albumin - publications

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1. Clin Drug Investig. 2012 May 9. doi: 10.2165/11632840-000000000-00000. [Epub
ahead of print]

Discomfort from an Alkaline Formulation Delivered Subcutaneously in Humans:
Albumin at pH 7 versus pH 10.

Ward WK, Castle JR, Branigan DL, Massoud RG, El Youssef J.

Legacy Health and Legacy Research Institute, Portland, OR, USA.

Background and Objective: There is a paucity of data regarding tolerability of
alkaline drugs administered subcutaneously. The aim of this study was to assess
the tolerability of alkaline preparations of human albumin delivered
subcutaneously to healthy humans. Methods: We compared the tolerability of
neutral versus alkaline (pH 10) formulations of human albumin in ten volunteers.
With an intent to minimize the time required to reach physiological pH after
injection, the alkaline formulation was buffered with a low concentration of
glycine (20 mmol/L). Each formulation was given at two rates: over 5 seconds and
over 60 seconds. A six-point scale was used to assess discomfort. Results: For
slow injections, there was a significant difference between pH 7.4 and pH 10
injections (0.4 ± 0.2 vs 1.1 ± 0.2, mean ± SEM; p = 0.025), though the degree of
discomfort at pH 10 injections was only 'mild or slight'. For fast injections,
the difference between neutral and alkaline formulations was of borderline
significance. Inflammation and oedema, as judged by a physician, were very
minimal for all injections, irrespective of pH. Conclusion: For subcutaneous drug
administration (especially when delivered slowly), there was more discomfort
associated with alkaline versus neutral formulations of albumin, though the
discomfort was mild. This study suggests that there is little discomfort and
inflammation resulting from subcutaneous administration of protein drugs
formulated with weak buffers at alkaline pH.

PMID: 22568666 [PubMed - as supplied by publisher]