DISSOLUTION ENHANCEMENT OF THIACETAZONE I: VIA SURFACE HYDROPHILIZATION

Ibrahim, S. A.; Hafez, E.; El-Faham, T. H.; Mohamed, F. A.

doi:10.21608/bfsa.1988.73513

DISSOLUTION ENHANCEMENT OF THIACETAZONE I: VIA SURFACE HYDROPHILIZATION

Document Type : Original Article

Authors

Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt

10.21608/bfsa.1988.73513

Abstract

Hydrophilized systems of thiacetazone with different hydrophilic Viz., surfactants, polymers, sugar alcohols and isoniazid were prepared. The tested drug was intimately wetted with small volume of alcoholic carrier solution, and left aside to dry at room temperature. The wettability and dissolution rate tests of the hydrophilized systems and their corresponding physical mixtures were performed. Also, the effect of the tested carriers on the aqueous solubility of thiacetazone was investigated. The USPXX dissolution test, exhibited a pronounced increase in dissolution of thiacetazone from its hydrophilized systems as compared to that of their physical mixtures and pure drug. Generally, a direct correlation was found between the wettability and dissolution rates. Hydrophilized systems with surfactants gave the highest dissolution and good wettability next to isoniazid. Surfactants then followed in order by sugar alcohols and then by polymers. The effect of surfactants is directly proportional to the concentration. After 10 minutes the relative dissolution rate was 14.34, 13.86 or 14.43 for 5% w/w. Tween 40, 60 or Myrj 53 respectively. However, with the other carriers higher concentrations led to reduction in the dissolution enhancing effect. The results denote the potential use of this technique to enhance thiacetazone dissolution.