clin Immunol 1999; 104(S53-S60): 215-229.
35. Blondino FE, Byron PR. Surfactant dissolution and water solubilization in chlorine-free liquefied gas propellants. Drug Dev Ind Pharm 1998; 24(10): 935-945.
36. Williams RO III, Hu C. Influence of water on the solubility of two steroid drugs in hydrofluoroalkane (HFA) propellants. Drug Dev Ind Pharm 2001; 27(1): 71-79.
37. Williams RO III, Hu C. Investigation of moisture scavengers in pressurized metered-dose inhalers. STP Pharma Sci 2000; 10(3): 243-250.
38. Williams RO III, Hu C. Moisture uptake and its influence on pressurized metered-dose inhaler. Pharma Dev Technol 2000; 5(2): 153-162.
39. Byron PR, Blondino FE, inventors; The Center for Innovative Technology, USA; Virginia Commonwealth University, assignee. Metered Dose Inhaler Formulations Which Include the Ozone-Friendly Propellant HFC 134a and Suspending, Solubilizing, Wetting, Emulsifying or Lubricating Agent. US Patent 5492688, 1996.
40. Byron PR, Miller NC, Blondino FE, Visich JE, Ward GH. Some aspects of alternative propellant solvency. Paper presented at: RDD IV, 1994.
41. Stein SW, Myrdal PB. A theoretical and experimental analysis of formulation and device parameters affecting solution MDI size distributions. J Pharma Sci 2004; 93(8): 2158-2175.
42. Byron PR. Dosing reproducibility from experimental albuterol suspension metered-dose inhalers. Pharm Res 1994; 11(4): 580-584.
43. Weers JG, Tarara TE, Gill H, English BS, Dellamary LA. Homodispersion technology for HFA suspensions: particle engineering to reduce dosing variance. Paper presented at: RDD VII, 2000.
44. Bowman PA, Greenleaf D. Non-CFC metered dose inhalers: the patent landscape. Int J Pharm 1999; 186(1): 91-94.
45. Stefely JS, Duan DC, Myrdal PB, Ross DL, Schultz DW, Leach C. Design and utility of a novel class of biocompatible excipients for HFA-based MDIs. Paper presented at: RDD VII, 2000.
46. Wright P. Polymers for the colloidal stabilization of drugs in HFAs. Paper presented at: RDD IV, 1994.
47. Stefely JS. Novel excipients for inhalation drug delivery: expanding the capability of the MDI. Drug Delivery Technol 2002; 2(6): 62, 64-69.
48. Williams RO, Repka MA, Barron MK. Application of cogrinding to formulate a model pMDI suspension. Eur J Pharma Biopharma 1999; 48: 131-140.
49. Hickey AJ, Dalby RN, Byron PR. Effects of surfactants on aerosol powders in suspension. Implications for airborne particle size. Int J Pharma 1988; 42: 267-270.
50. Leach CL, Davidson PJ, Boudreau RJ. Improved airway targeting with the CFC-free HFA-beclomethasone metered-dose inhaler compared with CFC-beclomethasone. Eur Respir J 1998; 12(6): 1346-1353.
51. Dellamary LA, Tarara TE, Smith DJ, et al. Hollow porous particles in metered dose inhalers. Pharm Res 2000; 17(2): 168-174.
52. Polli GP, Grim WM, Bacher FA, Yunker MH. Influence of formulation on aerosol particle size. J Pharma Sci 1969; 58: 484-486.
53. Baeckstroem K, Nilsson PG. Measurements of droplet size distributions from metered dose inhalers with different vapor pressures and contents of surfactant. J Aerosol Sci 1988; 19(7): 1097-1100.
54. Dalby RN, Byron PR. Comparison of output particle size distributions from pressurized aerosols formulated as solutions or suspensions. Pharm Res 1988; 5(1): 36-39.
55. Tzou TZ. Density, excess molar volume, and vapor pressure of propellant mixtures in metered-dose inhalers: deviation from ideal mixtures. Respir Drug Delivery VI, Int Symp 1998: 439-443.
