Influence on analgesic activity and serum levels after meloxicam complexation with beta-cyclodextrin in mice and rats.
The aim of the present study was to evaluate and compare the analgesic activity and serum levels of meloxicam (CAS 71125-38-7) after administration of meloxicam associated with beta-cyclodextrin (BCD, CAS 7585-39-9) and unmodified meloxicam. The analgesic activity was measured using the plantar test (rats) and the writhing test (mice). In the plantar test, BCD-meloxicam (3 mg/kg and 10 mg/kg orally) showed higher analgesic activity than corresponding doses of meloxicam alone; in the writhing test BCD-meloxicam (7 mg/kg and 15 mg/kg orally) showed stronger analgesic activity than unmodified meloxicam. Serum levels of meloxicam were significantly higher, at 0.5 h and 1 h after administration of BCD-meloxicam orally than those of unmodified meloxicam (both dosed at 10 mg/kg). The present results suggest that association with beta-cyclodextrin increases the analgesic activity of meloxicam. This may be due to an icreased systemic bioavailability of meloxicam after oral administration of its complex with beta-cyclodextrin.
Janovský
Martin
M
Department of Pharmacology, 3rd Faculty of Medicine, Charles University, Prague, Czech Republic. m.janovsky@gmail.com
Dolezal
Tomás
T
Procháizková
Michaela
M
Slíva
Jirí
J
Krsiak
Miloslav
M
D000700:Analgesics / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000097:blood / Q000494:pharmacology*; D002351:Carrageenan; D006930:Hyperalgesia / Q000139:chemically induced; D008297:Male; D000077239:Meloxicam; D051379:Mice; D010146:Pain / Q000188:drug therapy; D010147:Pain Measurement / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D013843:Thiazines / Q000097:blood* / Q000494:pharmacology*; D013844:Thiazoles / Q000097:blood* / Q000494:pharmacology*; D014680:Veins / Q000187:drug effects / Q000502:physiology; D047392:beta-Cyclodextrins / Q000097:blood*
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D013843:Thiazines; D013844:Thiazoles; D047392:beta-Cyclodextrins; D002351:Carrageenan; C031215:betadex; D000077239:Meloxicam