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Pharmacokinetics and tolerance of intravenous and intramuscular phylloquinone(vitamin K 1 ) mixed micelles formulation
Author(s) -
SOEDIRMAN J. R.,
DE BRUIJN E. A.,
MAES R. A. A.,
HANCK A.,
GRÜTER J.
Publication year - 1996
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1046/j.1365-2125.1996.03847.x
Subject(s) - pharmacokinetics , vitamin k , micelle , vitamin , pharmacology , chemistry , medicine , intramuscular injection , chromatography , anesthesia , organic chemistry , aqueous solution
1 The pharmacokinetics and tolerance of phylloquinone(vitamin K 1 ) mixed micelles formulation (Konakion ® MM) were evaluated, in normal human adult volunteers ( n =30) using an open randomized crossover design protocol following a 10 mg intravenous or intramuscular injection. 2 Blood samples were collected for up to 12 h after the intravenous and up to 72 h after the intramuscular injections and the phylloquinone(vitamin K 1 ) levels determined by reversed phase h.p.l.c. with fluorometric detection after post‐column electrochemical reduction. 3 Konakion ® MM was well tolerated after either route of administration. Pharmacokinetic analysis of plasma phylloquinone(vitamin K 1 ) concentration vs time profiles revealed that in one‐fifth of the subjects systemic availability of intramuscular phylloquinone(vitamin K 1 ) was below 65%. 4 Our data suggest that due to sustained, but irregular and unpredictable absorption of the phylloquinone(vitamin K 1 ) from the depot site, the intramuscular route of Konakion ® MM administration is not suitable and thus not recommended. 5 Konakion ® MM i.v. is indicated to be well tolerated and effective in antagonizing coumarin‐type‐anticoagulants like Marcoumar ®