56. Smyth HDC, Mejia-Millan EA, Hickey AJ. The effect of ethanol on solvency vapor pressure, and emitted droplet size of solution metered dose inhalers containing HFA 134a. Respir Drug Delivery VIII 2002; 2: 735-738.
57. Williams RO III, Repka M, Liu J. Influence of propellant composition on drug delivery from a pressurized metered-dose inhaler. Drug Dev Ind Pharm 1998; 24(8): 763-770.
58. Williams RO III, Liu J, Repka MA. Optimization of drug delivery from a MDI with propellants 134a and 227. Proc Int Symp. Controlled Release Bioact Mater 1997; 24: 745-746.
59. Hickey AJ. Pharmaceutical inhalation aerosol powder dispersion: an unbalancing act. Am Pharma Rev 2003; 6(4): 106-110.
60. Israelachvili J. Intermolecular and Surface Forces. 2d ed. London: Academic Press, 1992.
61. Zeng XM, Martin GP, Marriott C, Pritchard J. The effects of carrier size and morphology on the dispersion of salbutamol sulphate after aerosolization at different flow rates. J Pharm Pharmacol 2000; 52(10): 1211-1221.
62. Steckel H, Müller BW. In vitro evaluation of dry powder inhalers II: Influence of carrier particle size and concentration on in vitro deposition. Int J Pharma 1997; 154: 31-37.
63. Kassem NM, Ho KKL, Ganderton D. The effect of airflow and carrier size on the characteristics of an inspirable cloud. J Pharma Pharmacol 1989; 41: 14P.
64. French DL, Edwards DA, Niven RW. The influence of formulation on emission, deaggregation and deposition of dry powder for inhalation. J Aerosol Sci 1996; 27(5): 769-783.
65. Ganderton D. Generation of respirable clouds from coarse powder aggregates. J Biopharma Sci 1992; 3: 101-105.
66. Clarke MJ, Tobyn MJ, Staniforth JN. The formulation of powder inhalation systems containing a high mass of nedocromil sodium trihydrate. J Pharm Sci 2001; 90(2): 213-223.
67. Larhrib H, Martin GP, Marriott C, Prime D. The influence of carrier and drug morphology on drug delivery from dry powder formulations. Int J Pharm 2003; 257(1-2): 283-296.
68. Chan LW, Lim LT, Heng PW. Immobilization of fine particles on lactose carrier by precision coating and its effect on the performance of dry powder formulations. J Pharm Sci 2003; 92(5): 975-984.
69. Crowder TM, Rosati JA, Schroeter JD, Hickey AJ, Martonen TB. Fundamental effects of particle morphology on lung delivery: predictions of Stokes’ law and the particular relevance to dry powder inhaler formulation and development. Pharma Res 2002; 19: 239-245.
70. Zeng XM, Martin GP, Marriott C, Pritchard J. Lactose as a carrier in dry powder formulations: the influence of surface characteristics on drug delivery. J Pharma Sci 2001; 90(9): 1424-1434.
71. Zeng XM, Martin GP, Marriott C, Pritchard J. The influence of carrier morphology on drug delivery by dry powder inhalers. Int J Pharma 2000; 200: 93-106.
72. Kawashima Y, Serigano T, Hino T, Yamamoto H, Takeuchi H. Effect of surface morphology of carrier lactose on dry powder inhalation property of pranlukast hydrate. Int J Pharma 1998; 172: 179-188.
73. Podczeck F. The influence of particle size distribution and surface roughness of carrier particles on the in vitro properties of dry powder inhalations. Aerosol Sci Technol 1999; 31(4): 301-321.
74. Buckton G. Characterization of small changes in the physical properties of powders of significance for dry powder inhaler formulations. Adv Drug Delivery Rev 1997; 26: 17-27.
75. Harjunen P, Lehto VP, Martimo K, et al. Lactose modifications enhance its drug performance in the novel multiple dose Taifun DPI. Eur J Pharm Sci 2002; 16(4-5): 313-321.
76. Williams RO III, Brown J, Liu J. Influence of micronization method on the performance of a suspension triamcinolone acetonide pressurized metered-dose inhaler formulation. Pharm Dev Technol 1999; 4(2): 167-179.
