OBJECTIVE To prepare and characterize IFNα-2b dry powder inhalers (DPIs). METHODS IFNα-2b solution containing excipients was freeze-dried and grinded to obtain IFNα-2b DPIs. The appearance, particle size, hydroscopicity, emptying rate, tapped density, particle distribution and activity of IFNα-2b were investigated. The activity of IFNα-2b was determined by CPE. In addition, the pharmacokinetics of IFNα-2b DPIs in rats were also investigated with IFNα-2b subcutaneous injections as control. RESULTS The particles of IFNα-2b DPIs were almost round. The average diameter was 6.78 μm. The hydroscopicity at RH75% for 24 h was 5.80%. The emptying rate was 95.16%. The total amount of first and second distribution in particle distribution test was 58.23%. 99.58% IFNα-2b was active. cmax of IFNα-2b DPIs in rats was lower and tmax was shorter than those of IFNα-2b solution. The relative bioavailability for IFNα-2b DPIs in rats was 46.76%. CONCLUSIONS The activity of INFα-2b is maintained, and the bioavailability of IFNα-2b is high. All of the results suggest that IFNα-2b DPIs is helpful for the delivery of IFNα-2b into lung.
Key words
IFNα-2b /
dry powder inhalers /
pharmacokinetic
{{custom_keyword}} /
{{custom_sec.title}}
{{custom_sec.title}}
{{custom_sec.content}}
References
[1] LI F Q, HU J H, ZHU Q G . Dry powder inhalers system[J]. <>Foreign Med Sci(<>Sec Pharm) （国外医学：药学分册） ,2001, 28(3):167-170.
[2] JIANG R G,LIU H,WANG CH L, <>et al. An interferon dry powders for lung and its manufactural method.China, 1672731A [P]. 2005- 09-28 .
[3] MENDEL J, IAN D, THIERRY A, <>et al. Pulmonary delivery of TH9507, a growth hormone releasing factor analogue, in the dog[J]. <>Int J Pharm, 2004, 276: 75-81.
[4] XIONG L J, CHEN X J, ZHU J B . Dry powder inhalation-a novel pulmonary delivery system of peptides and proteins [J]. <>Prog Pharm Sci( 药学进展 ), 2001, 25(4): 224-227.
[5] JIANG R G. Design and evaluation of dry powder for inhalation of recombinant human interferon α-2b[D]. Shenyang : Shenyang Pharmaceutical University , 2005.
[6] <>Ch.P （ 2005 ） Vol Ⅱ ( 中国药典 2005 年版 . 二部 )[S].2005: 13a .
[7] <>Ch.P （ 2005 ） Vol = 3 \* ROMAN III ( 中国药典 2005 年版 . 三部 )[S].2005: 56a -57a .
[8] <>Ch.P （ 2005 ） Vol Ⅱ ( 中国药典 2005 年版 . 二部 )[S].2005: 77a .
[9] JING F, XIE B Y, SHI L X, <>et al. Studies on disodium cromoglycate carrier-free powder inhalation = 2 \* ROMAN ii <>in vitro evaluation of powders for inhalation[J]. <>Chin J Pharm( 中国医药工业杂志 ),1998,29(1):19-22.
[10] XIONG L J , ZHU J B. Preparation and pharmaceutical properties of salcatonin dry powder inhalations[J]. <>Acta Pharm Sin ( 药学学报 ), 2003, 38(3): 218-222.
[11] CHEN X J, ZHU J B, WANG G J, <>et al. Hypoglycemic efficacy of pulmonary delivered insulin dry powder aerosol in rats[J]. <> Acta Pharmcol Sin ( 中国药理学报 ) , 2002, 23(5): 467-470.
[12] VALERLE C, FRANCIS V, ROGER K.V, <>et al. Systemic delivery of parathyroid hormone (1-34) using inhalation dry powders in rats[J].<> J Pharm Sci, 2003, 92(5): 938-950.
[13] SFDA. <> Guidance for pharmaceutical quality of inhalers ( 吸入制剂质量控制研究技术指导原则 )[S].2007:14-19.
[14] SUNDAY A, SHOYELE A S. Prospects of formulating proteins/peptides as aerosols for pulmonary drug delivery [J]. <>Int J Pharm, 2006, 314: 1-8.
（ 收稿日期 ： 2009-06-11 ）
{{custom_fnGroup.title_en}}
Footnotes
{{custom_fn.content}}
PDF(2555 KB)
