A rapid, sensitive, and accurate stability-indicating high-performance liquid chromatographic assay method for determining the degradation of carprofen (CPF) is developed and validated under acidic, basic, or photo-irradiated conditions. The analysis is monitored with a Cosmosil 5C18-AR column using a mobile phase of CH3CN-H2O-AcOH (50:49:1, v/v/v) at 260 nm. The developed method satisfies the system suitability criteria, peak integrity, and resolution among the parent drug and its degradation products. The results indicate that the established assay method shows good selectivity and specificity suitable for stability measurements of CPF. CPF is found to be more sensitive to exposure to light and in acidic conditions, but it is stable in a basic medium. The kinetic study of the photodegradation of CPF follows an apparent first-order reaction in a variety of solvents. The solvent effects on the rates of degradation are in the decreasing order of chloroform > dichloromethane > methanol > ethanol > 2-propanol, which is irrelevant to the dielectric constant epsilon. However, the hydrogen-donating ability of the solvents is essential to the photochemical decomposition of CPF. A plot of log k versus the Kirkwood function exhibits a linear relationship in aqueous ethanolic solutions, which implies that degradation proceeds via an ionic mechanism.
Honokiol, a small-molecule pharmacological bioactive constituent of the bark of Magnolia plants, has shown anti-tumor effect in a variety of human cancer xenograft models through the induction of apoptosis. Additionally, honokiol could enhance the cytotoxicity in combination of oxaliplatin in colon cancer cells.
To investigate the anti-tumor effect and the pharmacokinetics (PK) of honokiol, honokiol was tested for anti-tumor activity in a colorectal cancer xenograft mice model and oral-bioavailability of honokiol was assayed in Sprague-Dawley rats.
The pharmacokinetic results of 5.0 mg/kg honokiol after intravenous injection showed that the elimination half time was about 0.79 ± 0.03 hours, the Cmax was about 752.67 ± 58.36 ng/mL, and the mean residence time (MRT) was about 0.85 ± 0.05 hours.
In vivo study for testing anti-cancer activity of honokiol is underwent and expected that honokiol would inhibit the tumor growth in colorectal tumor-bearing mice. In conclusion, honokiol may be developed be as therapeutic agent for cancer treatment in combination with PK and pharmacodynamics (PD) data.
Citation Format: Yung-Jen Tsai, Pei-Yi Tsai, Le-Mei Hung, Mei-Yin Su, Min-Hui Lin, Lung-Yu Kuan, Yih-Chiao Tsai, Hui-Ling Chen, Jia-Ming Chang. The pharmacokinetics and pharmacodynamics study of honokiol in Sprague-Dawley rats and colorectal tumor-bearing mice. [abstract]. In: Proceedings of the Third AACR International Conference on Frontiers in Basic Cancer Research; Sep 18-22, 2013; National Harbor, MD. Philadelphia (PA): AACR; Cancer Res 2013;73(19 Suppl):Abstract nr C46.
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