77. Larhrib H, Martin GP, Prime D, Marriott C. Characterization and deposition studies of engineered lactose crystals with potential for use as a carrier for aerosolized salbutamol sulfate from dry powder inhalers. Eur J Pharma Sci 2003; 19(4): 211-221.
78. Ahlneck C, Zografi G. The molecular basis of moisture effects on the physical and chemical stability of drugs in the solid state. Int J Pharm 1990; 62: 87-95.
79. Louey MD, Stewart PJ. Particle interactions involved in aerosol dispersion of ternary interactive mixtures. Pharma Res 2002; 19(10): 1524-1531.
80. Zeng XM, Martin GP, Tee SK, Ghoush AA, Marriott C. Effects of particle size and adding sequence of fine lactose on the deposition of salbutamol sulphate from a dry powder formulation. Int J Pharma 1999; 182: 133-144.
81. Lucas P, Anderson K, Potter UJ, Staniforth JN. Enhancement of small particle size dry powder aerosol formulations using an ultra low-density additive. Pharma Res 1999; 16(10): 1643-1647.
82. Zeng XM, Martin GP, Tee SK, Marriott C. The role of fine particle lactose on the dispersion and deaggregation of salbutamol sulphate in an air stream in vitro. Int J Pharma 1998; 176: 99-110.
83. Staniforth JN, inventor; Coordinated Drug Development Limited, assignee. Carrier Particles for Use in Dry Powder Inhalers. US Patent US 6,153,224, 28 Nov 2000.
84. Staniforth JN. Improvements in dry powder inhaler performance: surface passivation effects. Paper presented at: Drug Delivery to the Lungs VII, 1996: London.
85. Lucas P, Clarke MJ, Anderson K, Tobyn MJ, Staniforth JN. The role of fine particle excipients in pharmaceutical dry powder aerosols. Paper presented at: Respiratory Drug Delivery VI, 1998.
86. Islam N, Stewart PJ, Larson I, Hartley P. Lactose surface modification by decantation: are drug-fine lactose ratios the key to better dispersion of salmeterol xinafoate from lactose- interactive mixtures? Pharm Res 2004; 21(3): 492-499.
87. Edwards DA, Valente AX, Man J, Tsapis N. Recent advances related to the systemic delivery of therapeutic molecules by inhalation. In: Hickey A, ed. Pharmaceutical Inhalation Aerosol Technology. 2d ed. New York: Marcel Dekker, 2004: 541-550.
88. Choi WS, Murthy GG, Edwards DA, Langer R, Klibanov AM. Inhalation delivery of proteins from ethanol suspensions. Proc Natl Acad Sci USA 2001; 98(20): 11103-11107.
89. Norwood DL, Qiu F. Strategies for the analysis of pharmaceutical excipients and their trace level impurities. Am Pharma Rev 2004; 7(5): 92-99.
90. FDA. Metered dose inhaler (MDI) and dry powder inhaler (DPI) drug products chemistry, manufacturing, and controls documentation. CDER/FDA, 1998.
91. Howlett D, Colwell J, Goldsmith S, McCallion ON. Correlation of extractables and leachables from marketed pMDIs. Paper presented at: Respiratory Drug Delivery VIII, 2002.
92. Chi EY, Sampathkumar K, Randolph TW, Carpenter JF. Physical stability of proteins in aqueous solution: mechanism and driving forces in nonnative protein aggregation. Pharma Res 2003; 20(9): 1325-1336.
93. Manning MC, Patel K, Borchardt R. Stability of protein pharmaceuticals. Pharm Res 1989; 6: 903-918.
94. Immamura K, Iwai M, Ogawa T, Sakiyama T, Nakanishi K. Evaluation of hydration states of protein in freeze-dried amorphous sugar matrix. J Pharm Sci 2001; 90: 1955-1963.
95. Smyth HDC, Garmise RJ, Cooney DJ, Zimmerer RO, Pipkin JD, Hickey AJ. Influence of physical form of Captisol® particles on performance as a dry powder aerosol carrier. Paper presented at: Respiratory Drug Delivery IX, Palm Desert, California, 2004.