Arzneimittelforschung 2010; 60(6): 320-323
DOI: 10.1055/s-0031-1296294
Analgesics · Anti-inflammatories · Antiphlogistics · Antirheumatic Drugs
Editio Cantor Verlag Aulendorf (Germany)

Influence on analgesic activity and serum levels after meloxicam complexation with beta-cyclodextrin in mice and rats

Martin Janovský
Department of Pharmacology, 3rd Faculty of Medicine, Charles University, Prague, Czech Republic
,
Tomáš Doležal
Department of Pharmacology, 3rd Faculty of Medicine, Charles University, Prague, Czech Republic
,
Michaela Procházková
Department of Pharmacology, 3rd Faculty of Medicine, Charles University, Prague, Czech Republic
,
Jiří Slíva
Department of Pharmacology, 3rd Faculty of Medicine, Charles University, Prague, Czech Republic
,
Miloslav Kršiak
Department of Pharmacology, 3rd Faculty of Medicine, Charles University, Prague, Czech Republic
› Author Affiliations
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Publication History

Publication Date:
02 December 2011 (online)

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Abstract

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.