INTERACTION OF 1,4-BENZODIAZEPINES WITH CERTAIN MACROMOLECULES: I- EFFECT OF NON-IONIC SURFACTANTS ON THE DISSOLUTION RATE OF TEMAZEPAM

Document Type : Original Article

Authors

1 School of Pharmacy, Bradford University, England

2 Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt

3 Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt and School of Pharmacy, Bradford University, England

Abstract

A recycling and automatic recording system was adopted for studying the dissolution of Temazepam via dispersed particulate and intrinsic dissolution methods. The study involves the effect of concentrations below and above CMC of polysorbates and Myris on the solubility and dissolution rate of Temazepam at 37°C. These Surfactants in low concentrations (below their CMC) caused no change in Temazepam solubility referred to its water solubility.
T50% and RDR (relative dissolution rate) for Temazepam powder were calculated from the dissolution profiles. The presence of the studied surfactants in the dissolution medium caused an increase in the dissolution rate of the drug as demonstrated by a decrease in the T50% and the increase of the RDR. An explanation for these results is offered.
The static disc method of dissolution was adopted in order to investigate the effect of the studied surfactants on the dissolution rate of Temazepam compressed discs. Plots of the amount of Temazepam dissolved, in the presence of the studied surfactants, as a function of time, were linear for the intrensic dissolution of Temazepam discs.
 Correlation studies between the used surfactant concentrations and dissolution rate as well as solubility parameters of Temazepam were carried out and analyzed. It is suggested that the dissolution of Temazepam in the presence of the colloidal micellar surfactants is a diffusion controlled process and is related more to the diffusion layer mechanism of dissolution.