A Pharmacokinetic Study of Intramuscular Administration of Bulleyaconitine A in Healthy Volunteers(Pharmacology)

概要

論文の詳細を見る
The pharmacokinetics of bulleyaconitine A (BLA) after a single dose of 0.2mg intramuscular injection was evaluated in healthy volunteers. Physical exam, vital signs, clinical laboratory tests and electrocardiogram measurements were monitored to assess the safety and tolerance of the drug. The plasma levels of BLA in serial samples, collected over 15h, were measured by a validated high-performance liquid chromatography (HPLC)-electrospray ionization tandem mass spectrometry (MS-MS) method. It was demonstrated that BLA was absorbed rapidly after intramuscular injection. The pharmacokinetic parameters were as follows : the t_<max> value was 0.90±0.68h, the C_<max> value was 1.13±0.76ng/ml, the AUC_<0-t> was 5.16±2.05ng・h/ml, and t_<1/2> was found to be 4.88±0.97h. No subject showed any drug-related clinically significant changes on physical examination, vital signs or laboratory tests. Eight of ten subjects reported a distinct feeling of pain at the site of injection starting approximately at the time of their peak plasma concentration and lasting for 2-6h. The pain was tolerable, and no subject required additional treatment.
公益社団法人日本薬学会の論文
2005-04-01