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Photodegradation and Stabilization of betamethasone-17 Valerate in aqueous/organic Solvents and Topical Formulations

Photodegradation and Stabilization of betamethasone-17 Valerate in aqueous/organic Solvents and Topical Formulations

Saif-ur-Rehman Khattak, Dilnawaz Shaikh, Iqbal Ahmad, Khan Usmanghani, Muhammad Ali Sheraz, Sofia Ahmed

AAPS PharmSciTech. 2013 Mar;14(1):177-82.

PMID: 23250710

Abstract:

The effects of solvent [acetonitrile, methanol, and acetonitrile/water mixture (20:80, v/v)], buffer concentration (phosphate buffer, pH 7.5), ionic strength and commonly employed adjuvants on the photodegradation of betamethasone-17 valerate in cream and gel formulations have been studied on exposure to UV light (300-400 nm). A validated high-performance liquid chromatography method has been used to determine the parent compound and its photodegraded products. The photodegradation data in the studied solvents showed greater decomposition of the drug in solvents with a lower dielectric constant. A comparatively higher rate of photodegradation was observed in the cream formulation compared to that for the gel formulation. The kinetic treatment of the photodegradation data revealed that the degradation of the drug follows first-order kinetics and the apparent first-order rate constants for the photodegradation reactions, in the media studied, range from 1.62 to 11.30×10(-3) min(-1). The values of the rate constants decrease with increasing phosphate concentration and ionic strength which could be due to the deactivation of the excited state and radical quenching. The second-order rate constant (k') for the phosphate ion-inhibited reactions at pH 7.5 has been found to be 5.22×10(-2) M(-1) s(-1). An effective photostabilization of the drug has been achieved in cream and gel formulations with titanium dioxide (33.5-42.5%), vanillin (21.6-28.7%), and butyl hydroxytoluene (18.2-21.6%).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP591684	Butyl valerate		591-68-4	Price

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