Abstract：
:The novel anticancer agent BIBX1382BS is a representative of the human epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. BIBX1382BS, for parenteral use, is formulated pharmaceutically as a lyophilized product containing 100 mg BIBX1382BS per dosage unit. This in vitro study was performed to establish the optimal intravenous administration conditions (infusion concentration and infusion rate) for the forthcoming clinical absolute oral bioavailability study of BIBX1382BS. BIBX1382BS infusion solutions have a low pH in order to keep the substance in solution. We therefore decided to investigate the hemolytic and precipitation potential of the drug in vitro. Also, the ratio of formulation (F) solution volume and a blood simulans (B) volume necessary to reach the physiological pH, expressed as the FB-ratio, was determined in vitro. On the basis of the results obtained, it is advised to administer BIBX1382BS infusion at a concentration of 1 mg/ml and a maximum infusion rate of 10 ml/min. This article describes the in vitro biocompatibility screening program.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Nuijen B,Bouma M,Henrar RE,Brauns U,Bette P,Bult A,Beijnen JHdoi
10.1016/s0378-5173(99)00389-0keywords:
subject
Has Abstractpub_date
2000-01-25 00:00:00pages
261-7issue
2eissn
0378-5173issn
1873-3476pii
S0378517399003890journal_volume
194pub_type
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