A pharmacokinetic study of intramuscular administration of bulleyaconitine A in healthy volunteers.
The pharmacokinetics of bulleyaconitine A (BLA) after a single dose of 0.2 mg 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 15 h, 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+/-0.68 h, the C(max) value was 1.13+/-0.76 ng/ml, the AUC(0-t) was 5.16+/-2.05 ng.h/ml, and t(1/2) was found to be 4.88+/-0.97 h. 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 2-6 h. The pain was tolerable, and no subject required additional treatment.
Weng
Wei-Yu
WY
Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, People's Republic of China.
Xu
Hui-Nan
HN
Huang
Jian-Ming
JM
Wang
Guo-Quan
GQ
Shen
Teng
T
Zhang
Jian-Fang
JF
D000157:Aconitine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D007273:Injections, Intramuscular; D008297:Male
D000894:Anti-Inflammatory Agents, Non-Steroidal; C052509:bulleyaconitine A; D000157:Aconitine