The present investigation deals with the determination of bioavailability of Rofecoxib solid dispersion compared to pure rofecoxib (RFB). The study of a non-blinded, open-label, crossover design was conducted in six healthy volunteers. Blood samples were collected for 12 h at specified intervals of time after the administration of formulations and analysed by suitable HPLC method. The pharmacokinetic parameters such as maximum plasma concentration (Cmax), time to reach (tmax), elimination rate constant (Kel) biological half-life (t1/2), absorption rate constant (Ka) and area under curve (AUC0-12 and AUC0-) were determined. Significant difference in the bioavailability of pure rofecoxib and solid mixture of rofecoxib prepared using hupu gum as carrier has been reported from the studies. The Peak plasma concentrations (Cmax) of 8.34 ng/mL at tmax of 4 h and Cmax of 76.84 ng/mL at tmax of 3 h were observed for RFB and solid mixture respectively. The results clearly indicated an enhancement in the bioavailability of rofecoxib in solid mixture preparation.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.2174/15672018113109990039 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
One-Step Transformations from ACQ Luminogens to DSEgens via the Boc Protection Process.
ACS Omega
June 2023
Fujian Provincial Key Laboratory of Screening for Novel Microbial Products, Fujian Institute of Microbiology, Fuzhou, Fujian 350007, China.
Dual-state emission luminogens (DSEgens), as a new type of luminescent materials that can effectively emit light in solution and solid state, have attracted tremendous attention due to their potential application in chemical sensing, biological imaging, organic electronic devices, etc. In this study, two new rofecoxib derivatives and have been synthesized, and their photophysical properties are fully investigated by experimental studies and theoretical calculations. The key intermediate , resulting from one-step conjugation of rofecoxib with an indole unit, shows the classical aggregation-caused quenching (ACQ) effect.
View Article and Find Full Text PDFAutomatic evaluation of cyclooxygenase 2 inhibition induced by metal-based anticancer compounds.
J Inorg Biochem
May 2021
REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, n° 228, 4050-313 Porto, Portugal. Electronic address:
An automatic methodology based on micro sequential injection analysis coupled to a lab-on-valve system (termed μSIA-LOV) was developed and used to determine the ability of metal-based anticancer compounds to inhibit cyclooxygenase 2 (COX-2) activity. COX-2 may be involved in pathogenesis of cancer and it is overexpressed in several types of solid tumors. Since platinum-based compounds are extensively used in the treatment of cancer, and ruthenium compounds are considered as promising candidates for next generation of non-targeted anticancer drugs, it is interesting to establish whether COX-2 inhibition is relevant to their mode of action.
View Article and Find Full Text PDFThere are no reports about the pharmaceutical applications of hupu gum (HG). Hence the present study was undertaken to test its suitability in the dissolution enhancement of poorly water soluble drug. Rofecoxib (RFB) was taken as model drug.
View Article and Find Full Text PDFAdverse effects of nonsteroidal antiinflammatory drugs: an update of gastrointestinal, cardiovascular and renal complications.
J Pharm Pharm Sci
September 2014
Gatton College of Pharmacy, East Tennessee State University.
Non-steroidal anti-inflammatory drugs (NSAIDs) are used chronically to reduce pain and inflammation in patients with arthritic conditions, and also acutely as analgesics by many patients. Both therapeutic and adverse effects of NSAIDs are due to inhibition of cyclooxygenase (COX) enzyme. NSAIDs are classified as non-selective and COX-2-selective inhibitors (COXIBS) based on their extent of selectivity for COX inhibition.
View Article and Find Full Text PDFBioavailability and pharmacokinetic studies of rofecoxib solid dispersion.
Curr Drug Deliv
December 2013
Department. of Pharmaceutics, Sree Vidyanikethan College of Pharmacy, A. Rangampet, Tirupati, 517102, Andhra Pradesh, India.
The present investigation deals with the determination of bioavailability of Rofecoxib solid dispersion compared to pure rofecoxib (RFB). The study of a non-blinded, open-label, crossover design was conducted in six healthy volunteers. Blood samples were collected for 12 h at specified intervals of time after the administration of formulations and analysed by suitable HPLC method.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!