Improving Tenoxicam Solubility and Bioavailability by Cosolvent System

The formulation study of tenoxicam, a poorly water-soluble drug, was developed by use of a ternary cosolvent system and has significantly enhanced the solubility. Additionally, the relative bioavailability of testing formulation was also evaluated by New Zealand rabbit with a single i.m. injection....

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Bibliographic Details
Published in:AAPS PharmSciTech 2009, Vol.10 (1), p.166-171
Main Authors: Yeh, Ming-Kung, Chang, Li-Chien, Chiou, Andy Hong-Jey
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents, Non-Steroidal - administration & dosage
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics
Biochemistry
Biological Availability
Biomedical and Life Sciences
Biomedicine
Biotechnology
Castor Oil - analogs & derivatives
Castor Oil - chemistry
Chemistry, Pharmaceutical
Dimethyl Sulfoxide - chemistry
Ethanol - chemistry
Injections, Intramuscular
Pharmacology/Toxicology
Pharmacy
Piroxicam - administration & dosage
Piroxicam - analogs & derivatives
Piroxicam - chemistry
Piroxicam - pharmacokinetics
Propylene Glycol - chemistry
Rabbits
Research Article
Solubility
Solvents - chemistry
Technology, Pharmaceutical - methods
Viscosity
Water - chemistry
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Summary:The formulation study of tenoxicam, a poorly water-soluble drug, was developed by use of a ternary cosolvent system and has significantly enhanced the solubility. Additionally, the relative bioavailability of testing formulation was also evaluated by New Zealand rabbit with a single i.m. injection. The three-phase diagram for dimethylsulfoxide (DMSO)/propylene glycol/water, DMSO/ethanol/water, and DMSO/polyethoxylated castor oil/ethanol system was developed. The volume ratio of 5:4:1 in the DMSO/polyethoxylated castor oil/ethanol system resulted in a more suitable vehicle than other systems, with a high solubility (20.73 mg/ml) and low viscosity (10.0 Cp). A pharmacokinetic study of bioequivalence ( F rel  = 0.89) was also obtained. The present study not only provides a novel strategy improving tenoxicam solubility but also helps further scientific knowledge for the development of parenteral formulations.
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-009-9189-2