Abstract：
:The effect of the GlycoPEGylation process used for prolonging the half-life of recombinant factor IX (rFIX) has no impact on the primary and higher order structure of activated factor IX. Characterisation work performed on recombinant factor IX and on the GlycoPEGylated form of rFIX (N9-GP), confirm that the primary structure as well as the post translational modifications (PTMs) (disulphide bonds, γ-carboxylation, β-hydroxylation, sulphation and O- and N-linked glycan structures) were comparable for rFIX and N9-GP. Three O-linked glycan sites were identified in the activation peptide (Thr159, Thr163 and Thr169), where Thr163 has not been reported previously. For N9-GP, the mono GlycoPEGylation is directed toward one of the two N-linked glycans present at Asn157 and Asn167 in the activation peptide in a one to one ratio. Spectroscopic techniques, such as far and near UV Circular Dichroism studies show comparable secondary and tertiary structures of rFIX and N9-GP. The thermally induced unfolding of rFIX and N9-GP shows that the unfolding temperature is approximately 1 °C higher for N9-GP than that of the rFIX. Furthermore, the pH dependent degradation was reduced due to the GlycoPEGylation of rFIX. GlycoPEGylated rFIX (N9-GP) is used for the manufacturing of Refixia® (nonacog beta pegol, Rebinyn®, Novo Nordisk A/S, Bagsvaerd, Denmark).
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Nielsen FS,Schmidt AS,Kristensen AK,Nielsen AD,Kristensen BK,Palm Ldoi
10.1016/j.ijpharm.2020.119654subject
Has Abstractpub_date
2020-10-15 00:00:00pages
119654eissn
0378-5173issn
1873-3476pii
S0378-5173(20)30638-4journal_volume
588pub_type
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.11.048
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
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pub_type： 杂志文章
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abstract：:Over the last few decades, hot melt extrusion (HME) has emerged as a successful technology for a broad spectrum of applications in the pharmaceutical industry. As indicated by multiple publications and patents, HME is mainly used for the enhancement of solubility and bioavailability of poorly soluble drugs. This revie...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
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更新日期：2018-01-15 00:00:00
