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Bioavailability Enhancement: Drug Solubility Enhancement

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Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...

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Updated: Jun 25, 2026

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Published on: July 27, 2022

Improving tenoxicam solubility and bioavailability by cosolvent system.

Ming-Kung Yeh¹, Li-Chien Chang, Andy Hong-Jey Chiou

¹Department of Pharmacy Practice, Tri-Service General Hospital, Neihu, Taipei, Taiwan.

AAPS Pharmscitech

|February 19, 2009

Summary

This summary is machine-generated.

This study enhanced tenoxicam solubility using a ternary cosolvent system, improving its potential for parenteral formulations. Bioequivalence was confirmed in pharmacokinetic evaluations.

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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Published on: September 20, 2017

Area of Science:

Pharmaceutical Sciences
Drug Delivery Systems

Background:

Tenoxicam is a poorly water-soluble non-steroidal anti-inflammatory drug (NSAID).
Poor solubility limits the development of effective parenteral formulations.
Novel strategies are needed to enhance tenoxicam's solubility for intravenous or intramuscular administration.

Purpose of the Study:

To develop a ternary cosolvent system to enhance the solubility of tenoxicam.
To evaluate the physicochemical properties and pharmacokinetic profile of the developed formulation.
To assess the bioequivalence of the tenoxicam formulation in a preclinical model.

Main Methods:

Solubility studies were conducted using ternary cosolvent systems including dimethylsulfoxide (DMSO)/propylene glycol/water, DMSO/ethanol/water, and DMSO/polyethoxylated castor oil/ethanol.
Three-phase diagrams were constructed to identify optimal solvent ratios.
Viscosity measurements were performed on promising formulations.
Pharmacokinetic studies in New Zealand rabbits were conducted following intramuscular injection to determine relative bioavailability and bioequivalence.

Main Results:

The DMSO/polyethoxylated castor oil/ethanol system (volume ratio 5:4:1) demonstrated superior performance.
This optimized system achieved a high tenoxicam solubility of 20.73 mg/ml and a low viscosity of 10.0 cP.
Pharmacokinetic analysis indicated successful bioequivalence with a relative bioavailability (F(rel)) of 0.89.

Conclusions:

A ternary cosolvent system effectively enhances tenoxicam solubility, overcoming a major formulation challenge.
The developed formulation exhibits favorable physicochemical properties and achieves bioequivalence, suitable for parenteral administration.
This research offers a novel approach for developing parenteral formulations of poorly soluble drugs like tenoxicam.